phases
list
enrollmentCount
int64
allocation
string
interventionModel
string
primaryPurpose
class label
masking
class label
healthyVolunteers
bool
sex
class label
oversightHasDmc
bool
briefSummary
string
detailedDescription
string
conditions
string
conditionsKeywords
string
protocolPdfText
string
numArms
int64
armDescriptions
string
armGroupTypes
list
numInterventions
int64
interventionTypes
list
interventionDescriptions
string
interventionNames
string
numLocations
int64
locationDetails
string
target
int64
nctid
string
[ 4 ]
760
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
false
The purpose of this study is to evaluate the safety and efficacy of ABT-335 and rosuvastatin calcium combination therapy to monotherapy in subjects with dyslipidemia.
There are 3 treatment groups in the study: ABT-335 135 mg in combination with rosuvastatin 5 mg, ABT-335 135 mg monotherapy, and rosuvastatin 5 mg monotherapy. The 3 primary outcome measures only compare 2 of the treatment groups for each variable (mean percent change in HDL-C and TG comparing ABT-335 135 mg in combination with rosuvastatin 5 mg to rosuvastatin 5 mg monotherapy, and mean percent change in LDL-C comparing ABT-335 135 mg in combination with rosuvastatin 5 mg to ABT-335 135 mg monotherapy. The 6 secondary outcome measures only compare 2 of the treatment groups for each variable (mean percent change in Non-HDL-C comparing ABT-335 135 mg in combination with rosuvastatin 5 mg to ABT-335 135 mg monotherapy, mean percent change in Non-HDL-C, VLDL-C, ApoB, and Total Cholesterol comparing ABT-335 135 mg in combination with rosuvastatin 5 mg to rosuvastatin 5 mg monotherapy, and median percent change in hsCRP comparing ABT-335 135 mg in combination with rosuvastatin 5 mg to rosuvastatin 5 mg monotherapy).
Hypercholesterolemia Dyslipidemia
null
3
arm 1: ABT-335 135mg in combination with rosuvastatin calcium 5mg administered orally, once daily for 12 weeks arm 2: ABT-335 135mg monotherapy administered orally, once daily for 12 weeks arm 3: Rosuvastatin calcium 5mg monotherapy administered orally, once daily for 12 weeks
[ 0, 1, 1 ]
3
[ 0, 0, 0 ]
intervention 1: ABT-335 135 mg in combination with rosuvastatin calcium 5 mg administered orally, once daily for 12 weeks intervention 2: ABT-335 135 mg monotherapy administered orally, once daily for 12 weeks intervention 3: Rosuvastatin calcium 5 mg monotherapy administered orally, once daily for 12 weeks
intervention 1: ABT-335 and rosuvastatin calcium intervention 2: ABT-335 intervention 3: rosuvastatin calcium
168
Birmingham | Alabama | United States | -86.80249 | 33.52066 Birmingham | Alabama | United States | -86.80249 | 33.52066 Birmingham | Alabama | United States | -86.80249 | 33.52066 Huntsville | Alabama | United States | -86.58594 | 34.7304 Huntsville | Alabama | United States | -86.58594 | 34.7304 Ozark | Alabama | United States | -85.64049 | 31.45906 Tuscaloosa | Alabama | United States | -87.56917 | 33.20984 Chandler | Arizona | United States | -111.84125 | 33.30616 Gilbert | Arizona | United States | -111.78903 | 33.35283 Scottsdale | Arizona | United States | -111.89903 | 33.50921 Little Rock | Arkansas | United States | -92.28959 | 34.74648 Anaheim | California | United States | -117.9145 | 33.83529 Chula Vista | California | United States | -117.0842 | 32.64005 Concord | California | United States | -122.03107 | 37.97798 Encinitas | California | United States | -117.29198 | 33.03699 Fair Oaks | California | United States | -121.27217 | 38.64463 Fresno | California | United States | -119.77237 | 36.74773 Fresno | California | United States | -119.77237 | 36.74773 Lincoln | California | United States | -121.29301 | 38.89156 Long Beach | California | United States | -118.18923 | 33.76696 Los Angeles | California | United States | -118.24368 | 34.05223 Norwalk | California | United States | -118.08173 | 33.90224 Sacramento | California | United States | -121.4944 | 38.58157 Sacramento | California | United States | -121.4944 | 38.58157 San Diego | California | United States | -117.16472 | 32.71571 West Hills | California | United States | -118.64398 | 34.19731 Aurora | Colorado | United States | -104.83192 | 39.72943 Colorado Springs | Colorado | United States | -104.82136 | 38.83388 Waterbury | Connecticut | United States | -73.0515 | 41.55815 Coral Gables | Florida | United States | -80.26838 | 25.72149 Fort Lauderdale | Florida | United States | -80.14338 | 26.12231 Holly Hill | Florida | United States | -81.03756 | 29.24359 Hollywood | Florida | United States | -80.14949 | 26.0112 Jacksonville | Florida | United States | -81.65565 | 30.33218 Jacksonville | Florida | United States | -81.65565 | 30.33218 Jupiter | Florida | United States | -80.09421 | 26.93422 Kissimmee | Florida | United States | -81.41667 | 28.30468 Largo | Florida | United States | -82.78842 | 27.90979 Melbourne | Florida | United States | -80.60811 | 28.08363 Miami | Florida | United States | -80.19366 | 25.77427 New Port Richey | Florida | United States | -82.71927 | 28.24418 New Smyrna Beach | Florida | United States | -80.927 | 29.02582 Ocala | Florida | United States | -82.14009 | 29.1872 Ocala | Florida | United States | -82.14009 | 29.1872 Orlando | Florida | United States | -81.37924 | 28.53834 Ormond Beach | Florida | United States | -81.05589 | 29.28581 Pensacola | Florida | United States | -87.21691 | 30.42131 Sarasota | Florida | United States | -82.53065 | 27.33643 Sarasota | Florida | United States | -82.53065 | 27.33643 West Palm Beach | Florida | United States | -80.05337 | 26.71534 West Palm Beach | Florida | United States | -80.05337 | 26.71534 Winter Haven | Florida | United States | -81.73286 | 28.02224 Blue Ridge | Georgia | United States | -84.32409 | 34.86397 Decatur | Georgia | United States | -84.29631 | 33.77483 Dunwoody | Georgia | United States | -84.33465 | 33.94621 Roswell | Georgia | United States | -84.36159 | 34.02316 Roswell | Georgia | United States | -84.36159 | 34.02316 Suwanee | Georgia | United States | -84.0713 | 34.05149 Woodstock | Georgia | United States | -84.51938 | 34.10149 Arlington Heights | Illinois | United States | -87.98063 | 42.08836 Chicago | Illinois | United States | -87.65005 | 41.85003 Peoria | Illinois | United States | -89.58899 | 40.69365 Avon | Indiana | United States | -86.39972 | 39.76282 Evansville | Indiana | United States | -87.55585 | 37.97476 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Lafayette | Indiana | United States | -86.87529 | 40.4167 Newburgh | Indiana | United States | -87.40529 | 37.94449 Iowa City | Iowa | United States | -91.53017 | 41.66113 Arkansas City | Kansas | United States | -97.03837 | 37.06197 Overland Park | Kansas | United States | -94.67079 | 38.98223 Wichita | Kansas | United States | -97.33754 | 37.69224 Wichita | Kansas | United States | -97.33754 | 37.69224 Lexington | Kentucky | United States | -84.47772 | 37.98869 Louisville | Kentucky | United States | -85.75941 | 38.25424 New Orleans | Louisiana | United States | -90.07507 | 29.95465 Slidell | Louisiana | United States | -89.78117 | 30.27519 Auburn | Maine | United States | -70.23117 | 44.09785 Scarborough | Maine | United States | -70.32172 | 43.57814 Baltimore | Maryland | United States | -76.61219 | 39.29038 Haverhill | Massachusetts | United States | -71.07728 | 42.7762 Springfield | Massachusetts | United States | -72.58981 | 42.10148 Ann Arbor | Michigan | United States | -83.74088 | 42.27756 Ann Arbor | Michigan | United States | -83.74088 | 42.27756 Portage | Michigan | United States | -85.58 | 42.20115 Brooklyn Center | Minnesota | United States | -93.33273 | 45.07608 Jackson | Mississippi | United States | -90.18481 | 32.29876 Olive Branch | Mississippi | United States | -89.82953 | 34.96176 Tupelo | Mississippi | United States | -88.70464 | 34.25807 City of Saint Peters | Missouri | United States | -90.62651 | 38.80033 Kansas City | Missouri | United States | -94.57857 | 39.09973 Billings | Montana | United States | -108.50069 | 45.78329 Missoula | Montana | United States | -113.994 | 46.87215 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Concord | New Hampshire | United States | -71.53757 | 43.20814 Elizabeth | New Jersey | United States | -74.2107 | 40.66399 South Bound Brook | New Jersey | United States | -74.53154 | 40.55344 Toms River | New Jersey | United States | -74.19792 | 39.95373 Trenton | New Jersey | United States | -74.74294 | 40.21705 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 Bronxville | New York | United States | -73.83208 | 40.93815 New York | New York | United States | -74.00597 | 40.71427 Rochester | New York | United States | -77.61556 | 43.15478 Syracuse | New York | United States | -76.14742 | 43.04812 Williamsville | New York | United States | -78.73781 | 42.96395 Asheville | North Carolina | United States | -82.55402 | 35.60095 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Hickory | North Carolina | United States | -81.3412 | 35.73319 Morehead City | North Carolina | United States | -76.72604 | 34.72294 Raleigh | North Carolina | United States | -78.63861 | 35.7721 Salisbury | North Carolina | United States | -80.47423 | 35.67097 Statesville | North Carolina | United States | -80.8873 | 35.78264 Winston-Salem | North Carolina | United States | -80.24422 | 36.09986 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Columbus | Ohio | United States | -82.99879 | 39.96118 Mogadore | Ohio | United States | -81.39789 | 41.04645 Sandusky | Ohio | United States | -82.70796 | 41.44894 Warren | Ohio | United States | -80.81842 | 41.23756 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Tulsa | Oklahoma | United States | -95.99277 | 36.15398 Tulsa | Oklahoma | United States | -95.99277 | 36.15398 Medford | Oregon | United States | -122.87559 | 42.32652 Carlisle | Pennsylvania | United States | -77.18887 | 40.20148 Downingtown | Pennsylvania | United States | -75.70327 | 40.0065 Feasterville | Pennsylvania | United States | -74.997 | 40.15 Harleysville | Pennsylvania | United States | -75.38712 | 40.27955 Jersey Shore | Pennsylvania | United States | -77.26442 | 41.20202 Lansdale | Pennsylvania | United States | -75.28379 | 40.2415 Melrose Park | Pennsylvania | United States | -75.13184 | 40.06178 Newtown | Pennsylvania | United States | -74.93683 | 40.22928 Penndel | Pennsylvania | United States | -74.91656 | 40.15205 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Warminster | Pennsylvania | United States | -75.09962 | 40.20678 Charleston | South Carolina | United States | -79.93275 | 32.77632 Greenville | South Carolina | United States | -82.39401 | 34.85262 Greer | South Carolina | United States | -82.22706 | 34.93873 Moncks Corner | South Carolina | United States | -80.01429 | 33.19632 Mt. Pleasant | South Carolina | United States | -79.86259 | 32.79407 Simpsonville | South Carolina | United States | -82.25428 | 34.73706 Summerville | South Carolina | United States | -80.17565 | 33.0185 Sioux Falls | South Dakota | United States | -96.70033 | 43.54997 Jackson | Tennessee | United States | -88.81395 | 35.61452 Johnson City | Tennessee | United States | -82.35347 | 36.31344 Nashville | Tennessee | United States | -86.78444 | 36.16589 Arlington | Texas | United States | -97.10807 | 32.73569 Houston | Texas | United States | -95.36327 | 29.76328 Houston | Texas | United States | -95.36327 | 29.76328 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 Temple | Texas | United States | -97.34278 | 31.09823 Falls Church | Virginia | United States | -77.17109 | 38.88233 Richmond | Virginia | United States | -77.46026 | 37.55376 Richmond | Virginia | United States | -77.46026 | 37.55376 Lakewood | Washington | United States | -122.51846 | 47.17176 Madison | Wisconsin | United States | -89.40123 | 43.07305
0
NCT00463606
[ 5 ]
289
RANDOMIZED
FACTORIAL
0TREATMENT
4QUADRUPLE
false
0ALL
false
Metoclopramide is a dopamine antagonist frequently used for the treatment of nausea, vomiting, and migraine headaches in Emergency Departments. However, little research has focused on the optimal dose of metoclopramide for treatment of nausea in the emergency department. We propose a randomized, double-blind, placebo controlled trial to investigate the optimal dose of metoclopramide for treatment of nausea.
The most effective dose of metoclopramide for treatment of nausea in the emergency department setting has not been thoroughly investigated. One pilot study among emergency department patients in Australia found no statistical difference between 10 mg and 0.4 milligrams/kilogram; another investigation suggests that the anti-emetic effect of 10 milligrams of metoclopramide is no more effective than placebo. In contrast, investigations focusing on chemotherapy patients and post-operative patients suggest that higher dosage metoclopramide is more effective in treating nausea and vomiting. This emergency department study will compare the anti-emetic efficacy of 10 milligrams and 20 milligrams of metoclopramide by using the visual analog scale. In addition to evaluation of dose, we will evaluate one of the most common side affects of metoclopramide, akathisia. Akathisia is characterized by a subjective component of restlessness and an objective component in the form of the inability to remain motionless. Anti-cholinergic medications are known to reduce extrapyramidal symptoms such as akathisia when dopamine function is impaired in the basal ganglia. In fact, the use of diphenhydramine has been shown to reduce the incidence of akathisia in patients receiving a different anti-emetic, prochlorperazine. However, no research has focused on the use of anti-cholinergic medications to reduce metoclopramide induced akathisia. This investigation will assess the use of 25 mg of diphenhydramine in preventing metoclopramide induced akathisia in ED patients being treated for nausea/vomiting.
Nausea Extrapyramidal Symptoms
Metoclopramide Nausea Akathisia Emergency department
null
4
arm 1: Metoclopramide 20 mg + diphenhydramine, delivered intravenously over 15 minutes arm 2: Metoclopramide 20 mg + placebo, delivered intravenously over 15 minutes arm 3: Metoclopramide 10mg + placebo, delivered intravenously over 15 minutes arm 4: Metoclopramide 10 mg + diphenhydramine 25 mg, delivered intravenously over 15 minutes
[ 1, 1, 1, 1 ]
4
[ 0, 0, 0, 0 ]
intervention 1: an anti-emetic medication intervention 2: used for prophylaxis against akathisia intervention 3: placebo intervention 4: Metoclopramide 20 mg
intervention 1: metoclopramide 10 mg intervention 2: Diphenhydramine 25 mg intervention 3: Placebo intervention 4: Metoclopramide 20 mg
1
The Bronx | New York | United States | -73.86641 | 40.84985
0
NCT00475306
[ 4 ]
799
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
false
0ALL
true
The purpose of this study is to investigate the efficacy and safety of several doses of the melt formulation of desmopressin in a broad population of adult patients with nocturia.
null
Nocturia
null
5
arm 1: Participants took a placebo 'melt' for 28 days to complete part 1 of the study. In part 2, placebo patients were randomized to one of the other 4 treatment arms based on assignments predetermined at the initial randomization, to receive active desmopressin melt for between 1 and 6 months (until the database for part 1 was locked and treatment was unblinded). arm 2: Participants took desmopressin melt 10 μg for 28 days to complete part 1 of the study. Participants continued on this dose in part 2 of the study for between 1 and 6 months (until the database for part 1 was locked and treatment was unblinded). arm 3: Participants took desmopressin melt 25 μg for 28 days to complete part 1 of the study. Participants continued on this dose in part 2 of the study for between 1 and 6 months (until the database for part 1 was locked and treatment was unblinded). arm 4: Participants took desmopressin melt 50 μg for 28 days to complete part 1 of the study. Participants continued on this dose in part 2 of the study for between 1 and 6 months (until the database for part 1 was locked and treatment was unblinded). arm 5: Participants will take desmopressin melt 100 μg for 28 days to complete part 1 of the study. Participants will continue on this dose in part 2 of the study for between 1-6 months (until the database for part 1 is locked and treatment is unblinded).
[ 2, 0, 0, 0, 0 ]
2
[ 0, 0 ]
intervention 1: Oral lyophilisate of desmopressin acetate placed under the participant's tongue, without water, once daily approximately 1 hour before bedtime in the assigned dosage: 10, 25, 50 or 100 μg intervention 2: Oral placebo placed under the participant's tongue, without water, once daily approximately 1 hour before bedtime.
intervention 1: desmopressin acetate intervention 2: Placebo
80
Birmingham | Alabama | United States | -86.80249 | 33.52066 Scottsdale | Arizona | United States | -111.89903 | 33.50921 Little Rock | Arkansas | United States | -92.28959 | 34.74648 Anaheim | California | United States | -117.9145 | 33.83529 Beverly Hills | California | United States | -118.40036 | 34.07362 Long Beach | California | United States | -118.18923 | 33.76696 Newport Beach | California | United States | -117.92895 | 33.61891 San Diego | California | United States | -117.16472 | 32.71571 Santa Rosa | California | United States | -122.71443 | 38.44047 Tarzana | California | United States | -118.55397 | 34.17334 Torrance | California | United States | -118.34063 | 33.83585 Denver | Colorado | United States | -104.9847 | 39.73915 Denver | Colorado | United States | -104.9847 | 39.73915 Denver | Colorado | United States | -104.9847 | 39.73915 Middlebury | Connecticut | United States | -73.12761 | 41.52787 Aventura | Florida | United States | -80.13921 | 25.95648 Clearwater | Florida | United States | -82.8001 | 27.96585 Miami | Florida | United States | -80.19366 | 25.77427 Plantation | Florida | United States | -80.23184 | 26.13421 Stuart | Florida | United States | -80.25283 | 27.19755 Tallahassee | Florida | United States | -84.28073 | 30.43826 Tampa | Florida | United States | -82.45843 | 27.94752 West Palm Beach | Florida | United States | -80.05337 | 26.71534 Columbus | Georgia | United States | -84.98771 | 32.46098 Dunwoody | Georgia | United States | -84.33465 | 33.94621 Peoria | Illinois | United States | -89.58899 | 40.69365 Overland Park | Kansas | United States | -94.67079 | 38.98223 Metairie | Louisiana | United States | -90.15285 | 29.98409 Shreveport | Louisiana | United States | -93.75018 | 32.52515 Shreveport | Louisiana | United States | -93.75018 | 32.52515 Springfield | Massachusetts | United States | -72.58981 | 42.10148 St Louis | Missouri | United States | -90.19789 | 38.62727 Lincoln | Nebraska | United States | -96.66696 | 40.8 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Lawrenceville | New Jersey | United States | -74.7296 | 40.29733 Lawrenceville | New Jersey | United States | -74.7296 | 40.29733 Morristown | New Jersey | United States | -74.48154 | 40.79677 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 Albany | New York | United States | -73.75623 | 42.65258 Carmel | New York | United States | -73.68013 | 41.43009 Garden City | New York | United States | -73.6343 | 40.72677 New York | New York | United States | -74.00597 | 40.71427 Suffern | New York | United States | -74.14959 | 41.11482 Concord | North Carolina | United States | -80.58158 | 35.40888 Greensboro | North Carolina | United States | -79.79198 | 36.07264 Wilmington | North Carolina | United States | -77.94604 | 34.23556 Winston-Salem | North Carolina | United States | -80.24422 | 36.09986 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Mogadore | Ohio | United States | -81.39789 | 41.04645 Bala-Cynwyd | Pennsylvania | United States | -75.23407 | 40.00761 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Reading | Pennsylvania | United States | -75.92687 | 40.33565 Greenville | South Carolina | United States | -82.39401 | 34.85262 Greer | South Carolina | United States | -82.22706 | 34.93873 Mt. Pleasant | South Carolina | United States | -79.86259 | 32.79407 Myrtle Beach | South Carolina | United States | -78.88669 | 33.68906 Kingsport | Tennessee | United States | -82.56182 | 36.54843 Nashville | Tennessee | United States | -86.78444 | 36.16589 Corpus Christi | Texas | United States | -97.39638 | 27.80058 Dallas | Texas | United States | -96.80667 | 32.78306 Houston | Texas | United States | -95.36327 | 29.76328 Humble | Texas | United States | -95.26216 | 29.99883 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 Richmond | Virginia | United States | -77.46026 | 37.55376 Virginia Beach | Virginia | United States | -75.97799 | 36.85293 Seattle | Washington | United States | -122.33207 | 47.60621 Seattle | Washington | United States | -122.33207 | 47.60621 Seattle | Washington | United States | -122.33207 | 47.60621 Kelowna | British Columbia | Canada | -119.48568 | 49.88307 Victoria | British Columbia | Canada | -123.35155 | 48.4359 Victoria | British Columbia | Canada | -123.35155 | 48.4359 Fredericton | New Brunswick | Canada | -66.66558 | 45.94541 Barrie | Ontario | Canada | -79.66634 | 44.40011 Brantford | Ontario | Canada | -80.26636 | 43.1334 Guelph | Ontario | Canada | -80.25599 | 43.54594 North Bay | Ontario | Canada | -79.46633 | 46.3168 Oakville | Ontario | Canada | -79.68292 | 43.45011 Toronto | Ontario | Canada | -79.39864 | 43.70643
0
NCT00477490
[ 0 ]
101
RANDOMIZED
PARALLEL
4SUPPORTIVE_CARE
3TRIPLE
false
0ALL
false
Prior to surgery, a pharmacist will randomly assign participating patients to one of two groups. One group will get an injection in the knee during surgery that contains medications to limit pain and an antibiotic. A second group will get an injection in the knee during surgery that contains the same pain medications and antibiotic along with a corticosteroid to control inflammation. Corticosteroids are anti-inflammatory medications, not to be confused with muscle-building anabolic steroids you may have heard about in the news. Each patient will have an equal chance of being in either of the two groups. This study will test the safety and efficacy of methylprednisolone acetate in the treatment of pain and inflammation following total knee replacement.
Information collected during your office visits: The patient will be asked for a brief medical history so that we may determine if the patient can participate in the study. A member of our research team will ask the patient a series of questions about his/her knee. The patient will be asked to answer this series of questions a total of 4 times over the course of 1 year. Also, we will record how well the patient can bend and straighten your knee at these 4 office visits. We will have the patient rate the pain in his/her knee and ask the patient if he/she is satisfied with the surgery. If the patients have any complications, those will also be recorded. The patient will also have X-rays taken of the knee at the postoperative follow-up visits. This is the normal routine following total knee replacement. The X-rays will be read by the surgeon to help determine the success of the surgery. Injection during total knee replacement surgery: All patients will receive an injection containing bupivicaine HCl, morphine, epinephrine, clonidine, cefuroxime, and normal saline that will be placed directly into the knee during surgery. In addition, approximately half of the patients in the study will also receive methylprednisolone acetate as part of the injection. Information being collected during your hospital stay: During the hospital stay, information will be gathered for this study. A physical therapist will measure how well the patient can bend and straighten the knee. The amount of pain medication that was taken at the hospital will be recorded, and the number of days spent in the hospital will also be recorded.
Osteoarthritis Post-traumatic; Arthrosis
arthroplasty replacement knee
null
2
arm 1: Patients in the active comparator group will receive intraoperative injections containing bupivacaine HCl, morphine, epinephrine, clonidine, cefuroxime, and normal saline, as per the surgeon's standard of care. arm 2: Patients in the Corticosteroid group will have the same medications as the Control Group with the addition of a corticosteroid (methylprednisolone acetate)
[ 1, 0 ]
2
[ 0, 0 ]
intervention 1: Same medications and doses as the active comparator, but with the addition of 40 mg of methylprednisolone acetate intervention 2: bupivacaine HCl 80 mg, morphine 4 mg, epinephrine 300 micrograms, clonidine 100 micrograms, cefuroxime 750 mg, and normal saline
intervention 1: methylprednisolone acetate intervention 2: active comparator
1
Lexington | Kentucky | United States | -84.47772 | 37.98869
0
NCT00492973
[ 3 ]
48
RANDOMIZED
PARALLEL
1PREVENTION
2DOUBLE
false
0ALL
false
The study shall provide evidence for the save and efficient use of a fish oil containing lipid emulsion in parenteral nutrition of preterm infants.Safety will be assessed by monitoring hepatological and hematological laboratory parameters. Efficiency will be assessed by monitoring of inflammatory parameters.
null
Preterm Infants Parenteral Nutrition n-3 Fatty Acids
n-3 Polyunsaturated Fatty Acids (PUFA) parenteral nutrition preterm infant
null
2
arm 1: Lipidem 20 % arm 2: Lipofundin MCT/LCT 20%
[ 0, 1 ]
2
[ 0, 0 ]
intervention 1: daily i.v. infusion for up to 5 days intervention 2: daily i.v. infusion for up to 5 days
intervention 1: Lipofundin MCT/LCT 20 % intervention 2: Lipidem 20%
2
Munich | Bavaria | Germany | 11.57549 | 48.13743 Greifswald | N/A | Germany | 13.40244 | 54.08905
0
NCT00497289
[ 3 ]
163
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
false
0ALL
false
This is a multicenter study designed to compare the effect of exenatide plus a lifestyle modification plan versus placebo plus a lifestyle modification plan on weight loss in non-diabetic, obese subjects.
null
Obesity
exenatide obesity diabetes Amylin Lilly
null
2
arm 1: None arm 2: None
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: subcutaneous injection (5mcg or 10mcg), twice a day intervention 2: subcutaneous injection (equivalent volume to active dose), twice a day
intervention 1: exenatide intervention 2: placebo
16
Peoria | Arizona | United States | -112.23738 | 33.5806 Tucson | Arizona | United States | -110.92648 | 32.22174 Santa Ana | California | United States | -117.86783 | 33.74557 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Topeka | Kansas | United States | -95.67804 | 39.04833 Wichita | Kansas | United States | -97.33754 | 37.69224 Baton Rouge | Louisiana | United States | -91.18747 | 30.44332 St Louis | Missouri | United States | -90.19789 | 38.62727 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Goose Creek | South Carolina | United States | -80.03259 | 32.98101 Spartanburg | South Carolina | United States | -81.93205 | 34.94957 Dallas | Texas | United States | -96.80667 | 32.78306 San Antonio | Texas | United States | -98.49363 | 29.42412 Renton | Washington | United States | -122.21707 | 47.48288 Ponce | N/A | Puerto Rico | -66.62398 | 18.01031 San Juan | N/A | Puerto Rico | -66.10572 | 18.46633
0
NCT00500370
[ 4 ]
5
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
Primary Objective: To determine the risk of bleeding from ASA therapy in thrombocytopenic patients who develop Acute Coronary Syndrome (ACS), and assess its effect on the overall morbidity and mortality in these patients as well as platelet functions.
Aspirin is known to decrease death rate by as much as 50% in patients that suffer from heart attacks. Patients with low platelet count are not given aspirin for fear of an increased risk of bleeding. Researchers want to compare the risks versus the benefits of using aspirin in this patient population. Participants in this study who suffer chest pain will be treated with a single enteric coated aspirin 325 mg instead of the current treatment without aspirin. Participants will then be tested to confirm that they had a heart attack by EKG (a test to measure the electrical activity of the heart) and blood tests (5ml of blood) will be drawn every 8 hours to detect enzymes that are released from the heart due to the heart attack. Blood samples will also be examined for platelet number. Participants who are found to have had a heart attack and have a platelet count of between 100,000 and 20,000 will be continued on aspirin (160 mg per day). All other standard medications for heart attacks will also be given. Participants who are found to have had a heart attack but whose platelet number is more than 100,000 will be given the standard therapy for heart attack, including enteric coated aspirin 325 mg per day, and will no longer take part in this study. Participants who are found to have had a heart attack but whose platelet number is less than 20,000 will be not be included in the study and will be treated as deemed appropriate by their primary physician. Participants will be examined daily and evaluated for bleeding. Blood samples (30 ml of blood) will also be drawn before or after aspirin is given and 24 hours, 72 hours and 7 days after aspirin treatment to study platelet function. Participants will be followed up on the study for 7 days. Participants will be followed up in the cardiology clinic within 1-2 weeks after discharge from the hospital, then once a month for six month. Further follow up will be every 6 month. Patients are requested to follow up with cardiology by phone at any time for any bleeding. Participants who are not found to have had a heart attack will not receive any further aspirin treatment. This is an investigational study. Aspirin is an FDA approved drug for treatment of heart attacks and is commercially available. Aspirin is a standard therapy for patients who have had a heart attack. Thirty patients will take part in this study. All will be enrolled at M. D. Anderson.
Thrombocytopenia Myocardial Infarction
Thrombocytopenia Platelet Function Acute Coronary Syndrome Myocardial Infarction Heart Attack Aspirin
null
1
arm 1: None
[ 0 ]
1
[ 0 ]
intervention 1: 325 mg by mouth on Day 1 only, followed by 160 mg by mouth daily
intervention 1: Aspirin
1
Houston | Texas | United States | -95.36327 | 29.76328
0
NCT00501345
[ 3 ]
22
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
false
0ALL
true
The purpose of this study is to determine whether a phospholipid emulsion is effective in the treatment of chronic endotoxemia in hemodialysis patients.
Over 70% of dialysis patients suffer chronically from severe fatigue and tiredness. A possible inciting factor may be high levels of circulating endotoxin, which is well-established as a potent stimulator of inflammatory cytokine release. The source of increased endotoxin in dialysis patients remains unclear, with the most popular hypotheses including back-diffusion of bacterial products from nonsterile dialysate and translocation of bacterial products across what in most dialysis patients is an edematous gut wall. This endotoxin does not appear to be associated with the dialysis procedure itself and indeed, appears to be cleared with some efficiency by the procedure. However, by the next dialysis treatment, endotoxin levels rise rapidly to levels that are in some cases significantly higher than even those measured (via EAA) in patients suffering from septic shock. Although the mechanisms by which dialysis patients tolerate these high endotoxin levels without hemodynamic collapse are not understood, high levels have been shown by The Rogosin Institute to significantly correlate with patient fatigue. Given the potent ability of endotoxin to induce expression of inflammatory cytokines (which in turn are likely responsible for the debilitating symptoms of fatigue and malaise that afflict the majority of the dialysis population), it is logical that binding and inactivation of endotoxin may lead to improved clinical outcomes. Unfortunately, there are no products currently approved for this purpose in dialysis patients. One approach to this problem may be to augment the endogenous systems for endotoxin inactivation. For example, it has been suggested that the various serum lipoprotein fractions may in fact be a physiologic "sink" for endotoxin (and other toxins) via binding with surface phospholipids. Therefore, dialysis patients, who as a population are characterized with hypocholesterolemia and hypolipoproteinemia, are particularly at risk for the deleterious effects of endotoxemia. This has led to the development of "LIPIDOSE," a protein-free phospholipid emulsion. The proposed mechanism of action of this compound is via remodeling of the infused phospholipids into lipoproteins, thereby increasing lipoprotein and phospholipid content and facilitating greater endotoxin binding and neutralization. "LIPIDOSE" has undergone extensive testing in both animals and humans, and has been found to significantly increase serum phospholipid and lipoprotein concentrations, improve survival in a lethal animal model of septic peritonitis, and mitigate the symptoms of endotoxemia in healthy volunteers.
Fatigue End Stage Renal Disease (ESRD)
Fatigue Hemodialysis Endotoxemia Phospholipid Emulsion
null
2
arm 1: Dosage of 1.5 mL/kg of Lipidose over a 2-hour period. arm 2: Dosage of 1.5 mL/kg of Placebo over a 2-hour period.
[ 1, 2 ]
2
[ 0, 0 ]
intervention 1: Over the course of 2 weeks, immediately following subject's three (Monday/Wednesday/Friday (M/W/F)) normal dialysis treatments, based on subject's current weight, subject will receive 1.5 mL/kg of Lipidose over a 2-hour period. intervention 2: Over the course of 2 weeks, immediately following subject's three (M/W/F) normal dialysis treatments, based on subject's current weight, subject will receive 1.5 mL/kg of placebo over a 2-hour period.
intervention 1: Lipidose intervention 2: Placebo
1
New York | New York | United States | -74.00597 | 40.71427
0
NCT00506454
[ 3 ]
35
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
null
This study was designed to evaluate the safety, pharmacokinetic profile and efficacy in Restless Legs Syndrome patients.
null
Restless Legs Syndrome
Restless Legs Syndrome
null
1
arm 1: Subjects will orally take ropinirole CR-RLS tablet(s) once daily 1-2 hours before the onset of RLS symptoms at about the same time of the day. The time of taking ropinirole must be after 16:00.Adjustment of the Ropinirole CR-RLS tablets should be completed after the Week 1 visit up to the Week 10 visit. The dose will be increased at intervals of at least one week until sufficient efficacy is obtained (use "much improved" as a guide) without safety problem. Dose escalation will start at the initial dose 0.5 mg/day to 1 mg/day; after 1 mg/day, the dose will be increased by 1 mg/day to the maximum 6 mg/day.
[ 0 ]
1
[ 0 ]
intervention 1: White film-coated round-shaped tablet
intervention 1: ropinirole controlled release (CR)-RLS
11
Fukuoka | N/A | Japan | 130.41667 | 33.6 Fukuoka | N/A | Japan | 130.41667 | 33.6 Fukuoka | N/A | Japan | 130.41667 | 33.6 Hiroshima | N/A | Japan | 132.45 | 34.4 Kanagawa | N/A | Japan | 139.91667 | 37.58333 Osaka | N/A | Japan | 135.50107 | 34.69379 Osaka | N/A | Japan | 135.50107 | 34.69379 Osaka | N/A | Japan | 135.50107 | 34.69379 Tochigi | N/A | Japan | 139.73333 | 36.38333 Tokyo | N/A | Japan | 139.69171 | 35.6895 Tokyo | N/A | Japan | 139.69171 | 35.6895
0
NCT00530790
[ 4 ]
107
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
false
The purpose of the study is to compare Symbicort pMDI with and without spacer in terms of steroid potency, improvement of lung function and asthma symptoms in children with asthma (6-11 years).
null
Asthma
Symbicort pMDI spacer children
null
2
arm 1: Budesonide/formoterol pMDI 40/2.25ug + spacer arm 2: Budesonide/formoterol pMDI 40/2.25 ug
[ 0, 0 ]
2
[ 0, 0 ]
intervention 1: None intervention 2: None
intervention 1: Budesonide/formoterol pMDI 40/2.25ug + spacer intervention 2: Budesonide/formoterol pMDI 40/2.25 ug
11
Budapest | N/A | Hungary | 19.04045 | 47.49835 Debrecen | N/A | Hungary | 21.62444 | 47.53167 Kaposvár | N/A | Hungary | 17.8 | 46.36667 Bialystok | N/A | Poland | 23.16433 | 53.13333 Bydgoszcz | N/A | Poland | 18.00762 | 53.1235 Bytom | N/A | Poland | 18.93282 | 50.34802 Karpacz | N/A | Poland | 15.75594 | 50.77669 Krakow | N/A | Poland | 19.93658 | 50.06143 Lodz | N/A | Poland | 19.47395 | 51.77058 Warsaw | N/A | Poland | 21.01178 | 52.22977 Moscow | N/A | Russia | 37.61556 | 55.75222
0
NCT00536913
[ 3 ]
707
RANDOMIZED
PARALLEL
0TREATMENT
1SINGLE
false
0ALL
false
The primary objective of this study is to evaluate the efficacy of the combination of mometasone furoate nasal spray (MFNS) and oxymetazoline nasal spray (OXY) given together once a day in treating subjects with seasonal allergic rhinitis (SAR) in relieving symptoms including nasal congestion. The secondary objectives of this study are to evaluate the potential of the combination to produce tachyphylaxis and/or rebound congestion, and to evaluate the safety of the combination.
null
Seasonal Allergic Rhinitis
null
5
arm 1: Mometasone Furoate nasal spray (MFNS) with oxymetazoline nasal spray (OXY) 1 spray once daily arm 2: MFNS with OXY 3 sprays once daily arm 3: MFNS once daily arm 4: OXY twice daily arm 5: Placebo nasal spray
[ 0, 0, 1, 1, 2 ]
5
[ 0, 0, 0, 0, 0 ]
intervention 1: MFNS 2 sprays per nostril with OXY 1 spray per nostril once daily x 2 weeks. Matching placebo to MFNS given every evening (PM). intervention 2: MFNS 2 sprays per nostril with OXY 3 sprays per nostril once daily x 2 weeks. Matching placebo to MFNS given every evening. intervention 3: MFNS 2 sprays per nostril once daily x 2 weeks. Matching placebo to MFNS given every morning (AM) and every evening. intervention 4: OXY 2 sprays per nostril twice daily x 2 weeks. Matching placebo to MFNS given every morning. intervention 5: Matching placebo to MFNS given every morning and every evening x 2 weeks.
intervention 1: OXY combination: mometasone furoate nasal spray (MFNS) and oxymetazoline nasal spray (OXY) intervention 2: OXY combination: mometasone furoate nasal spray (MFNS) and oxymetazoline nasal spray (OXY) intervention 3: mometasone furoate nasal spray (MFNS) once daily intervention 4: oxymetazoline nasal spray (OXY) twice daily intervention 5: Placebo
0
null
0
NCT00552110
[ 4 ]
97
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
null
To determine the convenience and satisfaction of new orally disintegrating tablet formulation (ODT) of lamictal in subjects with a mood disorder. This was a multicenter, open-label study in participants with a mood disorder, who reported difficulty or discomfort in swallowing the currently marketed IR compressed tablet formulation of lamotrigine and who had a person (such as a spouse, partner, companion, aid, nurse, caregiver, etc) willing to complete a Companion/Caregiver Question. Subjects were switched from the currently marketed lamotrigine IR formulation to a matching dose of lamotrigine IR orally disintegrating tablet (ODT) for 3 weeks to determine convenience and satisfaction.
null
Mood Disorders
Mood disorder
null
1
arm 1: Lamictal orally disintegrating tablet (ODT)
[ 0 ]
1
[ 0 ]
intervention 1: Experimental formulation
intervention 1: Lamotrigine
18
San Diego | California | United States | -117.16472 | 32.71571 Santa Ana | California | United States | -117.86783 | 33.74557 Jacksonville | Florida | United States | -81.65565 | 30.33218 Orange City | Florida | United States | -81.29867 | 28.94888 Winter Park | Florida | United States | -81.33924 | 28.6 Marietta | Georgia | United States | -84.54993 | 33.9526 Fairview Heights | Illinois | United States | -89.99038 | 38.58894 Minneapolis | Minnesota | United States | -93.26384 | 44.97997 Saint Charles | Missouri | United States | -90.48123 | 38.78394 Olean | New York | United States | -78.42974 | 42.07756 Raleigh | North Carolina | United States | -78.63861 | 35.7721 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Cleveland | Ohio | United States | -81.69541 | 41.4995 Arlington | Texas | United States | -97.10807 | 32.73569 Houston | Texas | United States | -95.36327 | 29.76328 Houston | Texas | United States | -95.36327 | 29.76328 Norfolk | Virginia | United States | -76.28522 | 36.84681 Charleston | West Virginia | United States | -81.63262 | 38.34982
0
NCT00579982
[ 3 ]
102
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
2MALE
null
We postulate that multiple apoptototic events are indusce through testosterone depletion and repletion with taxotere given in conjunction with androgen withdrawal.
null
Prostate Cancer
Prostate Cancer Docetaxel 03-076
null
2
arm 1: None arm 2: None
[ 0, 1 ]
3
[ 0, 0, 0 ]
intervention 1: Leuprolide LUPRON intervention 2: Starting during week 3 (day 19) of cycle 1, 7.5G applied topically daily for 3 days (applied at approximately 9p) intervention 3: 70 mg/m2 given on day o1 of each 3 week cycle
intervention 1: GnRh (Leuprolide) intervention 2: Testosterone Gel intervention 3: Docetaxel
1
New York | New York | United States | -74.00597 | 40.71427
0
NCT00587431
[ 0 ]
79
RANDOMIZED
PARALLEL
1PREVENTION
4QUADRUPLE
false
0ALL
false
The purpose of this study is determine if subjects with alcohol withdrawal who receive oral baclofen, plus standard benzodiazepine therapy, will experience less severe withdrawal symptoms than those who receive placebo plus standard benzodiazepine therapy.Subjects with alcohol withdrawal syndrome(AWS)who receive baclofen plus standard benzodiazepine therapy will experience fewer complications of AWS (as measured by use of additional sedatives, restraints, and/or intensive care unit \[ICU\] admissions) compared with subjects who receive placebo plus standard benzodiazepine therapy.
Alcohol use is ubiquitous in American society. 83% of Americans have ever consumed alcohol, 51% have in the lst month. The average American consumes 2.18 gallons of ethanol yearly. Alcohol related morbidity and mortality are staggering problems in the USA. Symptoms of alcohol withdrawal occur because alcohol is a central nervous system depressant; abrupt withdrawal unmasks compensatory overactivity of certain parts of the nervous system, including sympathetic autonomic outflow. 5% of patients who undergo alcohol suffer from Delirium Tremors (DTs), a syndrome characterized by hallucinations, disorientation, tachycardia, hypertension, low grade fever, agitation, and diaphoresis. DTs typically begin between 48-96 hours after the last drink and last 1 to 5 days. DTs requires hospitalization and vigorous activity in an ICU setting. The most successful drug treatment for alcohol withdrawal has been found to be the benzodiazepines. Symptom triggered treatment was found to be as effective as a fixed dose treatment to result in less drug being used overall, with a trend toward shorter duration of withdrawal treatment. Baclofen is used orally for the treatment of spasticity resulting from multiple sclerosis, spinal cord injuries/diseases and intrathecally for spasticity related to cerebral palsy, spinal cord injury, and amyotrophic lateral sclerosis (ALS). Its proposed benefit in alcohol withdrawal is that it may reduce voluntary alcohol intake, alcohol craving, and may suppress the intensity of alcohol withdrawal treatment.
Alcohol Withdrawal Delirium
Alcohol withdrawal Delirium tremors
null
2
arm 1: Standard benzodiazepine therapy plus baclofen 10 mg every 8 hours for 72 hours (9 doses) as an inpatient, or until discharge if before 72 hours. arm 2: Standard benzodiazepine therapy plus placebo every eight hous as inpatients for 72 hours or until discharge if less than 72 hours.
[ 1, 2 ]
3
[ 0, 0, 0 ]
intervention 1: Baclofen 10 mg by mouth every 8 hours for 72 hours or until discharge if before 72 hours. intervention 2: Placebo intervention 3: Lorazepam was provided to all subjects (both arms of the study), as indicated by clinical condition. Standard "symptom-triggered dosing" of lorazepam for alcohol withdrawal was used. That is, the size and the frequency of the dose of lorazepam was determined by the severity of the alcohol withdrawal symptoms.
intervention 1: Baclofen intervention 2: Placebo intervention 3: Lorazepam
1
Duluth | Minnesota | United States | -92.10658 | 46.78327
0
NCT00597701
[ 2, 3 ]
4
NA
SINGLE_GROUP
0TREATMENT
0NONE
true
2MALE
false
We propose oral dosing of gastrointestinal permeation enhancement technology \[GIPET\] enhanced oral acyline at 20 mg everyday for one week to determine the steady-state (multiple-dose) pharmacokinetics of oral acyline in four normal, healthy young men.
The purpose of this study is to test how the body responds to a new oral form of acyline given for seven days and to also look at the safety of oral acyline. Acyline temporarily blocks the production of the hormone testosterone in healthy men. It has been tested in over 100 men in an injection form. This study will be testing acyline in a pill form for seven days. This study may help develop an oral form of testosterone-blocker which may be useful in the treatment of diseases such as prostate cancer, premature puberty and possibly in a male contraceptive. This study will evaluate a single dose of oral acyline given once a day for seven days and subsequent effects on Testosterone, FSH and LH blood serum concentrations.
Healthy
Male Contraception Acyline
null
0
null
null
1
[ 0 ]
intervention 1: 20 mg GIPET enhanced oral dose, daily for 7-days
intervention 1: Acyline
1
Seattle | Washington | United States | -122.33207 | 47.60621
0
NCT00603187
[ 4 ]
82
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
true
The purpose of this study is to determine the safety and effectivess of a single intramuscular injection of peramivir for the treatment of subjects with acute, uncomplicated influenza.
null
Influenza
Influenza Subjects with uncomplicated acute influenza
Prot_SAP_000.pdf: CLINICAL STUDY PROTOCOL Protocol No. BCX1812-311 IND No. 76,350 A PHASE 3 MULTICENTER, RANDOMIZED, DOUBLE BLIND, PLACEBO- CONTROLLED STUDY TO EVALUATE THE EFFICACY AND SAFETY OF INTRAMUSCULAR PERAMIVIR IN SUBJECTS WITH UNCOMPLICATED ACUTE INFLUENZA THE IMPROVE 1 STUDY (IntraMuscular Peramivir for the Relief Of symptoms and Virologic Efficacy) Short title: Intramuscular Peramivir for the Treatment of Uncomplicated Influenza Protocol Date: Version1.0: 24 August-2007 BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35244, USA Phone: +1 919 859 1302 Fax: +1 919 851 1416 The document contains trade secrets and proprietary information of BioCryst Pharmaceuticals, Inc. This information is confidential property of BioCryst Pharmaceuticals, Inc., and is subject to confidentiality agreements entered into with BioCryst Pharmaceuticals, Inc. No information contained herein should be disclosed without prior written approval. CONFIDENTIAL 157 157 BCX1812-311 (V1.0: 24-August-2007) Page 2 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1 TITLE PAGE Protocol Number: BCX1812-311 Study Title: A phase 3 m ulticenter, random ized, double-blind, placebo-controlled s tudy to evaluate th e effic acy and safety of intram uscular peram ivir in subjec ts with uncomplicated acute influenza IND Number: 76, 350 Investigational Product: Peramivir (BCX1812) Indication Studied: Uncomplicated acute influenza Sponsor: BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35233 Development Phase: 3 Sponsor Medical Officer: W. James Alexander, M.D., M.P.H. Senior Vice President, Clinical and Regulatory Operations Chief Medical Officer Phone: +1 919 859 1302 Fax: +1 919 851 1416 Email Address: jalexander@biocryst.com Compliance Statement: This study will be conducted in accordance with the ethical principles that have their origin in the Declaration of Helsinki and clinical research guidelines established by the Code of Federal Regulations (Title 21, CFR Parts 50, 56, and 312) and ICH Guidelines. Essential study documents will be archived in accordance with applicable regulations. Final Protocol Date: Version 1.0: 24-August-2007 Amendment(s) Date(s): None 158 158 159 159 BCX1812-311 (V1.0: 24-August-2007) Page 4 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1.2 Clinical Study Protocol Agreement Protocol No. BCX1812-311 Protocol Title: A phase 3 m ulticenter, random ized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peram ivir in subje cts with unc omplicated acute influenza I have caref ully read th is protoco l and agree that it contains all of the necessary information required to conduct this study. I agree to conduct this study as described and according to the Declaration of Helsinki, International Conference on Harmonization Guidelines for Good Clinical Practices, and all applicable regulatory requirements. Investigator’s Signature Date Name (Print) 160 160 BCX1812-311 (V1.0: 24-August-2007) Page 5 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 2 SYNOPSIS Protocol No. BCX1812-311 Protocol Title: A Phase 3, Multicenter, Random ized, Double-Blind, Placebo-Controlled Stu dy to Evaluate the Efficacy an d Safety of Intram uscular Peram ivir in Subjects with Uncomplicated Acute Influenza Sponsor: BioCryst Pharmaceuticals, Inc. Investigators/Study Sites: Multinational Development Phase: 3 Objectives: Primary: To evaluate the efficacy of peram ivir adm inistered intramuscularly com pared to p lacebo on th e tim e to alleviation of clinica l sym ptoms in adult sub jects with uncomplicated acute influenza. Secondary: 1. To evalua te the saf ety and tolera bility of pe ramivir administered intramuscularly; 2. To evaluate seconda ry clinical outcom es in response to treatment; 3. To evaluate changes in in fluenza virus titer (viral shedding) in response to treatment; 4. To assess p harmacoeconomic m easures in resp onse to treatment 5. To assess c hanges in inf luenza vir al suscep tibility to neuraminidase inhibitors following treatment Number of Subjects: Total enrollm ent: up t o 800 subjects random ized (160 subjects in the placebo treatment group, 320 subjects in the peramivir 150mg treatment group and 320 subjects in the peramivir 300m g treatm ent group). The study will close after enrollment of at least 500 subjects who have either a positive Influenza A or B antigen te st (Rapid Antigen Test – RAT) at screening, or who ha ve a negative RAT at screening but a positive influenza A or B PCR a ssay result from a baseline nasopharyngeal swab. Study Design: This is a multinational, random ized, double-blind study comparing the efficacy and safety of two single dos e regimens of peramivir administered intramuscularly versus placebo in adults with uncom plicated acute influenza. Each subjec t’s ass ignment to trea tment will be stra tified according to the Rapid Antigen Test (RAT) result at screening and current sm oking be havior, with 80% of subjects ce ntrally rand omized to one of the two activ e 161 161 BCX1812-311 (V1.0: 24-August-2007) Page 6 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL single dose regimens of peramivir (2:2:1 randomization) Treatment Group 1: Peramivir 150mg Treatment Group 2: Peramivir 300mg Treatment Group 3: Placebo Enrollment of subjects into the RAT negative s tratum will be permitted at individual sites that have identified 3 RAT positive su bjects a t s creening within a 10 d ay per iod, indicating activity of influenza in the site ’s vicinity. After identification of 3 RAT positive subjects within 10 days, a site m ay enroll 1 RAT negative s ubject tha t f ulfills the inclusion/ exclusion criteria. One additional RAT negative subject may be enrolled thereafter for each preceding RAT positive subject that is identified. Study drug will be adm inistered as one 2mL intramuscular injection in each glu teal muscle (total of 4m L injected in divided doses). Subjects eligible for s creening will have an anterior nasal or pharyngeal swab collected for t esting by RAT for influenza A and B, in accordan ce with the co mmercially available RAT kit instructi ons. I f the in itial RAT is negative, th e te st shou ld be repeated with a differen t commercially availab le RAT kit. Subjects m eeting the inclusion/ exclusion criteria may be enrolled into the study. All enrolled subjects will record the following in a Study Diary: • Oral temperature measurements taken with an electronic thermometer every 12 hours. W ith the exception of the baseline m easurement, all tem perature m easurements will be ob tained at least 4 hours after, or imm ediately before, adm inistration of oral acetaminophen (paracetamol), aspirin, ibuprofen or other NSAID. • Assessment of severity of each of s even sym ptoms of influenza on a 4-point scale (0, absent; 1, m ild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatm ent, then once daily (AM) through Day 14 • Assessment of subjec t’s ability to p erform usual activities, (rated as 0–10 on a visual analog scale) once daily through Day 14 • Assessment of subject’s tim e lost from work or usual activities and productivity compared to normal (rated as 162 162 BCX1812-311 (V1.0: 24-August-2007) Page 7 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 0-10 on a visual analog scal e) once daily through Day 14 • Doses of antipyretic, expe ctorant, and/ or t hroat lozenges taken for symptomatic relief each day through Day 14 Anterior nose (bilateral) and posterior pharynx specim ens (swabs) will be collected at Day 1 (pre-treatm ent) and at Days 3, 5, and 9, for quantitative virologic assessments. In a subset of a m inimum of 200 subjects, an additional virology sample will b e co llected on day 2. Specim ens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result). All virolog ic ass essments will b e p erformed by a c entral laboratory. At the study day 3 visit, when all subjects are evaluated for safety and a blood draw is com pleted for clinical laboratory investigations, a single pharm acokinetic (PK) sample will also be drawn. This sin gle PK sam ple will b e analyzed for plasm a concentrations of peram ivir (ng/mL) and evaluated in an exposure response analysis. At selected sites a separate sub-s tudy will be conducted to collect limited PK sam ples for the purpose of conducting an exposure-respons e analysis. T his sub-stud y will be conducted under a separate protocol, BCX1812-311PK. Study Population: Male and fem ale subjects, 18 y ears of age and older, with symptoms consisten t with a diagnosis of uncomplicated acute influenza infectio n may be screened for e nrollment. Subject eligibility will be dependent on the presence of two or more symptoms consistent with acute inf luenza as well as the results obtained f rom a rapid antigen test (RAT) for influenza A and B at screening. Inclusion Criteria: 1. Male and non-pregnant female subjects age ≥18 years 2. A positive Influenza A or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate specimen collected from an anterior nasal or pharyngeal swab, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated with a different commercially available RAT kit. A limited number of RAT negative 163 163 BCX1812-311 (V1.0: 24-August-2007) Page 8 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subjects may be enrolled in accordance with a defined screening algorithm. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. For subjects with a positive RAT at the time of screening, a subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at time of screening. For subjects with no positive RAT at screening, fever as defined above must be documented at time of screening 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of any severity (mild, moderate, or severe) 5. Presence of at least one constitutional symptom (myalgia [muscle aches], headache, feverishness, or fatigue) of any severity (mild, moderate, or severe) 6. Onset of symptoms no more than 48 hours before presentation for screening 7. Written informed consent Exclusion Criteria: 1. Women who are pregnant or breast-feeding 2. Presence of clinically significant signs of acute respiratory distress 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class IV functional status within the past 12 months 5. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min) 6. Current clinical evidence of active bacterial infection at any body site that requires therapy with oral or systemic antibiotics 7. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy 8. Current treatment for active viral hepatitis C 9. Presence of known HIV infection with a CD4 count <350 cell/mm3 10. Current therapy with oral warfarin or other systemic anticoagulant 11. Receipt of any doses of rimantadine, amantadine, 164 164 BCX1812-311 (V1.0: 24-August-2007) Page 9 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL zanamivir, or oseltamivir in the 7 days prior to screening 12. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days 13. History of alcohol abuse or drug addiction within 1 year prior to admission in the study 14. Participation in a previous study of peramivir as treatment for acute influenza or previous participation in this study 15. Participation in a study of any investigational drug within the last 30 days 16. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. Study Endpoints: Primary Endpoint: Clinical: Time to alleviation of clinical symptoms of influenza Secondary Endpoint(s): Safety Incidence of treatm ent-emergent adverse events and treatment-emergent changes in clinical laboratory tests Clinical: Time to resum ption of subjec t’s ab ility to perf orm usual activities Time to resolution of fever Incidence of influenza related complications Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID 50) and/or by quantitative polymerase chain reaction (PCR) assay Pharmacoeconomic: Medical resource utilization (M RU), missed days of work, and im pact of inf luenza illn ess on subject’s work performance and/or productivity. Exploratory Endpoint: Viral Susceptibility: Change in influenza virus susceptibility to neu raminidase inhibitors Investigational Product, Dose, and Mode of Administration: Peramivir (BCX-1812), 75m g/mL or placebo (buffered diluent), 2mL per injection, ad ministered intramuscularly in the gluteal muscle, bilaterally. Duration of Treatment: Following treatment on day 1, study duration for individual 165 165 BCX1812-311 (V1.0: 24-August-2007) Page 10 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subjects is expected to be up to 14 days (including all visits). Statistical Methods: Descriptive statistical methods will be used to summ arize the data from this study, with statistical testing utilized for the p rimary and secondary efficacy endpoints. Unless otherwise n oted, a ll s tatistical testing will be two-sided, and will be performed using a significance (alpha) level of 0.05. For assessment of the prim ary efficacy endpoint, th e overall sig nificance level will be m aintained by a Bonferroni adjustm ent fo r the planned com parisons between the two active trea tment groups and placebo. Detailed sta tistical pro cedures will be provided in a f ull statistical analysis plan (SAP) completed prior to database lock and study unblinding. Sample Size: From previous studies of neuram inidase treatm ent of uncomplicated influenza it is expected that the median time to alleviation of symptoms will be 103.3 hours for subjects receiving placebo. Addition ally, it is expected that the median time to alleviation for the low dose peram ivir arm will be 69.9 hours, yielding a hazard ratio of 0. 68. Using these assumptions, a sample si ze of 200 influenza-infected subjects per active treatm ent group and 100 infected subjects in the placebo group (a total of 500 influenza- infected su bjects) is s ufficient to provide at least 80% power to detect a hazard ratio of 0.68 using a log-rank statistic and α = 0.025 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). Up to 800 subjects will be enrolled to ach ieve the target number of at least 500 subjects with diagnostic evidence (R AT or PCR) of an acute influenza infection. Efficacy: The intent-to-treat infected population will include all subjects who are random ized, received study drug, and have proven influenza by any one of the following: primary viral culture, PCR, or paired serology showing ≥ 4-fold increase in antibody to influenza A or B. The primary efficacy v ariable is th e tim e to alleviation of symptoms, defined as the time from injection of study drug to the start of the tim e period when each of seven symptoms of influenza are either absent or are present at no more than mild severity level and remain at no worse than this severity status for a 24 hour period. Descriptive statistics for the primary efficacy variable will 166 166 BCX1812-311 (V1.0: 24-August-2007) Page 11 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL be tabulated by treatm ent group. Alleviation of sym ptoms will be determined by assessment of symptoms as reported on each su bject’s diary card. Tim e to alle viation of symptoms will b e sum marized for each treatm ent group. Treatment dif ference will be as sessed us ing a Cox Regression model with effects for RAT result at screening, current smoking behavior, tr eatment group, and influenza season at random ization. Pa irwise com parisons between each active group and placebo will be constructed from the Cox Regression m odel. Subj ects who do not experience alleviation of sym ptoms will be c ensored a t the date of their last non-m issing assessment. Tim e to resum ption of usual activities and tim e to resolution of f ever will be analyzed in a similar manner. Changes in viral titer s will be compared using the van Elteren sta tistic con trolling f or RAT result at screen ing, current smoking behavior and influenza season at randomization. Analyses of other continuous endpoints will be analyzed in a similar manner. Safety: Safety analyses will b e presen ted f or all sub jects in the safety population, defined as all randomized subjects who receive at least one dose of study drug. Adverse events will be m apped to a Medica l Dictiona ry f or Regulatory Activities (MedDRA) preferred term and system organ classification. The occurrence of treatm ent-emergent AEs will be summarized using preferre d term s, system organ classifications, and severit y. Separate summ aries of treatment-emergent SAEs and treatm ent-emergent AEs that are related to study m edication will be generated. All AEs will be listed f or individua l subjec ts sho wing both verbatim and preferred terms. Descriptive summaries of vital signs and quantitative clinical laboratory changes will be presented by study visit. Frequency and percentages of subjects with abnorm al laboratory test r esults will be su mmarized b y toxic ity grade. Concomitant m edications w ill be m apped to a W HO preferred term and drug classification. The num ber and percent of subjects taking concomitant medications will be summarized using preferred terms and drug classifications. The num ber and percent of subjects experiencing each 167 167 BCX1812-311 (V1.0: 24-August-2007) Page 12 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL abnormal physical examination finding will be presented. The number and percent of s ubjects discontinuing study as well as the reasons for discontinuation will be summarized by treatment group. Protocol Date Version 1.0: 24-August-2007 168 168 BCX1812-311 (V1.0: 24-August-2007) Page 13 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 3 TABLE OF CONTENTS 1 TITLE PAGE...................................................................................................... 2 1.1 PROTOCOL APPROVAL SIGNATURE PAGE............................................................. 3 1.2 CLINICAL STUDY PROTOCOL AGREEMENT .......................................................... 4 2 SYNOPSIS.......................................................................................................... 5 3 TABLE OF CONTENTS.................................................................................. 13 3.1 LIST OF FIGURES................................................................................................ 15 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS................... 16 5 INTRODUCTION ............................................................................................ 18 5.1 BACKGROUND.................................................................................................... 18 5.2 RATIONALE FOR STUDY..................................................................................... 18 5.3 NON-CLINICAL EXPERIENCE WITH PERAMIVIR.................................................. 19 5.3.1 In vitro Assays .............................................................................................. 19 5.3.2 Animal Models.............................................................................................. 20 5.4 PREVIOUS PHASE 3 CLINICAL EXPERIENCE WITH ORAL PERAMIVIR.................. 20 5.5 PREVIOUS PHASE 1 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR................ 21 5.6 DOSE RATIONALE .................................................................................................... 22 6 STUDY OBJECTIVES..................................................................................... 23 6.1 OBJECTIVES ....................................................................................................... 23 6.1.1 Primary Objective......................................................................................... 23 6.1.2 Secondary Objective(s)................................................................................. 23 6.2 STUDY ENDPOINTS............................................................................................. 23 6.2.1 Primary Endpoint.......................................................................................... 23 6.2.2 Secondary Endpoint(s).................................................................................. 23 6.2.3 Exploratory Endpoint.................................................................................... 23 7 STUDY DESIGN ............................................................................................. 24 7.1 OVERALL STUDY DESIGN AND PLAN ................................................................. 24 8 SELECTION AND WITHDRAWAL OF SUBJECTS.................................... 25 8.1.1 Inclusion Criteria .......................................................................................... 25 8.1.2 Exclusion Criteria ......................................................................................... 26 8.1.3 Removal of Subjects from Therapy or Assessment...................................... 27 9 TREATMENTS................................................................................................ 28 9.1 TREATMENTS ADMINISTERED............................................................................ 28 9.2 IDENTITY OF INVESTIGATIONAL PRODUCT(S) .................................................... 28 9.3 METHOD OF ASSIGNING SUBJECTS TO TREATMENT GROUPS ............................. 28 9.4 STUDY MEDICATION ACCOUNTABILITY............................................................. 29 9.5 BLINDING/UNBLINDING OF TREATMENTS.......................................................... 29 9.6 PRIOR AND CONCOMITANT THERAPIES.............................................................. 29 9.7 OVERDOSE AND TOXICITY MANAGEMENT......................................................... 29 9.8 DOSE INTERRUPTION.......................................................................................... 29 10 STUDY CONDUCT......................................................................................... 29 10.1 EVALUATIONS.................................................................................................... 30 10.1.1 Medical History ........................................................................................ 30 10.1.2 Rapid Antigen Test for Influenza ............................................................. 30 10.1.3 Physical Examination and Influenza-related Complications Assessments30 169 169 BCX1812-311 (V1.0: 24-August-2007) Page 14 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.4 Vital Signs................................................................................................. 30 10.1.5 Electrocardiogram Measurements ............................................................ 31 10.1.6 Clinical Chemistry Profiles....................................................................... 31 10.1.7 Hematology Profiles ................................................................................. 31 10.1.8 Serology for Influenza .............................................................................. 31 10.1.9 Urinalysis and Evaluation of Protein in Urine.......................................... 31 10.1.10 Urine Pregnancy Test................................................................................ 31 10.1.11 Samples for Virologic Laboratory Assessments....................................... 31 10.1.12 Subject Self Assessments.......................................................................... 32 10.1.13 Concomitant Medications......................................................................... 32 10.1.14 Adverse Events ......................................................................................... 32 10.1.15 Single Pharmacokinetic Exposure Sample ............................................... 33 10.2 SCREENING ........................................................................................................ 33 10.2.1 Informed Consent...................................................................................... 33 10.2.2 Screening/Baseline Evaluation and Enrollment........................................ 33 10.3 TREATMENT PERIOD—STUDY DAY 1................................................................ 33 10.3.1 Pre-dose Evaluations................................................................................. 34 10.4 POST-TREATMENT ASSESSMENT PERIOD........................................................... 34 10.4.1 Days 2, 3, 5, 9 and 14................................................................................ 34 11 ADVERSE EVENT MANAGEMENT............................................................ 37 11.1 DEFINITIONS ...................................................................................................... 37 11.1.1 Adverse Event........................................................................................... 37 11.1.2 Serious Adverse Event.............................................................................. 37 11.2 METHOD, FREQUENCY, AND TIME PERIOD F OR DETECTING ADVERSE EVENTS AND REPORTING SERIOUS ADVERSE EVENTS..................................................... 38 11.2.1 Definition of Severity ............................................................................... 38 11.2.2 Definition of Relationship to Study Drug................................................. 38 11.2.3 Reporting Serious Adverse Events ........................................................... 39 11.2.4 Emergency Procedures.............................................................................. 40 12 STATISTICAL METHODS............................................................................. 40 12.1 DATA COLLECTION METHODS........................................................................... 40 12.2 STATISTICAL ANALYSIS PLAN ........................................................................... 41 12.3 SAMPLE SIZE ESTIMATES................................................................................... 41 12.4 ANALYSIS POPULATIONS ................................................................................... 41 12.4.1 Intent-To-Treat Population ....................................................................... 41 12.4.2 Intent-To-Treat Infected Population ......................................................... 41 12.4.3 Safety Population...................................................................................... 42 12.5 INTERIM AND END OF STUDY ANALYSES........................................................... 42 12.6 EFFICACY ANALYSES......................................................................................... 42 12.6.1 Primary Efficacy Endpoint ....................................................................... 42 12.6.2 Secondary Efficacy Endpoints.................................................................. 43 12.6.3 Exploratory Endpoint................................................................................ 44 12.7 SAFETY ANALYSES ............................................................................................ 44 12.8 SUB-STUDY AND PHARMACOKINETIC ANALYSIS............................................... 45 12.9 GENERAL ISSUES FOR STATISTICAL ANALYSIS .................................................. 45 12.9.1 Multiple Comparisons and Multiplicity.................................................... 45 170 170 BCX1812-311 (V1.0: 24-August-2007) Page 15 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.9.2 Covariates ................................................................................................. 45 12.9.3 Planned Sub-Groups ................................................................................. 45 12.9.4 Missing Data............................................................................................. 45 13 STUDY ADMINISTRATION ......................................................................... 46 13.1 REGULATORY AND ETHICAL CONSIDERATIONS ................................................. 46 13.1.1 Regulatory Authority Approvals............................................................... 46 13.1.2 Ethics Committee Approvals.................................................................... 46 13.1.3 Subject Informed Consent......................................................................... 46 13.1.4 Payment to Subjects.................................................................................. 47 13.1.5 Investigator Reporting Requirements ....................................................... 47 13.2 STUDY MONITORING.......................................................................................... 47 13.3 QUALITY ASSURANCE........................................................................................ 47 13.4 STUDY TERMINATION AND SITE CLOSURE......................................................... 48 13.5 RECORDS RETENTION ........................................................................................ 48 13.6 STUDY ORGANIZATION...................................................................................... 48 13.6.1 Data Monitoring Committee..................................................................... 48 13.7 CONFIDENTIALITY OF INFORMATION ................................................................. 48 13.8 STUDY PUBLICATION ......................................................................................... 49 14 REFERENCES ................................................................................................. 50 15 APPENDICES .................................................................................................. 52 15.1 NYHA FUNCTIONAL CLASSIFICATION CRITERIA: HEART FAILURE AND ANGINA .......................................................................................................................... 52 3.1 List of Figures Figure 1 Study Measurements and Visit Schedule...................................................... 36 171 171 BCX1812-311 (V1.0: 24-August-2007) Page 16 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS AE adverse event ALT alanine aminotransferase AST aspartate aminotransferase AUC area under the curve AUC0–72 area under the curve from time 0 to 72 hours AUC0–∞ area under the curve extrapolated from time 0 to infinity CBC complete blood count CDC Centers for Disease Control and Prevention Cmax maximum plasma concentration CK creatine kinase CNS central nervous system COPD chronic obstructive pulmonary disease CRF Case Report Form CV coefficient of variation ECG Electrocardiogram GCP Good Clinical Practice HCG human chorionic gonadotropin HIV Human immunodeficiency virus IC50 median inhibitory concentration ICF informed consent form ICH International Conference on Harmonization IEC Independent Ethics Committee IRB Institutional Review Board IRC influenza related complications ITT intent-to-treat ITTI intent-to-treat infected IUD intrauterine device IVRS interactive voice response system LDH lactate dehydrogenase MedDRA Medical Dictionary for Regulatory Activities MRU medical resource utilization NSAID non-steroidal anti-inflammatory drug PCR polymerase chain reaction 172 172 BCX1812-311 (V1.0: 24-August-2007) Page 17 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL RAT Rapid Antigen Test RBC red blood cell SAE serious adverse event SAP statistical analysis plan SD standard deviation t1/2 elimination half-life t1/2 λz terminal half-life TCID50 time weighted change f rom baseline in log 10 tissue -culture infective dose50 TEAEs treatment-emergent adverse events Tmax time to attain maximum plasma concentration UPEP urine protein electrophoresis WBC white blood cell WHO World Health Organization 173 173 BCX1812-311 (V1.0: 24-August-2007) Page 18 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5 INTRODUCTION 5.1 Background Influenza v irus is a m ember of the orthomyxovirus fam ily and cau ses an acu te v iral disease of the respiratory tract. Typical influenza illness is characterized by abrupt onset of fever, headache, myalgia, sore throat, and nonproductive cough.1 The illness is usually self-limiting, with relief of symptoms occurring within 5 to 7 days. Nevertheless, it is an important disease for several reasons, including ease of comm unicability, short incubation time, rapid rate of viral mutation, morbidity with resultant loss of productivity, risk of com plicating conditions, and increased risk of death, pa rticularly in the e lderly. During 19 of the 23 influenza seasons between 1972/1973 a nd 1994/1995, estim ated influenza-associated deaths in the U nited States ranged from approxim ately 25 to m ore than 150 per 100,000 persons above 65 years of age, accounting for more than 90% of the deaths attributed to pneumonia and influenza.2 Presently, o nly a few m easures are availab le that can red uce th e im pact of influenza: active immunoprophylaxis with an inactivat ed or live attenu ated vaccine and chemoprophylaxis or therapy with an influe nza-specific antiviral drug. Neuram inidase inhibitors are the current m ainstay of an tiviral treatm ent for influenza. Mark eted neuraminidase inhib itors inc lude zanam ivir (Relenza®, GlaxoSm ithKline) an d oseltamivir (Tamiflu®, Roche-Gilead) , an oral prodrug of the activ e agent, oseltamivir carboxylate. Influenza neuram inidase is a surface glycoprotei n that cleaves sialic acid residues from glycoproteins and glycolipids. The enzyme is responsible for the release of new viral p articles from infected cells and may also ass ist in the sp reading of virus through the mucus within the respiratory tract. The neuraminidase inhibitors represent an important advance in the treatment of influenza with respect to activity against influenza A and B viruses, with p roven therapeutic value in reduc ing influenza lower resp iratory complications,3 and lower rates of antiviral drug resistance4. The use of curren tly av ailable neu raminidase inhibitors has been lim ited by concerns including, the degree of effectiv eness, the requirement for an inhaler device (zanamivir), and the em ergence of resistant influenza vi rus variants in som e treated populations. 5 In addition, there are risks of bronchospasm w ith zanam ivir; and gastrointestinal side effects, with oseltamivir. Peramivir is a neuraminidase inhibitor that represents a potentially promising addition to the armamentarium of drugs for the treatment of influenza infections due to its potential for parenteral administration and lower frequency of dosing. 5.2 Rationale for Study An oral formulation of peram ivir has previously been evaluated in a f ull range of safety, tolerability, pharmacokinetic, and efficacy studies. In a m ultinational phase 3 clinical trial conducted in 1999-2001, oral peram ivir de monstrated antiviral activity against influenza A and B inf ections, and im provement in the r elief of clin ical sym ptoms. Because of the lim ited bioavailability of peramivir following oral administration (<5%), it was de termined that the paren teral route of administration is m ore appropriate for the 174 174 BCX1812-311 (V1.0: 24-August-2007) Page 19 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL delivery of peram ivir. Subsequent phase 1 studies of intrave nous and intram uscular formulations of peram ivir have confirm ed that parenteral routes of administration result in plasma levels of drug that are as much as 100 times those achieved via the oral route. Further details of these studies are provided below and in the Investigator Brochure. A phase 2 random ized, double blind, placeb o controlled study of two single dose regimens (150mg or 300m g) of intram uscular peramivir in subjects with uncom plicated acute influenza infections (study B CX1812-211) was initiated in early 2007 in North America and the UK. The study has been extended to sites in Hong Kong, Australia, New Zealand and South Africa and is expected to complete enrollment in m id-2007. At a scheduled meeting on 21 May 2007, an independ ent data monitoring committee for this study com pleted a blinded revi ew of all reported adverse events and grade 3 and 4 clinical laboratory evaluations from the first 135 subjects random ized. Following this blinded saf ety review the DMC provided a written reco mmendation that the s tudy continue as planned. Because of the previo us dem onstration of significant an tiviral activ ity, th e strong suggestion of clinical efficacy of oral pe ramivir previously dem onstrated in acute influenza, and the encouraging pharm acokinetic and prelim inary safety profile of the intramuscular formulation of pera mivir demonstrated to date, this phas e 3 study will be conducted to evaluate the efficacy and safety profile of intram uscular peramivir and to determine the optimal single dose regimen. 5.3 Non-Clinical Experience with Peramivir 5.3.1 In vitro Assays Peramivir is a selective inhibitor of vi ral neuram inidase, with 50% inhibitory concentrations (IC50) for bacterial and m ammalian enzymes of >300µM. 6 In an in vitro study, 42 influenza A and 23 influenza B isolates were collected from untreated subjects during the 1999–2000 influenza season in Canada. 7 These isolates were tested for their susceptibility to the neuram inidase inhib itors zanam ivir, oseltam ivir carboxylate, and peramivir using a chem iluminescent neuram inidase assay. Inhibition of Type A influenza neuraminidase by peram ivir was appr oximately an order of m agnitude greater than inhibition of neuram inidase from Type B viruses. IC 50 values for the Type A enzymes ranged from <0.1 to 1.4nM, whereas the Type B enzym es ranged from <0.1 to 11nM, with three out of four values in the 5- to 11nM range. Peram ivir was the most potent drug against influenza A (H 3N2) viruses with a m ean IC50 of 0.60nM as well as most potent against influenza B with a mean IC50 of 0.87nM. In another in vitro comparison of peram ivir, oseltam ivir, and zanam ivir, using a neuraminidase inhibition assay with influenza A viruses, the m edian IC 50 of pera mivir (approximately 0.34nM) was com parable to that of oseltam ivir (0.45nM) and significantly lower than zanam ivir (0.95nM). F or influenza B virus clinical isolates, the IC50 of peramivir (1.36nM) was comparable to that of zanamivir (2.7nM) and lower than that of oseltamivir (8.5nM).8 The potency of peram ivir was evaluated ag ainst five zanam ivir-resistant an d six oseltamivir-resistant influenza viruses.9 Peramivir remained a potent inhibitor against all 175 175 BCX1812-311 (V1.0: 24-August-2007) Page 20 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL oseltamivir-resistant viruses includi ng the m utations H274Y, R292K, E119V, and D198N, with IC 50 values ≤40nM. Peram ivir also potently inhibited (IC 50 ≤ 26nM) the neuraminidase activity of zanamivir-resistant strains, which had the following mutations: R292K, E119G, E119A, and E119D. Howeve r, one zanam ivir-resistant influenza B virus, B/Mem /96, with a m utation R152K isol ated from cell cultur e, was relatively resistant to all neuraminidase inhibitors, including peramivir (IC50 = 400nM). 5.3.2 Animal Models In a m ouse model of influen za infection, a single intram uscular injection of pera mivir (10mg/kg) given 4 hours prior to inoculation with an A/NWS/33 (H1N1) influenza strain resulted in 100% survival in contrast to 100% mortality in a control group injected with saline.6 In the sam e mouse m odel, treatm ent of m ice up to 72 hours after influenza infection using peram ivir (20m g/kg) result ed in 100% survival, compared to 100% mortality in the control group injected with vehicle.10 Peramivir has also dem onstrated activity in animal models utilizing a clinical H5 N1 isolate as th e infecting virus strain. In a mouse model, a single intramuscular dose of peramivir (30mg/kg) injected 1 hour after inoculation with the highly pathogenic (H5N1) A/Vietnam/1203/04 strain, resulted in a 70% survival rate that wa s similar to that seen in mice treated with oseltam ivir given orally at 10m g/kg/day for 5 days 11. In s imilar experiments, mice inoculated with the sam e strain of H5N1 virus tha t were then trea ted for up to 8 days with intram uscular peramivir exhibited 100% survival 12. This longer duration of peram ivir treatment also prevented viral replic ation in the lungs, brain and spleen at days 3, 6 and 9 post inoculation. 5.4 Previous Phase 3 Clinical Experience with Oral Peramivir An oral formulation of peram ivir has prev iously dem onstrated an tiviral activity and preliminary clinical efficacy in ch allenge studies in hum an volunteers, as well as in treatment studies in patients with u ncomplicated acute inf luenza inf ections dur ing the influenza seasons of 1999-2001. A Phase 3 multinational study (B C-01-03) of oral peramivir was conducted. Two dos e regimens of oral peramivir, 800mg QD for 5 days, or 800mg QD on Day 1, followed by 400mg QD for 4 days, were compared to a matched placebo treatment group. A total of 1246 subjects were randomized to treatment at sites in the USA, W estern and Eastern Europe, S outh America, Australia and New Zealand. As presente d in the tab le below, th e prim ary end-point of tim e to relief of influenza symptoms was not found to be significantly different (p=0.17) between the three treatment groups.13 A sub-group analysis of the time to relief of symptoms by country or region demonstrated marked differences in the prim ary endpoint.. In the subset of influenza-infected subjects enrolled at sites in the US, clinically m eaningful differences in time to relief of influenza symptoms between the placebo and the two peram ivir arms were observed, that just m issed statistical significance (p=0.07). However, a num ber of secondary end-points in this phase 3 study, such as tim e to overall well-being, time to normal activity, incidence of infl uenza rela ted com plications and quantity of viral shedding, reached o r approach ed statistically significant differenced between the peramivir and placebo treatment groups (p=0.03-0.06). 176 176 BCX1812-311 (V1.0: 24-August-2007) Page 21 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Results of Study BC-01-03 Median Time to Relief of Influenza Symptoms (Hours) Dose and Regimen Overall Results (n=1246) US Sites (n=206) Peramivir 800mg po x 5d 89.0 70.8 Peramivir 800mg po x 1d and 400mg po x 4d 91.7 88.8 Placebo x 5 days 104.4 106.8 p value 0.17 0.07 5.5 Previous Phase 1 Experience with Intramuscular Peramivir Two phase one studies evaluating the safety and pharmacokinetics of an intram uscular formulation of pera mivir have been conduc ted in a total of 45 he althy volunteers receiving peramivir. Study Peramivir-Him-06-111 evaluated the single dose pharmacokinetics and tolerability of 75mg, 150mg and 300mg doses of peramivir administered as intramuscular (i.m.) and intravenous (i.v.) injections in a crossover design (9 subjects per group). Peak plasma levels of i.m. pera mivir generally occurre d within 30 m inutes fol lowing injection. Plasma pharm acokinetic param eters for i.m . peram ivir are summarized below for the three intramuscular single dose regimens evaluated: Dose (mg) Cmax (ng/mL) AUC0-∞ (hr·ng/mL) t½a (hr) 75 i.m. 4296±812 11659±1123 19.8±7.9 150 i.m. 7612±884 23952±3804 24.3±4.1 300 i.m. 15150±2367 49649±5619 22.8±2.5 aterminal half life In a second phase 1 study, Peram ivir-Him-06-112, the sam e dose levels of peram ivir were adm inistered as single i.m . injections on two consecutive days (6 subjects per group). This double-b lind study also includ ed a placebo arm . The pharm acokinetic parameters of i.m . peramivir following the second day of dosing were consistent with those seen following single doses of the drug. The observ ations of s afety and to lerability of i. m. peram ivir in each of the 2 phas e 1 studies were unrem arkable. No serious ad verse even ts were repo rted. The most commonly observed ad verse events or laborato ry abnormalities were h eadache, several reports of signs and symptom s of vasovagal reactions following injections, and transient increases in creatine kinase. No consisten t differences in frequency of adverse events were observed between the ac tive and placebo treatm ent groups, with the exception that CK elevations appeared to be dose rela ted in the peram ivir treatment groups. T he vasovagal reactions were attri buted to the receipt of rela tively large volum es of i.m. injection (2 injections each of 2mL) in the fasted state. 177 177 BCX1812-311 (V1.0: 24-August-2007) Page 22 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL An ongoing phase 2 study, BCX1812-211, is a random ized, double-blind placebo- controlled study to evaluate the efficacy and safety of two single d ose reg imens of peramivir. Up to 100 subjects per arm will receive either 150mg or 300mg of peramivir or placebo. The prim ary endpoint of the stu dy is the tim e to alleviation of clinical symptoms in adult subjects with u ncomplicated acute influenza. An independent dat a monitoring comm ittee reviewed grouped blinde d safety data on the first 135 subjects randomized. The study rem ains blinded. The fr equency of vasovagal reactions reported as adverse events in this ongoing study is 2/135 (to date) which is lower than that seen in the phase 1 volunteer studies. 5.6 Dose Rationale Oseltamivir is approved for the treatment of uncomplicated acute influenza at a dosage of 75mg twice daily in adults14. Oseltamivir was shown to be clinically effective in a Phase III study of oral oseltamivir versus placebo in naturally occurring seasonal influenza, and these data were sufficient for regulatory approval for marketing of oseltamivir. At least 75% of an oral dose of oseltam ivir reaches the sy stemic circu lation as oseltam ivir carboxylate. When oseltamivir is adm inistered orally at a dose of 75mg twice daily, the serum C max of oseltam ivir carboxylate is approxim ately 348ng/m L and the AUC 0-48 is 10,876 h·ng/mL. The clinical data indicate that this level of exposure to oseltamivir was sufficient to provide clinical improvement in uncomplicated acute influenza. The serum pharmacokinetic data (Cmax and AUC0-∞, respectively) following intramuscular doses of peram ivir are approxim ately 7600ng/mL and 24,000 h·ng/m L for the 150m g dose and are approxim ately 15,000ng/m L and 49,000 h·ng/m L for the 300m g dose. Previous s tudies hav e assess ed the concen trations of the neuram inidase inhibitor zanamivir in nasal and pharyngeal secretions after parenteral administration of this drug. . Within several hours after ad ministration, the concentrati ons in secretions wer e approximately 100-fold lower than in serum or plasma. In theory, relatively high levels of a neuram inidase inh ibitor in res piratory se cretions ar e desi rable in order to rapidly inactivate influenza virus and to delay or prevent th e d evelopment of resistan ce in infecting virus strains. Intramuscular doses of peramivir, including doses of 150m g and 300mg have been shown to be well tolerate d in previous P hase 1 studies and since no identified safety signal has been noted by an independent data monitoring committee in the ongoing Phase 2 study, it is appropriate for these two dose regim ens to undergo further evaluation in this Phase 3 study. 178 178 BCX1812-311 (V1.0: 24-August-2007) Page 23 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6 STUDY OBJECTIVES 6.1 Objectives 6.1.1 Primary Objective The primary objective of this study is to eval uate the efficacy of peram ivir administered intramuscularly compared to placebo on th e time to alleviation of clinical symptoms in adult subjects with uncomplicated influenza. 6.1.2 Secondary Objective(s) The secondary objectives of this study are: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly; 2. To evaluate secondary clinical outcomes in response to treatment; 3. To evaluate changes in influenza virus titer ( viral sheddi ng) in response to treatment; 4. To assess pharmacoeconomic measures in response to treatment; 5. To assess changes in influenza viral su sceptibility to neu raminidase inhibito rs following treatment; 6.2 Study Endpoints 6.2.1 Primary Endpoint Time to alleviation of clinical symptoms of influenza 6.2.2 Secondary Endpoint(s) Secondary efficacy endpoints will include evaluations in each subject of: 1. Safety parameters, including: treatment- emergent adverse events (TEAEs) and treatment-emergent changes in clinical laboratory tests; 2. Time to resolution of fever; 3. Time to resumption of subject’s ability to perform usual activities; 4. Incidence of influenza related complications 5. Quantitative change in influenza virus shedding measured by viral titer assay (TCID50) and/or by quantitative polymerase chain reaction (PCR) assay; 6. Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. 6.2.3 Exploratory Endpoint An exploratory endpoint will evaluate change in influenza virus susceptibility to neuraminidase inhibitors in viral isolates recovered from subjects pre and post treatment. 179 179 BCX1812-311 (V1.0: 24-August-2007) Page 24 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 7 STUDY DESIGN 7.1 Overall Study Design and Plan This is a multinational, random ized, double-blind study com paring the efficacy and safety of two single dose regim ens of pera mivir adm inistered intramuscularly versus placebo in adults with uncom plicated acute influenza. Up to 800 subjects will be enrolled in to the s tudy. Each su bject’s as signment to trea tment will be str atified according to a Rapid Antigen Test (RAT) result and current smoking behavior, with 80% of subjects centrally random ized via an Inte ractive Voice Response (IVR) system to one of the two active single dose regimens of peramivir (2:2:1 randomization): Treatment Group 1: Peramivir 150mg maximum n=320 Treatment Group 2: Peramivir 300mg maximum n=320 Treatment Group 3: Placebo maximum n=160 Previous studies evalu ating the efficacy of neuraminidase inh ibitors enro lled su bjects with inf luenza-like illness on the basis of presence of specific clinical s igns and symptoms. These studies were conducted before the widespread availability of rapid influenza antigen diagnostic test kits (Rapid Antigen Tests-RAT), and typically between 50-70% of subjects enrolled we re subsequently confirm ed by viral cu lture to hav e an active influ enza infection. The sen sitivity of comm ercially available RAT kits ranges from 62% to 83%, depending upon the virus sub-type. 15 In the phase 2 study of intramuscular peram ivir (study BCX1812-211) a positive RAT test was required for study entry. It is likely that a number of subjects with an influenza infection were excluded from this study due the sensitivity of this assay. In this ph ase 3 study a lim ited number of RA T negativ e subjects will be en rolled in accordance with the following al gorithm to minimize false negative test results: once an individual site has identified 3 RAT positive subjects at screening within a 10 day period, indicating influenza activity is present in the site’s vicinity, a RAT negative subject that meets the inclusion / ex clusion criteria m ay be enrolled. O ne additional RAT negative subject m ay be enro lled there after for each p receding RAT positive subjec t th at is identified. The RAT result for each subjec t screen ed will be reco rded on the s tudy Interactive Voice Response System (IVRS) to manage this enrollment algorithm. A baseline nasopharyngeal swab specimen will be sent to the central virology laboratory for each RAT negative subject that has been randomized into the study. These specimens will be tested for influenza A and B infection using a PCR assay. The PCR results for these specimens will be reported to BioCryst in real time. The study will close after enrollment of at least 500 subjects who have either a positive Influenza A or B RAT at screening, or who have a negative RAT at screening but a positive influenza A or B PCR assay result from a baseline nasopharyngeal swab. 180 180 BCX1812-311 (V1.0: 24-August-2007) Page 25 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Study drug will b e ad ministered as one 2m L intramuscular injection in each g luteal muscle (total of 4mL injected in divided doses). At screening, subjects will have an anterior nasal or pharyngeal swab collected for testing with a comm ercially available RAT kit for influenza A and B in accordance with the RAT manufacturer’s instructions. If this test is positive and the subject is enrolled, additional s pecimens will be obta ined f or isolation and c ulture of inf luenza viru s and quantitative PCR assay. If the initial RAT is negative, th e test should be repeated with a different commercially available RAT kit. A limited number of RA T negative subjects may be enrolled in accordance with the screening algorithm defined above. Enrolled subjects will record the following in a Study Diary: • Oral tem perature m easurements tak en w ith an electronic therm ometer every 12 hours. W ith the exception of the baseline m easurement, all tem perature measurements will be obtained at leas t 4 hours after, or imm ediately before, administration of oral acetaminophen (paracetamol- provided), aspirin, ibuprofen or other NSAID. • Assessment of seven symptom s of influenza on a 4-point severity scale (0, absent; 1, mild; 2, moderate; 3, se vere), twice daily (A M, PM) through Day 9, then once daily (AM) through Day 14 • Assessment of subject’s ability to perform usual activities, (0–10 on a visual analog scale) once daily through Day 14 • Assessment of a subject’s tim e lost from work or usual activities and productivity compared to normal (0-10 on a visual analogue scale) once daily through Day 14 • Doses of antipyretic (e. g. acetaminophen/ paracetamol), expectorant, and/or throat lozenges administered each day through Day 14. Anterior nose (bilateral) and posterior phar ynx specimens (swabs) will be collected at Day 1 (pre-treatment) and at Days 3, 5, and 9, for influenza viral culture and quantitative PCR assay. In a subset of a m inimum of 200 subjects an addition al viral culture/ P CR sample will be collecte d on Day 2. Anterior nose (bila teral) and poster ior pha rynx specimens (swabs) will be collected at Days 1, 3, 5, and 9 f or all subjects, and on Day 2 in the subset of 200 subjects, to assess for potential changes in influenza viral susceptibility to neuraminidase inhibitors in response to treatment. At selected sites a separate sub-study will be conducted to collect limited PK samples for the purpose of conducting an exposure-respo nse analysis. This sub-study will be conducted under a separate sub-study protocol, BCX1812-311PK. 8 SELECTION AND WITHDRAWAL OF SUBJECTS 8.1.1 Inclusion Criteria Subjects must meet all of the following criteria for inclusion in this study: 1. Male and female subjects age ≥18 years 2. A positive Influenza A or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate specimen collected from an 181 181 BCX1812-311 (V1.0: 24-August-2007) Page 26 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL anterior nasal or pharyngeal swab, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated with a second commercially available RAT kit. A limited number of RAT negative subjects may be enrolled in accordance with a defined screening algorithm.. 3. Presence of fever at time of screening of ≥38.0 C (≥100.4 ºF) taken orally, or ≥38.5ºC (≥101.2 F) taken rectally. For subjects who test RAT positive at the time of screening, a subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify in the absence of documented fever at time of screening. For subjects who test RAT negative at screening, fever as described above must be documented at time of screening. 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of any severity (mild, moderate, or severe) 5. Presence of at least one constitutional symptom (myalgia [muscle aches], headache, feverishness, or fatigue) of any severity (mild, moderate, or severe) 6. Onset of illness no more than 48 hours before presentation 7. Females of child-bearing potential must have a negative urine pregnancy test (Beta HCG) at screening/baseline AND report one of the following: • Be surgically sterile or practice monogamy with a partner who is surgically sterile • Have been sexually abstinent 4 weeks prior to date of screening evaluation and be willing to remain abstinent through 4 weeks after study drug administration • Use oral contraceptives or other form of hormonal birth control including hormonal vaginal rings or transdermal patches and have been using these for 3 months prior through 4 weeks after study drug administration • Use an intra-uterine device (IUD), or double barrier contraception (such as condom or diaphragm with spermicidal gel or foam) as birth control 4 weeks prior to date of screening through 4 weeks after study drug administration 8. Provide written informed consent 8.1.2 Exclusion Criteria Subjects to whom any of the following criteria apply will be excluded from the study: 1. Women who are pregnant or breast-feeding 2. Presence of clinically significant signs of acute respiratory distress 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class IV functional status within the past 12 months (section 15.1). 182 182 BCX1812-311 (V1.0: 24-August-2007) Page 27 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5. History of chronic renal impairment requiring hemodialysis or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min) 6. Clinical evidence of active bacterial infection at any body site requiring therapy with oral or systemic antibiotics 7. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy. 8. Current treatment of active viral hepatitis C 9. Presence of known HIV infection, with a CD4 count <350 cell/mm3 10. Current therapy with oral warfarin or other systemic anticoagulant 11. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening 12. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days 13. History of alcohol abuse or drug addiction within 1 year prior to admission in the study 14. Participation in a previous study of peramivir as treatment for acute influenza or previous participation in this study 15. Participation in a study of any investigational drug within the last 30 days 16. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 8.1.3 Removal of Subjects from Therapy or Assessment All subjects are permitted to withdraw from participation in this study at any time and for any reason, specified or unspeci fied, and without prejudice. The Investigator or sponsor may terminate the subject’s participation in the study at any tim e for reasons including the following: 1. Adverse event; 2. Intercurrent illness; 3. Non-compliance with study procedures; 4. Subject’s decision; 5. Administrative reasons; 6. Lack of efficacy; 7. Investigator’s opinion to protect the subject’s best interest. Any subject who withdraws because of an adverse event will be followed until the sign(s) or symptom(s) that constituted the adverse eve nt has/have resolved o r is dete rmined to represent a stable medical condition. A subject should be withdrawn fr om the trial if, in the opinion of the Investigator, it is medically necessary, or if it is the d esire of the subject. If a subjec t does not return for a scheduled visit, every effort should be m ade to contact the subject and determ ine the 183 183 BCX1812-311 (V1.0: 24-August-2007) Page 28 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subject’s medical condition. In any circum stance, ev ery effort sho uld be m ade to document subject outcome, if possible. If the sub ject withdraw s consen t, n o furt her evaluations should be perfor med and no attempts should be made to collect additional data. 9 TREATMENTS 9.1 Treatments Administered Peramivir is an investig ational drug. Peram ivir for intramuscular injection is a small- volume parenteral and will be supp lied as a 75 mg/mL solution in sodium citrate/ citric acid buffer. The pH is approximately 3.0. A m atched placebo solution of so dium citrat e/ citric acid buffer with 1.2% sod ium chloride at a pH of approximately 3.0 will be supplied. 9.2 Identity of Investigational Product(s) Peramivir and placebo peramivir will be supplied in clear 2mL vials. An individual study drug kit will contain 2 vials of blinded study drug (peramivir and/or placebo, depending upon the treatment group), 2 syringes and 2 need les in which to draw up the solution for intramuscular injection. All m aterials will be packaged in a labele d box container. All study drug kits m ust be stored at 2-8 oC. Each individual study drug kit will b e labeled with some or all of the following information as required by local regulations: • Sponsor nam e and contact inform ation, study protocol num ber, kit num ber, description of the contents of the container, instructions for the preparation of the syringe and adm inistration of the study dr ug, conditions f or st orage, statem ent regarding the investigationa l (clinical trial) use of the study drug and date for retest or expiry date. Each vial of study drug will be labeled with some or all of the following infor mation as required by local regulations: • Sponsor nam e, study protocol number, desc ription of the contents of the vial, instructions for the preparation of the s yringe, statem ent regarding the investigational (clinical trial) use of the study drug and lot number. 9.3 Method of Assigning Subjects to Treatment Groups Subjects will be centrally randomized in a ratio of 2:2:1 to one of three treatment groups: single dos e peramivir 1 50mg, single dose pera mivir 300mg or placeb o, in acco rdance with a computer-generated random ization schedule prepared by a non-study statistician. Subjects will be s tratified acco rding to the result of a RAT test and curren t sm oking behavior. Once a subject is eligible for randomization, he/she wi ll be assigned a study drug kit nu mber that will be obta ined by stu dy staf f f rom the study inter active voice response system (IVRS). Once a study drug kit nu mber has been assigned to a subject, it cannot be reassigned to any other subject. 184 184 BCX1812-311 (V1.0: 24-August-2007) Page 29 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 9.4 Study Medication Accountability The Investigator/pharmacist must maintain accurate records of the disposition of all study drugs received from the sponsor, issued to th e subject or directly adm inistered to the subject (including date and time), and any drug accidentally destroyed. The sponsor will supply a specific dru g-accountability form . At the en d of the study, information describing study drug s upplies (e.g., lot num bers) and disp osition of s upplies for each subject must be provided, signed by the Invest igator or designee, and colle cted by the study monitor. If any errors or irregularities in any shipment of study m edication to the site are discovered at any time, the Project Manager must be contacted immediately. At the end of the study, all medication not dispensed or administered and packaging materials will be collected with supervision of the monitor and returned to the sponsor or destroyed on site as dictated by the appropr iate Standard Operating P rocedure at the participating institution. 9.5 Blinding/Unblinding of Treatments This is a double-blind study. The treatment group assignment will not be known by the study subjects, the investigator , the clinical staff, the CRO or Sponsor staff during the conduct of the study. Section 11.2.4 provides inform ation regarding the process for unblinding the treatment assignment, if necessary, in the event of an SAE. 9.6 Prior and Concomitant Therapies All m edications, by any route of adm inistration, used during this study m ust be documented on the Case Report Form (CRF). Prescription as well as non-prescription medications should be recorded. Medication us ed for the treatm ent of influenza-related symptoms will be captured by the subject in the diary card provided by BioCryst. 9.7 Overdose and Toxicity Management To date there is no experience with overdose of in tramuscular or intravenous peramivir. If overdose occurs, subjects should receive indicated supportive therapy and evaluation of hematologic and clinical chem istry laboratory tests should be conducted. The effec t of hemodialysis on elimination of peramivir is unknown. 9.8 Dose Interruption As this is a study of a single injection of peramivir or placebo, guidelines for treatm ent interruption for drug related SAEs or toxicities are not applicable. 10 STUDY CONDUCT A study schedule of evaluations is presented in Figure 1 . A detailed lis t of the evaluations is also provided in the following sections. 185 185 BCX1812-311 (V1.0: 24-August-2007) Page 30 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1 Evaluations All subjects enrolled in this study will undergo the following evaluations: 10.1.1 Medical History Medical history, influenza va ccination s tatus within th e previous 12 m onths and demographic data (including smoking behavior) will be recorded at Screening/Baseline. 10.1.2 Rapid Antigen Test for Influenza At Screening/Baseline, a commercially available, rapid antigen tes t (RAT) for influenza A and B will be performed on an adequate specimen collected by swabbing the anterior nose or pharynx, in accordance with the RAT manufacturer’ instructions. A negative initial RAT should be repeated with a different commercially available RAT kit. Refer to the Study Manual f or instructions regarding the use of the RAT kits provided for this study. Sites m ay use the kits provided by the Sponsor or any other commercially approved RAT available at their site to document a confirmed influenza infection. A lim ited num ber of RAT negativ e subje cts will be enr olled in a ccordance with the following algorithm: Once an ind ividual site has identified 3 RAT positive sub jects at screening within a 10 day period, indicating that influenza activity is present in the site’s vicinity, a RAT negative subject that m eets the inclus ion/ exclus ion criteria m ay be enrolled. O ne additional RAT negative subj ect m ay be enrolled th ereafter for each preceding RAT positive subject that is iden tified. The RAT result for each subject screened will be record ed on the s tudy Inte ractive Voice response (IVR) system to manage this enrollment algorithm. 10.1.3 Physical Examination and Influenza-related Complications Assessments The Investigator will perform a physical ex amination at S creening/Baseline. Subject’s weight will be recorded at Screening/Baseline. Study personnel will be provided with an influenza-related complications (IRC) checklist in the CRF to evalua te the subject for the presence of clinical signs and /or symptoms of the following influenza-related complications: sinusitis, otitis, bronchitis and pneumonia. At each follow up assessm ent a t argeted physical exam ination will be conducted to record the presence of influenza related complications. If the investigator determines that the subject experiences (or is presumed to experience) an IRC as noted above, he/she will record that assessm ent on the IR C CRF pa ge and any m edication used to treat the condition will be recorded on the concom itant m edication page. Such inform ation describing IRC signs and/or sym ptoms should not be reported as adverse events. Any injection site reactions noted will be recorded in the CRFs as adverse events. 10.1.4 Vital Signs Vital signs evaluations will in clude blood press ure, pulse rate , and resp iration rate. The investigator will record or al body tem perature at baseline. Thereafter the subject will record oral temperature twice daily in the study diary card. Vital signs will be measured at Screening/Baseline, pre-dose, and at 15 minutes following the study drug injection on Day 1, then once da ily on Days 2 (for those subjects who are 186 186 BCX1812-311 (V1.0: 24-August-2007) Page 31 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL seen on day 2), 3, 5, 9, and 14. 10.1.5 Electrocardiogram Measurements A 12-lead elec trocardiogram (ECG) will b e obtained at Screen ing/ Baselin e. I f this baseline ECG is interpreted by the conductin g physician as m eeting the exclusionary criteria listed in section 8.1.2 the subject will no t be enrolled in this study. If the ECG is interpreted as being abnorm al and does not m eet the exclusionary criteria (e.g. acute ischemia, medically significant dysrhythmia) th en this subject m ay be enrolled, taking into con sideration th e subjec t’s m edical history. Appropriate follow-up evaluations, including but not limited to repeat ECGs, should be completed at subsequent study visits as directed by the investigator. 10.1.6 Clinical Chemistry Profiles Clinical ch emistry pro files will include a C hemistry 20 panel ( includes sod ium, potassium, chloride, total CO 2 [bicarbonate], creatinine, glucose, urea nitrogen, album in, total calcium , total m agnesium, phosphor us, alkaline phosphatase, alanine aminotransferase (ALT), aspartate am inotransferase (AST), total bilirubin, d irect bilirubin, lactate dehydrogenase [LDH], total protein, total creatine kinase, and uric acid) Blood samples for clinical chem istry profiles will be collected at Screen ing/Baseline, and on Days 3, 5 and 14. 10.1.7 Hematology Profiles Hematology will include complete blood count (CBC) with differential. Blood samples for he matology profiles will be collected at Screening/Baseline, and on Days 3, Days 5 and 14. 10.1.8 Serology for Influenza Paired blood samples for determination of antibody to influenza A and B (serology) will be obtained with the clinical laboratory tests at Screenin g/Enrollment and at Day 14. These specimens will be stored at the central laboratory and will be analyzed if needed to confirm the diagnosis of influenza. 10.1.9 Urinalysis and Evaluation of Protein in Urine Urinalysis will in clude dipstick tests for protein, glucose, ketones, blood, urobilinogen, nitrite, pH, and spec ific gr avity a nd m icroscopic evaluation for R BCs and WBCs. Samples for urinalysis will be collected at Screening/Baseline, and on Days 3, 5, and 14. 10.1.10Urine Pregnancy Test Females of childbearing potential will be ev aluated for pregnancy at Screening/Baseline and Day 14 using a urine pregnancy test. 10.1.11 Samples for Virologic Laboratory Assessments An adequate spec imen will b e co llected by sw abbing the anter ior nos e (bila teral) and posterior pharynx for virologic laboratory a ssessments including culture for the isolation of influenza virus and/or quantitative PCR assa y at Screening/Baseline, and at Days 3, 5, and 9. In a subset of a m inimum of 200 subjects an additio nal sample will be taken at 187 187 BCX1812-311 (V1.0: 24-August-2007) Page 32 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Day 2. Refer to the L aboratory Manual for instructions re garding the processing and shipment of these specimens. 10.1.12 Subject Self Assessments Subject self assessments will be performed beginning pre-dose on Day 1 and recorde d in the subject’s Study Diary including the following: • Oral temperature measurements with an electronic thermometer (provided by the Sponsor for the study) every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol, provided) aspirin, ibuprofen or other NSAID. The times of each temperature determination will be recorded in the Study Diary. The baseline temperature will be recorded at the screening/Day 1 visit prior to dosing, regardless of whether the subject had recently taken an anti-pyretic; the time of anti-pyretic use pre-treatment will be recorded in the CRF, if applicable. • Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [muscle aches], headache, feverishness, and fatigue) on a 4-point severity scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily, beginning pre-dose on Day 1 and through Day 9, then once daily through Day 14. • Assessment of the subject’s ability to perform usual activities using a 0–10 visual analogue scale once daily through Day 14. • Assessment of the subject’s time lost from work or usual activities and productivity compared to normal using a 0-10 visual analogue scale once daily through Day 14. The subject’s diary card will be reviewed by study staff at each visit for completion of the record of all required ite ms, with particular emphasis on alleviation of symptoms as well as relapse of sym ptoms. Relapse is defined as the recurrence of at leas t one respiratory symptom and one constitutiona l sy mptom (both greater th an m ild in severity) f or 24 hours and the presence of fever (unless influenc ed by antipyretic use). Relapse can only occur after the subject has m et the endpoint cr iteria for alleviation of symptoms. Study staff will not attem pt to ask subjec ts to retrospectively complete missing diary card data for any scheduled assessm ents that have not b een com pleted prio r to the c linic visit. Study staff should, however, rem ind the subject to com plete the diary card at all scheduled times. 10.1.13 Concomitant Medications All concom itant m edications used during this study, with the exception of those medications taken for symptomatic relief of influenza symptoms, which will be reco rded by the subject in their diary card, must be documented on the Case Report Form (CRF). 10.1.14 Adverse Events AEs will be assess ed from the tim e of ad ministration of stu dy medication through the final study visit. 188 188 BCX1812-311 (V1.0: 24-August-2007) Page 33 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.15 Single Pharmacokinetic Exposure Sample On study day 3 a single PK sample will be drawn in concert with the day 3 safety clinical laboratory blood draw. This sample will be sent for subsequent analys is of the concentration of peramivir at this time point. Data f rom this sing le PK sample will b e combined with data from the PK s ub-study (BCX1812-311PK) to perfor m an exposure- response analysis. This analysis will be described as part of the sub-study analysis plan.. 10.2 Screening 10.2.1 Informed Consent The nature and purpose of the study and the expectations of a participating subject will be described to potential study subjects , their que stions will be answered, and the subjects will th en b e asked to sign an inf ormed c onsent docum ent. Study s ubjects will then undergo the screening evaluation as noted in Section 10.2.2 10.2.2 Screening/Baseline Evaluation and Enrollment Screening/baseline evaluation may be conducted in the investigator’s office or clinic, or in the subject’s hom e, in which case all ev aluations must be conducted by appropriately trained and qualified staff. Clinical laboratory assessm ents perform ed at Screenin g are for the purpose of establishing a baseline. Subjects m ay be enrolled and receive treatm ent with study drug prior to r eceiving re sults of the laboratory a ssessments (with the ex ception of urine pregnancy test result, which must be known). Eligible sub jects will be enrolled and ra ndomized to blin ded study treatm ent. The randomization will include stratification by RA T status and current s moking behavior. The Investigator will prepare a request for blinded study drug assignment which includes the subject’s screening number. The Investigator or designee at the clinical study center will contact the central randomization Interactive Voice System (IVRS call center). The IVRS call center will advise the study center of the investigational study drug kit number that is assigned to that subject at enrollment. Subjects that are d etermined to be ineligible will be advi sed accordingly, and the reason for ineligibility will b e discussed. If desired by the subjec t the reason for ineligibility may be pr ovided/discussed with their hea lth-care provider by the Investigator or designee. Ineligible subjects who have been screen ed for the study will also be entered on the IVRS. For such subjects, the screening num ber assigned, subject’s date of birth and a reason for ineligibility will be entered on to th e IVRS. All ineligible subjects must be entered onto the IVRS within 24 hours of screening, to assis t with surve illance analysis during the course of the study. 10.3 Treatment Period—Study Day 1 Day 1 represents the only day of study dr ug dosing. Study drug adm inistration should 189 189 BCX1812-311 (V1.0: 24-August-2007) Page 34 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL occur as soon as possible following inform ed consent, screening and random ization. Therefore, it is expec ted that the da te of Screening/ Baseline and Day 1 will usua lly be the same date. 10.3.1 Pre-dose Evaluations Following an explanation of the Subject Self Assessment measures (Section 10.1.11), the subject shall complete the record of these assessments in their Study Diary prior to dosing. The subject will be counseled regarding the expectations for recording these assessments through Day 14. Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) and a 12 lead ECG will be obtained prior to dosing. At Hour 0, the blinded study drug will be administered intramuscularly (one injection in the left gluteal muscle, and one injection in the right gluteal muscle within a period of ≤ 10 minutes.). The calendar date and 24-hour clock time of the first and second injections will be recorded. The following evaluations will be performed post-dose on Study Day 1: • Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) at 15 minutes after the study drug administration • Record any concomitant medications • Record any AEs 10.4 Post-Treatment Assessment Period 10.4.1 Days 2, 3, 5, 9 and 14 Study evaluations will be perform ed on Days 2 [subset], 3, 5, 9 and 14 in accordance with the schedule of evaluations (Figure 1). Visits may be conducted in the investigator’s o ffice or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and qualified staff. The Day 2 assessm ent will be con ducted in pe rson only f or the subse t of subjects who will provide additional Day 2 viro logy samples. For all o ther study subjects, study staff will attempt to contact the subjects on Day 2 by telephon e to confirm their com pliance with completion of the Subject Self Assessments, to note any concom itant medications and adverse events. Any adverse events repo rted by the subject during this telephone contact will be recorded on the adverse event form and verified during the visit on day 3. At each v isit it is im portant that the sub ject’s Study Diar y record be rev iewed for completion of daily Subject Self Assessm ents. The subjects should be counseled as necessary regarding self assessments and Study Diary record requirements. The subject’s diary card will be reviewed by study staff for alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the r ecurrence of at least one resp iratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours an d the presence of fever (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Day 3: 190 190 BCX1812-311 (V1.0: 24-August-2007) Page 35 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL The results of the CK assay a t Da y 3 will no t be m ade available to investiga tors, to BioCryst or to any study personnel unless the C K result at Day 3 is ≥ 2000 IU/mL. A single PK sample will be drawn as part of the safety clinical laboratory study on Day 3. Day 14: If a subject does not have resolution of all influenza-related sym ptoms (defined as a patient-recorded sym ptom score of m oderate [ 2] or seve re [ 3]), the investigato r will schedule a follow-up assessm ent with the pati ent at Day 21 and, if required, Day 28. These follow-up assessm ents m ay be conduc ted in person or by telephone at the investigator’s discr etion. The subjec ts will no t be required to continu e to reco rd da ily symptom sc ores, but w ill report th ese sco res to the inv estigator on Day 21 and, if required, on Day 28. No protocol-m andated follow up will occur after Day 28. Further management of the subject will be in acco rdance with the investigator’s stan dard practice. 191 191 BCX1812-311 (V1.0: 24-August-2007) Page 36 Figure 1 Study Measurements and Visit Schedule Treatment Period Assessment Day End of Study Early Withdrawal Screening 1 (Baseline) Day 11 Day 22 Day 3 Day 5 (±1 day) Day 9 (±3 day) Day 14 (±3 day) 8 Informed Consent X Rapid Antigen test for Influenza A & B X Medical History/Physical Exam3 X Influenza-related complications checklist3 X X X X X X Inclusion/Exclusion X Clinical Chemistries4 X X X X Hematology4 X X X X Exposure Pharmacokinetic Sample X4 Serology (serum) Sample X X Urinalysis4 X X X X Urine Pregnancy Test X X Vital Signs5 X X X X X X X ECG6 X Sample (nasophar yngeal swab) for Influenza Virus Culture/ PCR assay and for resistance studies X X X X X Study Drug Administration X Subject Diary Review7 X X X X X X Concomitant Medications X X X X X X X Adverse Events X X X X X X 1 It is expected that the date of Screening and Day 1 (date of administration of study drug) will be the same. Visits at Screening and on subsequent study days may occur in subject’s home by the investigator (all visits) or appropriately trained study center staff (Day 2, 3, 5, 9 visits). 2 Day 2 visit required only for a subset of subjects for whom additional Day 2 virology sample is required. For all other subjects, Day 2 will be a telephone contact with the subject to ensure compliance with diary card completion, concomitant medication and adverse event review. 3 Medical history and physical exam at screening to include weight, and smoking behavior. Targeted physical examinations will be performed to complete the influenza-related complications checklist by the appropriate medical personnel at appropriate visits. 4 Clinical laboratory assessments performed at Screening are for the purpose of establishing a baseline. Subject may be enrolled and begin treatment with study drug prior to receiving results. On Day 3 an extra tube will be included with the safety blood sample for evaluation of peramivir concentrations. 5 Vital sign measures will include blood pressure, pulse rate and respiration rate. Vital signs will be recorded at Screening, pre-dose and at 15 min following the study drug administration on Day 1, then once on remaining days as stipulated. The investigator will record oral temperature at baseline. Thereafter the subject will report oral temperature measurements twice daily in the Study Diary 6 If the baseline ECG is interpreted by the conducting physician as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal and does not meet the exclusionary criteria (e.g. acute ischemia, medically significant dysrhythmia) then this subject may be enrolled, taking into consideration the subject’s medical history. Appropriate follow-up evaluations, including but not limited to repeat ECGs, should be completed at subsequent study visits as directed by the investigator. 7 Subjects record symptom assessment in Study Diary, twice dail y, beginning pr e-dose on Day 1 thr ough Day 9, then once daily through Day 14; subjects record ability to perform usual activities once daily, beginning pre-dose on Day 1 through Day 14. Subjects record oral temperature twice daily throughout as well as all concomitant medication and adverse events 8 For any subject with unresolved influenza symptoms(moderate or severe) or unresolved adverse events, a follow up assessment (in person or by phone) will be scheduled at Day 21 and Day 28 if required BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 192 192 BCX1812-311 (V1.0: 24-August-2007) Page 37 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11 ADVERSE EVENT MANAGEMENT 11.1 Definitions 11.1.1 Adverse Event An AE is any untoward m edical occurrence in a clinical study subject. No causal relationship with the study drug or with the clinical study itself is implied. An AE may be an unfavorable and unintended sign, sym ptom, syndrome, or illness that dev elops or worsens during the clinical st udy. Clinically relevant ab normal results of diagnostic procedures including abnorm al laborator y findings (e.g., requ iring unscheduled diagnostic procedures or treatm ent measures, or resulting in withdrawal from the study) are considered to be AEs. AEs may be designated as “nonserious” or “serious” (see Section 11.1.2). Surgical procedures are not AEs but m ay constitute therapeutic m easures for conditions that require surgery. The condition for which the surgery is required is an AE, if it occurs or is detected during the study period. Planned surgical m easures perm itted by the clinical study protocol and the conditions(s) leading to these measures are not AEs, if the condition(s) was (were) known befo re the start of study treatm ent. In the latter case the condition should be reported as medical history. Assessment of seven influenza sym ptoms (cough, sore throat, nasal obstruction, m yalgia [muscle aches], headache, f everishness, and f atigue) will be documented in a subject’s study diary and analy zed as a m easure of efficacy of the study treatm ent. These symptoms will not b e reported as AEs unless the sym ptom(s) worsen to the exte nt that the outcome fulfils the def inition of an SAE, which then must be recorded as such (see Section 11.1.2). Likewise, a RAT for influenza is required at screening in order to determine eligibility for the study, and therefore a positive RAT is not considered an AE. 11.1.2 Serious Adverse Event A SAE is an adverse event that results in any of the following outcomes: • Death • Is life-threatening (subject is at immediate risk of death at the time of the event; it does not refer to an event that hypothetically might have caused death if it were more severe) • Requires in-subject hospitalization (formal admission to a hospital for medical reasons) or prolongation of existing hospitalization • Results in persistent or significant disability/incapacity (i.e., there is a substantial disruption of a person’s ability to carry out normal life functions) • Is a congenital anomaly/birth defect • Is an important medical event 193 193 BCX1812-311 (V1.0: 24-August-2007) Page 38 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Important medical events that may not result in death, are no t life-threatening, or do not require hospitalization may be considered an SAE when, based upon appropriate medical judgment, they m ay j eopardize the subject or m ay r equire m edical or surgical intervention to prevent one of the outcom es listed in this definition. E xamples of such events include allergic bronchospasm requiri ng intensive treatm ent in an e mergency room or at hom e, blood dyscrasias or c onvulsions that do not result in subject hospitalization, or the development of drug dependency or drug abuse. 11.2 Method, Frequency, and Time Period for Detecting Adverse Events and Reporting Serious Adverse Events Reports of AEs are to be collected from the time of study drug administration through the follow-up period ending on Day 28. The Invest igator or de signee must completely and promptly record each AE on the appropriate CRF. The Investig ator should attem pt, if possible, to establish a diagnosis based on th e presenting signs and symptom s. In such cases, the diagnosis should be docum ented as the A E and not the individual sign/symptom. If a clear diagnosis cannot be established, each si gn and symptom must be recorded individually. The Investigator should attem pt to follo w all unresolved AEs and/or SAEs observed during the study until they are reso lved, or for 30 days after th e subject’s last study visit, whichever comes first. 11.2.1 Definition of Severity All AEs will be as sessed (graded ) f or severity and class ified into on e of f our clearly defined categories as follows: • Mild: (Grade 1): Transient or mild symptoms; no limitation in activity; no intervention required. The AE does not interfere with the participant’s normal functioning level. It may be an annoyance. • Moderate: (Grade 2): Symptom results in mild to moderate limitation in activity; no or minimal intervention required. The AE produces some impairment of functioning, but it is not hazardous to health. It is uncomfortable or an embarrassment. • Severe: (Grade 3): Symptom results in significant limitation in activity; medical intervention may be required. The AE produces significant impairment of functioning or incapacitation. • Life-threatening: (Grade 4): Extreme limitation in activity, significant assistance required; significant medical intervention or therapy required; hospitalization. 11.2.2 Definition of Relationship to Study Drug The blinded Principal Investigator must rev iew each AE and m ake the determ ination of relationship to study drug using the following guidelines: Not Related: The event can be readily explained by other factors such as the 194 194 BCX1812-311 (V1.0: 24-August-2007) Page 39 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subject’s underlying m edical c ondition, concom itant therapy, or accident, an d no tem poral relati onship ex ists b etween the study drug and the event. Unlikely: The event d oes not follow a reason able tem poral sequ ence from drug adm inistration and is read ily explained by the subject’s clinical state or by other m odes of therapy adm inistered to the subject. Possibly Related: There is so me tem poral relationship between the event an d th e administration of the study drug a nd the event is unlikely to be explained by the subject’s m edical condition, other therapies, or accident. Probably Related: The event follows a reasonable tem poral sequence from drug administration, abates upon discontinuation of the drug, and cannot be reasonably explained by th e known characteristics of the subject’s clinical state. Definitely Related: The event follows a reason able tem poral sequen ce from administration of the m edication, follows a known or suspected response pattern to the m edication, is confirm ed by im provement upon stopping the m edication (dec hallenge), and reappears upon repeated exposure (rechallenge, if rechallenge is m edically appropriate). 11.2.3 Reporting Serious Adverse Events Any SAE must be reported to BioCryst or its designee within 24 hours of the Investigator’s recognition of the SAE by fi rst notifying the Medical Monitor at the number listed below: Telephone: Europe: +44 1628 548000; North America: 1-888-724-4908 Facsimile: Europe: +44 1628 540028; North America: 1-888-887-8097 or 1-609-734-9208 The site is required to fax a completed SAE Report Form (provided as a separate report form) within 24 hours. All additional follow-up evaluations of the SAE must be reported and sent by facsimile to BioCryst or its designee as soon as they are available. The Principal Investigator or designee at each site is respons ible for submitting the IND safety report (initial a nd follow -up) or other safety inform ation (e.g., revised Investigator’s Brochure) to the Institutional Review Board/Independent Ethics Committee (IRB/IEC) and for retaining a copy in their files. If the Inv estigator becomes aware of any SA E occurring within 30 days after a s ubject has com pleted or withdrawn from t he study, he or she should notify BioCryst or its designee. Any SAEs considered possibly related to treatment will be reported to the FDA and other Regulatory Competent Authorities as applicab le via the MedW atch reporting system i n 195 195 BCX1812-311 (V1.0: 24-August-2007) Page 40 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL accordance with FDA and other ap plicable regulations. However, the Investig ator is not obligated to actively seek reports of AEs in former study participants. While pregnancy is not considered an AE, a ll cases of fetal drug exposure via parent as study participant (see S ection 4.4) are to be reported immediately to BioCryst or its designee. Inform ation rela ted to the pregnancy m ust be given on a “Pregnancy Confirmation and Outcome” form that will be provided by the Sponsor or its designee. 11.2.4 Emergency Procedures In the even t of an SAE, the Principal Inve stigator m ay request the unblinding of the treatment assignm ent for the subject affected . If tim e allows (i.e., if appropriate treatment for the SAE is not im peded), the Principal Investigator wi ll first consult with the Med ical Monito r r egarding the need to unblind the treatm ent assignm ent for the subject. At all times, the clinical well-being of any subject outweighs the need to consult with the Medical Monitor. The Principal Investigator m ay contact th e IVRS central random ization center and request the unblinding of the treatm ent assi gnment that corresponds to the affected subject. Th e IVRS center will record the na me of the Investigator making the request, the date and time of the request, the reason for the request, the subject number and study drug kit number, and whether the Medical M onitor was consulted prior to the request being made. The Sponsor will be informed within 24 hours if unblinding occurred. 12 STATISTICAL METHODS Descriptive statistical methods will be used to summ arize the data from this study, with hypothesis testing perform ed for the prim ary and other selected efficacy endpoints. Unless stated otherwise, the term “descriptive statistics” refers to number of subjects (n), mean, median, standard deviation (SD), minimum, and maximum for continuous data and frequencies and percentages for categorical da ta. The term “treatm ent group” refers to randomized treatment assignment: peramivir 150 mg, peramivir 300 mg, or placebo. All data collected during the study wi ll be included in data listin gs. Unless otherwise noted, the data will be sorted first by treatm ent assignment, subject num ber, and then by date within each subject number. Unless specified otherwise, all statistical testing will be two-sided and will be performed using a significance (alpha) level of 0.05. All statistical analyses will be conducted with the SAS® System, version 9.1.3 or higher. 12.1 Data Collection Methods The data will be reco rded on the CRF appr oved by BioCryst. The Investigator must submit a completed CRF for each subject who signs an inform ed consent form (ICF), regardless of duration. All documentation supporting the CRF data, such as laboratory or hospital records, must be readily available to verify entries in the CRF. Documents (including laborator y reports, hospital records s ubsequent to SAEs, etc.) transmitted to BioCryst should not carry the s ubject’s name. This will help to ensure 196 196 BCX1812-311 (V1.0: 24-August-2007) Page 41 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subject confidentiality. The Investigator m ust consult the “CRF Com pletion Manual” for com prehensive instruction for completion of the CRF. 12.2 Statistical Analysis Plan A statistical analysis plan (SAP) will be cre ated prior to the review of any data. This document will provide a m ore technical and detailed description of the proposed data analysis methods and procedures. 12.3 Sample Size Estimates From published resu lts, it is exp ected that th e median time to a lleviation of symptoms will be between 103.3-116 hours for subjects receiving p lacebo. 16 , 1 7 For sam ple size calculations the best placebo respon se (103.3 hours) will p rovide the most conserv ative estimate of an observed hazard ratio. Additionally, it is expected that the median time to alleviation for the lowes t dose peramivir arm will be 69.9 h ours, yielding a hazard ratio of 0.68. Using these assum ptions, a sa mple size of 200 infected subjects per active treatment group and 100 infected subjects in th e placebo group is sufficient to provide at least 80% power to detect a hazard ratio of 0.68 usi ng a log-rank statistic and α = 0.025 (SAS version 9.1.3; tota l accrual time 7 months; total enrollment time 6 months). Up to 800 subjects will b e enrolled to achieve the target num ber of at least 5 00 subjects with diagnostic evidence (RAT or PCR) of an acute influenza infection (200 per active treatment; 100 receiving placebo) as described in section 12.4.2. 12.4 Analysis Populations The populations for analysis will include the intent-to-treat (ITT), intent-to-treat infected (ITTI), and safety populations. 12.4.1 Intent-To-Treat Population The ITT population will include all subject s who are random ized. Subjects will be analyzed in the treatment group to which they were randomized. The ITT population will be used for analyses of accountability and demographics. 12.4.2 Intent-To-Treat Infected Population The ITTI po pulation will include all subj ects who are rando mized, received study d rug, and have proven influenza by any one of the fo llowing: culture, PCR, or paired serology showing ≥ 4-fold increase in antibody to influe nza A or B, and received study drug. Subjects will be an alyzed accord ing to the treatment random ized. If a discrepancy is noted in the final database for any subject, such that the drug differs from the randomized treatment assignm ent, efficacy analyses m ay be repeated with the su bjects analy zed according to the treatm ent received. The ITTI population will be used for prim ary analyses of efficacy. 197 197 BCX1812-311 (V1.0: 24-August-2007) Page 42 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.4.3 Safety Population The safety population will include all subjects who received study drug. Subjects will be analyzed according to the treatm ent received. This population will be used for all safety analyses. 12.5 Interim and End of Study Analyses Interim Analysis An independent DMC will review safety data on an ongoing basi s. Safety analyses will be presented in a manner consistent with the presentations intended for the final analysis. End of Study Analysis A final analysis is planned after the last su bject completes or discontinues the study, and the resulting clinical database has been cleaned, quality checked, and locked. 12.6 Efficacy Analyses 12.6.1 Primary Efficacy Endpoint The primary efficacy endpoint is the time to alleviation of symptoms, defined as the time from injection of study drug to the start of th e time period when a subject has Alleviation of Symptoms. A subject has Alleviation of Symptoms if all of the seven symptoms of influenza (nasal congestion, so re throat, cough, aches and pains, fatigue (tiredness), headache, feeling feverish) assessed on his/he r subject diary are eith er absent o r are present at no m ore than m ild severity leve l and at this status for at least 21.5 hours (24 hours - 10%). Descriptive statistics for the prim ary effi cacy endpoint will be tabulated by treatment group. Alleviation of sym ptoms will be d etermined by assessm ent of sym ptoms as reported on each subject’s diary card. T ime to alle viation of sym ptoms will b e summarized overall and for i ndividual sym ptoms for each treatm ent group. Overall treatment dif ferences will be assess ed using a Cox Regression m odel with ef fects f or RAT result at screening, current smoking behavior, treatment group, and influenza season at randomization (if necessary). Subjects who do not experience alleviation of symptoms will be censored at the date of their last non-missing post-baseline assessment. Pairwise differences in tim e to alleviation of sy mptoms am ong the treatm ent groups will be evaluated using contrast statem ents from the final Cox m odel. In orde r to m aintain the overall type I error in the presence of the planned comparisons between the two peramivir treatments and placebo, a Bonfe rroni correction will be app lied to the p rimary efficacy endpoint analysis. P -values for the planne d com parisons of each peram ivir arm to placebo will be adjusted via a Bonferroni corr ection (i.e., if the unadjusted p-value for an active com parison versus place bo, p, is less th an 0.05, then p a=p*number of planned comparisons=p*2; otherwise, p a=p). Superiority of peram ivir to placebo will be established if the adjusted p-value is less than or equal to 0.05. 198 198 BCX1812-311 (V1.0: 24-August-2007) Page 43 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.6.2 Secondary Efficacy Endpoints All secondary endpoints will be summ arized using descriptive statistics by treatm ent group and study day/time, if appropriate. St atistical comparisons for each endpoint will be constructed without adjustment for multiple endpoints. The reduction in viral shedding will be assessed as the change in viral titers defined as the time-weighted change from baseline in log10 tissue culture infective dose50 (TCID50/mL) and will be summarized for each treatm ent group. The tim e-weighted average change from baseline will be calculated on a by-subject basis through Day 9 using the trapezoidal rule with a ll available post-bas eline on-tre atment data (d ata af ter initia tion of study treatment) minus the baseline value. Specifically, the time-weighted area under the curve for time a (ta) to time b (tb) is given by the formula ) ( ) ( b a b a t t t t AUC TWAUC − − = , where ∑ − = − + − + = − 1 1 1 2 ) )( ( ) ( b a i i i i i b a t t y y t t AUC and ti represents the date of the ith viral titer assessment and y i represents the log10 value of the i th viral titer as sessment. If there is a baseline value and only one follow-up value, y i then the tim e-weighted change from baseline is defined as the difference between y i and baseline. If there is a baselin e value and no follow-up value, the subject is exclude d from analysis. The differences between each of the peramivir treatment groups and placebo will be evaluated using a van Elteren Test ad justing for RAT result at screen ing, current sm oking be havior and influenza season at randomization (if necessary). Analyses of the PCR results will be analy zed in a similar manner. Subject’s ability to perform usual activities as determined from the visual analog scale will be summarized by study visit day and treatment group. Differences between the treatment groups will be assessed using the van Elteren Test adjusting for smoking behavior and influenza season at randomization (if necessary). The time (days) to resumption of a subject’s ability to perform usual activities (i.e., subject scores ability to perform usual activities as 10) will be estimated using the method of Kaplan-Meier. Differences between each of the peramivir treatment groups and placebo will be assessed using the log rank statistic adjusting for RAT result at screening, current smoking behavior and influenza season at randomization (if necessary). Subjects who do not return to the pre-study level of performance of usual activities will be censored at the time of their last non-missing post-baseline visual analog scale value. Subject’s oral tem perature will be summ arized by study visit and treatm ent group. Differences between the treatment groups will be assessed using the Wilcoxon Rank Sum Test con trolling for RAT resu lt at screen ing, current sm oking behavior and influenza season at randomization (if necessary). A subject has Resolution of Fever if he/she has a temperature < 37.2°C (99.0°F) and no antipyretic medications have been taken for at least 12 hours. The tim e to resolution of fever will be estimated using the method of Ka plan- Meier using temperature and sym ptom relief medication information obtained from the subject diary data. Difference between the tr eatment groups will be assessed using the 199 199 BCX1812-311 (V1.0: 24-August-2007) Page 44 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL log rank sta tistic controlling for RAT result a t screening, current sm oking behavior and influenza season at randomization (if necessary). Subjects who do not have resolution of fever will be censored at the tim e of their last non- missing post-baseline tem perature assessment. The MRU, MRU-related direct co sts, and indirect co sts attributable to days m issed of work and work productivity and/or perform ance losses will be summ arized by treatment group. Differences between each of the peramivir treatment groups and placebo group will be evaluated using both param etric and/or non-parametric tests, as appropriate. If necessary, bootstrapping techniques will be used to calculate confidence intervals around the incremental differences in costs. 12.6.3 Exploratory Endpoint Genotypic (including Hem agglutinin and Neurom inidase), phenotypic, viral culture and PCR data will be lis ted for each sub ject. These listings will be constructed in a m anner consistent with the F DA June 2006 Guidance Docum ent:“Guidance for Subm itting Influenza R esistance D ata”.18 Ad ditionally, the num ber and percen tage of genotypic changes from wild-type a mino acid will be summarized separately for treatm ent group, protein type, and study visit. 12.7 Safety Analyses AEs will be m apped to a MedDRA-pref erred term and system organ classification. The occurrence of TEAEs will be summarized by treatment group using MedDRA-preferred terms, system organ classifications, and severity. If a subject experiences multiple events that m ap to a s ingle p referred term, the grea test severity and st rongest Investigator assessment of relation to study d rug will be assigned to the preferred term for the appropriate sum maries. All AEs will be li sted f or individual subje cts showing both verbatim and preferred terms. Separate summaries of treatment-emergent SAEs and AEs related to study drug will be generated. Descriptive summaries of vital s igns and clinic al laboratory results will be presented by study visit. Laboratory abnorm alities will be graded according to the DAIDS Table for Grading Adverse Events for Adults and Pedi atrics (Publish Date: December 2004). The number and percentage of subjects experien cing treatm ent-emergent graded toxicities will be summarized by treatment group. Laborator y toxicity shifts from baseline to Day 3, Day 5, and Day 14 will be summarized by treatment group. Abnormal physical exam ination findings wi ll be presented by treatm ent group. The number and percent of subjects experiencing each abnormal physical examination finding will be included. Concomitant medications will be co ded using the WHO dictionary. The se data will be summarized by treatment group. Subject disposition will be presented for a ll s ubjects. The num ber of subjects who completed the study and discontinued from the study will be provided. The reasons for early discontinuation also will be presented. 200 200 BCX1812-311 (V1.0: 24-August-2007) Page 45 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.8 Sub-Study and Pharmacokinetic Analysis The sub-study to exam ine exposure respons e, along with the corresponding single PK samples collected on all subjects on study day 3 will be co mpleted as part of the sub- study. All s tatistical m ethods will be outlin ed as part of the sub-stu dy protocol and exposure-response analysis plan. All sub-study analyses will be reported in a separate sub-study report. 12.9 General Issues for Statistical Analysis 12.9.1 Multiple Comparisons and Multiplicity In order to m aintain the overall typ e I e rror in the presen ce of the plann ed comparisons between the two peram ivir treatm ents and pl acebo, a Bonferroni correction will be applied to the prim ary efficacy end point an alysis. No oth er ad justments for m ultiple comparisons are planned. 12.9.2 Covariates Primary and secondary efficacy analyses will be adjusted for RAT result at screen ing, current smoking behavior and influenza season at randomization (if necessary). 12.9.3 Planned Sub-Groups The prim ary efficacy endpoint will be summ arized separately by stratification group (current sm oking behavior [sm oker or non-smoker] and RAT result at screening [negative or positive]) and by viral subtype using descriptive statistics by treatment group and study day, if appropriate. No formal statistical testing will be utilized. Additional analyses m ay be perform ed by count ry, if necessary, for subm ission to local regulatory authorities. 12.9.4 Missing Data Every effort will be m ade to obtain required data at each s cheduled evaluation from all subjects who have been random ized. No attemp t will be m ade retrospectively to obtain missing subject reported data (including in fluenza symptom severity assessm ents, temperature, ability to perf orm usual activi ties, m issed days of work and im pact of influenza on subject’s work perform ance and/or productivity) that has not been completed by the subject at the time of return of the subject diary to the investigative site. In situations where it is not possible to obt ain all da ta, it m ay be necessary to im pute missing data. In assessing the p rimary efficacy endpoint, fo r subjects w ho withdraw or who d o no t experience allev iation of sym ptoms, m issing data will be censored using the date of subject’s last non-m issing assessment of infl uenza symptoms. Missing assessm ents of influenza symptoms conservatively will be im puted as h aving severity above absen t or mild (as f ailures). For the subjec t diary data, the f ollowing data con ventions will be utilized. Missing diary com pletion will be imputed as 11:59 for diary entries designated 201 201 BCX1812-311 (V1.0: 24-August-2007) Page 46 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL as m orning and 23:59 for evening and daily reported v alues. Entr ies with va lues exceeding the 24-hour clock will b e set to 23:59 of the day recorded. Select explo ratory sensitivity analyses m ay be conducted to ascert ain the effect, if any, of these m ethods. These sensitivity analy ses are further de scribed in the SAP. Secondary efficacy endpoints with tim e to event da ta will be censored using the date of subject’s last non- missing assessment of the given endpoint. 13 STUDY ADMINISTRATION 13.1 Regulatory and Ethical Considerations 13.1.1 Regulatory Authority Approvals This study will be conducted in com pliance with th e protoco l; GCPs, including International Conference on Harmonization (ICH) of Te chnical Requirem ents for Registration of Pharm aceuticals for Hu man Use G uidelines; FDA regulatory requirements and in accordance with the ethical principles of the Declaration of Helsinki. In addition, all applicable loca l laws and regu latory requirements relevant to the use of new therapeutic agents in the countries involved will be adhered to. The Investigator should submit written reports of clinical study status to their Institutional Review Board (IRB)/ Independent E thics Committee (IEC) annually or more frequently if requested by the IRB/ IEC. A final s tudy notification will also be forwarded to the IRB/IEC af ter the study is com pleted or in the event of prem ature ter mination of the study in accordance with the appl icable regulations. Copies of all contact with the IRB/ IEC should be m aintained in the study docum ents file. Copies of clinical study status reports (including termination) should be provided to BioCryst. 13.1.2 Ethics Committee Approvals Before initiation of the study at each invest igational site, the pr otocol, the inform ed consent form, the subject inform ation sheet, and any other relevant study documentation will be sub mitted to th e appropriate IRB/IE C. W ritten approval of th e study m ust be obtained before the study center can be initiated or the investigational medicinal product is re leased to the Inv estigator. A ny necessa ry extension s or renew als of IRB/IEC approval must be obtained, in particular, for changes to the study such as modification of the pro tocol, the inf ormed consent f orm, th e written inform ation provided to subjects and/or other procedures. The Investigator will report promptly to the IRB/IEC any new inform ation that m ay adversely affect the safety of the subjects or the conduct of the study. On completion of the study, the Investigator will prov ide the IRB/IEC with a report of the outcom e of the study. 13.1.3 Subject Informed Consent Signed info rmed consent m ust be obtained from each subject p rior to performing any 202 202 BCX1812-311 (V1.0: 24-August-2007) Page 47 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL study-related procedures. E ach subject should be given both verbal and w ritten information describing the nature and durati on of the clinical st udy. The inf ormed consent process should take place u nder conditions where the subject h as adequate time to consider the risks and bene fits associated with his/her participation in the study. Subjects will not be screened or treated until the subjec t has signed an approved ICF written in a language in which the subject is fluent. The ICF that is used must be approved both by BioCryst and by the reviewing IRB/ IEC. The informed consent should be in acco rdance with the curren t revision o f the Declaration of Helsinki, current ICH and GCP guidelines, and BioCryst policy. The Investigator must explain to potential subjects or their legal representatives the aims, methods, reasonably anticipated benefits, a nd potential hazards of the trial and any discomfort it may entail. Subjects will be informed that they are free not to participate in the trial and that they may withdraw consent to participate at any time. They will be told that refusal to participate in the study will not prejudice future treatment. They will a lso be told tha t their recor ds m ay be exam ined by com petent autho rities and au thorized persons but that pe rsonal information will be tr eated as strictly confidential and will not be publicly available. Subjects must be given the opportunity to ask questions. After this explanation and before entry in to the trial, consent should be appropriately recorded by means of the subject’s dated signature. The subject shoul d receive a signed and dated copy of the ICF. The original signed infor med consent should be retained in the study files. The Investigator shall maintain a log of all subjects who sign the ICF and indicate if the subject was enrolled into the study or reason for non-enrollment. 13.1.4 Payment to Subjects Reasonable compensation to study subjects may be provided if approved by the IRB/IEC responsible for the study at the Investigator’s site. 13.1.5 Investigator Reporting Requirements The Investigator will provide tim ely repo rts regard ing s afety to his /her IRB/IE C as required. 13.2 Study Monitoring During trial conduct, BioCryst or its designee will conduct period ic monitoring visits to ensure that the protocol and GCPs a re being followed. The monitors may review source documents to conf irm that th e data recorded on CRFs is accurate. The investigator and institution will allow BioCryst m onitors or its des ignees and app ropriate regulatory authorities direct access to source documents to perform this verification. 13.3 Quality Assurance The trial site may be subject to review by the IRB/IEC, and/or to quality assurance audits performed by BioCryst, and/or to inspection by appropriate regulatory authorities. It is important that the investigator(s) and their relevant personnel are available during the monitoring visits and possible a udits or inspections and that sufficient tim e is devoted to 203 203 BCX1812-311 (V1.0: 24-August-2007) Page 48 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL the process. 13.4 Study Termination and Site Closure BioCryst reserves the right to disc ontinue the tr ial prio r to inc lusion of the in tended number of subjects but intends only to exer cise this r ight f or valid scientif ic or administrative reasons. After such a deci sion, the Investigator must contact all participating subjects immediately after notification. As directed by BioCryst, all study materials must be collected a nd all case report forms completed to the greatest extent possible. 13.5 Records Retention To enable evaluations and/or audits from regulatory au thorities o r BioCryst, the Investigator agrees to k eep records, includi ng the iden tity of all p articipating sub jects (sufficient inf ormation to link re cords, case report forms and hospital records), all original signed inform ed consent form s, copies of all case report form s and detailed records of treatm ent disposition. The reco rds should be retained by the Investigator according to local regulations or as specified in the Clinical Trial Agreem ent, whichever is longer. If the Investigator relocates, retires, or for any reason withdraws from the study, the study records m ay be transferred to an acceptab le designee, such as another investigato r, another institution, or to BioCryst. The I nvestigator m ust obtain BioCryst’s written permission before disposing of any records. 13.6 Study Organization 13.6.1 Data Monitoring Committee BioCryst will a ssemble an indep endent Data M onitoring C ommittee ( DMC) to as sess safety parameters of the trial on a period ic, ongoing basis while the tr ial is in prog ress. The comm ittee will include a s tatistician and th ree phys icians, tw o of whom will be Infectious Disease specialists. Full detail s of the com position of the D MC and how the DMC is to operate will be described in a separate DMC charter. 13.7 Confidentiality of Information BioCryst affirms the subject’s right to prot ection against invasion of privacy. Only a subject id entification n umber, initials and /or date of birth will id entify subject data retrieved by BioCryst . However, in com pliance with federal regulations, BioCryst requires the investigato r to p ermit BioCryst ’s representatives and, when neces sary, representatives of the FDA or other regu latory authoritie s to review and/or copy any medical records relevant to the study. BioCryst will ensure that the use and disclosur e of protected health information obtained during a research study com plies with the HIPAA Privacy Rule. Th e Rule pro vides federal protection for the privacy of prot ected health inf ormation by im plementing standards to protec t an d guard ag ainst the m isuse of ind ividually id entifiable h ealth 204 204 BCX1812-311 (V1.0: 24-August-2007) Page 49 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL information of subj ects participating in BioCryst-sponsored Clinical Trials. "Authorization" is required from each research subject, i.e., specified permission granted by an individual to a covered entity for the us e or disclosure of an indi vidual's protected health information. A valid au thorization must meet the implem entation specifications under the HIPAA Pri vacy Rule. Authorizat ion m ay be com bined in the Inform ed Consent docum ent (approved by the IRB/IE C) or it may be a separate docum ent, (approved by the IRB/IEC) or provided by the Investigator or Sponsor (without IRB/IEC approval). It is the responsibility of the investigator and institution to obtain such waiver/authorization in writing f rom the appr opriate ind ividual. HIPAA authoriz ations are required for U.S. sites only. 13.8 Study Publication All data generated from this study are the propert y of BioCryst and shall be held in strict confidence along with all inform ation furnis hed by BioCryst. Independent analysis and/or publication of these data by the Investigator or any member of his/her staff are not permitted without prior written consent of BioCryst. W ritten perm ission to the Investigator will be contingen t on the review by BioCryst of the statistical ana lysis and manuscript and will provide fo r nondisclosure of BioCryst confidential or proprietary information. In all case s, the partie s agree to s ubmit all m anuscripts or abstracts to all other par ties 30 days prior to su bmission. This will e nable all parties to pr otect proprietary information and to provide comme nts based on infor mation that may not yet be available to other parties. 205 205 BCX1812-311 (V1.0: 24-August-2007) Page 50 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 14 REFERENCES 1. Cox NJ, Subbarao K. Influenza. Lancet 1999;354(9186):1277–1282. 2. Thompson WW, Shay KD, Weintraub E, Branner L, Cox N, et al. Mortality associated with influenza and respiratory syncytial virus in the United States. JAMA 2003;289(2):179–186. 3. Kaiser L, Wat C, Mills T, Mahoney P, Ward P, et al. Impact of oseltamivir treatment on influenza-related lower respiratory tract complications and hospitalizations. Arch Intern Med 2003;163(14):1667–1672. 4. Hayden FG, Treanor JJ, Fritz RS, Lobo M, Betts RF, et al. Use of the oral neuraminidase inhibitor oseltamivir in experimental human influenza: randomized controlled trials for prevention and treatment. JAMA 1999;282(13):1240–1246. 5. Kiso M, Mitamura K, Sakai-Tagawa Y, Shiraishi K, Kawakami C, et al. Resistant influenza A viruses in children treated with oseltamivir: descriptive study. Lancet 2004;364(9436):759–765. 6. Bantia S, Parker CD, Ananth SL, Horn LL, Andries K, et al. Comparison of the anti- influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir. Antimicrob Agents Chemother 2001;45(4):1162–1167. 7. Boivin G, Goyette N. Susceptibility of recent Canadian influenza A and B virus isolates to different neuraminidase inhibitors. Antiviral Res 2002;54(3):143–147. 8. Gubareva LV, Webster RG, Hayden FG. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother 2001;45(12):3403–3408. 9. Govorkova EA, Fang HB, Tan M, Webster RG. Neuraminidase inhibitor-rimantadine combinations exert additive and synergistic anti-influenza virus effects in MDCK cells. Antimicrob Agents Chemother 2004;48(12):4855–4863. 10. BioCryst Pharmaceuticals. Unpublished data. 11. Arnold CS, Zacks MA, Dziuba N, Yun N, Linde N, Smith J, Babu YS, Paessler S. Injectable peramivir promotes survival in mice and ferrets infected with highly pathogenic avian influenza A/Vietnam/1203/04 (H5N1). V-2041B, ICAAC 2006, San Francisco 12. Boltz, DA, Ilyushina NA, Arnold CS, Babu, YS, Webster RG and Govorkova EA. Intramuscular administration of neuraminidase inhibitor peramivir promotes survival against lethal H5N1 influenza infection in mice. Antiviral Research,2007; 74 (3): A32 13. BioCryst Pharmaceuticals unpublished clinical study report BC-01-03. 14. Tamiflu® Package Insert. Roche Pharmaceuticals. Rev. December 2005. 15. Quidel QuickVue Influenza A+B and Binax NOW Influenza A&B Test Kit product information sheets 206 206 BCX1812-311 (V1.0: 24-August-2007) Page 51 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 16. Treanor JJ, Hayden FG, Vrooman PS, Barbarash R et al. Efficacy and safety of the oral neuraminidase inhibitor oseltamivir in treating acute influenza. JAMA 2000; 283(8): 1016-1024. 17. Nicholson KG, Aoki FY, Osterhaus AD, Trottier S et al. Efficacy and safety of oseltamivir in treatment of influenza: a randomised controlled trial. Lancet 2000; 355(9218): 1845-1850. 18. US Department of Health and Human Services, Food and Drug Administration Center for Drug Evaluation and Reserach (CDER). Attachment to Guidance on Antiviral Product Development- Conducting and Submitting Virology Studies to the Agency: Guidance for Submitting Influenza Resistance Data. http://www.fda.gov/cder/guidance/7070fnlFLU.htm 207 207 BCX1812-311 (V1.0: 24-August-2007) Page 52 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15 APPENDICES 15.1 NYHA Functional Classification Criteria: Heart Failure and Angina NYHA Functional Classification of Heart Failure Class I No symptoms. Ordinary physical activity such as walking and climbing stairs does not cause fatigue or dyspnea. Class II Symptoms with ordinary physical activity. W alking or climbing stairs rapidly; walking uphill; walking or st air climbing after meals, in cold weather, in wind, or when under em otional stress causes undue fatigue or dyspnea. Class III Symptoms with less than ordinary physical activity. W alking one to two blocks on the level and clim bing more than one flight of stairs in normal conditions causes undue fatigue or dyspnea. Class IV Symptoms at res t. Inab ility to carry on any ph ysical activity without fatigue or dyspnea. NYHA Functional Classification of Angina Class I Angina only with unusually strenuous activity. Class II Angina with slightly m ore prolonged or slightly more vigorous activity than usual. Class III Angina with usual daily activity. Class IV Angina at rest. 208 208 CLINICAL STUDY PROTOCOL Protocol No. BCX1812-311 IND No. 76,350 A PHASE 3 MULTICENTER, RANDOMIZED, DOUBLE BLIND, PLACEBO- CONTROLLED STUDY TO EVALUATE THE EFFICACY AND SAFETY OF INTRAMUSCULAR PERAMIVIR IN SUBJECTS WITH UNCOMPLICATED ACUTE INFLUENZA THE IMPROVE 1 STUDY (IntraMuscular Peramivir for the Relief Of symptoms and Virologic Efficacy) Short title: Intramuscular Peramivir for the Treatment of Uncomplicated Influenza Protocol Date: Version1.0: 04 September 2007 BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35244, USA Phone: +1 919 859 1302 Fax: +1 919 851 1416 The document contains trade secrets and proprietary information of BioCryst Pharmaceuticals, Inc. This information is confidential property of BioCryst Pharmaceuticals, Inc., and is subject to confidentiality agreements entered into with BioCryst Pharmaceuticals, Inc. No information contained herein should be disclosed without prior written approval. CONFIDENTIAL 209 209 BCX1812-311 (V1.0: 04-September-2007) Page 2 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1 TITLE PAGE Protocol Number: BCX1812-311 Study Title: A phase 3 m ulticenter, random ized, double-blind, placebo-controlled s tudy to evaluate th e effic acy and safety of intram uscular peram ivir in subjec ts with uncomplicated acute influenza IND Number: 76, 350 Investigational Product: Peramivir (BCX1812) Indication Studied: Uncomplicated acute influenza Sponsor: BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35233 Development Phase: 3 Sponsor Medical Officer: W. James Alexander, M.D., M.P.H. Senior Vice President, Clinical Development Chief Medical Officer Phone: +1 919 859 1302 Fax: +1 919 851 1416 Email Address: jalexander@biocryst.com Compliance Statement: This study will be conducted in accordance with the ethical principles that have their origin in the Declaration of Helsinki and clinical research guidelines established by the Code of Federal Regulations (Title 21, CFR Parts 50, 56, and 312) and ICH Guidelines. Essential study documents will be archived in accordance with applicable regulations. Final Protocol Date: Version 1.0: 04 September 2007 Amendment(s) Date(s): None 210 210 211 211 BCX1812-311 (V1.0: 04-September-2007) Page 4 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1.2 Clinical Study Protocol Agreement Protocol No. BCX1812-311 Protocol Title: A phase 3 m ulticenter, random ized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peram ivir in subj ects with uncom plicated acute influenza I have caref ully read th is protoco l and agree that it contains all of the necessary information required to conduct this study. I agree to conduct this study as described and according to the Declaration of Helsinki, International Conference on Harmonization Guidelines for Good Clinical Practices, and all applicable regulatory requirements. Investigator’s Signature Date Name (Print) 212 212 BCX1812-311 (V1.0: 04-September-2007) Page 5 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 2 SYNOPSIS Protocol No. BCX1812-311 Protocol Title: A Phase 3, Multicenter, Random ized, Double-Blind, Placebo-Controlled Stu dy to Evaluate the Efficacy an d Safety of Intram uscular Peram ivir in Subjects with Uncomplicated Acute Influenza Sponsor: BioCryst Pharmaceuticals, Inc. Investigators/Study Sites: Multinational Development Phase: 3 Objectives: Primary: To evaluate the efficacy of peram ivir adm inistered intramuscularly com pared to p lacebo on th e tim e to alleviation of clinica l sym ptoms in adult sub jects with uncomplicated acute influenza. Secondary: 1. To evalua te the saf ety and tolera bility of pe ramivir administered intramuscularly; 2. To evaluate seconda ry clinical outcom es in response to treatment; 3. To evaluate changes in in fluenza virus titer (viral shedding) in response to treatment; 4. To assess p harmacoeconomic m easures in resp onse to treatment 5. To assess c hanges in inf luenza vir al suscep tibility to neuraminidase inhibitors following treatment Number of Subjects: Total enrollm ent: up t o 800 subjects random ized (160 subjects in the placebo treatment group, 320 subjects in the peramivir 150mg treatment group and 320 subjects in the peramivir 300m g treatm ent group). The study will close after enrollment of at least 500 subjects who have either a positive Influenza A or B antigen te st (Rapid Antigen Test – RAT) at screening, or who ha ve a negative RAT at screening but a positive influenza A or B PCR a ssay result from a baseline nasopharyngeal swab. Study Design: This is a multinational, random ized, double-blind study comparing the efficacy and safety of two single dos e regimens of peramivir administered intramuscularly versus placebo in adults with uncom plicated acute influenza. Each subjec t’s ass ignment to trea tment will be stra tified according to the Rapid Antigen Test (RAT) result at screening and current sm oking be havior, with 80% of subjects ce ntrally rand omized to one of the two activ e 213 213 BCX1812-311 (V1.0: 04-September-2007) Page 6 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL single dose regimens of peramivir (2:2:1 randomization) Treatment Group 1: Peramivir 150mg Treatment Group 2: Peramivir 300mg Treatment Group 3: Placebo Enrollment of subjects into the RAT negative s tratum will be permitted at individual sites that have identified 3 RAT positive su bjects a t s creening within a 10 d ay per iod, indicating activity of influenza in the site ’s vicinity. After identification of 3 RAT positive subjects within 10 days, a site m ay enroll 1 RAT negative s ubject tha t f ulfills the inclusion/ exclusion criteria. One additional RAT negative subject may be enrolled thereafter for each preceding RAT positive subject that is identified. Study drug will be adm inistered as one 2mL intramuscular injection in each glu teal muscle (total of 4m L injected in divided doses). Subjects eligible for s creening will have an anterior nasal or pharyngeal swab collected for t esting by RAT for influenza A and B, in accordan ce with the co mmercially available RAT kit instructi ons. I f the in itial RAT is negative, th e te st shou ld be repeated with a differen t commercially availab le RAT kit. Subjects m eeting the inclusion/ exclusion criteria may be enrolled into the study. All enrolled subjects will record the following in a Study Diary: • Oral temperature measurements taken with an electronic thermometer every 12 hours. W ith the exception of the baseline m easurement, all tem perature m easurements will be ob tained at least 4 hours after, or imm ediately before, adm inistration of oral acetaminophen (paracetamol), aspirin, ibuprofen or other NSAID. • Assessment of severity of each of s even sym ptoms of influenza on a 4-point scale (0, absent; 1, m ild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatm ent, then once daily (AM) through Day 14 • Assessment of subjec t’s ability to p erform usual activities, (rated as 0–10 on a visual analog scale) once daily through Day 14 • Assessment of subject’s tim e lost from work or usual activities and productivity compared to normal (rated as 214 214 BCX1812-311 (V1.0: 04-September-2007) Page 7 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 0-10 on a visual analog scal e) once daily through Day 14 • Doses of antipyretic, expe ctorant, and/ or t hroat lozenges taken for symptomatic relief each day through Day 14 Anterior nose (bilateral) and posterior pharynx specim ens (swabs) will be collected at Day 1 (pre-treatm ent) and at Days 3, 5, and 9, for quantitative virologic assessments. In a subset of a m inimum of 200 subjects, an additional virology sample will b e co llected on day 2. Specim ens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result). All virolog ic ass essments will b e p erformed by a c entral laboratory. At the study day 3 visit, when all subjects are evaluated for safety and a blood draw is com pleted for clinical laboratory investigations, a single pharm acokinetic (PK) sample will also be drawn. This sin gle PK sam ple will b e analyzed for plasm a concentrations of peram ivir (ng/mL) and evaluated in an exposure response analysis. At selected sites a separate sub-s tudy will be conducted to collect limited PK sam ples for the purpose of conducting an exposure-respons e analysis. T his sub-stud y will be conducted under a separate protocol, BCX1812-311PK. Study Population: Male and fem ale subjects, 18 y ears of age and older, with symptoms consisten t with a diagnosis of uncomplicated acute influenza infectio n may be screened for e nrollment. Subject eligibility will be dependent on the presence of two or more symptoms consistent with acute inf luenza as well as the results obtained f rom a rapid antigen test (RAT) for influenza A and B at screening. Inclusion Criteria: 1. Male and non-pregnant female subjects age ≥18 years 2. A positive Influenza A or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate specimen collected from an anterior nasal or pharyngeal swab, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated with a different commercially available RAT kit. A limited number of RAT negative 215 215 BCX1812-311 (V1.0: 04-September-2007) Page 8 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subjects may be enrolled in accordance with a defined screening algorithm. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. For subjects with a positive RAT at the time of screening, a subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at time of screening. For subjects with no positive RAT at screening, fever as defined above must be documented at time of screening 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of any severity (mild, moderate, or severe) 5. Presence of at least one constitutional symptom (myalgia [muscle aches], headache, feverishness, or fatigue) of any severity (mild, moderate, or severe) 6. Onset of symptoms no more than 48 hours before presentation for screening 7. Written informed consent Exclusion Criteria: 1. Women who are pregnant or breast-feeding 2. Presence of clinically significant signs of acute respiratory distress 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class IV functional status within the past 12 months 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 6. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min) 7. Current clinical evidence of active bacterial infection at any body site that requires therapy with oral or systemic antibiotics 8. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy 9. Current treatment for active viral hepatitis C 10. Presence of known HIV infection with a CD4 count <350 cell/mm3 11. Current therapy with oral warfarin or other systemic 216 216 BCX1812-311 (V1.0: 04-September-2007) Page 9 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL anticoagulant 12. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening 13. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days 14. History of alcohol abuse or drug addiction within 1 year prior to admission in the study 15. Participation in a previous study of peramivir as treatment for acute influenza or previous participation in this study 16. Participation in a study of any investigational drug within the last 30 days Study Endpoints: Primary Endpoint: Clinical: Time to alleviation of clinical symptoms of influenza Secondary Endpoint(s): Safety Incidence of treatm ent-emergent adverse events and treatment-emergent changes in clinical laboratory tests Clinical: Time to resum ption of subjec t’s ab ility to perf orm usual activities Time to resolution of fever Incidence of influenza related complications Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID 50) and/or by quantitative polymerase chain reaction (PCR) assay Pharmacoeconomic: Medical resource utilization (M RU), missed days of work, and im pact of inf luenza illn ess on subject’s work performance and/or productivity. Exploratory Endpoint: Viral Susceptibility: Change in influenza virus susceptibility to neu raminidase inhibitors Investigational Product, Dose, and Mode of Administration: Peramivir (BCX-1812), 75m g/mL or placebo (buffered diluent), 2mL per injection, ad ministered intramuscularly in the gluteal muscle, bilaterally. Duration of Treatment: Following treatment on day 1, study duration for individual 217 217 BCX1812-311 (V1.0: 04-September-2007) Page 10 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subjects is expected to be up to 14 days (including all visits). Statistical Methods: Descriptive statistical methods will be used to summ arize the data from this study, with statistical testing utilized for the p rimary and secondary efficacy endpoints. Unless otherwise n oted, a ll s tatistical testing will be two-sided, and will be performed using a significance (alpha) level of 0.05. For assessment of the prim ary efficacy endpoint, th e overall sig nificance level will be m aintained by a Bonferroni adjustm ent fo r the planned com parisons between the two active trea tment groups and placebo. Detailed sta tistical pro cedures will be provided in a f ull statistical analysis plan (SAP) completed prior to database lock and study unblinding. Sample Size: From previous studies of neuram inidase treatm ent of uncomplicated influenza it is expected that the median time to alleviation of symptoms will be 103.3 hours for subjects receiving placebo. Addition ally, it is expected that the median time to alleviation for the low dose peram ivir arm will be 69.9 hours, yielding a hazard ratio of 0. 68. Using these assumptions, a sample si ze of 200 influenza-infected subjects per active treatm ent group and 100 infected subjects in the placebo group (a total of 500 influenza- infected su bjects) is s ufficient to provide at least 80% power to detect a hazard ratio of 0.68 using a log-rank statistic and α = 0.025 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). Up to 800 subjects will be enrolled to ach ieve the target number of at least 500 subjects with diagnostic evidence (R AT or PCR) of an acute influenza infection. Efficacy: The intent-to-treat infected population will include all subjects who are random ized, received study drug, and have proven influenza by any one of the following: primary viral culture, PCR, or paired serology showing ≥ 4-fold increase in antibody to influenza A or B. The primary efficacy v ariable is th e tim e to alleviation of symptoms, defined as the time from injection of study drug to the start of the tim e period when each of seven symptoms of influenza are either absent or are present at no more than mild severity level and remain at no worse than this severity status for a 24 hour period. Descriptive statistics for the primary efficacy variable will 218 218 BCX1812-311 (V1.0: 04-September-2007) Page 11 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL be tabulated by treatm ent group. Alleviation of sym ptoms will be determined by assessment of symptoms as reported on each su bject’s diary card. Tim e to alle viation of symptoms will b e sum marized for each treatm ent group. Treatment dif ference will be as sessed us ing a Cox Regression model with effects for RAT result at screening, current smoking behavior, tr eatment group, and influenza season at random ization. Pa irwise com parisons between each active group and placebo will be constructed from the Cox Regression m odel. Subj ects who do not experience alleviation of sym ptoms will be c ensored a t the date of their last non-m issing assessment. Tim e to resum ption of usual activities and tim e to resolution of f ever will be analyzed in a similar manner. Changes in viral titer s will be compared using the van Elteren sta tistic con trolling f or RAT result at screen ing, current smoking behavior and influenza season at randomization. Analyses of other continuous endpoints will be analyzed in a similar manner. Safety: Safety analyses will b e presen ted f or all sub jects in the safety population, defined as all randomized subjects who receive at least one dose of study drug. Adverse events will be m apped to a Medica l Dictiona ry f or Regulatory Activities (MedDRA) preferred term and system organ classification. The occurrence of treatm ent-emergent AEs will be summarized using preferre d term s, system organ classifications, and severit y. Separate summ aries of treatment-emergent SAEs and treatm ent-emergent AEs that are related to study m edication will be generated. All AEs will be listed f or individua l subjec ts sho wing both verbatim and preferred terms. Descriptive summaries of vital signs and quantitative clinical laboratory changes will be presented by study visit. Frequency and percentages of subjects with abnorm al laboratory test r esults will be su mmarized b y toxic ity grade. Concomitant m edications w ill be m apped to a W HO preferred term and drug classification. The num ber and percent of subjects taking concomitant medications will be summarized using preferred terms and drug classifications. The num ber and percent of subjects experiencing each 219 219 BCX1812-311 (V1.0: 04-September-2007) Page 12 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL abnormal physical examination finding will be presented. The number and percent of s ubjects discontinuing study as well as the reasons for discontinuation will be summarized by treatment group. Protocol Date Version 1.0: 04 September 2007 220 220 BCX1812-311 (V1.0: 04-September-2007) Page 13 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 3 TABLE OF CONTENTS 1 TITLE PAGE...................................................................................................... 2 1.1 PROTOCOL APPROVAL SIGNATURE PAGE............................................................. 3 1.2 CLINICAL STUDY PROTOCOL AGREEMENT .......................................................... 4 2 SYNOPSIS.......................................................................................................... 5 3 TABLE OF CONTENTS.................................................................................. 13 3.1 LIST OF FIGURES................................................................................................ 15 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS................... 16 5 INTRODUCTION ............................................................................................ 18 5.1 BACKGROUND.................................................................................................... 18 5.2 RATIONALE FOR STUDY..................................................................................... 18 5.3 NON-CLINICAL EXPERIENCE WITH PERAMIVIR.................................................. 19 5.3.1 In vitro Assays .............................................................................................. 19 5.3.2 Animal Models.............................................................................................. 20 5.4 PREVIOUS PHASE 3 CLINICAL EXPERIENCE WITH ORAL PERAMIVIR.................. 20 5.5 PREVIOUS PHASE 1 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR................ 21 5.6 DOSE RATIONALE .................................................................................................... 22 6 STUDY OBJECTIVES..................................................................................... 23 6.1 OBJECTIVES ....................................................................................................... 23 6.1.1 Primary Objective......................................................................................... 23 6.1.2 Secondary Objective(s)................................................................................. 23 6.2 STUDY ENDPOINTS............................................................................................. 23 6.2.1 Primary Endpoint.......................................................................................... 23 6.2.2 Secondary Endpoint(s).................................................................................. 23 6.2.3 Exploratory Endpoint.................................................................................... 23 7 STUDY DESIGN ............................................................................................. 24 7.1 OVERALL STUDY DESIGN AND PLAN ................................................................. 24 8 SELECTION AND WITHDRAWAL OF SUBJECTS.................................... 25 8.1.1 Inclusion Criteria .......................................................................................... 25 8.1.2 Exclusion Criteria ......................................................................................... 26 8.1.3 Removal of Subjects from Therapy or Assessment...................................... 27 9 TREATMENTS................................................................................................ 28 9.1 TREATMENTS ADMINISTERED............................................................................ 28 9.2 IDENTITY OF INVESTIGATIONAL PRODUCT(S) .................................................... 28 9.3 METHOD OF ASSIGNING SUBJECTS TO TREATMENT GROUPS ............................. 28 9.4 STUDY MEDICATION ACCOUNTABILITY............................................................. 29 9.5 BLINDING/UNBLINDING OF TREATMENTS.......................................................... 29 9.6 PRIOR AND CONCOMITANT THERAPIES.............................................................. 29 9.7 OVERDOSE AND TOXICITY MANAGEMENT......................................................... 29 9.8 DOSE INTERRUPTION.......................................................................................... 29 10 STUDY CONDUCT......................................................................................... 30 10.1 EVALUATIONS.................................................................................................... 30 10.1.1 Medical History ........................................................................................ 30 10.1.2 Rapid Antigen Test for Influenza ............................................................. 30 10.1.3 Physical Examination and Influenza-related Complications Assessments30 221 221 BCX1812-311 (V1.0: 04-September-2007) Page 14 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.4 Vital Signs................................................................................................. 31 10.1.5 Electrocardiogram Measurements ............................................................ 31 10.1.6 Clinical Chemistry Profiles....................................................................... 31 10.1.7 Hematology Profiles ................................................................................. 31 10.1.8 Serology for Influenza .............................................................................. 31 10.1.9 Urinalysis and Evaluation of Protein in Urine.......................................... 31 10.1.10 Urine Pregnancy Test................................................................................ 32 10.1.11 Samples for Virologic Laboratory Assessments....................................... 32 10.1.12 Subject Self Assessments.......................................................................... 32 10.1.13 Concomitant Medications......................................................................... 33 10.1.14 Adverse Events ......................................................................................... 33 10.1.15 Single Pharmacokinetic Exposure Sample ............................................... 33 10.2 SCREENING ........................................................................................................ 33 10.2.1 Informed Consent...................................................................................... 33 10.2.2 Screening/Baseline Evaluation and Enrollment........................................ 33 10.3 TREATMENT PERIOD—STUDY DAY 1................................................................ 34 10.3.1 Pre-dose Evaluations................................................................................. 34 10.4 POST-TREATMENT ASSESSMENT PERIOD........................................................... 34 10.4.1 Days 2, 3, 5, 9 and 14................................................................................ 34 10.4.2 Adverse Events Reported at Post-treatment Visits................................... 35 11 ADVERSE EVENT MANAGEMENT............................................................ 38 11.1 DEFINITIONS ...................................................................................................... 38 11.1.1 Adverse Event........................................................................................... 38 11.1.2 Serious Adverse Event.............................................................................. 38 11.2 METHOD, FREQUENCY, AND TIME PERIOD F OR DETECTING ADVERSE EVENTS AND REPORTING SERIOUS ADVERSE EVENTS..................................................... 39 11.2.1 Definition of Severity ............................................................................... 39 11.2.2 Definition of Relationship to Study Drug................................................. 39 11.2.3 Reporting Serious Adverse Events ........................................................... 40 11.2.4 Emergency Procedures.............................................................................. 41 12 STATISTICAL METHODS............................................................................. 41 12.1 DATA COLLECTION METHODS........................................................................... 41 12.2 STATISTICAL ANALYSIS PLAN ........................................................................... 42 12.3 SAMPLE SIZE ESTIMATES................................................................................... 42 12.4 ANALYSIS POPULATIONS ................................................................................... 42 12.4.1 Intent-To-Treat Population ....................................................................... 42 12.4.2 Intent-To-Treat Infected Population ......................................................... 42 12.4.3 Safety Population...................................................................................... 43 12.5 INTERIM AND END OF STUDY ANALYSES........................................................... 43 12.6 EFFICACY ANALYSES......................................................................................... 43 12.6.1 Primary Efficacy Endpoint ....................................................................... 43 12.6.2 Secondary Efficacy Endpoints.................................................................. 44 12.6.3 Exploratory Endpoint................................................................................ 45 12.7 SAFETY ANALYSES ............................................................................................ 45 12.8 SUB-STUDY AND PHARMACOKINETIC ANALYSIS............................................... 46 12.9 GENERAL ISSUES FOR STATISTICAL ANALYSIS .................................................. 46 222 222 BCX1812-311 (V1.0: 04-September-2007) Page 15 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.9.1 Multiple Comparisons and Multiplicity.................................................... 46 12.9.2 Covariates ................................................................................................. 46 12.9.3 Planned Sub-Groups ................................................................................. 46 12.9.4 Missing Data............................................................................................. 46 13 STUDY ADMINISTRATION ......................................................................... 47 13.1 REGULATORY AND ETHICAL CONSIDERATIONS ................................................. 47 13.1.1 Regulatory Authority Approvals............................................................... 47 13.1.2 Ethics Committee Approvals.................................................................... 47 13.1.3 Subject Informed Consent......................................................................... 47 13.1.4 Payment to Subjects.................................................................................. 48 13.1.5 Investigator Reporting Requirements ....................................................... 48 13.2 STUDY MONITORING.......................................................................................... 48 13.3 QUALITY ASSURANCE........................................................................................ 48 13.4 STUDY TERMINATION AND SITE CLOSURE......................................................... 49 13.5 RECORDS RETENTION ........................................................................................ 49 13.6 STUDY ORGANIZATION...................................................................................... 49 13.6.1 Data Monitoring Committee..................................................................... 49 13.7 CONFIDENTIALITY OF INFORMATION ................................................................. 49 13.8 STUDY PUBLICATION ......................................................................................... 50 14 REFERENCES ................................................................................................. 51 15 APPENDICES .................................................................................................. 53 15.1 NYHA FUNCTIONAL CLASSIFICATION CRITERIA: HEART FAILURE AND ANGINA .......................................................................................................................... 53 3.1 List of Figures Figure 1 Study Measurements and Visit Schedule...................................................... 37 223 223 BCX1812-311 (V1.0: 04-September-2007) Page 16 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS AE adverse event ALT alanine aminotransferase AST aspartate aminotransferase AUC area under the curve AUC0–72 area under the curve from time 0 to 72 hours AUC0–∞ area under the curve extrapolated from time 0 to infinity CBC complete blood count CDC Centers for Disease Control and Prevention Cmax maximum plasma concentration CK creatine kinase CNS central nervous system COPD chronic obstructive pulmonary disease CRF Case Report Form CV coefficient of variation ECG Electrocardiogram GCP Good Clinical Practice HCG human chorionic gonadotropin HIV Human immunodeficiency virus IC50 median inhibitory concentration ICF informed consent form ICH International Conference on Harmonization IEC Independent Ethics Committee IRB Institutional Review Board IRC influenza related complications ITT intent-to-treat ITTI intent-to-treat infected IUD intrauterine device IVRS interactive voice response system LDH lactate dehydrogenase MedDRA Medical Dictionary for Regulatory Activities MRU medical resource utilization NSAID non-steroidal anti-inflammatory drug PCR polymerase chain reaction 224 224 BCX1812-311 (V1.0: 04-September-2007) Page 17 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL RAT Rapid Antigen Test RBC red blood cell SAE serious adverse event SAP statistical analysis plan SD standard deviation t1/2 elimination half-life t1/2 λz terminal half-life TCID50 time weighted change f rom baseline in log 10 tissue -culture infective dose50 TEAEs treatment-emergent adverse events Tmax time to attain maximum plasma concentration UPEP urine protein electrophoresis WBC white blood cell WHO World Health Organization 225 225 BCX1812-311 (V1.0: 04-September-2007) Page 18 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5 INTRODUCTION 5.1 Background Influenza v irus is a m ember of the orthomyxovirus fam ily and cau ses an acu te v iral disease of the respiratory tract. Typical influenza illness is characterized by abrupt onset of fever, headache, myalgia, sore throat, and nonproductive cough.1 The illness is usually self-limiting, with relief of symptoms occurring within 5 to 7 days. Nevertheless, it is an important disease for several reasons, including ease of comm unicability, short incubation time, rapid rate of viral mutation, morbidity with resultant loss of productivity, risk of com plicating conditions, and increased risk of death, pa rticularly in the e lderly. During 19 of the 23 influenza seasons between 1972/1973 a nd 1994/1995, estim ated influenza-associated deaths in the U nited States ranged from approxim ately 25 to m ore than 150 per 100,000 persons above 65 years of age, accounting for more than 90% of the deaths attributed to pneumonia and influenza.2 Presently, o nly a few m easures are availab le that can red uce th e im pact of influenza: active immunoprophylaxis with an inactivat ed or live attenu ated vaccine and chemoprophylaxis or therapy with an influe nza-specific antiviral drug. Neuram inidase inhibitors are the current m ainstay of an tiviral treatm ent for influenza. Mark eted neuraminidase inhib itors inc lude zanam ivir (Relenza ®, GlaxoSm ithKline) an d oseltamivir (Tamiflu®, Roche-Gilead) , an oral prodrug of the activ e agent, oseltamivir carboxylate. Influenza neuram inidase is a surface glycoprotei n that cleaves sialic acid residues from glycoproteins and glycolipids. The enzyme is responsible for the release of new viral p articles from infected cells and may also ass ist in the sp reading of virus through the mucus within the respiratory tract. The neuraminidase inhibitors represent an important advance in the treatment of influenza with respect to activity against influenza A and B viruses, with p roven therapeutic value in reduc ing influenza lower resp iratory complications,3 and lower rates of antiviral drug resistance4. The use of curren tly av ailable neu raminidase inhibitors has been lim ited by concerns including, the degree of effectiv eness, the requirement for an inhaler device (zanamivir), and the em ergence of resistant influenza vi rus variants in som e treated populations. 5 In addition, there are risks of bronchospasm w ith zanam ivir; and gastrointestinal side effects, with oseltamivir. Peramivir is a neuraminidase inhibitor that represents a potentially promising addition to the armamentarium of drugs for the treatment of influenza infections due to its potential for parenteral administration and lower frequency of dosing. 5.2 Rationale for Study An oral formulation of peram ivir has previously been evaluated in a f ull range of safety, tolerability, pharmacokinetic, and efficacy studies. In a m ultinational phase 3 clinical trial conducted in 1999-2001, oral peram ivir de monstrated antiviral activity against influenza A and B inf ections, and im provement in the r elief of clin ical sym ptoms. Because of the lim ited bioavailability of peramivir following oral administration (<5%), it was de termined that the paren teral route of administration is m ore appropriate for the 226 226 BCX1812-311 (V1.0: 04-September-2007) Page 19 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL delivery of peram ivir. Subsequent phase 1 studies of intrave nous and intram uscular formulations of peram ivir have confirm ed that parenteral routes of administration result in plasma levels of drug that are as much as 100 times those achieved via the oral route. Further details of these studies are provided below and in the Investigator Brochure. A phase 2 random ized, double blind, placeb o controlled study of two single dose regimens (150mg or 300m g) of intram uscular peramivir in subjects with uncom plicated acute influenza infections (study B CX1812-211) was initiated in early 2007 in North America and the UK. The study has been extended to sites in Hong Kong, Australia, New Zealand and South Africa and is expected to complete enrollment in m id-2007. At a scheduled meeting on 21 May 2007, an independ ent data monitoring committee for this study com pleted a blinded revi ew of all reported adverse events and grade 3 and 4 clinical laboratory evaluations from the first 135 subjects random ized. Following this blinded saf ety review the DMC provided a written reco mmendation that the s tudy continue as planned. Because of the previo us dem onstration of significant an tiviral activ ity, th e strong suggestion of clinical efficacy of oral pe ramivir previously dem onstrated in acute influenza, and the encouraging pharm acokinetic and prelim inary safety profile of the intramuscular formulation of pera mivir demonstrated to date, this phas e 3 study will be conducted to evaluate the efficacy and safety profile of intram uscular peramivir and to determine the optimal single dose regimen. 5.3 Non-Clinical Experience with Peramivir 5.3.1 In vitro Assays Peramivir is a selective inhibitor of vi ral neuram inidase, with 50% inhibitory concentrations (IC50) for bacterial and m ammalian enzymes of >300µM. 6 In an in vitro study, 42 influenza A and 23 influenza B isolates were collected from untreated subjects during the 1999–2000 influenza season in Canada. 7 These isolates were tested for their susceptibility to the neuram inidase inhib itors zanam ivir, oseltam ivir carboxylate, and peramivir using a chem iluminescent neuram inidase assay. Inhibition of Type A influenza neuraminidase by peram ivir was appr oximately an order of m agnitude greater than inhibition of neuram inidase from Type B viruses. IC 50 values for the Type A enzymes ranged from <0.1 to 1.4nM, whereas the Type B enzym es ranged from <0.1 to 11nM, with three out of four values in the 5- to 11nM range. Peram ivir was the most potent drug against influenza A (H 3N2) viruses with a m ean IC50 of 0.60nM as well as most potent against influenza B with a mean IC50 of 0.87nM. In another in vitro comparison of peram ivir, oseltam ivir, and zanam ivir, using a neuraminidase inhibition assay with influenza A viruses, the m edian IC 50 of pera mivir (approximately 0.34nM) was com parable to that of oseltam ivir (0.45nM) and significantly lower than zanam ivir (0.95nM). F or influenza B virus clinical isolates, the IC50 of peramivir (1.36nM) was comparable to that of zanamivir (2.7nM) and lower than that of oseltamivir (8.5nM).8 The potency of peram ivir was evaluated ag ainst five zanam ivir-resistant an d six oseltamivir-resistant influenza viruses.9 Peramivir remained a potent inhibitor against all 227 227 BCX1812-311 (V1.0: 04-September-2007) Page 20 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL oseltamivir-resistant viruses includi ng the m utations H274Y, R292K, E119V, and D198N, with IC 50 values ≤40nM. Peram ivir also potently inhibited (IC 50 ≤ 26nM) the neuraminidase activity of zanamivir-resistant strains, which had the following mutations: R292K, E119G, E119A, and E119D. Howeve r, one zanam ivir-resistant influenza B virus, B/Mem /96, with a m utation R152K isol ated from cell cultur e, was relatively resistant to all neuraminidase inhibitors, including peramivir (IC50 = 400nM). 5.3.2 Animal Models In a m ouse model of influen za infection, a single intram uscular injection of pera mivir (10mg/kg) given 4 hours prior to inoculation with an A/NWS/33 (H1N1) influenza strain resulted in 100% survival in contrast to 100% mortality in a control group injected with saline.6 In the sam e mouse m odel, treatm ent of m ice up to 72 hours after influenza infection using peram ivir (20m g/kg) result ed in 100% survival, compared to 100% mortality in the control group injected with vehicle.10 Peramivir has also dem onstrated activity in animal models utilizing a clinical H5 N1 isolate as th e infecting virus strain. In a mouse model, a single intramuscular dose of peramivir (30mg/kg) injected 1 hour after inoculation with the highly pathogenic (H5N1) A/Vietnam/1203/04 strain, resulted in a 70% survival rate that wa s similar to that seen in mice treated with oseltam ivir given orally at 10m g/kg/day for 5 days 11. In s imilar experiments, mice inoculated with the sam e strain of H5N1 virus tha t were then trea ted for up to 8 days with intram uscular peramivir exhibited 100% survival 12. This longer duration of peram ivir treatment also prevented viral replic ation in the lungs, brain and spleen at days 3, 6 and 9 post inoculation. 5.4 Previous Phase 3 Clinical Experience with Oral Peramivir An oral formulation of peram ivir has prev iously dem onstrated an tiviral activity and preliminary clinical efficacy in ch allenge studies in hum an volunteers, as well as in treatment studies in patients with u ncomplicated acute inf luenza inf ections dur ing the influenza seasons of 1999-2001. A Phase 3 multinational study (B C-01-03) of oral peramivir was conducted. Two dos e regimens of oral peramivir, 800mg QD for 5 days, or 800mg QD on Day 1, followed by 400mg QD for 4 days, were compared to a matched placebo treatment group. A total of 1246 subjects were randomized to treatment at sites in the USA, W estern and Eastern Europe, S outh America, Australia and New Zealand. As presente d in the tab le below, th e prim ary end-point of tim e to relief of influenza symptoms was not found to be significantly different (p=0.17) between the three treatment groups.13 A sub-group analysis of the time to relief of symptoms by country or region demonstrated marked differences in the prim ary endpoint.. In the subset of influenza-infected subjects enrolled at sites in the US, clinically m eaningful differences in time to relief of influenza symptoms between the placebo and the two peram ivir arms were observed, that just m issed statistical significance (p=0.07). However, a num ber of secondary end-points in this phase 3 study, such as tim e to overall well-being, time to normal activity, incidence of infl uenza rela ted com plications and quantity of viral shedding, reached o r approach ed statistically significant differenced between the peramivir and placebo treatment groups (p=0.03-0.06). 228 228 BCX1812-311 (V1.0: 04-September-2007) Page 21 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Results of Study BC-01-03 Median Time to Relief of Influenza Symptoms (Hours) Dose and Regimen Overall Results (n=1246) US Sites (n=206) Peramivir 800mg po x 5d 89.0 70.8 Peramivir 800mg po x 1d and 400mg po x 4d 91.7 88.8 Placebo x 5 days 104.4 106.8 p value 0.17 0.07 5.5 Previous Phase 1 Experience with Intramuscular Peramivir Two phase one studies evaluating the safety and pharmacokinetics of an intram uscular formulation of pera mivir have been conduc ted in a total of 45 he althy volunteers receiving peramivir. Study Peramivir-Him-06-111 evaluated the single dose pharmacokinetics and tolerability of 75mg, 150mg and 300mg doses of peramivir administered as intramuscular (i.m.) and intravenous (i.v.) injections in a crossover design (9 subjects per group). Peak plasma levels of i.m. pera mivir generally occurre d within 30 m inutes fol lowing injection. Plasma pharm acokinetic param eters for i.m . peram ivir are summarized below for the three intramuscular single dose regimens evaluated: Dose (mg) Cmax (ng/mL) AUC0-∞ (hr·ng/mL) t½a (hr) 75 i.m. 4296±812 11659±1123 19.8±7.9 150 i.m. 7612±884 23952±3804 24.3±4.1 300 i.m. 15150±2367 49649±5619 22.8±2.5 aterminal half life In a second phase 1 study, Peram ivir-Him-06-112, the sam e dose levels of peram ivir were adm inistered as single i.m . injections on two consecutive days (6 subjects per group). This double-b lind study also includ ed a placebo arm . The pharm acokinetic parameters of i.m . peramivir following the second day of dosing were consistent with those seen following single doses of the drug. The observ ations of s afety and to lerability of i. m. peram ivir in each of the 2 phas e 1 studies were unrem arkable. No serious ad verse even ts were repo rted. The most commonly observed ad verse events or laborato ry abnormalities were h eadache, several reports of signs and symptom s of vasovagal reactions following injections, and transient increases in creatine kinase. No consisten t differences in frequency of adverse events were observed between the ac tive and placebo treatm ent groups, with the exception that CK elevations appeared to be dose rela ted in the peram ivir treatment groups. T he vasovagal reactions were attri buted to the receipt of rela tively large volum es of i.m. injection (2 injections each of 2mL) in the fasted state. 229 229 BCX1812-311 (V1.0: 04-September-2007) Page 22 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL An ongoing phase 2 study, BCX1812-211, is a random ized, double-blind placebo- controlled study to evaluate the efficacy and safety of two single d ose reg imens of peramivir. Up to 100 subjects per arm will receive either 150mg or 300mg of peramivir or placebo. The prim ary endpoint of the stu dy is the tim e to alleviation of clinical symptoms in adult subjects with u ncomplicated acute influenza. An independent dat a monitoring comm ittee reviewed grouped blinde d safety data on the first 135 subjects randomized. The study rem ains blinded. The fr equency of vasovagal reactions reported as adverse events in this ongoing study is 2/135 (to date) which is lower than that seen in the phase 1 volunteer studies. 5.6 Dose Rationale Oseltamivir is approved for the treatment of uncomplicated acute influenza at a dosage of 75mg twice daily in adults14. Oseltamivir was shown to be clinically effective in a Phase III study of oral oseltamivir versus placebo in naturally occurring seasonal influenza, and these data were sufficient for regulatory approval for marketing of oseltamivir. At least 75% of an oral dose of oseltam ivir reaches the sy stemic circu lation as oseltam ivir carboxylate. When oseltamivir is adm inistered orally at a dose of 75mg twice daily, the serum C max of oseltam ivir carboxylate is approxim ately 348ng/m L and the AUC 0-48 is 10,876 h·ng/mL. The clinical data indicate that this level of exposure to oseltamivir was sufficient to provide clinical improvement in uncomplicated acute influenza. The serum pharmacokinetic data (Cmax and AUC0-∞, respectively) following intramuscular doses of peram ivir are approxim ately 7600ng/mL and 24,000 h·ng/m L for the 150m g dose and are approxim ately 15,000ng/m L and 49,000 h·ng/m L for the 300m g dose. Previous s tudies hav e assess ed the concen trations of the neuram inidase inhibitor zanamivir in nasal and pharyngeal secretions after parenteral administration of this drug. . Within several hours after ad ministration, the concentrati ons in secretions wer e approximately 100-fold lower than in serum or plasma. In theory, relatively high levels of a neuram inidase inh ibitor in res piratory se cretions ar e desi rable in order to rapidly inactivate influenza virus and to delay or prevent th e d evelopment of resistan ce in infecting virus strains. Intramuscular doses of peramivir, including doses of 150m g and 300mg have been shown to be well tolerate d in previous P hase 1 studies and since no identified safety signal has been noted by an independent data monitoring committee in the ongoing Phase 2 study, it is appropriate for these two dose regim ens to undergo further evaluation in this Phase 3 study. 230 230 BCX1812-311 (V1.0: 04-September-2007) Page 23 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6 STUDY OBJECTIVES 6.1 Objectives 6.1.1 Primary Objective The primary objective of this study is to eval uate the efficacy of peram ivir administered intramuscularly compared to placebo on th e time to alleviation of clinical symptoms in adult subjects with uncomplicated influenza. 6.1.2 Secondary Objective(s) The secondary objectives of this study are: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly; 2. To evaluate secondary clinical outcomes in response to treatment; 3. To evaluate changes in influenza virus titer ( viral sheddi ng) in response to treatment; 4. To assess pharmacoeconomic measures in response to treatment; 5. To assess changes in influenza viral su sceptibility to neu raminidase inhibito rs following treatment; 6.2 Study Endpoints 6.2.1 Primary Endpoint Time to alleviation of clinical symptoms of influenza 6.2.2 Secondary Endpoint(s) Secondary efficacy endpoints will include evaluations in each subject of: 1. Safety parameters, including: treatment- emergent adverse events (TEAEs) and treatment-emergent changes in clinical laboratory tests; 2. Time to resolution of fever; 3. Time to resumption of subject’s ability to perform usual activities; 4. Incidence of influenza related complications 5. Quantitative change in influenza virus shedding measured by viral titer assay (TCID50) and/or by quantitative polymerase chain reaction (PCR) assay; 6. Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. 6.2.3 Exploratory Endpoint An exploratory endpoint will evaluate change in influenza virus susceptibility to neuraminidase inhibitors in viral isolates recovered from subjects pre and post treatment. 231 231 BCX1812-311 (V1.0: 04-September-2007) Page 24 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 7 STUDY DESIGN 7.1 Overall Study Design and Plan This is a multinational, random ized, double-blind study com paring the efficacy and safety of two single dose regim ens of pera mivir adm inistered intramuscularly versus placebo in adults with uncom plicated acute influenza. Up to 800 subjects will be enrolled in to the s tudy. Each su bject’s as signment to trea tment will be str atified according to a Rapid Antigen Test (RAT) result and current smoking behavior, with 80% of subjects centrally random ized via an Inte ractive Voice Response (IVR) system to one of the two active single dose regimens of peramivir (2:2:1 randomization): Treatment Group 1: Peramivir 150mg maximum n=320 Treatment Group 2: Peramivir 300mg maximum n=320 Treatment Group 3: Placebo maximum n=160 Previous studies evalu ating the efficacy of neuraminidase inh ibitors enro lled su bjects with inf luenza-like illness on the basis of presence of specific clinical signs and symptoms. These studies were conducted before the widespread availability of rapid influenza antigen diagnostic test kits (Rapid Antigen Tests-RAT), and typically between 50-70% of subjects enrolled we re subsequently confirm ed by viral cu lture to hav e an active influ enza infection. The sen sitivity of comm ercially available RAT kits ranges from 62% to 83%, depending upon the virus sub-type. 15 In the phase 2 study of intramuscular peram ivir (study BCX1812-211) a positive RAT test was required for study entry. It is likely that a number of subjects with an influenza infection were excluded from this study due the sensitivity of this assay. In this ph ase 3 study a lim ited number of RA T negativ e subjects will be en rolled in accordance with the following al gorithm to minimize false negative test results: once an individual site has identified 3 RAT positive subjects at screening within a 10 day period, indicating influenza activity is present in the site’s vicinity, a RAT negative subject that meets the inclusion / ex clusion criteria m ay be enrolled. O ne additional RAT negative subject m ay be enro lled there after for each p receding RAT positive subjec t th at is identified. The RAT result for each subjec t screen ed will be reco rded on the s tudy Interactive Voice Response System (IVRS) to manage this enrollment algorithm. A baseline nasopharyngeal swab specimen will be sent to the central virology laboratory for each RAT negative subject that has been randomized into the study. These specimens will be tested for influenza A and B infection using a PCR assay. The PCR results for these specimens will be reported to BioCryst in real time. The study will close after enrollment of at least 500 subjects who have either a positive Influenza A or B RAT at screening, or who have a negative RAT at screening but a positive influenza A or B PCR assay result from a baseline nasopharyngeal swab. 232 232 BCX1812-311 (V1.0: 04-September-2007) Page 25 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Study drug will b e ad ministered as one 2m L intramuscular injection in each g luteal muscle (total of 4mL injected in divided doses). At screening, subjects will have an anterior nasal or pharyngeal swab collected for testing with a comm ercially available RAT kit for influenza A and B in accordance with the RAT manufacturer’s instructions. If this test is positive and the subject is enrolled, additional s pecimens will be obta ined f or isolation and c ulture of inf luenza viru s and quantitative PCR assay. If the initial RAT is negative, th e test should be repeated with a different commercially available RAT kit. A limited number of RA T negative subjects may be enrolled in accordance with the screening algorithm defined above. Enrolled subjects will record the following in a Study Diary: • Oral tem perature m easurements tak en w ith an electronic therm ometer every 12 hours. W ith the exception of the baseline m easurement, all tem perature measurements will be obtained at leas t 4 hours after, or imm ediately before, administration of oral acetaminophen (paracetamol- provided), aspirin, ibuprofen or other NSAID. • Assessment of seven symptom s of influenza on a 4-point severity scale (0, absent; 1, mild; 2, moderate; 3, se vere), twice daily (A M, PM) through Day 9, then once daily (AM) through Day 14 • Assessment of subject’s ability to perform usual activities, (0–10 on a visual analog scale) once daily through Day 14 • Assessment of a subject’s tim e lost from work or usual activities and productivity compared to normal (0-10 on a visual analogue scale) once daily through Day 14 • Doses of antipyretic (e. g. acetaminophen/ paracetamol), expectorant, and/or throat lozenges administered each day through Day 14. Anterior nose (bilateral) and posterior phar ynx specimens (swabs) will be collected at Day 1 (pre-treatment) and at Days 3, 5, and 9, for influenza viral culture and quantitative PCR assay. In a subset of a m inimum of 200 subjects an addition al viral culture/ P CR sample will be collecte d on Day 2. Anterior nose (bila teral) and poster ior pha rynx specimens (swabs) will be collected at Days 1, 3, 5, and 9 f or all subjects, and on Day 2 in the subset of 200 subjects, to assess for potential changes in influenza viral susceptibility to neuraminidase inhibitors in response to treatment. At selected sites a separate sub-study will be conducted to collect limited PK samples for the purpose of conducting an exposure-respo nse analysis. This sub-study will be conducted under a separate sub-study protocol, BCX1812-311PK. 8 SELECTION AND WITHDRAWAL OF SUBJECTS 8.1.1 Inclusion Criteria Subjects must meet all of the following criteria for inclusion in this study: 1. Male and female subjects age ≥18 years 2. A positive Influenza A or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate specimen collected from an 233 233 BCX1812-311 (V1.0: 04-September-2007) Page 26 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL anterior nasal or pharyngeal swab, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated with a second commercially available RAT kit. A limited number of RAT negative subjects may be enrolled in accordance with a defined screening algorithm.. 3. Presence of fever at time of screening of ≥38.0 C (≥100.4 ºF) taken orally, or ≥38.5ºC (≥101.2 F) taken rectally. For subjects who test RAT positive at the time of screening, a subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify in the absence of documented fever at time of screening. For subjects who test RAT negative at screening, fever as described above must be documented at time of screening. 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of any severity (mild, moderate, or severe) 5. Presence of at least one constitutional symptom (myalgia [muscle aches], headache, feverishness, or fatigue) of any severity (mild, moderate, or severe) 6. Onset of illness no more than 48 hours before presentation 7. Females of child-bearing potential must have a negative urine pregnancy test (Beta HCG) at screening/baseline AND report one of the following: • Be surgically sterile or practice monogamy with a partner who is surgically sterile • Have been sexually abstinent 4 weeks prior to date of screening evaluation and be willing to remain abstinent through 4 weeks after study drug administration • Use oral contraceptives or other form of hormonal birth control including hormonal vaginal rings or transdermal patches and have been using these for 3 months prior through 4 weeks after study drug administration • Use an intra-uterine device (IUD), or double barrier contraception (such as condom or diaphragm with spermicidal gel or foam) as birth control 4 weeks prior to date of screening through 4 weeks after study drug administration 8. Provide written informed consent 8.1.2 Exclusion Criteria Subjects to whom any of the following criteria apply will be excluded from the study: 1. Women who are pregnant or breast-feeding 2. Presence of clinically significant signs of acute respiratory distress 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class IV functional status within the past 12 months (section 15.1). 234 234 BCX1812-311 (V1.0: 04-September-2007) Page 27 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 6. History of chronic renal impairment requiring hemodialysis or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min) 7. Clinical evidence of active bacterial infection at any body site requiring therapy with oral or systemic antibiotics 8. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy. 9. Current treatment of active viral hepatitis C 10. Presence of known HIV infection, with a CD4 count <350 cell/mm3 11. Current therapy with oral warfarin or other systemic anticoagulant 12. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening 13. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days 14. History of alcohol abuse or drug addiction within 1 year prior to admission in the study 15. Participation in a previous study of peramivir as treatment for acute influenza or previous participation in this study 16. Participation in a study of any investigational drug within the last 30 days 8.1.3 Removal of Subjects from Therapy or Assessment All subjects are permitted to withdraw from participation in this study at any time and for any reason, specified or unspeci fied, and without prejudice. The Investigator or sponsor may terminate the subject’s participation in the study at any tim e for reasons including the following: 1. Adverse event; 2. Intercurrent illness; 3. Non-compliance with study procedures; 4. Subject’s decision; 5. Administrative reasons; 6. Lack of efficacy; 7. Investigator’s opinion to protect the subject’s best interest. Any subject who withdraws because of an adverse event will be followed until the sign(s) or symptom(s) that constituted the adverse eve nt has/have resolved o r is dete rmined to represent a stable medical condition. A subject should be withdrawn fr om the trial if, in the opinion of the Investigator, it is medically necessary, or if it is the d esire of the subject. If a subjec t does not return for a scheduled visit, every effort should be m ade to contact the subject and determ ine the 235 235 BCX1812-311 (V1.0: 04-September-2007) Page 28 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subject’s medical condition. In any circum stance, ev ery effort sho uld be m ade to document subject outcome, if possible. If the sub ject withdraw s consen t, n o furt her evaluations should be perfor med and no attempts should be made to collect additional data. 9 TREATMENTS 9.1 Treatments Administered Peramivir is an investig ational drug. Peram ivir for intramuscular injection is a small- volume parenteral and will be supp lied as a 75 mg/mL solution in sodium citrate/ citric acid buffer. The pH is approximately 3.0. A m atched placebo solution of so dium citrat e/ citric acid buffer with 1.2% sod ium chloride at a pH of approximately 3.0 will be supplied. 9.2 Identity of Investigational Product(s) Peramivir and placebo peramivir will be supplied in clear 2mL vials. An individual study drug kit will contain 2 vials of blinded study drug (peramivir and/or placebo, depending upon the treatment group), 2 syringes and 2 need les in which to draw up the solution for intramuscular injection. All m aterials will be packaged in a labele d box container. All study drug kits m ust be stored at 2-8 oC. Each individual study drug kit will b e labeled with some or all of the following information as required by local regulations: • Sponsor nam e and contact inform ation, study protocol num ber, kit num ber, description of the contents of the container, instructions for the preparation of the syringe and adm inistration of the study dr ug, conditions f or st orage, statem ent regarding the investigationa l (clinical trial) use of the study drug and date for retest or expiry date. Each vial of study drug will be labeled with some or all of the following infor mation as required by local regulations: • Sponsor nam e, study protocol number, desc ription of the contents of the vial, instructions for the preparation of the s yringe, statem ent regarding the investigational (clinical trial) use of the study drug and lot number. 9.3 Method of Assigning Subjects to Treatment Groups Subjects will be centrally randomized in a ratio of 2:2:1 to one of three treatment groups: single dos e peramivir 1 50mg, single dose pera mivir 300mg or placeb o, in acco rdance with a computer-generated random ization schedule prepared by a non-study statistician. Subjects will be s tratified acco rding to the result of a RAT test and curren t sm oking behavior. Once a subject is eligible for randomization, he/she wi ll be assigned a study drug kit nu mber that will be obta ined by stu dy staf f f rom the study inter active voice response system (IVRS). Once a study drug kit nu mber has been assigned to a subject, it cannot be reassigned to any other subject. 236 236 BCX1812-311 (V1.0: 04-September-2007) Page 29 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 9.4 Study Medication Accountability The Investigator/pharmacist must maintain accurate records of the disposition of all study drugs received from the sponsor, issued to th e subject or directly adm inistered to the subject (including date and time), and any drug accidentally destroyed. The sponsor will supply a specific dru g-accountability form . At the en d of the study, information describing study drug s upplies (e.g., lot num bers) and disp osition of s upplies for each subject must be provided, signed by the Invest igator or designee, and collected by the study monitor. If any errors or irregularities in any shipment of study m edication to the site are discovered at any time, the Project Manager must be contacted immediately. At the end of the study, all medication not dispensed or administered and packaging materials will be collected with supervision of the monitor and returned to the sponsor or destroyed on site as dictated by the appropr iate Standard Operating P rocedure at the participating institution. 9.5 Blinding/Unblinding of Treatments This is a double-blind study. The treatment group assignment will not be known by the study subjects, the investigator , the clinical staff, the CRO or Sponsor staff during the conduct of the study. Section 11.2.4 provides inform ation regarding the process for unblinding the treatment assignment, if necessary, in the event of an SAE. 9.6 Prior and Concomitant Therapies All m edications, by any route of adm inistration, used during this study m ust be documented on the Case Report Form (CRF). Prescription as well as non-prescription medications should be recorded. Medication us ed for the treatm ent of influenza-related symptoms will be captured by the subject in the diary card provided by BioCryst. 9.7 Overdose and Toxicity Management To date there is no experience with overdose of in tramuscular or intravenous peramivir. If overdose occurs, subjects should receive indicated supportive therapy and evaluation of hematologic and clinical chem istry laboratory tests should be conducted. The effec t of hemodialysis on elimination of peramivir is unknown. 9.8 Dose Interruption As this is a study of a single injection of peramivir or placebo, guidelines for treatm ent interruption for drug related SAEs or toxicities are not applicable. 237 237 BCX1812-311 (V1.0: 04-September-2007) Page 30 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10 STUDY CONDUCT A study schedule of evaluations is presented in Figure 1 . A detailed lis t of the evaluations is also provided in the following sections. 10.1 Evaluations All subjects enrolled in this study will undergo the following evaluations: 10.1.1 Medical History Medical history, influenza va ccination s tatus within th e previous 12 m onths and demographic data (including smoking behavior) will be recorded at Screening/Baseline. 10.1.2 Rapid Antigen Test for Influenza At Screening/Baseline, a commercially available, rapid antigen tes t (RAT) for influenza A and B will be performed on an adequate specimen collected by swabbing the anterior nose or pharynx, in accordance with the RAT manufacturer’ instructions. A negative initial RAT should be repeated with a different commercially available RAT kit. Refer to the Study Manual f or instructions regarding the use of the RAT kits provided for this study. Sites m ay use the kits provided by the Sponsor or any other commercially approved RAT available at their site to document a confirmed influenza infection. A lim ited num ber of RAT negativ e subje cts will be enr olled in a ccordance with the following algorithm: Once an ind ividual site has identified 3 RAT positive sub jects at screening within a 10 day period, indicating that influenza activity is present in the site’s vicinity, a RAT negative subject that m eets the inclus ion/ exclus ion criteria m ay be enrolled. O ne additional RAT negative subj ect m ay be enrolled th ereafter for each preceding RAT positive subject that is iden tified. The RAT result for each subject screened will be record ed on the s tudy Inte ractive Voice response (IVR) system to manage this enrollment algorithm. 10.1.3 Physical Examination and Influenza-related Complications Assessments The Investigator will perform a physical ex amination at S creening/Baseline. Subject’s weight will be recorded at Screening/Baseline. Study personnel will be provided with an influenza-related complications (IRC) checklist in the CRF to evalua te the subject for the presence of clinical signs and /or symptoms of the following influenza-related complications: sinusitis, otitis, bronchitis and pneumonia. At each follow up assessm ent a t argeted physical exam ination will be conducted to record the presence of influenza related complications. If the investigator determines that the subject experiences (or is presumed to experience) an IRC as noted above, he/she will record that assessm ent on the IR C CRF pa ge and any m edication used to treat the condition will be reco rded on the concom itant medication page. The investigato r will promptly provide appropriate treatm ent fo r any suspected or proven IRC, as such treatment will not affect the efficacy assessments. Such information describing IRC signs and/or symptoms should not be reported as adverse events. Any inj ection site reactions noted will be recorded in the CRFs as adverse events. 238 238 BCX1812-311 (V1.0: 04-September-2007) Page 31 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.4 Vital Signs Vital signs evaluations will in clude blood press ure, pulse rate , and resp iration rate. The investigator will record or al body tem perature at baseline. Thereafter the subject will record oral temperature twice daily in the study diary card. Vital signs will be measured at Screening/Baseline, pre-dose, and at 15 minutes following the study drug injection on Day 1, then once da ily on Days 2 (for those subjects who are seen on day 2), 3, 5, 9, and 14. 10.1.5 Electrocardiogram Measurements A 12-lead elec trocardiogram (ECG) will be obtained a t Screen ing/ Baseline. The principal investigator will be re sponsible for interpretation of the Screening ECG. This interpretation may be performed by the investigator or he/she may delegate this action to another physician and the investigator wi ll acknowledge the interp retation. If this baseline ECG is interpreted as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal but does not meet the exclusionary criteria, the subject m ay be enrolled unless other exclusion criteria apply. The principal investigator is responsible to ensure that such an enrolled subject be inform ed of the nature of the abnorm al ECG and that any m edically indicated repeat ECG examinations and/or referral of the subject for further evaluation is made either during subject' s participation in the study or imm ediately after the subject' s discharge from the study. 10.1.6 Clinical Chemistry Profiles Clinical ch emistry pro files will include a C hemistry 20 panel ( includes sod ium, potassium, chloride, total CO 2 [bicarbonate], creatinine, glucose, urea nitrogen, album in, total calcium , total m agnesium, phosphor us, alkaline phosphatase, alanine aminotransferase (ALT), aspartate am inotransferase (AST), total bilirubin, d irect bilirubin, lactate dehydrogenase [LDH], total protein, total creatine kinase, and uric acid) Blood samples for clinical chem istry profiles will be collected at Screen ing/Baseline, and on Days 3, 5 and 14. 10.1.7 Hematology Profiles Hematology will include complete blood count (CBC) with differential. Blood samples for he matology profiles will be collected at Screening/Baseline, and on Days 3, Days 5 and 14. 10.1.8 Serology for Influenza Paired blood samples for determination of antibody to influenza A and B (serology) will be obtained with the clinical laboratory tests at Screenin g/Enrollment and at Day 14. These specimens will be stored at the central laboratory and will be analyzed if needed to confirm the diagnosis of influenza. 10.1.9 Urinalysis and Evaluation of Protein in Urine Urinalysis will in clude dipstick tests for protein, glucose, ketones, blood, urobilinogen, nitrite, pH, and spec ific gr avity a nd m icroscopic evaluation for R BCs and WBCs. 239 239 BCX1812-311 (V1.0: 04-September-2007) Page 32 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Samples for urinalysis will be collected at Screening/Baseline, and on Days 3, 5, and 14. 10.1.10Urine Pregnancy Test Females of childbearing potential will be ev aluated for pregnancy at Screening/Baseline and Day 14 using a urine pregnancy test. 10.1.11 Samples for Virologic Laboratory Assessments An adequate spec imen will b e co llected by sw abbing the anter ior nos e (bila teral) and posterior pharynx for virologic laboratory a ssessments including culture for the isolation of influenza virus and/or quantitative PCR assa y at Screening/Baseline, and at Days 3, 5, and 9. In a subset of a m inimum of 200 subjects an additio nal sample will be taken at Day 2. Refer to the L aboratory Manual for instructions re garding the processing and shipment of these specimens. 10.1.12 Subject Self Assessments Subject self assessments will be performed beginning pre-dose on Day 1 and recorde d in the subject’s Study Diary including the following: • Oral temperature measurements with an electronic thermometer (provided by the Sponsor for the study) every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol, provided) aspirin, ibuprofen or other NSAID. The times of each temperature determination will be recorded in the Study Diary. The baseline temperature will be recorded at the screening/Day 1 visit prior to dosing, regardless of whether the subject had recently taken an anti-pyretic; the time of anti-pyretic use pre-treatment will be recorded in the CRF, if applicable. • Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [muscle aches], headache, feverishness, and fatigue) on a 4-point severity scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily, beginning pre-dose on Day 1 and through Day 9, then once daily through Day 14. • Assessment of the subject’s ability to perform usual activities using a 0–10 visual analogue scale once daily through Day 14. • Assessment of the subject’s time lost from work or usual activities and productivity compared to normal using a 0-10 visual analogue scale once daily through Day 14. The subject’s diary card will be reviewed by study staff at each visit for completion of the record of all required ite ms, with particular emphasis on alleviation of symptoms as well as relapse of sym ptoms. Relapse is defined as the recurrence of at leas t one respiratory symptom and one constitutiona l sy mptom (both greater th an m ild in severity) f or 24 hours and the presence of fever (unless influenc ed by antipyretic use). Relapse can only occur after the subject has m et the endpoint cr iteria for alleviation of symptoms. Study staff will not attem pt to ask subjec ts to retrospectively complete missing diary card data for any scheduled assessm ents that have not b een com pleted prio r to the c linic visit. Study staff should, however, rem ind the subject to com plete the diary card at all scheduled times. 240 240 BCX1812-311 (V1.0: 04-September-2007) Page 33 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.13 Concomitant Medications All concom itant m edications used during this study, with the exception of those medications taken for symptomatic relief of influenza symptoms, which will be reco rded by the subject in their diary card, must be documented on the Case Report Form (CRF). 10.1.14 Adverse Events AEs will be assess ed from the tim e of ad ministration of stu dy medication through the final study visit. 10.1.15 Single Pharmacokinetic Exposure Sample On study day 3 a single PK sample will be drawn in concert with the day 3 safety clinical laboratory blood draw. This sample will be sent for subsequent analys is of the concentration of peramivir at this time point. Data f rom this sing le PK sample will b e combined with data from the PK s ub-study (BCX1812-311PK) to perfor m an exposure- response analysis. This analysis will be described as part of the sub-study analysis plan.. 10.2 Screening 10.2.1 Informed Consent The nature and purpose of the study and the expectations of a participating subject will be described to potential study subjects , their que stions will be answered, and the subjects will th en b e asked to sign an inf ormed c onsent docum ent. Study s ubjects will then undergo the screening evaluation as noted in Section 10.2.2 10.2.2 Screening/Baseline Evaluation and Enrollment Screening/baseline evaluation may be conducted in the investigator’s office or clinic, or in the subject’s hom e, in which case all ev aluations must be conducted by appropriately trained and qualified staff. Clinical laboratory assessm ents perform ed at Screenin g are for the purpose of establishing a baseline. Subjects m ay be enrolled and receive treatm ent with study drug prior to r eceiving re sults of the laboratory a ssessments (with the ex ception of urine pregnancy test result, which must be known). Eligible sub jects will be enrolled and ra ndomized to blin ded study treatm ent. The randomization will include stratification by RA T status and current s moking behavior. The Investigator will prepare a request for blinded study drug assignment which includes the subject’s screening number. The Investigator or designee at the clinical study center will contact the central randomization Interactive Voice System (IVRS call center). The IVRS call center will advise the study center of the investigational study drug kit number that is assigned to that subject at enrollment. Subjects that are d etermined to be ineligible will be advi sed accordingly, and the reason for ineligibility will b e discussed. If desired by the subjec t the reason for ineligibility may be pr ovided/discussed with their hea lth-care provider by the Investigator or designee. Ineligible subjects who have been screen ed for the study will also be entered on the 241 241 BCX1812-311 (V1.0: 04-September-2007) Page 34 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL IVRS. For such subjects, the screening num ber assigned, subject’s date of birth and a reason for ineligibility will be entered on to th e IVRS. All ineligible subjects must be entered onto the IVRS within 24 hours of screening, to assis t with surve illance analysis during the course of the study. 10.3 Treatment Period—Study Day 1 Day 1 represents the only day of study dr ug dosing. Study drug adm inistration should occur as soon as possible following inform ed consent, screening and random ization. Therefore, it is expec ted that the da te of Screening/ Baseline and Day 1 will usua lly be the same date. 10.3.1 Pre-dose Evaluations Following an explanation of the Subject Self Assessment measures (Section 10.1.11), the subject shall complete the record of these assessments in their Study Diary prior to dosing. The subject will be counseled regarding the expectations for recording these assessments through Day 14. Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) and a 12 lead ECG will be obtained prior to dosing. At Hour 0, the blinded study drug will be administered intramuscularly (one injection in the left gluteal muscle, and one injection in the right gluteal muscle within a period of ≤ 10 minutes.). The calendar date and 24-hour clock time of the first and second injections will be recorded. The following evaluations will be performed post-dose on Study Day 1: • Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) at 15 minutes after the study drug administration • Record any concomitant medications • Record any AEs 10.4 Post-Treatment Assessment Period 10.4.1 Days 2, 3, 5, 9 and 14 Study evaluations will be performed on Days 2 [subset of subjects only], 3, 5, 9 and 14 in accordance with the schedule of evaluations (Figure 1). Subjects with persistent moderate or severe influenza symptoms at day 14 will also complete a Day 21 visit. Visits may be conducted in the investigator’s o ffice or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and qualified staff. The Day 2 assessment will be conducted in clinic or by study staff only for the subset o f subjects who will provide additional Day 2 virology samples. For all other study subjects, study staff will attem pt to contact the subjec ts on Day 2 by telephone to confirm their compliance with com pletion of the Subject Self Assessments, to note any concom itant medications and adverse events. A ny adverse events reported by the subject during this telephone contact will be recorded on the adverse event form and verified during the visit 242 242 BCX1812-311 (V1.0: 04-September-2007) Page 35 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL on day 3. At each v isit it is im portant that the sub ject’s Study Diar y record be rev iewed for completion of daily Subject Self Assessm ents. The subjects should be counseled as necessary regarding self assessments and Study Diary record requirements. The subject’s diary card will be reviewed by study staff for alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the r ecurrence of at least one resp iratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours an d the presence of fever (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Day 3: The results of the serum CK result obtained a t Day 3 will not be m ade available to investigators, to BioCryst or to any study personnel, unless the CK result at Day 3 is ≥ 2000 IU/mL. A single PK sa mple will be obt ained on Day 3 at the sam e time as the clinical laboratory blood specimen is obtained. Day 14: If a subject has one or more persistent or recurrent symptoms of influenza (of the seven symptoms assessed) of either m oderate or se vere intensity at th e Day 14 visit th en the subject must be evaluated in further follow-up visits, at day 21 (± 3 days), and if required at day 28 (± 3 days) If a subject reports m oderate or severe influenza symptoms then the investigator will record the intensity of each of the influenza symptoms on a visit specific CRF page at the day 21 and day 28 visits. A fter day 14 the subjec t will not re cord symptoms in a diary. Day 21 (if applicable): The day 21 visit is to be completed only if the subject reports sym ptoms of influenza of moderate or severe intensity at day 14. The investigator will make a clinical judgment as to the appropriate medical course of action for such subjects at the Day 2 1 visit and such action(s) will be re corded on the Day 21 CRF page. The investigator will re call the subject for a further study visit at day 28 (± 3 days) if m oderate or severe symptom(s) of influenza persist at Day 21. Day 28 (if applicable): The day 28 visit is to be completed only if the subject reports sym ptoms of influenza of moderate or severe intensity at day 21. The investigator will make a clinical judgment as to the appropriate m edical course of action for such subjects at this visit and such action(s) will be recorded on the Da y 28 CR F page. No further follow-up visits beyond day 28 are to be form ally scheduled unless in the clinical judgm ent of the investigator further follow-up is required. The investigat or will use his/her clinical judgm ent to manage the subject, referring the subject, if appropriate, for further care. 10.4.2 Adverse Events Reported at Post-treatment Visits In this stud y, symptoms of influenza will be considered separately from adverse e vents reported during the post-treatment period. Accordingly, adverse events that have onset in the post-treatment period will be assessed and followed as specified in 11.2. Specifically, 243 243 BCX1812-311 (V1.0: 04-September-2007) Page 36 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL the inves tigator shou ld attem pt to f ollow all unresolved AEs and/or SAEs observed during the study until they are resolved, or ar e judged medically stable, or are otherwise medically explained. 244 244 BCX1812-311 (V1.0: 04-September-2007) Page 37 Figure 1 Study Measurements and Visit Schedule Treatment Period Assessment Day End of Study Early Withdrawal Screening 1 (Baseline) Day 11 Day 22 Day 3 Day 5 (±1 day) Day 9 (±3 day) Day 14 (±3 day) 8 Informed Consent X Rapid Antigen test for Influenza A & B X Medical History/Physical Exam3 X Influenza-related complications checklist3 X X X X X X Inclusion/Exclusion X Clinical Chemistries4 X X X X Hematology4 X X X X Exposure Pharmacokinetic Sample X4 Serology (serum) Sample X X Urinalysis4 X X X X Urine Pregnancy Test X X Vital Signs5 X X X X X X X ECG6 X Sample (nasopharyngeal swab) for Influenza Virus Culture/ PCR assay and for resistance studies X X X X X Study Drug Administration X Subject Diary Review7 X X X X X X Concomitant Medications X X X X X X X Adverse Events X X X X X X 1 It is expected that the date of Screening and Day 1 (date of administration of study drug) will be the same. Visits at Screening and on subsequent study days may occur in subject’s home by the investigator (all visits) or appropriately trained study center staff (Day 2, 3, 5, 9 visits). 2 Day 2 visit required only for a subset of subjects for whom additional Day 2 virology sample is required. For all other subjects, Day 2 will be a telephone contact with the subject to ensure compliance with diary card completion, concomitant medication and adverse event review. 3 Medical history and physical exam at screening to include weight, and smoking behavior. Targeted physical examinations will be performed to complete the influenza-related complications checklist by the appropriate medical personnel at appropriate visits. 4 Clinical laboratory assessments performed at Screening are for the purpose of establishing a baseline. Subject may be enrolled and begin treatment with study drug prior to receiving results. On Day 3 an extra tube will be included with the safety blood sample for evaluation of peramivir concentrations. 5 Vital sign measures will include blood pressure, pulse rate and respiration rate. Vital signs will be recorded at Screening, pre-dose and at 15 min following the study drug administration on Day 1, then once on remaining days as stipulated. The investigator will record oral temperature at baseline. Thereafter the subject will report oral temperature measurements twice daily in the Study Diary 6 If the baseline ECG is interpreted by the conducting physician as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal and does not meet the exclusionary criteria (e.g. acute ischemia, medically significant dysrhythmia) then this subject may be enrolled If the conditions highlighted in section 10.1.5 are met for the subject. 7 Subjects record symptom assessment in Study Diary, twice dail y, beginning pr e-dose on Day 1 through Day 9, then once daily through Day 1 4; subjects record ability to perform usual activities once daily, beginning pre-dose on Day 1 through Day 14. Subjects record oral temperature twice daily throughout as well as all concomitant medication and adverse events 8 For any subjec t with unresolved moderate or severe intensity influenza sym ptoms a follow up assess ment will be schedul ed at Day 21 ( ± 3 day s) and Day 28 (± 3 day s) if r equired (See Section 10.4.1). BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 245 245 BCX1812-311 (V1.0: 04-September-2007) Page 38 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11 ADVERSE EVENT MANAGEMENT 11.1 Definitions 11.1.1 Adverse Event An AE is any untoward m edical occurrence in a clinical study subject. No causal relationship with the study drug or with the clinical study itself is implied. An AE may be an unfavorable and unintended sign, sym ptom, syndrome, or illness that dev elops or worsens during the clinical st udy. Clinically relevant ab normal results of diagnostic procedures including abnorm al laborator y findings (e.g., requ iring unscheduled diagnostic procedures or treatm ent measures, or resulting in withdrawal from the study) are considered to be AEs. AEs may be designated as “nonserious” or “serious” (see Section 11.1.2). Surgical procedures are not AEs but m ay constitute therapeutic m easures for conditions that require surgery. The condition for which the surgery is required is an AE, if it occurs or is detected during the study period. Planned surgical m easures perm itted by the clinical study protocol and the conditions(s) leading to these measures are not AEs, if the condition(s) was (were) known befo re the start of study treatm ent. In the latter case the condition should be reported as medical history. Assessment of seven influenza sym ptoms (cough, sore throat, nasal obstruction, m yalgia [muscle aches], headache, f everishness, and f atigue) will be documented in a subject’s study diary and analy zed as a m easure of efficacy of the study treatm ent. These symptoms will not b e reported as AEs unless the sym ptom(s) worsen to the exte nt that the outcome fulfils the def inition of an SAE, which then must be recorded as such (see Section 11.1.2). Likewise, a RAT for influenza is required at screening in order to determine eligibility for the study, and therefore a positive RAT is not considered an AE. 11.1.2 Serious Adverse Event A SAE is an adverse event that results in any of the following outcomes: • Death • Is life-threatening (subject is at immediate risk of death at the time of the event; it does not refer to an event that hypothetically might have caused death if it were more severe) • Requires in-subject hospitalization (formal admission to a hospital for medical reasons) or prolongation of existing hospitalization • Results in persistent or significant disability/incapacity (i.e., there is a substantial disruption of a person’s ability to carry out normal life functions) • Is a congenital anomaly/birth defect • Is an important medical event 246 246 BCX1812-311 (V1.0: 04-September-2007) Page 39 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Important medical events that may not result in death, are no t life-threatening, or do not require hospitalization may be considered an SAE when, based upon appropriate medical judgment, they m ay j eopardize the subject or m ay r equire m edical or surgical intervention to prevent one of the outcom es listed in this definition. E xamples of such events include allergic bronchospasm requiri ng intensive treatm ent in an e mergency room or at hom e, blood dyscrasias or c onvulsions that do not result in subject hospitalization, or the development of drug dependency or drug abuse. 11.2 Method, Frequency, and Time Period for Detecting Adverse Events and Reporting Serious Adverse Events Reports of AEs are to be collected from the time of study drug administration through the follow-up period ending on Day 14. The Invest igator or de signee must completely and promptly record each AE on the appropriate CRF. The Investig ator should attem pt, if possible, to establish a diagnosis based on th e presenting signs and symptom s. In such cases, the diagnosis should be docum ented as the A E and not the individual sign/symptom. If a clear diagnosis cannot be established, each si gn and symptom must be recorded individually. The Investigator should attem pt to follo w all unresolved AEs and/or SAEs observed during the study until they are resolved, or ar e judged medically stable, or are otherwise medically explained. 11.2.1 Definition of Severity All AEs will be as sessed (graded ) f or severity and class ified into on e of f our clearly defined categories as follows: • Mild: (Grade 1): Transient or mild symptoms; no limitation in activity; no intervention required. The AE does not interfere with the participant’s normal functioning level. It may be an annoyance. • Moderate: (Grade 2): Symptom results in mild to moderate limitation in activity; no or minimal intervention required. The AE produces some impairment of functioning, but it is not hazardous to health. It is uncomfortable or an embarrassment. • Severe: (Grade 3): Symptom results in significant limitation in activity; medical intervention may be required. The AE produces significant impairment of functioning or incapacitation. • Life-threatening: (Grade 4): Extreme limitation in activity, significant assistance required; significant medical intervention or therapy required; hospitalization. 11.2.2 Definition of Relationship to Study Drug The blinded Principal Investigator must rev iew each AE and m ake the determ ination of relationship to study drug using the following guidelines: Not Related: The event can be readily explained by other factors such as the 247 247 BCX1812-311 (V1.0: 04-September-2007) Page 40 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subject’s underlying m edical c ondition, concom itant therapy, or accident, an d no tem poral relati onship ex ists b etween the study drug and the event. Unlikely: The event d oes not follow a reason able tem poral sequ ence from drug adm inistration and is read ily explained by the subject’s clinical state or by other m odes of therapy adm inistered to the subject. Possibly Related: There is so me tem poral relationship between the event an d th e administration of the study drug a nd the event is unlikely to be explained by the subject’s m edical condition, other therapies, or accident. Probably Related: The event follows a reasonable tem poral sequence from drug administration, abates upon discontinuation of the drug, and cannot be reasonably explained by th e known characteristics of the subject’s clinical state. Definitely Related: The event follows a reason able tem poral sequen ce from administration of the m edication, follows a known or suspected response pattern to the m edication, is confirm ed by im provement upon stopping the m edication (dec hallenge), and reappears upon repeated exposure (rechallenge, if rechallenge is m edically appropriate). 11.2.3 Reporting Serious Adverse Events Any SAE must be reported to BioCryst or its designee within 24 hours of the Investigator’s recognition of the SAE by fi rst notifying the Medical Monitor at the number listed below: Telephone: Europe: +44 1628 548000; North America: 1-888-724-4908 Facsimile: Europe: +44 1628 540028; North America: 1-888-887-8097 or 1-609-734-9208 The site is required to fax a completed SAE Report Form (provided as a separate report form) within 24 hours. All additional follow-up evaluations of the SAE must be reported and sent by facsimile to BioCryst or its designee as soon as they are available. The Principal Investigator or designee at each site is respons ible for submitting the IND safety report (initial a nd follow -up) or other safety inform ation (e.g., revised Investigator’s Brochure) to the Institutional Review Board/Independent Ethics Committee (IRB/IEC) and for retaining a copy in their files. If the Inv estigator becomes aware of any SA E occurring within 30 days after a s ubject has com pleted or withdrawn from t he study, he or she should notify BioCryst or its designee. Any SAEs considered possibly related to treatment will be reported to the FDA and other Regulatory Competent Authorities as applicab le via the MedW atch reporting system i n 248 248 BCX1812-311 (V1.0: 04-September-2007) Page 41 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL accordance with FDA and other ap plicable regulations. However, the Investig ator is not obligated to actively seek reports of AEs in former study participants. While pregnancy is not considered an AE, a ll cases of fetal drug exposure via parent as study participant (see S ection 4.4) are to be reported immediately to BioCryst or its designee. Inform ation rela ted to the pregnancy m ust be given on a “Pregnancy Confirmation and Outcome” form that will be provided by the Sponsor or its designee. 11.2.4 Emergency Procedures In the even t of an SAE, the Principal Inve stigator m ay request the unblinding of the treatment assignm ent for the subject affected . If tim e allows (i.e., if appropriate treatment for the SAE is not im peded), the Principal Investigator wi ll first consult with the Med ical Monito r r egarding the need to unblind the treatm ent assignm ent for the subject. At all times, the clinical well-being of any subject outweighs the need to consult with the Medical Monitor. The Principal Investigator m ay contact th e IVRS central random ization center and request the unblinding of the treatm ent assi gnment that corresponds to the affected subject. Th e IVRS center will record the na me of the Investigator making the request, the date and time of the request, the reason for the request, the subject number and study drug kit number, and whether the Medical M onitor was consulted prior to the request being made. The Sponsor will be informed within 24 hours if unblinding occurred. 12 STATISTICAL METHODS Descriptive statistical methods will be used to summ arize the data from this study, with hypothesis testing perform ed for the prim ary and other selected efficacy endpoints. Unless stated otherwise, the term “descriptive statistics” refers to number of subjects (n), mean, median, standard deviation (SD), minimum, and maximum for continuous data and frequencies and percentages for categorical da ta. The term “treatm ent group” refers to randomized treatment assignment: peramivir 150 mg, peramivir 300 mg, or placebo. All data collected during the study wi ll be included in data listin gs. Unless otherwise noted, the data will be sorted first by treatm ent assignment, subject num ber, and then by date within each subject number. Unless specified otherwise, all statistical testing will be two-sided and will be performed using a significance (alpha) level of 0.05. All statistical analyses will be conducted with the SAS® System, version 9.1.3 or higher. 12.1 Data Collection Methods The data will be reco rded on the CRF appr oved by BioCryst. The Investigator must submit a completed CRF for each subject who signs an inform ed consent form (ICF), regardless of duration. All documentation supporting the CRF data, such as laboratory or hospital records, must be readily available to verify entries in the CRF. Documents (including laborator y reports, hospital records s ubsequent to SAEs, etc.) transmitted to BioCryst should not carry the s ubject’s name. This will help to ensure 249 249 BCX1812-311 (V1.0: 04-September-2007) Page 42 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL subject confidentiality. 12.2 Statistical Analysis Plan A statistical analysis plan (SAP) will be cre ated prior to the review of any data. This document will provide a m ore technical and detailed description of the proposed data analysis methods and procedures. 12.3 Sample Size Estimates From published resu lts, it is exp ected that th e median time to a lleviation of symptoms will be between 103.3-116 hours for subjects receiving p lacebo. 16 , 1 7 For sam ple size calculations the best placebo respon se (103.3 hours) will p rovide the most conserv ative estimate of an observed hazard ratio. Additionally, it is expected that the median time to alleviation for the lowes t dose peramivir arm will be 69.9 h ours, yielding a hazard ratio of 0.68. Using these assum ptions, a sa mple size of 200 infected subjects per active treatment group and 100 infected subjects in th e placebo group is sufficient to provide at least 80% power to detect a hazard ratio of 0.68 usi ng a log-rank statistic and α = 0.025 (SAS version 9.1.3; tota l accrual time 7 months; total enrollment time 6 months). Up to 800 subjects will b e enrolled to achieve the target num ber of at least 5 00 subjects with diagnostic evidence (RAT or PCR) of an acute influenza infection (200 per active treatment; 100 receiving placebo) as described in section 12.4.2. 12.4 Analysis Populations The populations for analysis will include the intent-to-treat (ITT), intent-to-treat infected (ITTI), and safety populations. 12.4.1 Intent-To-Treat Population The ITT population will include all subject s who are random ized. Subjects will be analyzed in the treatment group to which they were randomized. The ITT population will be used for analyses of accountability and demographics. 12.4.2 Intent-To-Treat Infected Population The ITTI po pulation will include all subj ects who are rando mized, received study d rug, and have proven influenza by any one of the fo llowing: culture, PCR, or paired serology showing ≥ 4-fold increase in antibody to influe nza A or B, and received study drug. Subjects will be an alyzed accord ing to the treatment random ized. If a discrepancy is noted in the final database for any subject, such that the drug differs from the randomized treatment assignm ent, efficacy analyses m ay be repeated with the su bjects analy zed according to the treatm ent received. The ITTI population will be used for prim ary analyses of efficacy. 250 250 BCX1812-311 (V1.0: 04-September-2007) Page 43 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.4.3 Safety Population The safety population will include all subjects who received study drug. Subjects will be analyzed according to the treatm ent received. This population will be used for all safety analyses. 12.5 Interim and End of Study Analyses Interim Analysis An independent DMC will review safety data on an ongoing basi s. Safety analyses will be presented in a manner consistent with the presentations intended for the final analysis. End of Study Analysis A final analysis is planned after the last su bject completes or discontinues the study, and the resulting clinical database has been cleaned, quality checked, and locked. 12.6 Efficacy Analyses 12.6.1 Primary Efficacy Endpoint The primary efficacy endpoint is the time to alleviation of symptoms, defined as the time from injection of study drug to the start of th e time period when a subject has Alleviation of Symptoms. A subject has Alleviation of Symptoms if all of the seven symptoms of influenza (nasal congestion, so re throat, cough, aches and pains, fatigue (tiredness), headache, feeling feverish) assessed on his/he r subject diary are eith er absent o r are present at no m ore than m ild severity leve l and at this status for at least 21.5 hours (24 hours - 10%). Descriptive statistics for the prim ary effi cacy endpoint will be tabulated by treatment group. Alleviation of sym ptoms will be d etermined by assessm ent of sym ptoms as reported on each subject’s diary card. T ime to alle viation of sym ptoms will b e summarized overall and for i ndividual sym ptoms for each treatm ent group. Overall treatment dif ferences will be assess ed using a Cox Regression m odel with ef fects f or RAT result at screening, current smoking behavior, treatment group, and influenza season at randomization (if necessary). Subjects who do not experience alleviation of symptoms will be censored at the date of their last non-missing post-baseline assessment. Pairwise differences in tim e to alleviation of sy mptoms am ong the treatm ent groups will be evaluated using contrast statem ents from the final Cox m odel. In orde r to m aintain the overall type I error in the presence of the planned comparisons between the two peramivir treatments and placebo, a Bonfe rroni correction will be app lied to the p rimary efficacy endpoint analysis. P -values for the planne d com parisons of each peram ivir arm to placebo will be adjusted via a Bonferroni corr ection (i.e., if the unadjusted p-value for an active com parison versus place bo, p, is less th an 0.05, then p a=p*number of planned comparisons=p*2; otherwise, p a=p). Superiority of peram ivir to placebo will be established if the adjusted p-value is less than or equal to 0.05. 251 251 BCX1812-311 (V1.0: 04-September-2007) Page 44 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.6.2 Secondary Efficacy Endpoints All secondary endpoints will be summ arized using descriptive statistics by treatm ent group and study day/time, if appropriate. St atistical comparisons for each endpoint will be constructed without adjustment for multiple endpoints. The reduction in viral shedding will be assessed as the change in viral titers defined as the time-weighted change from baseline in log10 tissue culture infective dose50 (TCID50/mL) and will be summarized for each treatm ent group. The tim e-weighted average change from baseline will be calculated on a by-subject basis through Day 9 using the trapezoidal rule with a ll available post-bas eline on-tre atment data (d ata af ter initia tion of study treatment) minus the baseline value. Specifically, the time-weighted area under the curve for time a (ta) to time b (tb) is given by the formula ) ( ) ( b a b a t t t t AUC TWAUC − − = , where ∑ − = − + − + = − 1 1 1 2 ) )( ( ) ( b a i i i i i b a t t y y t t AUC and ti represents the date of the ith viral titer assessment and y i represents the log10 value of the i th viral titer as sessment. If there is a baseline value and only one follow-up value, y i then the tim e-weighted change from baseline is defined as the difference between y i and baseline. If there is a baselin e value and no follow-up value, the subject is exclude d from analysis. The differences between each of the peramivir treatment groups and placebo will be evaluated using a van Elteren Test ad justing for RAT result at screen ing, current sm oking be havior and influenza season at randomization (if necessary). Analyses of the PCR results will be analy zed in a similar manner. Subject’s ability to perform usual activities as determined from the visual analog scale will be summarized by study visit day and treatment group. Differences between the treatment groups will be assessed using the van Elteren Test adjusting for smoking behavior and influenza season at randomization (if necessary). The time (days) to resumption of a subject’s ability to perform usual activities (i.e., subject scores ability to perform usual activities as 10) will be estimated using the method of Kaplan-Meier. Differences between each of the peramivir treatment groups and placebo will be assessed using the log rank statistic adjusting for RAT result at screening, current smoking behavior and influenza season at randomization (if necessary). Subjects who do not return to the pre-study level of performance of usual activities will be censored at the time of their last non-missing post-baseline visual analog scale value. Subject’s oral tem perature will be summ arized by study visit and treatm ent group. Differences between the treatment groups will be assessed using the Wilcoxon Rank Sum Test con trolling for RAT resu lt at screen ing, current sm oking behavior and influenza season at randomization (if necessary). A subject has Resolution of Fever if he/she has a temperature < 37.2°C (99.0°F) and no antipyretic medications have been taken for at least 12 hours. The tim e to resolution of fever will be estimated using the method of Ka plan- Meier using temperature and sym ptom relief medication information obtained from the subject diary data. Difference between the tr eatment groups will be assessed using the 252 252 BCX1812-311 (V1.0: 04-September-2007) Page 45 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL log rank sta tistic controlling for RAT result a t screening, current sm oking behavior and influenza season at randomization (if necessary). Subjects who do not have resolution of fever will be censored at the tim e of their last non- missing post-baseline tem perature assessment. The MRU, MRU-related direct co sts, and indirect co sts attributable to days m issed of work and work productivity and/or perform ance losses will be summ arized by treatment group. Differences between each of the peramivir treatment groups and placebo group will be evaluated using both param etric and/or non-parametric tests, as appropriate. If necessary, bootstrapping techniques will be used to calculate confidence intervals around the incremental differences in costs. 12.6.3 Exploratory Endpoint Genotypic (including Hem agglutinin and Neurom inidase), phenotypic, viral culture and PCR data will be lis ted for each sub ject. These listings will be constructed in a m anner consistent with the F DA June 2006 Guidance Docum ent:“Guidance for Subm itting Influenza R esistance D ata”.18 Ad ditionally, the num ber and percen tage of genotypic changes from wild-type a mino acid will be summarized separately for treatm ent group, protein type, and study visit. 12.7 Safety Analyses AEs will be m apped to a MedDRA-pref erred term and system organ classification. The occurrence of TEAEs will be summarized by treatment group using MedDRA-preferred terms, system organ classifications, and severity. If a subject experiences multiple events that m ap to a s ingle p referred term, the grea test severity and st rongest Investigator assessment of relation to study d rug will be assigned to the preferred term for the appropriate sum maries. All AEs will be li sted f or individual subje cts showing both verbatim and preferred terms. Separate summaries of treatment-emergent SAEs and AEs related to study drug will be generated. Descriptive summaries of vital s igns and clinic al laboratory results will be presented by study visit. Laboratory abnorm alities will be graded according to the DAIDS Table for Grading Adverse Events for Adults and Pedi atrics (Publish Date: December 2004). The number and percentage of subjects experien cing treatm ent-emergent graded toxicities will be summarized by treatment group. Laborator y toxicity shifts from baseline to Day 3, Day 5, and Day 14 will be summarized by treatment group. Abnormal physical exam ination findings wi ll be presented by treatm ent group. The number and percent of subjects experiencing each abnormal physical examination finding will be included. Concomitant medications will be co ded using the WHO dictionary. The se data will be summarized by treatment group. Subject disposition will be presented for a ll s ubjects. The num ber of subjects who completed the study and discontinued from the study will be provided. The reasons for early discontinuation also will be presented. 253 253 BCX1812-311 (V1.0: 04-September-2007) Page 46 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.8 Sub-Study and Pharmacokinetic Analysis The sub-study to exam ine exposure respons e, along with the corresponding single PK samples collected on all subjects on study day 3 will be co mpleted as part of the sub- study. All s tatistical m ethods will be outlin ed as part of the sub-stu dy protocol and exposure-response analysis plan. All sub-study analyses will be reported in a separate sub-study report. 12.9 General Issues for Statistical Analysis 12.9.1 Multiple Comparisons and Multiplicity In order to m aintain the overall typ e I e rror in the presen ce of the plann ed comparisons between the two peram ivir treatm ents and pl acebo, a Bonferroni correction will be applied to the prim ary efficacy end point an alysis. No oth er ad justments for m ultiple comparisons are planned. 12.9.2 Covariates Primary and secondary efficacy analyses will be adjusted for RAT result at screen ing, current smoking behavior and influenza season at randomization (if necessary). 12.9.3 Planned Sub-Groups The prim ary efficacy endpoint will be summ arized separately by stratification group (current sm oking behavior [sm oker or non-smoker] and RAT result at screening [negative or positive]) and by viral subtype using descriptive statistics by treatment group and study day, if appropriate. No formal statistical testing will be utilized. Additional analyses m ay be perform ed by count ry, if necessary, for subm ission to local regulatory authorities. 12.9.4 Missing Data Every effort will be m ade to obtain required data at each s cheduled evaluation from all subjects who have been random ized. No attemp t will be m ade retrospectively to obtain missing subject reported data (including in fluenza symptom severity assessm ents, temperature, ability to perf orm usual activi ties, m issed days of work and im pact of influenza on subject’s work perform ance and/or productivity) that has not been completed by the subject at the time of return of the subject diary to the investigative site. In situations where it is not possible to obt ain all da ta, it m ay be necessary to im pute missing data. In assessing the p rimary efficacy endpoint, fo r subjects w ho withdraw or who d o no t experience allev iation of sym ptoms, m issing data will be censored using the date of subject’s last non-m issing assessment of infl uenza symptoms. Missing assessm ents of influenza symptoms conservatively will be im puted as h aving severity above absen t or mild (as f ailures). For the subjec t diary data, the f ollowing data con ventions will be utilized. Missing diary com pletion will be imputed as 11:59 for diary entries designated 254 254 BCX1812-311 (V1.0: 04-September-2007) Page 47 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL as m orning and 23:59 for evening and daily reported v alues. Entr ies with va lues exceeding the 24-hour clock will b e set to 23:59 of the day recorded. Select explo ratory sensitivity analyses m ay be conducted to ascert ain the effect, if any, of these m ethods. These sensitivity analy ses are further de scribed in the SAP. Secondary efficacy endpoints with tim e to event da ta will be censored using the date of subject’s last non- missing assessment of the given endpoint. 13 STUDY ADMINISTRATION 13.1 Regulatory and Ethical Considerations 13.1.1 Regulatory Authority Approvals This study will be conducted in com pliance with th e protoco l; GCPs, including International Conference on Harmonization (ICH) of Te chnical Requirem ents for Registration of Pharm aceuticals for Hu man Use G uidelines; FDA regulatory requirements and in accordance with the ethical principles of the Declaration of Helsinki. In addition, all applicable loca l laws and regu latory requirements relevant to the use of new therapeutic agents in the countries involved will be adhered to. The Investigator should submit written reports of clinical study status to their Institutional Review Board (IRB)/ Independent E thics Committee (IEC) annually or more frequently if requested by the IRB/ IEC. A final s tudy notification will also be forwarded to the IRB/IEC af ter the study is com pleted or in the event of prem ature ter mination of the study in accordance with the appl icable regulations. Copies of all contact with the IRB/ IEC should be m aintained in the study docum ents file. Copies of clinical study status reports (including termination) should be provided to BioCryst. 13.1.2 Ethics Committee Approvals Before initiation of the study at each invest igational site, the pr otocol, the inform ed consent form, the subject inform ation sheet, and any other relevant study documentation will be sub mitted to th e appropriate IRB/IE C. W ritten approval of th e study m ust be obtained before the study center can be initiated or the investigational medicinal product is re leased to the Inv estigator. A ny necessa ry extension s or renew als of IRB/IEC approval must be obtained, in particular, for changes to the study such as modification of the pro tocol, the inf ormed consent f orm, th e written inform ation provided to subjects and/or other procedures. The Investigator will report promptly to the IRB/IEC any new inform ation that m ay adversely affect the safety of the subjects or the conduct of the study. On completion of the study, the Investigator will prov ide the IRB/IEC with a report of the outcom e of the study. 13.1.3 Subject Informed Consent Signed info rmed consent m ust be obtained from each subject p rior to performing any 255 255 BCX1812-311 (V1.0: 04-September-2007) Page 48 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL study-related procedures. E ach subject should be given both verbal and w ritten information describing the nature and durati on of the clinical st udy. The inf ormed consent process should take place u nder conditions where the subject h as adequate time to consider the risks and bene fits associated with his/her participation in the study. Subjects will not be screened or treated until the subjec t has signed an approved ICF written in a language in which the subject is fluent. The ICF that is used must be approved both by BioCryst and by the reviewing IRB/ IEC. The informed consent should be in acco rdance with the curren t revision o f the Declaration of Helsinki, current ICH and GCP guidelines, and BioCryst policy. The Investigator must explain to potential subjects or their legal representatives the aims, methods, reasonably anticipated benefits, a nd potential hazards of the trial and any discomfort it may entail. Subjects will be informed that they are free not to participate in the trial and that they may withdraw consent to participate at any time. They will be told that refusal to participate in the study will not prejudice future treatment. They will a lso be told tha t their recor ds m ay be exam ined by com petent autho rities and au thorized persons but that pe rsonal information will be tr eated as strictly confidential and will not be publicly available. Subjects must be given the opportunity to ask questions. After this explanation and before entry in to the trial, consent should be appropriately recorded by means of the subject’s dated signature. The subject shoul d receive a signed and dated copy of the ICF. The original signed infor med consent should be retained in the study files. The Investigator shall maintain a log of all subjects who sign the ICF and indicate if the subject was enrolled into the study or reason for non-enrollment. 13.1.4 Payment to Subjects Reasonable compensation to study subjects may be provided if approved by the IRB/IEC responsible for the study at the Investigator’s site. 13.1.5 Investigator Reporting Requirements The Investigator will provide tim ely repo rts regard ing s afety to his /her IRB/IE C as required. 13.2 Study Monitoring During trial conduct, BioCryst or its designee will conduct period ic monitoring visits to ensure that the protocol and GCPs a re being followed. The monitors may review source documents to conf irm that th e data recorded on CRFs is accurate. The investigator and institution will allow BioCryst m onitors or its des ignees and app ropriate regulatory authorities direct access to source documents to perform this verification. 13.3 Quality Assurance The trial site may be subject to review by the IRB/IEC, and/or to quality assurance audits performed by BioCryst, and/or to inspection by appropriate regulatory authorities. It is important that the investigator(s) and their relevant personnel are available during the monitoring visits and possible a udits or inspections and that sufficient tim e is devoted to 256 256 BCX1812-311 (V1.0: 04-September-2007) Page 49 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL the process. 13.4 Study Termination and Site Closure BioCryst reserves the right to disc ontinue the tr ial prio r to inc lusion of the in tended number of subjects but intends only to exer cise this r ight f or valid scientif ic or administrative reasons. After such a deci sion, the Investigator must contact all participating subjects immediately after notification. As directed by BioCryst, all study materials must be collected a nd all case report forms completed to the greatest extent possible. 13.5 Records Retention To enable evaluations and/or audits from regulatory au thorities o r BioCryst, the Investigator agrees to k eep records, includi ng the iden tity of all p articipating sub jects (sufficient inf ormation to link re cords, case report forms and hospital records), all original signed inform ed consent form s, copies of all case report form s and detailed records of treatm ent disposition. The reco rds should be retained by the Investigator according to local regulations or as specified in the Clinical Trial Agreem ent, whichever is longer. If the Investigator relocates, retires, or for any reason withdraws from the study, the study records m ay be transferred to an acceptab le designee, such as another investigato r, another institution, or to BioCryst. The I nvestigator m ust obtain BioCryst’s written permission before disposing of any records. 13.6 Study Organization 13.6.1 Data Monitoring Committee BioCryst will a ssemble an indep endent Data M onitoring C ommittee ( DMC) to as sess safety parameters of the trial on a period ic, ongoing basis while the tr ial is in prog ress. The comm ittee will include a s tatistician and th ree phys icians, tw o of whom will be Infectious Disease specialists. Full detail s of the com position of the D MC and how the DMC is to operate will be described in a separate DMC charter. 13.7 Confidentiality of Information BioCryst affirms the subject’s right to prot ection against invasion of privacy. Only a subject id entification n umber, initials and /or date of birth will id entify subject data retrieved by BioCryst . However, in com pliance with federal regulations, BioCryst requires the investigato r to p ermit BioCryst ’s representatives and, when neces sary, representatives of the FDA or other regu latory authoritie s to review and/or copy any medical records relevant to the study. BioCryst will ensure that the use and disclosur e of protected health information obtained during a research study com plies with the HIPAA Privacy Rule. Th e Rule pro vides federal protection for the privacy of prot ected health inf ormation by im plementing standards to protec t an d guard ag ainst the m isuse of ind ividually id entifiable h ealth 257 257 BCX1812-311 (V1.0: 04-September-2007) Page 50 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL information of subj ects participating in BioCryst-sponsored Clinical Trials. "Authorization" is required from each research subject, i.e., specified permission granted by an individual to a covered entity for the us e or disclosure of an indi vidual's protected health information. A valid au thorization must meet the implem entation specifications under the HIPAA Pri vacy Rule. Authorizat ion m ay be com bined in the Inform ed Consent docum ent (approved by the IRB/IE C) or it may be a separate docum ent, (approved by the IRB/IEC) or provided by the Investigator or Sponsor (without IRB/IEC approval). It is the responsibility of the investigator and institution to obtain such waiver/authorization in writing f rom the appr opriate ind ividual. HIPAA authoriz ations are required for U.S. sites only. 13.8 Study Publication All data generated from this study are the propert y of BioCryst and shall be held in strict confidence along with all inform ation furnis hed by BioCryst. Independent analysis and/or publication of these data by the Investigator or any member of his/her staff are not permitted without prior written consent of BioCryst. W ritten perm ission to the Investigator will be contingen t on the review by BioCryst of the statistical ana lysis and manuscript and will provide fo r nondisclosure of BioCryst confidential or proprietary information. In all case s, the partie s agree to s ubmit all m anuscripts or abstracts to all other par ties 30 days prior to su bmission. This will e nable all parties to pr otect proprietary information and to provide comme nts based on infor mation that may not yet be available to other parties. 258 258 BCX1812-311 (V1.0: 04-September-2007) Page 51 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 14 REFERENCES 1. Cox NJ, Subbarao K. Influenza. Lancet 1999;354(9186):1277–1282. 2. Thompson WW, Shay KD, Weintraub E, Branner L, Cox N, et al. Mortality associated with influenza and respiratory syncytial virus in the United States. JAMA 2003;289(2):179–186. 3. Kaiser L, Wat C, Mills T, Mahoney P, Ward P, et al. Impact of oseltamivir treatment on influenza-related lower respiratory tract complications and hospitalizations. Arch Intern Med 2003;163(14):1667–1672. 4. Hayden FG, Treanor JJ, Fritz RS, Lobo M, Betts RF, et al. Use of the oral neuraminidase inhibitor oseltamivir in experimental human influenza: randomized controlled trials for prevention and treatment. JAMA 1999;282(13):1240–1246. 5. Kiso M, Mitamura K, Sakai-Tagawa Y, Shiraishi K, Kawakami C, et al. Resistant influenza A viruses in children treated with oseltamivir: descriptive study. Lancet 2004;364(9436):759–765. 6. Bantia S, Parker CD, Ananth SL, Horn LL, Andries K, et al. Comparison of the anti- influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir. Antimicrob Agents Chemother 2001;45(4):1162–1167. 7. Boivin G, Goyette N. Susceptibility of recent Canadian influenza A and B virus isolates to different neuraminidase inhibitors. Antiviral Res 2002;54(3):143–147. 8. Gubareva LV, Webster RG, Hayden FG. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother 2001;45(12):3403–3408. 9. Govorkova EA, Fang HB, Tan M, Webster RG. Neuraminidase inhibitor-rimantadine combinations exert additive and synergistic anti-influenza virus effects in MDCK cells. Antimicrob Agents Chemother 2004;48(12):4855–4863. 10. BioCryst Pharmaceuticals. Unpublished data. 11. Arnold CS, Zacks MA, Dziuba N, Yun N, Linde N, Smith J, Babu YS, Paessler S. Injectable peramivir promotes survival in mice and ferrets infected with highly pathogenic avian influenza A/Vietnam/1203/04 (H5N1). V-2041B, ICAAC 2006, San Francisco 12. Boltz, DA, Ilyushina NA, Arnold CS, Babu, YS, Webster RG and Govorkova EA. Intramuscular administration of neuraminidase inhibitor peramivir promotes survival against lethal H5N1 influenza infection in mice. Antiviral Research,2007; 74 (3): A32 13. BioCryst Pharmaceuticals unpublished clinical study report BC-01-03. 14. Tamiflu® Package Insert. Roche Pharmaceuticals. Rev. December 2005. 15. Quidel QuickVue Influenza A+B and Binax NOW Influenza A&B Test Kit product information sheets 259 259 BCX1812-311 (V1.0: 04-September-2007) Page 52 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 16. Treanor JJ, Hayden FG, Vrooman PS, Barbarash R et al. Efficacy and safety of the oral neuraminidase inhibitor oseltamivir in treating acute influenza. JAMA 2000; 283(8): 1016-1024. 17. Nicholson KG, Aoki FY, Osterhaus AD, Trottier S et al. Efficacy and safety of oseltamivir in treatment of influenza: a randomised controlled trial. Lancet 2000; 355(9218): 1845-1850. 18. US Department of Health and Human Services, Food and Drug Administration Center for Drug Evaluation and Reserach (CDER). Attachment to Guidance on Antiviral Product Development- Conducting and Submitting Virology Studies to the Agency: Guidance for Submitting Influenza Resistance Data. http://www.fda.gov/cder/guidance/7070fnlFLU.htm 260 260 BCX1812-311 (V1.0: 04-September-2007) Page 53 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15 APPENDICES 15.1 NYHA Functional Classification Criteria: Heart Failure and Angina NYHA Functional Classification of Heart Failure Class I No symptoms. Ordinary physical activity such as walking and climbing stairs does not cause fatigue or dyspnea. Class II Symptoms with ordinary physical activity. W alking or climbing stairs rapidly; walking uphill; walking or st air climbing after meals, in cold weather, in wind, or when under em otional stress causes undue fatigue or dyspnea. Class III Symptoms with less than ordinary physical activity. W alking one to two blocks on the level and clim bing more than one flight of stairs in normal conditions causes undue fatigue or dyspnea. Class IV Symptoms at res t. Inab ility to carry on any ph ysical activity without fatigue or dyspnea. NYHA Functional Classification of Angina Class I Angina only with unusually strenuous activity. Class II Angina with slightly m ore prolonged or slightly more vigorous activity than usual. Class III Angina with usual daily activity. Class IV Angina at rest. 261 261 CLINICAL STUDY PROTOCOL Protocol No. BCX1812-311 IND No. 76,350 A PHASE 3 MULTICENTER, RANDOMIZED, DOUBLE BLIND, PLACEBO- CONTROLLED STUDY TO EVALUATE THE EFFICACY AND SAFETY OF INTRAMUSCULAR PERAMIVIR IN SUBJECTS WITH UNCOMPLICATED ACUTE INFLUENZA THE IMPROVE I STUDY (IntraMuscular Peramivir for the Relief Of symptoms and Virologic Efficacy) Short title: Intramuscular Peramivir for the Treatment of Uncomplicated Influenza Protocol Date(s): Version 1.0: 04 September 2007 Version 2.0: 05 October 2007 BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35244, USA Phone: +1 919 859 1302 Fax: +1 919 851 1416 The document contains trade secrets and proprietary information of BioCryst Pharmaceuticals, Inc. This information is confidential property of BioCryst Pharmaceuticals, Inc., and is subject to confidentiality agreements entered into with BioCryst Pharmaceuticals, Inc. No information contained herein should be disclosed without prior written approval. CONFIDENTIAL 262 262 BCX1812-311 (V2.0: 05-October-2007) Page 2 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1 TITLE PAGE Protocol Number: BCX1812-311 Study Title: A phase 3 multicenter, randomized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza IND Number: 76, 350 Investigational Product: Peramivir (BCX1812) Indication Studied: Uncomplicated acute influenza Sponsor: BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35233 Development Phase: 3 Sponsor Medical Officer: W. James Alexander, M.D., M.P.H. Senior Vice President, Clinical Development Chief Medical Officer Phone: +1 919 859 1302 Fax: +1 919 851 1416 Email Address: jalexander@biocryst.com Compliance Statement: This study will be conducted in accordance with the ethical principles that have their origin in the Declaration of Helsinki and clinical research guidelines established by the Code of Federal Regulations (Title 21, CFR Parts 50, 56, and 312) and ICH Guidelines. Essential study documents will be archived in accordance with applicable regulations. Final Protocol Date: Version 1.0: 04 September 2007 Amendment(s) Date(s): Version 2.0: 05 October 2007 263 263 264 264 BCX1812-311 (V2.0: 05-October-2007) Page 4 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1.2 Clinical Study Protocol Agreement Protocol No. BCX1812-311 Protocol Title: A phase 3 multicenter, random ized, double-blind, placebo-controlled study to evaluate the effic acy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza I have carefully read this protocol and agree that it contains all of the necessary information required to conduct this study. I agree to c onduct this study as described and according t o the Decl aration of Helsinki, Internationa l Conference on Har monization Guidelines for Good Clinical Practices, and all applicable regulatory requirements. Investigator’s Signature Date Name (Print) 265 265 BCX1812-311 (V2.0: 05-October-2007) Page 5 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 2 SYNOPSIS Protocol No. BCX1812-311 Protocol Title: A phase 3, multicenter, randomized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza Sponsor: BioCryst Pharmaceuticals, Inc. Investigators/Study Sites: Multinational Development Phase: 3 Objectives: Primary: To evaluate the efficacy of peramivir administered intramuscularly compared to placebo on the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. Secondary: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly 2. To evaluate secondary clinical outcomes in response to treatment 3. To evaluate changes in influenza virus titer in nasopharyngeal samples (viral shedding) in response to treatment Exploratory: 1. To assess pharmacoeconomic measures as response to treatment 2. To assess changes in influenza viral susceptibility to neuraminidase inhibitors following treatment Number of Subjects: Total enrollment: a total of 750 evaluable subjects will be randomized to treatment (150 subjects in the placebo treatment group, 300 subjects in the peramivir 150mg treatment group and 300 subjects in the peramivir 300mg treatment group). An evaluable subject is one who is randomized, receives study drug, and has confirmed acute influenza by primary viral culture or PCR. A positive Rapid Antigen Test (RAT) at screening will be required for enrollment. Because results of clinic-based RAT tests may not precisely indicate presence of influenza infection, it is expected that at least 850 subjects will be randomized to treatment to ensure that 750 evaluable subjects are treated. Study Design: This is a multinational, randomized, double-blind study comparing the efficacy and safety of two single dose regimens of peramivir administered intramuscularly versus placebo in adults with uncomplicated acute influenza. 266 266 BCX1812-311 (V2.0: 05-October-2007) Page 6 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Each subject’s assignment to treatment will be stratified according to body mass index (BMI). Two BMI strata are planned: Normal-Overweight (≤ 29.9 kg/m2), and Obese (≥ 30.0 kg/m2). The number of subjects enrolled who have a BMI ≤ 29.9 kg/m2 (Normal-Overweight) will be at least 75% of the total enrollment. The number of subjects enrolled who have a BMI ≥ 30.0 kg/m2 (Obese) will be ≤ 25% of total enrollment. All subjects will be centrally randomized to one of three treatment groups according to BMI strata in a ratio of 2:2:1 such that 80% of subjects are randomized to one of the two single dose regimens of peramivir. Treatment Group 1: Peramivir 150mg Treatment Group 2: Peramivir 300mg Treatment Group 3: Placebo Study drug will be administered as bilateral 2mL intramuscular injections (total of 4mL injected in equally divided doses). Procedures for gluteal intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. Subjects eligible for screening will have an anterior nasal swab collected for testing by rapid antigen testing (RAT) for influenza A and B, in accordance with the commercially available RAT kit instructions. If the initial RAT is negative, the test should be repeated within one hour. Subjects meeting the inclusion/exclusion criteria may be enrolled into the study. All enrolled subjects will record the following information in a Study Diary: • Assessment of the presence and severity of each of seven symptoms of influenza on a 4-point scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatment, then once daily (AM) through Day 14 • Oral temperature measurements taken with an electronic thermometer every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol) or other anti-pyretic medications. • Assessment of subject’s time lost from work or usual activities and rating of productivity compared to normal (rated as 0-10 on a visual analog scale) once daily through Day 14 • Doses of antipyretic, expectorant, and/or throat lozenges 267 267 BCX1812-311 (V2.0: 05-October-2007) Page 7 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL taken for symptomatic relief each day through Day 14 Anterior nose (bilateral) and posterior pharynx specimens (swabs) will be collected at Day 1 (pre-treatment) and at Days 3, 5, and 9, for quantitative virologic assessments. Specimens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result on culture) as well as other virologic assessments (e.g. PCR, genotypic testing) All virologic assessments will be performed by a central laboratory. Two samples for pharmacokinetic (PK) testing for plasma levels of peramivir will be obtained from all subjects randomized. The first PK sample will be obtained between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be obtained at the day 3 visit in all subjects. The data from these PK samples will be utilized in a population exposure-response analysis. At selected sites a separate sub-study will be conducted to collect additional PK samples between treatment and Day 3 for the purpose of conducting a separate exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Study Population: Male and female subjects, 18 years of age and older, with symptoms consistent with a diagnosis of uncomplicated acute influenza infection may be screened for enrollment. Subject eligibility will require the presence of two or more symptoms consistent with acute influenza as well as positive results obtained from a rapid antigen test (RAT) for influenza A or B at screening. Inclusion Criteria: 1. Male and non-pregnant female subjects age ≥18 years. 2. A positive Influenza A or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate anterior nasal specimen, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated within one-hour. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. A subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at the time of screening. 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of at least moderate severity. 268 268 BCX1812-311 (V2.0: 05-October-2007) Page 8 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5. Presence of at least one constitutional symptom (myalgia [aches and pains], headache, feverishness, or fatigue) of at least moderate severity. 6. Onset of symptoms no more than 48 hours before presentation for screening. 7. Written informed consent. Exclusion Criteria: 1. Women who are pregnant or breast-feeding. 2. Presence of clinically significant signs of acute respiratory distress. 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma. 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class III or IV functional status within the past 12 months. 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 6. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min). 7. Clinical evidence of worsening of any chronic medical condition (temporally associated with the onset of symptoms of influenza) which, in the investigator’s opinion, indicates that such finding(s) could represent complications of influenza. 8. Current clinical evidence, including clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis and/or pneumonia, or active bacterial infection at any body site that requires therapy with oral or systemic antibiotics. 9. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy which would include oral or systemic treatment with > 10 mg prednisone or equivalent on a daily basis within 30 days of screening. 10. Currently receiving treatment for viral hepatitis B or viral hepatitis C. 11. Presence of known HIV infection with a CD4 count <350 cell/mm3. 12. Current therapy with oral warfarin or other systemic anticoagulant. 13. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening. 14. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days. 15. Immunized against influenza with inactivated virus vaccine within the previous 14 days. 16. Receipt of any intramuscular injection within the previous 269 269 BCX1812-311 (V2.0: 05-October-2007) Page 9 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 14 days. 17. History of alcohol abuse or drug addiction within 1 year prior to admission in the study. 18. Participation in a previous study of intramuscular or intravenous peramivir or previous participation in this study 19. Participation in a study of any investigational drug or device within the last 30 days. Study Endpoints: Primary Endpoint: Clinical: Time to alleviation of clinical symptoms of influenza. Secondary Endpoint(s): Safety: Incidence of treatment-emergent adverse events and treatment- emergent changes in clinical laboratory tests. Clinical: Time to resolution of fever. Incidence of influenza related complications. Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID50). Exploratory Endpoint(s): Pharmacoeconomic: Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. Virologic: Quantitative change in influenza virus shedding, measured by PCR. Change in influenza virus susceptibility to neuraminidase inhibitors. Investigational Product, Dose, and Mode of Administration: Peramivir (BCX-1812), 75mg/mL, 2mL per injection, administered as bilateral injections. Reference Therapy, Dose, and Mode of Administration: Matching Placebo (buffered diluent), 2mL per injection administered as bilateral injections. Duration of Treatment: Following treatment on day 1, study duration for all subjects is expected to be up to 14 days (including all visits). Presence of unresolved adverse events and/or treatment-emergent laboratory findings at the Day 14 visit, or persistent or recurrent symptoms of influenza (of the seven symptoms assessed) of either moderate or severe intensity at the Day 14 visit, will require additional follow up. Statistical Methods: Study Hypothesis: The null hypothesis (H0) for this study is that the time to 270 270 BCX1812-311 (V2.0: 05-October-2007) Page 10 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL alleviation of influenza symptoms is the same for subjects treated with placebo and for subjects treated with peramivir 150mg (H01) or peramivir 300mg (H02). The alternative hypothesis (H1) is that subjects treated with peramivir 150mg (H11) or peramivir 300mg (H12) have an improvement in time to alleviation of influenza symptoms over those treated with placebo. Sample Size: From preliminary results of a phase 2 study evaluating peramivir treatment of uncomplicated influenza, it is expected that the median time to alleviation of symptoms will be 137.0 hours (95% CI: 115.9, 165.8) for subjects receiving placebo treatment. Additionally, it is expected that the median time to alleviation for the 150 mg dose peramivir arm will be reduced by 30% compared to placebo (see table below) yielding a hazard ratio of 0.70. Median Time To Alleviation of Symptoms (Hours) Placebo Peramivir 150mg Difference (hours) 145.0 101.5 43.5 140.0 98.0 42.0 135.0 94.5 40.5 130.0 91.0 39.0 125.0 87.5 37.5 120.0 84.0 36.0 115.0 80.5 34.5 110.0 77.0 33.0 105.0 73.5 31.5 100.0 70.0 30.0 Using these assumptions, a sample size of 300 evaluable subjects per active treatment group and 150 evaluable subjects in the placebo group (a total of 750 evaluable subjects) is sufficient to provide at least 90% power to detect a hazard ratio of 0.70 using a log-rank statistic and α = 0.025 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). Efficacy: The intent-to-treat infected population (ITTI) will include all subjects who are randomized, received study drug, and have confirmed influenza by primary viral culture or PCR. The primary efficacy variable is the time to alleviation of symptoms, defined as the time from injection of study drug to the start of the time period when each of seven symptoms of influenza are either absent or are present at no more than mild severity level and remain at no worse than this severity status for a 21.5 hour (24 hours – 10%) period. 271 271 BCX1812-311 (V2.0: 05-October-2007) Page 11 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Descriptive statistics for the primary efficacy variable will be tabulated by treatment group. Alleviation of symptoms will be determined by assessment of symptoms as reported on each subject’s diary card. Time to alleviation of symptoms will be summarized for each treatment group. Treatment difference will be assessed using a Cox Regression model with effects for BMI at screening, influenza type by PCR at screening, treatment group, and, if necessary, influenza season at randomization. Pairwise comparisons between each active group and placebo will be constructed from the Cox Regression model. Subjects who do not experience alleviation of symptoms will be censored at the date of their last non-missing assessment. Time to resolution of fever will be analyzed in a similar manner. Efficacy analyses will be repeated for a Per-Protocol Infected population (PPI). This population will include those subjects in the ITTI population who received an adequate intramuscular injection. Details of this population will be described in the statistical analysis plan. The PPI population analysis will be used as supportive to the primary analysis with the ITTI. Changes in influenza virus TCID50 (viral titers from nasopharyngeal specimens) will be compared using the van Elteren statistic controlling for BMI at screening, influenza type by PCR, and, if necessary, for influenza season at randomization. Analyses of other continuous endpoints will be analyzed in a similar manner. The number and percentage of subjects experiencing influenza related complications (IRC) will be summarized by complication preferred term and treatment group. The difference between the treatment groups will be assessed using a logistic regression model with factors for treatment group, BMI at screening, influenza type by PCR, and influenza season at randomization (if necessary). Pairwise differences between the treatment groups will be evaluated using contrasts from the final logistic regression model. Safety: Safety analyses will be presented for all subjects in the safety population, defined as all randomized subjects who receive at least one dose of study drug. Adverse events will be mapped to a Medical Dictionary for Regulatory Activities (MedDRA) preferred term and system organ classification. The occurrence of treatment-emergent AEs will be summarized using preferred terms, system organ classifications, and severity. Separate summaries of treatment-emergent SAEs and treatment- emergent AEs that are related to study medication will be 272 272 BCX1812-311 (V2.0: 05-October-2007) Page 12 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL generated. All AEs will be listed for individual subjects showing both verbatim and preferred terms. Descriptive summaries of vital signs and quantitative clinical laboratory changes will be presented by study visit. Frequency and percentages of subjects with abnormal laboratory test results will be summarized by toxicity grade. Concomitant medications will be mapped to a WHO preferred term and drug classification. The number and percent of subjects taking concomitant medications will be summarized using preferred terms and drug classifications. The number and percent of subjects experiencing each abnormal physical examination finding will be presented. The number and percent of subjects discontinuing study as well as the reasons for discontinuation will be summarized by treatment group. Date of Protocol: Version 1.0: 04-September-2007 Amendment (Dates): Version 2.0: 05-October-2007 273 273 BCX1812-311 (V2.0: 05-October-2007) Page 13 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 3 TABLE OF CONTENTS 1 TITLE PAGE .................................................................................................................2 1.1 P ROTOCOL APPROVAL SIGNATURE PAGE ......................................................................3 1.2 C LINICAL STUDY PROTOCOL AGREEMENT ....................................................................4 2 SYNOPSIS .....................................................................................................................5 3 TABLE OF CONTENTS .............................................................................................13 3.1 L IST OF FIGURES...........................................................................................................15 3.2 L IST OF TABLES............................................................................................................15 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS ..............................16 5 INTRODUCTION ........................................................................................................18 5.1 B ACKGROUND...............................................................................................................18 5.2 R ATIONALE FOR STUDY................................................................................................18 5.3 N ON-CLINICAL EXPERIENCE WITH PERAMIVIR............................................................19 5.3.1 In vitro Assays..........................................................................................................19 5.3.2 Anim al Models.........................................................................................................19 5.4 P REVIOUS PHASE 3 CLINICAL EXPERIENCE WITH ORAL PERAMIVIR...........................20 5.5 P REVIOUS PHASE 1 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR ........................20 5.6 P HASE 2 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR..........................................21 5.7 DOSE RATIONALE ................................................................................................................23 6 STUDY OBJECTIVES ................................................................................................24 6.1 O BJECTIVES ..................................................................................................................24 6.1.1 Prim ary Objective ....................................................................................................24 6.1.2 Secondary Objective(s) ............................................................................................24 6.1.3 Explorator y Objective(s)..........................................................................................24 6.2 S TUDY ENDPOINTS .......................................................................................................24 6.2.1 Prim ary Endpoint .....................................................................................................24 6.2.2 Secondary Endpoint(s).............................................................................................24 6.2.3 Explorator y Endpoints .............................................................................................25 7 STUDY DESIGN.........................................................................................................25 7.1 O VERALL STUDY DESIGN AND PLAN ...........................................................................25 8 SELECTION AND WITHDRAWAL OF SUBJECTS................................................26 8.1.1 Inclusion Criteria......................................................................................................26 8.1.2 Exclusion Criteria.....................................................................................................27 8.1.3 Removal of Subjects from Therapy or Assessment .................................................27 9 TREATMENTS ............................................................................................................28 9.1 T REATMENTS ADMINISTERED ......................................................................................28 9.2 I DENTITY OF INVESTIGATIONAL PRODUCT(S)..............................................................28 9.3 M ETHOD OF ASSIGNING SUBJECTS TO TREATMENT GROUPS ......................................29 9.4 S TUDY MEDICATION ACCOUNTABILITY ......................................................................29 9.5 B LINDING/UNBLINDING OF TREATMENTS....................................................................29 9.6 P RIOR AND CONCOMITANT THERAPIES........................................................................30 9.7 O VERDOSE AND TOXICITY MANAGEMENT...................................................................30 9.8 D OSE INTERRUPTION ....................................................................................................30 10 STUDY CONDUCT ....................................................................................................30 10.1 E VALUATIONS...............................................................................................................30 10.1.1 Medical History ...................................................................................................30 10.1.2 Rapid Antigen Test for Influenza ........................................................................30 10.1.3 Physical Examination and Influenza-related Complications Assessments..........31 10.1.4 Vital Signs ...........................................................................................................31 274 274 BCX1812-311 (V2.0: 05-October-2007) Page 14 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.5 Electrocardiogram Measurements .......................................................................31 10.1.6 Clinical Laboratories............................................................................................31 10.1.7 Urine Pregnancy Test...........................................................................................32 10.1.8 Serology for Influenza .........................................................................................32 10.1.9 Samples for Virologic Laboratory Assessments..................................................32 10.1.10 Subject Self Assessments.....................................................................................32 10.1.11 Concom itant Medications....................................................................................33 10.1.12 Adverse Events ....................................................................................................33 10.1.13 Pharmacokinetic Exposure Samples....................................................................33 10.2 S CREENING PERIOD ......................................................................................................33 10.2.1 Inform ed Consent ................................................................................................33 10.2.2 Screening/Baseline Evaluation and Enrollment...................................................33 10.3 T REATMENT PERIOD—STUDY DAY 1 ..........................................................................34 10.3.1 Pre-dose Evaluations-Study Day 1 ......................................................................34 10.3.2 Post-dose Evaluations-Study Day 1.....................................................................34 10.4 P OST-TREATMENT ASSESSMENT PERIOD.....................................................................35 10.4.1 Days 2, 3, 5, 9 and 14 ..........................................................................................35 10.4.2 Adverse Events Reported at Post-treatment Visits ..............................................36 11 ADVERSE EVENT MANAGEMENT........................................................................39 11.1 D EFINITIONS .................................................................................................................39 11.1.1 Adverse Event......................................................................................................39 11.1.2 Serious Adverse Event.........................................................................................39 11.2 M ETHOD, FREQUENCY, AND TIME PERIOD FOR DETECTING ADVERSE EVENTS AND REPORTING SERIOUS ADVERSE EVENTS ......................................................................40 11.2.1 Definition of Severity ..........................................................................................40 11.2.2 Definition of Relationship to Study Drug............................................................41 11.2.3 Reporting Serious Adverse Events ......................................................................41 11.2.4 E mergency Procedures ........................................................................................42 12 STATISTICAL METHODS ........................................................................................42 12.1 D ATA COLLECTION METHODS .....................................................................................42 12.2 S TATISTICAL ANALYSIS PLAN......................................................................................43 12.3 S TUDY HYPOTHESIS .....................................................................................................43 12.4 S AMPLE SIZE ESTIMATES .............................................................................................43 12.5 A NALYSIS POPULATIONS..............................................................................................44 12.6 I NTERIM AND END OF STUDY ANALYSES.....................................................................45 12.7 E FFICACY ANALYSES ...................................................................................................45 12.7.1 Primary Efficacy Endpoint ..................................................................................45 12.7.2 Secondary Efficacy Endpoints.............................................................................45 12.7.3 Explorator y Endpoint...........................................................................................46 12.8 S AFETY ANALYSES.......................................................................................................47 12.9 S UB-STUDY AND PHARMACOKINETIC ANALYSIS.........................................................47 12.10 G ENERAL ISSUES FOR STATISTICAL ANALYSIS............................................................47 12.10.1 Multiple Comparisons and Multiplicity...............................................................47 12.10.2 Covariates ............................................................................................................48 12.10.3 Planned Sub-Groups ............................................................................................48 12.10.4 Missing Data........................................................................................................48 13 STUDY ADMINISTRATION.....................................................................................48 13.1 R EGULATORY AND ETHICAL CONSIDERATIONS...........................................................48 13.1.1 Regulatory Authority Approvals .........................................................................48 13.1.2 Ethics Committee Approvals...............................................................................49 275 275 BCX1812-311 (V2.0: 05-October-2007) Page 15 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.1.3 Subject Informed Consent ...................................................................................49 13.1.4 Payment to Subjects.............................................................................................50 13.1.5 Investigator Reporting Requirements ..................................................................50 13.2 S TUDY MONITORING ....................................................................................................50 13.3 Q UALITY ASSURANCE ..................................................................................................50 13.4 S TUDY TERMINATION AND SITE CLOSURE...................................................................50 13.5 R ECORDS RETENTION...................................................................................................50 13.6 S TUDY ORGANIZATION.................................................................................................51 13.6.1 Data Monitoring Committee................................................................................51 13.7 C ONFIDENTIALITY OF INFORMATION ...........................................................................51 13.8 S TUDY PUBLICATION....................................................................................................51 14 REFERENCES .............................................................................................................52 15 APPENDICE S..............................................................................................................54 15.1 NYHA FUNCTIONAL CLASSIFICATION CRITERIA: HEART FAILURE AND ANGINA......54 15.2 C RITERIA FOR SEVERE COPD AND SEVERE ASTHMA..................................................55 3.1 List of Figures Figure 1 Study Measurements and Visit Schedule.................................................................37 3.2 List of Tables Table 1 Results of study BC-01-03.......................................................................................20 Table 2 Pharmacokinetic parameters from study Him-06-111. ............................................21 Table 3 Summary of Efficacy from BCX1812-211. .............................................................22 Table 4 Summary of Safety from BCX1812-211. ................................................................23 Table 5 Median time to alleviation of symptoms (30% reduction, 0.70 hazard ratio)..........44 276 276 BCX1812-311 (V2.0: 05-October-2007) Page 16 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS AE adverse event ALT alanine aminotransferase AST aspartate aminotransferase AUC area under the curve AUC0–72 area under the curve from time 0 to 72 hours AUC0–∞ area under the curve extrapolated from time 0 to infinity BMI Body Mass Index in kg/m2 CBC complete blood count CDC Centers for Disease Control and Prevention CIOMS Council for International Organizations of Medical sciences Cmax maximum plasma concentration CK creatine kinase CNS central nervous system COPD chronic obstructive pulmonary disease CRF Case Report Form CV coefficient of variation ECG Electrocardiogram GCP Good Clinical Practice HCG human chorionic gonadotropin HIV Human immunodeficiency virus IC50 median inhibitory concentration ICF informed consent form ICH International Conference on Harmonization IEC Independent Ethics Committee IRB Institutional Review Board IRC influenza related complications ITT intent-to-treat ITTI intent-to-treat infected IUD intrauterine device IVRS interactive voice response system LDH lactate dehydrogenase MedDRA Medical Dictionary for Regulatory Activities MRU medical resource utilization NSAID non-steroidal anti-inflammatory drug PCR polymerase chain reaction RAT Rapid Antigen Test RBC red blood cell SAE serious adverse event SAP statistical analysis plan 277 277 BCX1812-311 (V2.0: 05-October-2007) Page 17 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL SD standard deviation SUSAR Suspected Unexpected Serious Adverse Event t1/2 elimination half-life t1/2 λz terminal half-life TCID50 tissue-culture infective dose50 TEAEs treatment-emergent adverse events Tmax time to attain maximum plasma concentration WBC white blood cell WHO World Health Organization 278 278 BCX1812-311 (V2.0: 05-October-2007) Page 18 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5 INTRODUCTION 5.1 Background Influenza virus is a member of the orthomyxovirus family and causes an acute viral disease of the respiratory tract. Typical influenza illness is characterized by abrupt onset of fever, headache, myalgia, sore throat, and nonproductive cough.1 The illness is usually self-limiting, with relief of symptoms occurring within 5 to 7 days. Nevertheless, it is an important disease for several reasons, including ease of communicability, short incubation time, rapid rate of viral mutation, morbidity with resultant loss of productivity, risk of complicating conditions, and increased risk of death, particularly in the elderly. During 19 of the 23 influenza seasons between 1972/1973 and 1994/1995, estimated influenza-associated deaths in the United States ranged from approximately 25 to more than 150 per 100,000 persons above 65 years of age, accounting for more than 90% of the deaths attributed to pneumonia and influenza.2 Presently, only a few measures are available that can reduce the impact of influenza: active immunoprophylaxis with an inactivated or live attenuated vaccine and chemoprophylaxis or therapy with an influenza-specific antiviral drug. Neuraminidase inhibitors are the current mainstay of antiviral treatment for influenza. Marketed neuraminidase inhibitors include zanamivir (Relenza®, GlaxoSmithKline) and oseltamivir (Tamiflu®, Roche-Gilead), an oral prodrug of the active agent, oseltamivir carboxylate. Influenza neuraminidase is a surface glycoprotein that cleaves sialic acid residues from glycoproteins and glycolipids. The enzyme is responsible for the release of new viral particles from infected cells and may also assist in the spreading of virus through the mucus within the respiratory tract. The neuraminidase inhibitors represent an important advance in the treatment of influenza with respect to activity against influenza A and B viruses, with proven therapeutic value in reducing influenza lower respiratory complications,3 and lower rates of antiviral drug resistance4. The use of currently available neuraminidase inhibitors has been limited by concerns including, the degree of effectiveness, the requirement for an inhaler device (zanamivir), and the emergence of resistant influenza virus variants in some treated populations.5 In addition, there are risks of bronchospasm with zanamivir; and gastrointestinal side effects, with oseltamivir. Peramivir is a neuraminidase inhibitor that represents a potentially promising addition to the armamentarium of drugs for the treatment of influenza infections due to its potential for parenteral administration and lower frequency of dosing. 5.2 Rationale for Study An oral formulation of peramivir has previously been evaluated in a full range of safety, tolerability, pharmacokinetic, and efficacy studies. In a multinational phase 3 clinical trial conducted in 1999-2001, oral peramivir demonstrated antiviral activity against influenza A and B infections, and improvement in the relief of clinical symptoms. Because of the limited bioavailability of peramivir following oral administration (<5%), it was determined that the parenteral route of administration is more appropriate for the delivery of peramivir. Subsequent phase 1 studies of intravenous and intramuscular formulations of peramivir have confirmed that parenteral routes of administration result in plasma levels of drug that are as much as 100 times those achieved via the oral route. Further details of these studies are provided below and in the Investigator Brochure. 279 279 BCX1812-311 (V2.0: 05-October-2007) Page 19 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Because of the previous demonstration of significant antiviral activity, the strong suggestion of clinical efficacy of oral peramivir previously demonstrated in acute influenza, and the encouraging pharmacokinetic and preliminary safety profile of the intramuscular formulation of peramivir demonstrated to date, this phase 3 study will be conducted to evaluate the efficacy and safety profile of intramuscular peramivir and to determine the optimal single dose regimen. 5.3 Non-Clinical Experience with Peramivir 5.3.1 In vitro Assays Peramivir is a selective inhibitor of viral neuraminidase, with 50% inhibitory concentrations (IC50) for bacterial and mammalian enzymes of >300µM.6 In an in vitro study, 42 influenza A and 23 influenza B isolates were collected from untreated subjects during the 1999–2000 influenza season in Canada.7 These isolates were tested for their susceptibility to the neuraminidase inhibitors zanamivir, oseltamivir carboxylate, and peramivir using a chemiluminescent neuraminidase assay. Inhibition of Type A influenza neuraminidase by peramivir was approximately an order of magnitude greater than inhibition of neuraminidase from Type B viruses. IC50 values for the Type A enzymes ranged from <0.1 to 1.4nM, whereas the Type B enzymes ranged from <0.1 to 11nM, with three out of four values in the 5- to 11nM range. Peramivir was the most potent drug against influenza A (H3N2) viruses with a mean IC50 of 0.60nM as well as most potent against influenza B with a mean IC50 of 0.87nM. In another in vitro comparison of peramivir, oseltamivir, and zanamivir, using a neuraminidase inhibition assay with influenza A viruses, the median IC50 of peramivir (approximately 0.34nM) was comparable to that of oseltamivir (0.45nM) and significantly lower than zanamivir (0.95nM). For influenza B virus clinical isolates, the median IC50 of peramivir (1.36nM) was comparable to that of zanamivir (2.7nM) and lower than that of oseltamivir (8.5nM).8 The potency of peramivir was evaluated against five zanamivir-resistant and six oseltamivir- resistant influenza viruses.9 Peramivir remained a potent inhibitor against all oseltamivir-resistant viruses including the mutations H274Y, R292K, E119V, and D198N, with IC50 values ≤40nM. Peramivir also potently inhibited (IC50 ≤ 26nM) the neuraminidase activity of zanamivir-resistant strains, which had the following mutations: R292K, E119G, E119A, and E119D. However, one zanamivir-resistant influenza B virus, B/Mem/96, with a mutation R152K isolated from cell culture, was relatively resistant to all neuraminidase inhibitors, including peramivir (IC50 = 400nM). 5.3.2 Animal Models In a mouse model of influenza infection, a single intramuscular injection of peramivir (10mg/kg) given 4 hours prior to inoculation with an A/NWS/33 (H1N1) influenza strain resulted in 100% survival in contrast to 100% mortality in a control group injected with saline.6 In the same mouse model, treatment of mice up to 72 hours after influenza infection using peramivir (20mg/kg) resulted in 100% survival, compared to 100% mortality in the control group injected with vehicle.10 Peramivir has also demonstrated activity in animal models utilizing a clinical H5N1 isolate as the infecting virus strain. In a mouse model, a single intramuscular dose of peramivir (30mg/kg) injected 1 hour after inoculation with the highly pathogenic (H5N1) A/Vietnam/1203/04 strain, resulted in a 70% survival rate that was similar to that seen in mice treated with oseltamivir given 280 280 BCX1812-311 (V2.0: 05-October-2007) Page 20 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL orally at 10mg/kg/day for 5 days11. In similar experiments, mice inoculated with the same strain of H5N1 virus that were then treated for up to 8 days with intramuscular peramivir exhibited 100% survival12. This longer duration of peramivir treatment also prevented viral replication in the lungs, brain and spleen at days 3, 6 and 9 post inoculation. 5.4 Previous Phase 3 Clinical Experience with Oral Peramivir An oral formulation of peramivir has previously demonstrated antiviral activity and preliminary clinical efficacy in challenge studies in human volunteers, as well as in treatment studies in patients with uncomplicated acute influenza infections during the influenza seasons of 1999- 2001. A Phase 3 multinational study (BC-01-03) of oral peramivir was conducted. Two dose regimens of oral peramivir, 800mg QD for 5 days, or 800mg QD on Day 1, followed by 400mg QD for 4 days, were compared to a matched placebo treatment group. A total of 1246 subjects were randomized to treatment at sites in the USA, Western and Eastern Europe, South America, Australia and New Zealand. As presented in the Table 1 below, the primary end-point of time to relief of influenza symptoms in 694 subjects with confirmed influenza was not found to be significantly different (p=0.17) between the three treatment groups.13 A sub-group analysis of the time to relief of symptoms by country or region demonstrated marked differences in the primary endpoint.. In the subset of influenza-infected subjects enrolled at sites in the US, clinically meaningful differences in time to relief of influenza symptoms between the placebo and the two peramivir arms were observed, however statistical significance (p=0.07) was not achieved. However, a number of secondary endpoints in this phase 3 study, such as time to overall well- being, time to normal activity, incidence of influenza related complications and quantity of viral shedding, achieved or approached statistically significant differences between the peramivir and placebo treatment groups (p=0.03-0.06). Table 1 Results of study BC-01-03 Median Time to Relief of Influenza Symptoms (Hours) Dose and Regimen Overall Results (n=694) US Sites (n=198) Peramivir 800mg po x 5d 89.0 70.8 Peramivir 800mg po x 1d and 400mg po x 4d 91.7 88.8 Placebo x 5 days 104.4 106.8 p value 0.17 0.07 5.5 Previous Phase 1 Experience with Intramuscular Peramivir Two phase 1studies evaluating the safety and pharmacokinetics of an intramuscular formulation of peramivir have been conducted in a total of 45 healthy volunteers receiving peramivir. Study Peramivir-Him-06-111 evaluated the single dose pharmacokinetics and tolerability of 75mg, 150mg and 300mg doses of peramivir administered as intramuscular (i.m.) and intravenous (i.v.) injections in a crossover design (9 subjects per group). Peak plasma levels of 281 281 BCX1812-311 (V2.0: 05-October-2007) Page 21 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL i.m. peramivir generally occurred within 30 minutes following injection. Plasma pharmacokinetic parameters for i.m. peramivir are summarized in Table 2 below for the three intramuscular single dose regimens evaluated. Table 2 Pharmacokinetic parameters from study Him-06-111. Dose (mg) Cmax (ng/mL) AUC0-∞ (hr·ng/mL) t½a (hr) 75 i.m. 4296 ± 812 11659 ± 1123 19.8 ± 7.9 150 i.m. 7612 ± 884 23952 ± 3804 24.3 ± 4.1 300 i.m. 15150 ± 2367 49649 ± 5619 22.8 ± 2.5 aterminal half life In a second phase 1 study, Peramivir-Him-06-112, the same dose levels of peramivir were administered as single i.m. injections on two consecutive days (6 subjects per group). This double-blind study also included a placebo arm. The pharmacokinetic parameters of i.m. peramivir following the second day of dosing were consistent with those seen following single doses of the drug. The observations of safety and tolerability of i.m. peramivir in each of the 2 phase 1 studies were unremarkable. No serious adverse events were reported. The most commonly observed adverse events or laboratory abnormalities were headache, several reports of signs and symptoms of vasovagal reactions following injections, and transient increases in creatine kinase. No consistent differences in frequency of adverse events were observed between the active and placebo treatment groups, with the exception that CK elevations appeared to be dose related in the peramivir treatment groups. The vasovagal reactions were attributed to the receipt of relatively large volumes of i.m. injection (2 injections each of 2mL) in the fasted state. 5.6 Phase 2 Experience with Intramuscular Peramivir A phase 2 study BCX1812-211 was completed in 2007. This study was a randomized, double- blind placebo- controlled study to evaluate the efficacy and safety of two single dose regimens of peramivir. A total of 344 subjects were enrolled into this study with 115 subjects randomized to Placebo; 114 subjects randomized to peramivir 150 mg; and 114 subjects randomized to peramivir 300 mg. The primary endpoint of the study was the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. Based on preliminary data, the primary endpoint of time to alleviation of clinical symptoms in BCX1812-211 did not achieve statistical significance in the pre-planned ITTI study population (Table 3). Based on pre-planned and post hoc analyses, it appeared that a majority of subjects within this phase 2 study did not receive an adequate intramuscular injection. In phase 1 studies (Hi m-06-111 and Him-06-112) of i.m . per amivir, significant increases in creatine kinase (CK) were observed at Day 3 compared with Baseline (Day 1) in all subjects who received active study drug or placebo. CK is a well established marker of muscle damage, and it was hypothesized that CK increase may act as a surrogate marker of an adequate i.m. injection. Within the phase 2 study, an increase in CK between Baseline (Day 1) and Day 3 was not observed in a majority of subjects. In the phase 1 studies study drug was administered with a 1½ 282 282 BCX1812-311 (V2.0: 05-October-2007) Page 22 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL inch needle. In the phase 2 study a shorter needle (1 inch) was supplied with the study drug, with guidance that a longer needle (1½ inch) should be used for larger subjects. Based on the observed lack of CK increases at Day 3 compared to baseline, the Sponsor hypothesized that the needle used for injection failed to penetrate muscle and deliver intramuscular study medication in many subjects. A sub group of subjects was identified in which a Day 3 CK increase of at least 50U/L was observed over baseline. Within this adequate intramuscular injection sub-group, notable improvements in the time to alleviation of symptoms were observed for both peramivir dose groups: 44.6 hours for peramivir 150 mg treatment and 64.8 hours for the peramivir 300 mg treatment (Table 3). These efficacy data support the further development of peramivir as a single dose, intramuscular treatment for acute influenza. Table 3 Summary of Efficacy from BCX1812-211. Placebo Peramivir 150mg Peramivir 300mg Intent-to-Treat Infected Population1 (n=313) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=107 137.0 115.9-163.8 n=104 114.1 95.2-145.5 22.9 n=102 115.9 77.8-136.6 21.1 Adequate Injection Population2 (n=101) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=40 152.2 103.8-183.9 n=32 107.6 76.8-175.1 44.6 n=29 87.4 40.8-163.8 64.8 1: Intent-to-Treat Infected Population: PCR+ for either Influenza A and/or Influenza B at baseline/screening visit. 2: Adequate Injection Population: ITTI subjects in who study drug reached target muscle tissue, as evidenced by an increase in serum CK levels of ≥ 50 U/L over baseline at the Day 3 study visit. An independent data monitoring committee reviewed grouped blinded safety data throughout study BCX1812-211. In the overall safety population (n=342), doses of peramivir 150 mg and 300 mg were both found to be well tolerated and no safety concerns were identified by the DMC. The three treatment groups were similar with respect to the frequency and severity of adverse events. Two serious adverse events were reported in the study, and neither was considered by the investigator to be related to treatment. One SAE (pyelonephritis) occurred 5-days after study treatment in a subject who received placebo, and one SAE (meningitis, resulting in death) occurred 10-days after study treatment in a subject who received 300 mg of peramivir. There were no meaningful differences among the three treatment groups with respect to the frequency or severity of graded laboratory toxicities. A summary of the adverse events and graded toxicities, together with a list of the most frequently reported adverse events, is presented in Table 4. 283 283 BCX1812-311 (V2.0: 05-October-2007) Page 23 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 4 Summary of Safety from BCX1812-211. Safety Parameters Placebo (N=114) Peramivir 150 mg (N=113) Peramivir 300 mg (N=115) Any Clinical Adverse Event 49 (43%) 43 (38%) 44 (38%) Any Graded Laboratory Toxicity 99 (87%) 93 (82%) 92 (80%) Any Serious Adverse Event 1 (<1%) 0 1 (<1%) Most Frequent Adverse Events Assessed as Study Drug-Related Diarrhea Nausea Vasovagal Reaction 5 (4%) 7 (6%) 4 (4%) 5 (4%) 7 (6%) 2 (2%) 6 (5%) 9 (8%) 0 5.7 Dose Rationale Oseltamivir is approved for the treatment of uncomplicated acute influenza at a dosage of 75mg twice daily in adults14. Oseltamivir was shown to be clinically effective in a phase 3 study of oral oseltamivir versus placebo in naturally occurring seasonal influenza, and these data were sufficient for regulatory approval for marketing of oseltamivir. At least 75% of an oral dose of oseltamivir reaches the systemic circulation as oseltamivir carboxylate. When oseltamivir is administered orally at a dose of 75mg twice daily, the serum Cmax of oseltamivir carboxylate is approximately 348ng/mL and the AUC0-48 is 10,876 h·ng/mL. The clinical data indicate that this level of exposure to oseltamivir was sufficient to provide clinical improvement in uncomplicated acute influenza. The serum pharmacokinetic data (Cmax and AUC0-∞, respectively) following intramuscular doses of peramivir are approximately 7600ng/mL and 24,000 h·ng/mL for the 150mg dose and are approximately 15,000ng/mL and 49,000 h·ng/mL for the 300mg dose. Previous studies have assessed the concentrations of the neuraminidase inhibitor zanamivir in nasal and pharyngeal secretions after parenteral administration of this drug. . Within several hours after administration, the concentrations in secretions were approximately 100-fold lower than in serum or plasma. In theory, relatively high levels of a neuraminidase inhibitor in respiratory secretions are desirable in order to rapidly inactivate influenza virus and to delay or prevent the development of resistance in infecting virus strains. Intramuscular doses of peramivir, including doses of 150mg and 300mg have been shown to be well tolerated in previous Phase 1 studies. In the completed Phase 2 study, both doses of peramivir (150 mg and 300 mg) were well tolerated and no safety concerns were apparent. Therefore, it is appropriate for these two dose regimens to undergo further evaluation in this Phase 3 study. 284 284 BCX1812-311 (V2.0: 05-October-2007) Page 24 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6 STUDY OBJECTIVES 6.1 Objectives 6.1.1 Primary Objective To evaluate the efficacy of peramivir administered intramuscularly compared to placebo on the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. 6.1.2 Secondary Objective(s) The secondary objectives of this study are: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly, 2. To evaluate secondary clinical outcomes in response to treatment, 3. To evaluate changes in influenza virus titer in nasopharyngeal samples (viral shedding) in response to treatment. 6.1.3 Exploratory Objective(s) The following exploratory objectives have been identified for this study. 1. To assess pharmacoeconomic measures as response to treatment. 2. To assess changes in influenza viral susceptibility to neuraminidase inhibitors following treatment. 6.2 Study Endpoints 6.2.1 Primary Endpoint The primary clinical endpoint is the time to alleviation of clinical symptoms of influenza for each subject. 6.2.2 Secondary Endpoint(s) Secondary safety, clinical, and virologic endpoints will include evaluations in each subject of: Safety: Incidence of treatment-emergent adverse events and treatment-emergent changes in clinical laboratory tests. Clinical: Time to resolution of fever; Incidence of influenza related complications. Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID50). 285 285 BCX1812-311 (V2.0: 05-October-2007) Page 25 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6.2.3 Exploratory Endpoints Pharmacoeconomic and virologic evaluations in each subject for exploratory endpoints will also be assessed and include: Pharmacoeconomic: Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. Virologic: Quantitative change in influenza virus shedding, measured by PCR; Change in influenza virus susceptibility to neuraminidase inhibitors. 7 STUDY DESIGN 7.1 Overall Study Design and Plan This is a multinational, randomized, double-blind study comparing the efficacy and safety of two single dose regimens of peramivir administered intramuscularly versus placebo in adults with uncomplicated acute influenza. Each subject’s assignment to treatment will be stratified according to body mass index (BMI). Two BMI strata are planned: Normal-Overweight (≤ 29.9 kg/m2), and Obese (≥ 30.0 kg/m2). The number of subjects enrolled who have a BMI ≤ 29.9 kg/m2 (Normal-Overweight) will be at least 75% of the total enrollment. The number of subjects enrolled who have a BMI ≥ 30.0 kg/m2 (Obese) will be ≤ 25% of total enrollment. All subjects will be centrally randomized to one of three treatment groups in a ratio of 2:2:1 such that 80% of subjects are randomized to one of the two single dose regimens of peramivir. Treatment Group 1: Peramivir 150mg Treatment Group 2: Peramivir 300mg Treatment Group 3: Placebo Study drug will be administered as bilateral 2mL intramuscular injections (total of 4mL injected in equally divided doses). Procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. Subjects eligible for screening will have an anterior nasal swab collected for testing by RAT for influenza A and B, in accordance with the commercially available RAT kit instructions. If the initial RAT is negative, the test should be repeated within one hour. Subjects meeting the inclusion/ exclusion criteria may be enrolled into the study. All enrolled subjects will record the following information in a Study Diary. • Assessment of the presence and severity of each of seven symptoms of influenza on a 4-point scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatment, then once daily (AM) through Day 14. 286 286 BCX1812-311 (V2.0: 05-October-2007) Page 26 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL • Oral temperature measurements will be taken with an electronic thermometer every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol) or other antipyretic medication. • Assessment of subject’s time lost from work or usual activities and rating of productivity compared to normal (rated as 0-10 on a visual analog scale) once daily through Day 14 • Doses of antipy retic, expectorant, and/or th roat lozenges taken for s ymptomatic relief each day through Day 14 Anterior nose (bilateral) and posterior pharynx specimens (swabs) will be collected at Day 1 (pre- treatment) and at Days 3, 5, and 9, for quantitative virologic assessments. Specimens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result) as well as other virologic assessments (e.g. PCR, genotypic testing). All virologic assessments will be performed by a central laboratory. Two samples for pharmacokinetic (PK) testing for plasma levels of peramivir will be obtained from all subjects randomized. The first PK sample will be obtained between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be obtained at the day 3 visit in all subjects. The data from these PK samples will be utilized in a population exposure-response analysis. At selected sites a separate sub-study will be conducted to collect additional PK samples between treatment and Day 3 for the purpose of conducting a separate exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Study drug will be administered as bilateral 2mL intramuscular injections (total of 4mL injected in divided doses). Procedures for intramuscular injection, with a recommended needle length appropriate to the size and weight of the subject, are provided in the study drug administration manual. 8 SELECTION AND WITHDRAWAL OF SUBJECTS 8.1.1 Inclusion Criteria Subjects must meet all of the following criteria for inclusion in this study: 1. Male and non-pregnant female subjects age ≥18 years. 2. A positive Influenza A or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate anterior nasal specimen, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated within one hour. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. A subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at the time of screening. 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of at least moderate severity. 287 287 BCX1812-311 (V2.0: 05-October-2007) Page 27 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5. Presence of at least one constitutional symptom (myalgia [aches and pains], headache, feverishness, or fatigue) of at least moderate severity. 6. Onset of symptoms no more than 48 hours before presentation for screening. 7. Written informed consent. 8.1.2 Exclusion Criteria Subjects to whom any of the following criteria apply will be excluded from the study: 1. Women who are pregnant or breast-feeding. 2. Presence of clinically significant signs of acute respiratory distress 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma. (See Section 15.2). 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class III or IV functional status within the past 12 months. (See Section 15.1). 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 6. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min). 7. Clinical evidence of worsening of any chronic medical condition (temporally associated with the onset of symptoms of influenza) which, in the investigator’s opinion, indicates that such finding(s) could represent complications of influenza. 8. Current clinical evidence, including clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis and/or pneumonia, or active bacterial infection at any body site that requires therapy with oral or systemic antibiotics. 9. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy which would include oral or systemic treatment with > 10 mg prednisone or equivalent on a daily basis within 30 days of screening. 10. Currently receiving treatment for viral hepatitis B or viral hepatitis C. 11. Presence of known HIV infection with a CD4 count <350 cell/mm3. 12. Current therapy with oral warfarin or other systemic anticoagulant. 13. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening. 14. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days. 15. Immunized against influenza with inactivated virus vaccine within the previous 14 days. 16. Receipt of any intramuscular injection within the previous 14 days. 17. History of alcohol abuse or drug addiction within 1 year prior to admission in the study. 18. Participation in a previous study of intramuscular or intravenous peramivir or previous participation in this study. 19. Participation in a study of any investigational drug or device within the last 30 days. 8.1.3 Removal of Subjects from Therapy or Assessment All subjects are permitted to withdraw fro m participation in this study at any ti me and for any reason, specified or unspecified, and without prejudice. T he Investigator or sp onsor m ay 288 288 BCX1812-311 (V2.0: 05-October-2007) Page 28 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL terminate the subject’s participation in the study at any time for reasons including the following: 1. Adverse event; 2. Intercurrent illness; 3. Non-compliance with study procedures; 4. Subject’s decision; 5. Administrative reasons; 6. Lack of efficacy; 7. Investigator’s opinion to protect the subject’s best interest. Any subject who withdraws because of an adve rse event will be followe d until the sign(s) or symptom(s) that constituted the adverse event has/ha ve resolved or is determ ined to represent a stable medical condition. A subject should be with drawn from the trial if, in the opinion of the Investigator, it is medically necessary, or if it is the desire of the subject. If a subject does not return for a scheduled visit, every effort should be made to contact the subject and determine the subject’s medical condition. In any circumstance, every effort should be made to document subject outcome, if possible. If the subject withdraws consent, no fu rther ev aluations should b e perfo rmed and no attempts should be made to collect additional data. 9 TREATMENTS 9.1 Treatments Administered Peramivir is an investigational drug. Peramivir for intramuscular injection is a small-volume parenteral and will be supplied as a 75mg/mL solution in sodium citrate/ citric acid buffer. The pH is approximately 3.0. A matched placebo solution of sodium citrate/ citric acid buffer with 1.2% sodium chloride at a pH of approximately 3.0 will be supplied. The gluteal site of injection and the syringe needle length are to be recorded in the subjects CRF. Procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. 9.2 Identity of Investigational Product(s) Peramivir and placebo peramivir will be supplied in clear 2mL vials. An individual study drug kit will contain 2 vials of blinded study drug (peramivir and/or placebo, depending upon the treatment group), 2 syringes and 2 needles in which to draw up the solution for intramuscular injection. All materials will be packaged in a labeled box container. All study drug kits must be stored at 2-8oC. Each individual study drug kit will be labeled with some or all of the following information as required by local regulations: 289 289 BCX1812-311 (V2.0: 05-October-2007) Page 29 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL • Sponsor name and contact information, study protocol number, kit number, description of the contents of the container, instructions for the preparation of the syringe and administration of the study drug, conditions for storage, statement regarding the investigational (clinical trial) use of the study drug and date for retest or expiry date. Each vial of study drug will be labeled with some or all of the following information as required by local regulations: • Sponsor name, study protocol number, description of the contents of the vial, instructions for the preparation of the syringe, statement regarding the investigational (clinical trial) use of the study drug and lot number. 9.3 Method of Assigning Subjects to Treatment Groups Subjects will be centrally randomized according to BMI strata in a ratio of 2:2:1 to one of three treatment groups: single dose peramivir 150mg, single dose peramivir 300mg or placebo, in accordance with a computer-generated randomization schedule prepared by a non-study statistician. Eighty percent (80%) of subjects will be randomized to treatment with one of the two single dose regimens of peramivir, 20% will be randomized to treatment with placebo. Each subject’s assignment to treatment will be stratified according to body mass index (BMI). Two BMI strata are planned: Normal-Overweight (≤ 29.9 kg/m2), and Obese (≥ 30.0 kg/m2). The number of subjects enrolled who have a BMI ≤ 29.9 kg/m2 (Normal-Overweight) will be at least 75% of the total enrollment. The number of subjects enrolled who have a BMI ≥ 30.0 kg/m2 (Obese) will be ≤ 25% of total enrollment. Once a subject is eligible for randomization, he/she will be assigned a study drug kit number that will be obtained by study staff from the study interactive voice response system (IVRS). Once a study drug kit number has been assigned to a subject, it cannot be reassigned to any other subject. 9.4 Study Medication Accountability The Investigator/pharmacist must maintain accurate records of the disposition of all study drugs received from the sponsor, issued to the subject or directly administered to the subject (including date and time), and any drug accidentally destroyed. The sponsor will supply a specific drug- accountability form. At the end of the study, information describing study drug supplies (e.g., lot numbers) and disposition of supplies for each subject must be provided, signed by the Investigator or designee, and collected by the study monitor. If any errors or irregularities in any shipment of study medication to the site are discovered at any time, the Project Manager must be contacted immediately. At the end of the study, all medication not dispensed or administered and packaging materials will be collected with supervision of the monitor and returned to the sponsor or destroyed on site as dictated by the appropriate Standard Operating Procedure at the participating institution. 9.5 Blinding/Unblinding of Treatments This is a double-blind study. The treatment group assignment will not be known by the study subjects, the investigator, the clinical staff, the CRO or Sponsor staff during the conduct of the 290 290 BCX1812-311 (V2.0: 05-October-2007) Page 30 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL study. Section 11.2.4 provides information regarding the process for unblinding the treatment assignment, if necessary, in the event of an SAE. 9.6 Prior and Concomitant Therapies All medications, by any route of administration, used during this study must be documented on the Case Report Form (CRF). Prescription as well as non-prescription medications should be recorded. Medication used for the treatment of influenza-related symptoms will be captured by the subject in the diary card provided by BioCryst. 9.7 Overdose and Toxicity Management To date there is no experience with overdose of intramuscular or intravenous peramivir. If overdose occurs, subjects should receive indicated supportive therapy and evaluation of hematologic and clinical chemistry laboratory tests should be conducted. The effect of hemodialysis on elimination of peramivir is unknown. 9.8 Dose Interruption As this is a study of a single injection of peramivir or placebo, guidelines for treatment interruption for drug related SAEs or toxicities are not applicable. 10 STUDY CONDUCT A study schedule of evaluations is presented in Figure 1. A detailed list of the evaluations an visits is also provided in the following sections. 10.1 Evaluations All subjects enrolled in this study will undergo the following evaluations: 10.1.1 Medical History Medical history, influenza vaccination status within the previous 12 months and demographic data (including smoking behavior) will be recorded at Screening/Baseline. 10.1.2 Rapid Antigen Test for Influenza At Screening/Baseline, a commercially available, rapid antigen test (RAT) for influenza A and B will be performed on an adequate specimen collected by swabbing the anterior nose in accordance with the RAT manufacturer’ instructions. A negative initial RAT should be repeated within one hour. Refer to the Study Manual for instructions regarding the use of the RAT kits provided for this study. Sites may use the kits provided by the Sponsor or any other commercially approved RAT available at their site to document a confirmed influenza infection. 291 291 BCX1812-311 (V2.0: 05-October-2007) Page 31 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.3 Physical Examination and Influenza-related Complications Assessments The Investigator will perform a physical examination at Screening/Baseline. Subject’s height and weight, and BMI will be recorded at Screening/Baseline in the subjects CRF. Study personnel will be provided with an influenza-related complications (IRC) checklist in the CRF to evaluate the subject for the presence of clinical signs and/or symptoms of the following influenza-related complications: sinusitis, otitis, bronchitis and pneumonia. Note that subjects with clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis, and/or pneumonia at screening are not eligible for enrollment in this study (See Section 8.1.2: exclusion criteria number 8). A targeted physical examination will be conducted at each visit to record the presence/absence of influenza related complications (IRC). If the investigator determines that the subject experiences (or is presumed to experience) an IRC as noted above, he/she will record that assessment on the IRC CRF page and any medication used to treat the condition will be recorded on the concomitant medication page. The investigator will promptly provide appropriate treatment for any suspected or proven IRC. Such information describing IRC signs and/or symptoms should not be reported as adverse events. Any injection site reactions noted will be recorded in the CRFs as adverse events. 10.1.4 Vital Signs Vital signs evaluations will include blood pressure, pulse rate, and respiration rate. The investigator will record oral body temperature at baseline. Thereafter the subject will record oral temperature twice daily in the study diary card. Vital signs will be measured at Screening/Baseline, pre-dose, and at 15 minutes following the study drug injection on Day 1, then once daily on Days 3, 5, 9, and 14. 10.1.5 Electrocardiogram Measurements A 12-lead electrocardiogram (ECG) will be obtained at Screening/Baseline. The principal investigator will be responsible for interpretation of the Screening ECG. This interpretation may be performed by the investigator or he/she may delegate this action to another physician and the investigator will acknowledge the interpretation. If this baseline ECG is interpreted as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal but does not meet the exclusionary criteria, the subject may be enrolled unless other exclusion criteria apply. The principal investigator is responsible to ensure that such an enrolled subject be informed of the nature of the abnormal ECG and that any medically indicated repeat ECG examinations and/or referral of the subject for further evaluation is made either during subject's participation in the study or immediately after the subject's discharge from the study. 10.1.6 Clinical Laboratories Clinical chemistry profiles will include a Chemistry 20 panel (includes sodium, potassium, chloride, total CO2 [bicarbonate], creatinine, glucose, urea nitrogen, albumin, total calcium, total magnesium, phosphorus, alkaline phosphatase, alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin, direct bilirubin, lactate dehydrogenase [LDH], total protein, total creatine kinase, and uric acid). 292 292 BCX1812-311 (V2.0: 05-October-2007) Page 32 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Hematology will include complete blood count (CBC) with differential. Urinalysis will include dipstick tests for protein, glucose, ketones, blood, urobilinogen, nitrite, pH, and specific gravity and microscopic evaluation for RBCs and WBCs. Clinical laboratory studies (clinical chemistries, hematology, and urinalysis) will be completed at Screening/Baseline, and on Days 3, 5 and 14. 10.1.7 Urine Pregnancy Test Females of childbearing potential will be evaluated for pregnancy at Screening/Baseline and Day 14 using a urine pregnancy test. 10.1.8 Serology for Influenza Paired blood samples for determination of antibody to influenza A and B (serology) will be obtained with the clinical laboratory tests at Screening/Enrollment and at Day 14. These specimens will be stored at the central laboratory and will be analyzed if needed to confirm the diagnosis of influenza. 10.1.9 Samples for Virologic Laboratory Assessments An adequate specimen will be collected by swabbing the anterior nose (bilateral) and posterior pharynx for virologic laboratory assessments including culture for the isolation of influenza virus and/or quantitative PCR assay at Screening/Baseline, and at Days 3, 5, and 9. Refer to the Laboratory Manual for instructions regarding the processing and shipment of these specimens. 10.1.10 Subject Self Assessments Subject self assessments will be performed beginning pre-dose on Day 1 and recorded in the subject’s Study Diary including the following: • Oral temperature measurements with an electronic thermometer (provided by the Sponsor for the study) every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol, provided) or other anti-pyretic medications. The times of each temperature determination will be recorded in the Study Diary. The baseline temperature will be recorded at the screening/Day 1 visit prior to dosing, regardless of whether the subject had recently taken an anti-pyretic; the time of anti-pyretic use pre- treatment will be recorded in the CRF, if applicable. • Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [aches and pains], headache, feverishness, and fatigue) on a 4-point severity scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily, beginning pre-dose on Day 1 and through Day 9, then once daily through Day 14. • Assessment of the subject’s time lost from work or usual activities and productivity compared to normal using a 0-10 visual analogue scale once daily through Day 14. The subject’s diary card will be reviewed by study staff at each visit for completion of the record of all required items, with particular emphasis on alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the recurrence of at least one respiratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours and the presence of fever 293 293 BCX1812-311 (V2.0: 05-October-2007) Page 33 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Study staff will not attempt to ask subjects to retrospectively complete missing diary card data for any scheduled assessments that have not been completed prior to the clinic visit. Study staff should, however, remind the subject to complete the diary card at all scheduled times. 10.1.11 Concomitant Medications All concomitant medications used during this study, with the exception of those medications taken for symptomatic relief of influenza symptoms, which will be recorded by the subject in their diary card, must be documented on the Case Report Form (CRF). 10.1.12 Adverse Events AEs will be assessed from the time of administration of study medication through the final study visit. 10.1.13 Pharmacokinetic Exposure Samples All subjects will have two pharmacokinetic (PK) samples drawn to assess peramivir drug levels. The first PK sample will be drawn on day 1 between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be drawn at the day 3 visit in all subjects. The sample will be drawn at the same time as the blood draw is completed for clinical laboratory investigations. The 30-60 minute sample (treatment day 1) and the day 3 PK sample will be analyzed for plasma concentrations of peramivir (ng/mL) and evaluated in a population exposure response analysis. At selected sites a separate sub-study will also be conducted to collect additional PK samples for the purpose of conducting an exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Data from these two PK samples in all subjects will be combined with data from the PK sub-study (BCX1812-311PK) to perform a population based exposure-response analysis. This analysis will be described as part of the sub-study analysis plan. All PK samples will be processed at a central bioanalytical laboratory. Refer to the instructions provided regarding the processing and shipment of these PK samples. 10.2 Screening Period 10.2.1 Informed Consent The nature and purpose of the study and the expectations of a participating subject will be described to potential study subjects, their questions will be answered, and the subjects will then be asked to sign an informed consent document. Study subjects will then undergo the screening evaluation as noted in Section 10.2.2 10.2.2 Screening/Baseline Evaluation and Enrollment Screening/baseline evaluation may be conducted in the investigator’s office or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and qualified staff. Clinical laboratory assessments performed at Screening are for the purpose of establishing a 294 294 BCX1812-311 (V2.0: 05-October-2007) Page 34 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL baseline. Subjects may be enrolled and receive treatment with study drug prior to receiving results of the laboratory assessments (with the exception of urine pregnancy test result, which must be known). Eligible subjects will be enrolled and randomized to blinded study treatment. The randomization will be stratified by BMI: Normal-Overweight (BMI ≤ 29.9 kg/m2) and Obese (BMI ≥ 30.0 kg/m2). The Investigator will prepare a request for blinded study drug assignment which includes the subject’s screening number. The Investigator or designee at the clinical study center will contact the central randomization Interactive Voice System (IVRS call center). The IVRS call center will advise the study center of the investigational study drug kit number that is assigned to that subject at enrollment. Subjects that are determined to be ineligible will be advised accordingly, and the reason for ineligibility will be discussed. If desired by the subject the reason for ineligibility may be provided and/or discussed with their health-care provider by the Investigator or designee. Ineligible subjects who have been screened for the study will also be entered on the IVRS. For such subjects, the screening number assigned, subject’s date of birth and a reason for ineligibility will be entered on to the IVRS. All ineligible subjects must be entered onto the IVRS within 24 hours of screening, to assist with surveillance analysis during the course of the study. 10.3 Treatment Period—Study Day 1 Day 1 represents the only day of study drug dosing. Study drug administration should occur as soon as possible following informed consent, screening and randomization. Therefore, it is expected that the date of Screening/ Baseline and Day 1 will usually be the same date. 10.3.1 Pre-dose Evaluations-Study Day 1 Following an explanation of the Subject Self Assessment measures (Section 10.1.11), the subject shall complete the record of these assessments in their Study Diary prior to dosing. The subject will be counseled regarding the expectations for recording these assessments through Day 14. Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) and a 12 lead ECG will be obtained prior to dosing. 10.3.2 Post-dose Evaluations-Study Day 1 The blinded study drug will be administered (hour 0) as bilateral intramuscular injections within a period of ≤ 10 minutes. The calendar date and 24-hour clock time of the first and second injections will be recorded. The gluteal site of injection and the syringe needle length are also to be recorded in the subjects CRF. Sites are instructed to follow procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, provided in the study drug administration manual. The following evaluations will be performed post-dose on Study Day 1: • Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) 15 minutes following the second intramuscular injection of blinded study drug; record the exact 24-hour clock time of the vital sign measurements in the subjects CRF. 295 295 BCX1812-311 (V2.0: 05-October-2007) Page 35 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL • Draw a PK sample between 30 and 60 minutes following the second intramuscular injection of blinded study drug; record the exact 24-hour clock time of the blood draw. • Record any concomitant medications. • Record any AEs. 10.4 Post-Treatment Assessment Period 10.4.1 Days 2, 3, 5, 9 and 14 Study evaluations will be performed on Days 2, 3, 5, 9 and 14 in accordance with the schedule of evaluations (Figure 1). Subjects with persistent moderate or severe influenza symptoms at day 14 will also complete a Day 21 visit, and if required a Day 28 visit. Visits may be conducted in the investigator’s office or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and qualified staff. Study staff will attempt to contact the subjects on Day 2 by telephone to confirm their compliance with completion of the Subject Self Assessments, to note any concomitant medications and adverse events. Any adverse events reported by the subject during this telephone contact will be recorded on the adverse event form and verified during the visit on day 3. At each visit it is important that the subject’s Study Diary record be reviewed for completion of daily Subject Self Assessments. The subjects should be counseled as necessary regarding self assessments and Study Diary record requirements. The subject’s diary card will be reviewed by study staff for alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the recurrence of at least one respiratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours and the presence of fever (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Day 3: The second PK sample for all subjects will be obtained on Day 3 at the same time as the clinical laboratory blood specimen is obtained. The exact 24-hour clock time of the blood draw will be recorded in the subjects CRF. Day 14: If a subject has one or more persistent or recurrent symptoms of influenza (of the seven symptoms assessed) of either moderate or severe intensity at the Day 14 visit then the subject must be evaluated in further follow-up visits, at day 21 (± 3 days), and if required at day 28 (± 3 days) If a subject reports moderate or severe influenza symptoms then the investigator will record the intensity of each of the influenza symptoms on a visit specific CRF page at the day 21 and day 28 visits. After day 14 the subject will not record symptoms in a diary. Day 21 (if applicable): The day 21 visit is to be completed only if the subject reports symptoms of influenza of moderate or severe intensity at day 14. The investigator will make a clinical judgment as to the appropriate medical course of action for such subjects at the Day 21 visit and such action(s) will be recorded 296 296 BCX1812-311 (V2.0: 05-October-2007) Page 36 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL on the Day 21 CRF page. The investigator will recall the subject for a further study visit at day 28 (± 3 days) if moderate or severe symptom(s) of influenza persist at Day 21. Day 28 (if applicable): The day 28 visit is to be completed only if the subject reports symptoms of influenza of moderate or severe intensity at day 21. The investigator will make a clinical judgment as to the appropriate medical course of action for such subjects at this visit and such action(s) will be recorded on the Day 28 CRF page. No further follow-up visits beyond day 28 are to be formally scheduled unless in the clinical judgment of the investigator further follow-up is required. The investigator will use his/her clinical judgment to manage the subject, referring the subject, if appropriate, for further medical care. 10.4.2 Adverse Events Reported at Post-treatment Visits In this study, symptoms of influenza will be considered separately from adverse events reported during the post-treatment period. Accordingly, adverse events that have onset in the post- treatment period will be assessed and followed as specified in 11.2. Specifically, the investigator should attempt to follow all unresolved AEs and/or SAEs observed during the study until they are resolved, or are judged medically stable, or are otherwise medically explained. 297 297 BCX1812-311 (V2.0: 05-October-2007) Page 37 Figure 1 Study Measurements and Visit Schedule Treatment Period Assessment Day End of Study Early Withdrawal Assessments Screening 1 (Baseline) Day 11 Day 22 Day 3 Day 5 (±1 day) Day 9 (±3 day) Day 14 (±3 day) 8 Informed Consent X Rapid Antigen test for Influenza A & B X Medical History/Physical Exam X Influenza-related complications checklist3 X X X X X Inclusion/Exclusion X Clinical Chemistries4 X X X X Hematology4 X X X X Exposure Pharmacokinetic Sample X X4 Serology (serum) Sample X X Urinalysis4 X X X X Urine Pregnancy Test X X Vital Signs5 X X X X X X ECG6 X Sample (nasopharyngeal swab) for Influenza Virus Culture/ PCR assay and for resistance studies X X X X Study Drug Administration X Subject Diary Review7 X X X X X X Concomitant Medications X X X X X X X Adverse Events X X X X X X Study Measurements and Visit Schedule Figure Legend on Next Page BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 298 298 BCX1812-311 (V2.0: 05-October-2007) Page 38 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Study Measurements and Visit Schedule Figure Legend 1 It is expected that the date of Screening and Day 1 (date of administration of study drug) will be the same. Visits at Screening and on subsequent study days may occur in subject’s home by the investigator (all visits) or appropriately trained study center staff (Day 3, 5, 9 visits). 2 Day 2 will be a telephone contact with the subject to ensure compliance with diary card completion, concomitant medication and adverse event review. 3 A targeted physical examination will be conducted at each visit to record the presence/absence of influenza related complications. 4 Clinical laboratory assessments performed at Screening are for the purpose of establishing a baseline. Subject may be enrolled and begin treatment with study drug prior to receiving results. A PK sample will be drawn 30-60 minutes following the second treatment administration injection. On Day 3 an extra tube will be included with the safety blood sample to collect the second PK sample for evaluation of peramivir concentrations. 5 Vital sign measures will include blood pressure, pulse rate and respiration rate. Vital signs will be recorded at Screening, pre-dose and at 15 min following the study drug administration on Day 1, then once on remaining days as stipulated. The investigator will record oral temperature at baseline. Thereafter the subject will report oral temperature measurements twice daily in the Study Diary 6 If the baseline ECG is interpreted by the conducting physician as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal and does not meet the exclusionary criteria (e.g. acute ischemia, medically significant dysrhythmia) then this subject may be enrolled If the conditions highlighted in section 10.1.5 are met for the subject. 7 Subjects record symptom assessment in Study Diary, twice daily, beginning pre-dose on Day 1 through Day 9, then once daily through Day 14. Subjects record time lost from work or usual activities and rating of productivity compared to normal once daily through Day 14. Subjects record oral temperature twice daily throughout as well as all concomitant medication and adverse events. 8 For any subject with unresolved moderate or severe intensity influenza symptoms a follow up assessment will be scheduled at Day 21 (± 3 days) and Day 28 (± 3 days) if required (See Section 10.4.1). 299 299 BCX1812-311 (V2.0: 05-October-2007) Page 39 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11 ADVERSE EVENT MANAGEMENT 11.1 Definitions 11.1.1 Adverse Event An AE is any untoward medical occurrence in a clinical study subject. No causal relationship with the study drug or with the clinical study itself is implied. An AE may be an unfavorable and unintended sign, symptom, syndrome, or illness that develops or worsens during the clinical study. Clinically relevant abnormal results of diagnostic procedures including abnormal laboratory findings (e.g., requiring unscheduled diagnostic procedures or treatment measures, or resulting in withdrawal from the study) are considered to be AEs. AEs may be designated as “nonserious” or “serious” (see Section 11.1.2). Surgical procedures are not AEs but may constitute therapeutic measures for conditions that require surgery. The condition for which the surgery is required is an AE, if it occurs or is detected during the study period. Planned surgical measures permitted by the clinical study protocol and the conditions(s) leading to these measures are not AEs, if the condition(s) was (were) known before the start of study treatment. In the latter case the condition should be reported as medical history. Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [aches and pains], headache, feverishness, and fatigue) will be documented in a subject’s study diary and analyzed as a measure of efficacy of the study treatment. These symptoms will not be reported as AEs unless the symptom(s) worsen to the extent that the outcome fulfils the definition of an SAE, which then must be recorded as such (see Section 11.1.2). Likewise, a RAT for influenza is required at screening in order to determine eligibility for the study, and therefore a positive RAT is not considered an AE. 11.1.2 Serious Adverse Event A SAE is an adverse event that results in any of the following outcomes: • Death • Is life-threatening (subject is at immediate risk of death at the time of the event; it does not refer to an event that hypothetically might have caused death if it were more severe) • Requires in-subject hospitalization (formal admission to a hospital for medical reasons) or prolongation of existing hospitalization • Results in persistent or significant disability/incapacity (i.e., there is a substantial disruption of a person’s ability to carry out normal life functions) • Is a congenital anomaly/birth defect • Is an important medical event Important medical events that may not result in death, are not life-threatening, or do not require hospitalization may be considered an SAE when, based upon appropriate medical judgment, they may jeopardize the subject or may require medical or surgical intervention to prevent one of the 300 300 BCX1812-311 (V2.0: 05-October-2007) Page 40 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL outcomes listed in this definition. Examples of such events include allergic bronchospasm requiring intensive treatment in an emergency room or at home, blood dyscrasias or convulsions that do not result in subject hospitalization, or the development of drug dependency or drug abuse. In addition Suspected Unexpected Serious Adverse Reactions (SUSAR) may also be reported to competent authorities where this type of reporting is required (e.g. European Union Directives). See section 11.2.3. 11.2 Method, Frequency, and Time Period for Detecting Adverse Events and Reporting Serious Adverse Events Reports of AEs are to be collected from the time of study drug administration through the follow-up period ending on Day 14. The Investigator or designee must completely and promptly record each AE on the appropriate CRF. The Investigator should attempt, if possible, to establish a diagnosis based on the presenting signs and symptoms. In such cases, the diagnosis should be documented as the AE and not the individual sign/symptom. If a clear diagnosis cannot be established, each sign and symptom must be recorded individually. The Investigator should attempt to follow all unresolved AEs and/or SAEs observed during the study until they are resolved, or are judged medically stable, or are otherwise medically explained. 11.2.1 Definition of Severity All AEs will be assessed (graded) for severity and classified into one of four clearly defined categories as follows: • Mild: (Grade 1): Transient or mild symptoms; no limitation in activity; no intervention required. The AE does not interfere with the participant’s normal functioning level. It may be an annoyance. • Moderate: (Grade 2): Symptom results in mild to moderate limitation in activity; no or minimal intervention required. The AE produces some impairment of functioning, but it is not hazardous to health. It is uncomfortable or an embarrassment. • Severe: (Grade 3): Symptom results in significant limitation in activity; medical intervention may be required. The AE produces significant impairment of functioning or incapacitation. • Life-threatening: (Grade 4): Extreme limitation in activity, significant assistance required; significant medical intervention or therapy required; hospitalization. 301 301 BCX1812-311 (V2.0: 05-October-2007) Page 41 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11.2.2 Definition of Relationship to Study Drug The blinded Principal Investigator must review each AE and make the determination of relationship to study drug using the following guidelines: Not Related: The event can be readily explained by other factors such as the subject’s underlying medical condition, concomitant therapy, or accident, and no temporal relationship exists between the study drug and the event. Unlikely: The event does not follow a reasonable temporal sequence from drug administration and is readily explained by the subject’s clinical state or by other modes of therapy administered to the subject. Possibly Related: There is some temporal relationship between the event and the administration of the study drug and the event is unlikely to be explained by the subject’s medical condition, other therapies, or accident. Probably Related: The event follows a reasonable temporal sequence from drug administration, abates upon discontinuation of the drug, and cannot be reasonably explained by the known characteristics of the subject’s clinical state. Definitely Related: The event follows a reasonable temporal sequence from administration of the medication, follows a known or suspected response pattern to the medication, is confirmed by improvement upon stopping the medication (dechallenge), and reappears upon repeated exposure (rechallenge, if rechallenge is medically appropriate). 11.2.3 Reporting Serious Adverse Events Any SAE / SUSAR (Suspected Unexpected Serious Adverse Reaction) must be reported to BioCryst or its designee within 24 hours of the Investigator’s recognition of the SAE by first notifying the Medical Monitor at the number listed below: Telephone: Europe: +44 1628 548000; North America: 1-888-724-4908 Facsimile: Europe: +44 1628 540028; North America: 1-888-887-8097 or 1-609-734-9208 In addition to the telephone numbers listed above, local country-specific toll free numbers may be provided within the study reference manual. The site is required to fax a completed SAE / SUSAR Report Form (provided as a separate report form) within 24 hours. All additional follow-up evaluations of the SAE / SUSAR must be reported and sent by facsimile to BioCryst or its designee as soon as they are available. The Principal Investigator or designee at each site is responsible for submitting the IND safety report (initial and follow-up) or other safety information (e.g., revised Investigator’s Brochure) to the Institutional Review Board/Independent Ethics Committee (IRB/IEC) and for retaining a copy in their files. 302 302 BCX1812-311 (V2.0: 05-October-2007) Page 42 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL If the Investigator becomes aware of any SAE / SUSAR occurring within 30 days after a subject has completed or withdrawn from the study, he or she should notify BioCryst or its designee. Any SAEs / SUSARs considered possibly related to treatment will be reported to the FDA and other Regulatory Competent Authorities as applicable via the MedWatch / CIOMS reporting system in accordance with FDA and other applicable regulations. However, the Investigator is not obligated to actively seek reports of AEs in former study participants. While pregnancy is not considered an AE, all cases of fetal drug exposure via parent as study participant (see Section 4.4) are to be reported immediately to BioCryst or its designee. Information related to the pregnancy must be given on a “Pregnancy Confirmation and Outcome” form that will be provided by the Sponsor or its designee. 11.2.4 Emergency Procedures In the event of an SAE / SUSAR, the Principal Investigator may request the unblinding of the treatment assignment for the subject affected. If time allows (i.e., if appropriate treatment for the SAE is not impeded), the Principal Investigator will first consult with the Medical Monitor regarding the need to unblind the treatment assignment for the subject. At all times, the clinical well-being of any subject outweighs the need to consult with the Medical Monitor. The Principal Investigator may contact the IVRS central randomization center and request the unblinding of the treatment assignment that corresponds to the affected subject. The IVRS center will record the name of the Investigator making the request, the date and time of the request, the subject number and date of birth. The Sponsor will be informed within 24 hours if unblinding occurred. 12 STATISTICAL METHODS Descriptive statistical methods will be used to summarize the data from this study, with hypothesis testing performed for the primary and other selected efficacy endpoints. Unless stated otherwise, the term “descriptive statistics” refers to number of subjects (n), mean, median, standard deviation (SD), minimum, and maximum for continuous data and frequencies and percentages for categorical data. The term “treatment group” refers to randomized treatment assignment: peramivir 150 mg, peramivir 300 mg, or placebo. All data collected during the study will be included in data listings. Unless otherwise noted, the data will be sorted first by treatment assignment, subject number, and then by date within each subject number. Unless specified otherwise, all statistical testing will be two-sided and will be performed using a significance (alpha) level of 0.05. All statistical analyses will be conducted with the SAS® System, version 9.1.3 or higher. 12.1 Data Collection Methods The data will be recorded on the CRF approved by BioCryst. The Investigator must submit a completed CRF for each subject who signs an informed consent form (ICF), regardless of duration. All documentation supporting the CRF data, such as laboratory or hospital records, must be readily available to verify entries in the CRF. Documents (including laboratory reports, hospital records subsequent to SAEs, etc.) transmitted 303 303 BCX1812-311 (V2.0: 05-October-2007) Page 43 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL to BioCryst should not carry the subject’s name. This will help to ensure subject confidentiality. 12.2 Statistical Analysis Plan A statistical analysis plan (SAP) will be created and approved prior to the review of any data. This document will provide a more technical and detailed description of the proposed data analysis methods and procedures. 12.3 Study Hypothesis The primary hypothesis for evaluating the primary objective may be stated as follows: The null hypothesis (H0) is that the time to alleviation of influenza symptoms is the same for subjects treated with placebo and for subjects treated with peramivir 150mg (H01) or peramivir 300mg (H02). The alternative hypothesis (H1) is that subjects treated with peramivir 150mg (H11) or peramivir 300mg (H12) have an improvement in time to alleviation of influenza symptoms over those treated with placebo. 12.4 Sample Size Estimates A total of 750 evaluable subjects randomized in a 2:2:1 (300 subjects treated with peramivir 150mg: 300 subjects treated with peramivir 300 mg: 150 subjects treated with placebo) are estimated for this phase 3 study. Because results of clinic-based RAT tests may not precisely indicate presence of influenza infection, it is expected that at least 850 subjects will be randomized to treatment to ensure that 750 evaluable subjects are treated. From preliminary results of a phase 2 study evaluating peramivir treatment of uncomplicated influenza, it is expected that the median time to alleviation of symptoms will be 137.0 hours (95% CI: 115.9, 165.8) for subjects receiving placebo treatment. Additionally, it is expected that the median time to alleviation for the 150 mg dose peramivir arm will be reduced by 30% compared to placebo (Table 5) yielding a hazard ratio of 0.70. 304 304 BCX1812-311 (V2.0: 05-October-2007) Page 44 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 5 Median time to alleviation of symptoms (30% reduction, 0.70 hazard ratio). Median Time To Alleviation of Symptoms (Hours) Placebo Peramivir 150mg Difference (hours) 145.0 101.5 43.5 140.0 98.0 42.0 135.0 94.5 40.5 130.0 91.0 39.0 125.0 87.5 37.5 120.0 84.0 36.0 115.0 80.5 34.5 110.0 77.0 33.0 105.0 73.5 31.5 100.0 70.0 30.0 Using these assumptions, a sample size of 300 evaluable subjects per active treatment group and 150 evaluable subjects in the placebo group (a total of 750 evaluable subjects) is sufficient to provide at least 90% power to detect a hazard ratio of 0.70 using a log-rank statistic and α = 0.025 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). 12.5 Analysis Populations The populations for analysis will include the intent-to-treat (ITT), intent-to-treat infected (ITTI), per-protocol infected (PPI), and safety populations. Additional analysis populations may be defined to evaluate study results. Any additional analysis populations will be defined in the SAP. Intent-To-Treat Population: The ITT population will include all subjects who are randomized. Subjects will be analyzed in the treatment group to which they were randomized. The ITT population will be used for analyses of accountability and demographics. Intent-To-Treat Infected Population: The ITTI population will include all subjects who are randomized, received study drug, and have confirmed influenza by culture or PCR. Subjects will be analyzed according to the treatment randomized. If a discrepancy is noted in the final database for any subject, such that the drug differs from the randomized treatment assignment, efficacy analyses may be repeated with the subjects analyzed according to the treatment received. The ITTI population will be used for primary analyses of efficacy. Per-Protocol Infected: The PPI population includes all subjects in the ITTI population who receive an adequate intramuscular injection. The definition of an adequate intramuscular injection will be further described in the SAP. The PPI population will be used as supportive of the primary analyses for efficacy completed with the ITTI population. Safety Population: The safety population will include all subjects who received study drug. Subjects will be analyzed according to the treatment received. This population will be used for all safety analyses. 305 305 BCX1812-311 (V2.0: 05-October-2007) Page 45 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.6 Interim and End of Study Analyses Interim Analysis An independent DMC will review safety data on an ongoing basis. Safety analyses will be presented in a manner consistent with the presentations intended for the final analysis. End of Study Analysis A final analysis is planned after the last subject completes or discontinues the study, and the resulting clinical database has been cleaned, quality checked, and locked. 12.7 Efficacy Analyses 12.7.1 Primary Efficacy Endpoint The primary efficacy endpoint is the time to alleviation of symptoms, defined as the time from injection of study drug to the start of the time period when a subject has Alleviation of Symptoms. A subject has Alleviation of Symptoms if all of the seven symptoms of influenza (nasal congestion, sore throat, cough, aches and pains, fatigue (tiredness), headache, feeling feverish) assessed on his/her subject diary are either absent or are present at no more than mild severity level and at this status for at least 21.5 hours (24 hours - 10%). Descriptive statistics for the primary efficacy endpoint will be tabulated by treatment group. Alleviation of symptoms will be determined by assessment of symptoms as reported on each subject’s diary card. Time to alleviation of symptoms will be summarized overall and for individual symptoms for each treatment group. Overall treatment differences will be assessed using a Cox Regression model with effects for BMI at screening, influenza type by PCR, treatment group, and influenza season at randomization (if necessary). Subjects who do not experience alleviation of symptoms will be censored at the date of their last non-missing post- baseline assessment. Pairwise differences in time to alleviation of symptoms among the treatment groups will be evaluated using contrast statements from the final Cox model. In order to maintain the overall type I error in the presence of the planned comparisons between the two peramivir treatments and placebo, a Bonferroni correction will be applied to the primary efficacy endpoint analysis. P-values for the planned comparisons of each peramivir arm to placebo will be adjusted via a Bonferroni correction (i.e., if the unadjusted p-value for an active comparison versus placebo, p, is less than 0.05, then pa=p*number of planned comparisons=p*2; otherwise, pa=p). Superiority of peramivir to placebo will be established if the adjusted p-value is less than or equal to 0.05. 12.7.2 Secondary Efficacy Endpoints All secondary endpoints will be summarized using descriptive statistics by treatment group, and study day/time, if appropriate. Statistical comparisons for each endpoint will be constructed without adjustment for multiple endpoints. The reduction in viral shedding will be assessed as the change in viral titers defined as the time- weighted change from baseline in log10 tissue culture infective dose50 (TCID50/mL) and will be 306 306 BCX1812-311 (V2.0: 05-October-2007) Page 46 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL summarized for each treatment group. The time-weighted average change from baseline will be calculated on a by-subject basis through Day 9 using the trapezoidal rule with all available post- baseline on-treatment data (data after initiation of study treatment) minus the baseline value. Specifically, the time-weighted area under the curve for time a (ta) to time b (tb) is given by the formula ) ( ) ( b a b a t t t t AUC TWAUC − − = , where ∑ − = − + − + = − 1 1 1 2 ) )( ( ) ( b a i i i i i b a t t y y t t AUC and ti represents the date of the ith viral titer assessment and yi represents the log10 value of the ith viral titer assessment. If there is a baseline value and only one follow-up value, yi then the time-weighted change from baseline is defined as the difference between yi and baseline. If there is a baseline value and no follow-up value, the subject is excluded from analysis. The differences between each of the peramivir treatment groups and placebo will be evaluated using a van Elteren Test adjusting for BMI at screening, influenza type by PCR, and influenza season at randomization (if necessary). Analyses of the PCR results will be analyzed in a similar manner. Subject’s oral temperature will be summarized by study visit and treatment group. Differences between the treatment groups will be assessed using the Wilcoxon Rank Sum Test controlling for BMI at screening, influenza type by PCR, and influenza season at randomization (if necessary). A subject has Resolution of Fever if he/she has a temperature < 37.2°C (99.0°F) and no antipyretic medications have been taken for at least 12 hours. The time to resolution of fever will be estimated using the method of Kaplan-Meier using temperature and symptom relief medication information obtained from the subject diary data. Difference between the treatment groups will be assessed using the log rank statistic controlling for BMI at screening, influenza type by PCR, and influenza season at randomization (if necessary). Subjects who do not have resolution of fever will be censored at the time of their last non-missing post-baseline temperature assessment. The number and percentage of subjects experiencing influenza related complications will be summarized by complication preferred term and treatment group. The difference between the treatment groups will be assessed a logistic regression model with factors for treatment group, BMI at screening, influenza type by PCR, and influenza season at randomization (if necessary). Pairwise differences between the treatment groups will be evaluated using contrasts from the final logistic regression model. 12.7.3 Exploratory Endpoint The MRU, MRU-related direct costs, and indirect costs attributable to days missed of work and work productivity and/or performance losses will be summarized by treatment group and BMI. Methods for describing differences between treatment groups will be presented in the SAP. Genotypic (including Hemagglutinin and Neuraminidase), phenotypic, viral culture and PCR data will be listed for each subject. These listings will be constructed in a manner consistent with the FDA June 2006 Guidance Document: “Guidance for Submitting Influenza Resistance Data”.18 Additionally, the number and percentage of genotypic changes from wild-type amino acid will be summarized separately for treatment group, protein type, and study visit. 307 307 BCX1812-311 (V2.0: 05-October-2007) Page 47 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.8 Safety Analyses AEs will be mapped to a MedDRA-preferred term and system organ classification. The occurrence of TEAEs will be summarized by treatment group using MedDRA-preferred terms, system organ classifications, and severity. If a subject experiences multiple events that map to a single preferred term, the greatest severity and strongest Investigator assessment of relation to study drug will be assigned to the preferred term for the appropriate summaries. All AEs will be listed for individual subjects showing both verbatim and preferred terms. Separate summaries of treatment-emergent SAEs and AEs related to study drug will be generated. Descriptive summaries of vital signs and clinical laboratory results will be presented by study visit. Laboratory abnormalities will be graded according to the DAIDS Table for Grading Adverse Events for Adults and Pediatrics (Publish Date: December 2004). The number and percentage of subjects experiencing treatment-emergent graded toxicities will be summarized by treatment group. Laboratory toxicity shifts from baseline to Day 3, Day 5, and Day 14 will be summarized by treatment group. Abnormal physical examination findings will be presented by treatment group. The number and percent of subjects experiencing each abnormal physical examination finding will be included. Concomitant medications will be coded using the WHO dictionary. These data will be summarized by treatment group. Subject disposition will be presented for all subjects. The number of subjects who completed the study and discontinued from the study will be provided. The reasons for early discontinuation also will be presented. 12.9 Sub-Study and Pharmacokinetic Analysis A sub-study to collect pharmacokinetic samples in up to 60 peramivir treated subjects to examine exposure response will be conducted at selected sites. The data from the sub-study will be combined with the two PK samples (collected on all subjects at 30-60 minutes following administration of study drug and on study day 3) to perform a population exposure-response analysis. All analyses related to exposure-response will be completed as part of the sub-study. All statistical methods will be outlined as part of the sub-study protocol and exposure-response analysis plan. All sub-study analyses, and exposure-response analyses from PK samples obtained in this study and a companion study BCX1812-312, will be reported in a separate sub-study report. 12.10 General Issues for Statistical Analysis 12.10.1 Multiple Comparisons and Multiplicity In order to maintain the overall type I error in the presence of the planned comparisons between the two peramivir treatments and placebo, a Bonferroni correction will be applied to the primary efficacy endpoint analysis. No other adjustments for multiple comparisons are planned. 308 308 BCX1812-311 (V2.0: 05-October-2007) Page 48 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.10.2 Covariates Primary and secondary efficacy analyses will be adjusted for BMI at screening, influenza type by PCR, and influenza season at randomization (if necessary). 12.10.3 Planned Sub-Groups The primary efficacy endpoint will be summarized separately by BMI, influenza season at randomization (if necessary), and by viral subtype by PCR using descriptive statistics by treatment group and study day, if appropriate. No formal statistical testing will be utilized. Additional analyses may be performed by country, if necessary, for submission to local regulatory authorities. 12.10.4 Missing Data Every effort will be made to obtain required data at each scheduled evaluation from all subjects who have been randomized. No attempt will be made retrospectively to obtain missing subject reported data (including influenza symptom severity assessments, temperature, ability to perform usual activities, missed days of work and impact of influenza on subject’s work performance and/or productivity) that has not been completed by the subject at the time of return of the subject diary to the investigative site. In situations where it is not possible to obtain all data, it may be necessary to impute missing data. In assessing the primary efficacy endpoint, for subjects who withdraw or who do not experience alleviation of symptoms, missing data will be censored using the date of subject’s last non- missing assessment of influenza symptoms. Missing assessments of influenza symptoms conservatively will be imputed as having severity above absent or mild (as failures). For the subject diary data, the following data conventions will be utilized. Missing diary completion will be imputed as 11:59 for diary entries designated as morning and 23:59 for evening and daily reported values. Entries with values exceeding the 24-hour clock will be set to 23:59 of the day recorded. Select exploratory sensitivity analyses may be conducted to ascertain the effect, if any, of these methods. These sensitivity analyses are further described in the SAP. Secondary efficacy endpoints with time to event data will be censored using the date of subject’s last non- missing assessment of the given endpoint. 13 STUDY ADMINISTRATION 13.1 Regulatory and Ethical Considerations 13.1.1 Regulatory Authority Approvals This study will be conducted in compliance with the protocol; GCPs, including International Conference on Harmonization (ICH) of Technical Requirements for Registration of Pharmaceuticals for Human Use Guidelines; FDA regulatory requirements and in accordance with the ethical principles of the Declaration of Helsinki. In addition, all applicable local laws 309 309 BCX1812-311 (V2.0: 05-October-2007) Page 49 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL and regulatory requirements relevant to the use of new therapeutic agents in the countries involved will be adhered to. The Investigator should submit written reports of clinical study status to their Institutional Review Board (IRB)/ Independent Ethics Committee (IEC) annually or more frequently if requested by the IRB/ IEC. A final study notification will also be forwarded to the IRB/IEC after the study is completed or in the event of premature termination of the study in accordance with the applicable regulations. Copies of all contact with the IRB/ IEC should be maintained in the study documents file. Copies of clinical study status reports (including termination) should be provided to BioCryst. 13.1.2 Ethics Committee Approvals Before initiation of the study at each investigational site, the protocol, the informed consent form, the subject information sheet, and any other relevant study documentation will be submitted to the appropriate IRB/IEC. Written approval of the study must be obtained before the study center can be initiated or the investigational medicinal product is released to the Investigator. Any necessary extensions or renewals of IRB/IEC approval must be obtained, in particular, for changes to the study such as modification of the protocol, the informed consent form, the written information provided to subjects and/or other procedures. The Investigator will report promptly to the IRB/IEC any new information that may adversely affect the safety of the subjects or the conduct of the study. On completion of the study, the Investigator will provide the IRB/IEC with a report of the outcome of the study. 13.1.3 Subject Informed Consent Signed informed consent must be obtained from each subject prior to performing any study- related procedures. Each subject should be given both verbal and written information describing the nature and duration of the clinical study. The informed consent process should take place under conditions where the subject has adequate time to consider the risks and benefits associated with his/her participation in the study. Subjects will not be screened or treated until the subject has signed an approved ICF written in a language in which the subject is fluent. The ICF that is used must be approved both by BioCryst and by the reviewing IRB/ IEC. The informed consent should be in accordance with the current revision of the Declaration of Helsinki, current ICH and GCP guidelines, and BioCryst policy. The Investigator must explain to potential subjects or their legal representatives the aims, methods, reasonably anticipated benefits, and potential hazards of the trial and any discomfort it may entail. Subjects will be informed that they are free not to participate in the trial and that they may withdraw consent to participate at any time. They will be told that refusal to participate in the study will not prejudice future treatment. They will also be told that their records may be examined by competent authorities and authorized persons but that personal information will be treated as strictly confidential and will not be publicly available. Subjects must be given the opportunity to ask questions. After this explanation and before entry into the trial, consent should be appropriately recorded by means of the subject’s dated signature. The subject should receive a signed and dated copy of the ICF. The original signed informed consent should be retained in the study files. The Investigator shall maintain a log of all subjects who sign the ICF and indicate if the subject was enrolled into the study or reason for non-enrollment. 310 310 BCX1812-311 (V2.0: 05-October-2007) Page 50 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.1.4 Payment to Subjects Reasonable compensation to study subjects may be provided if approved by the IRB/IEC responsible for the study at the Investigator’s site. 13.1.5 Investigator Reporting Requirements The Investigator will provide timely reports regarding safety to his/her IRB/IEC as required. 13.2 Study Monitoring During trial conduct, BioCryst or its designee will conduct periodic monitoring visits to ensure that the protocol and GCPs are being followed. The monitors may review source documents to confirm that the data recorded on CRFs is accurate. The investigator and institution will allow BioCryst monitors or its designees and appropriate regulatory authorities direct access to source documents to perform this verification. 13.3 Quality Assurance The trial site may be subject to review by the IRB/IEC, and/or to quality assurance audits performed by BioCryst, and/or to inspection by appropriate regulatory authorities. It is important that the investigator(s) and their relevant personnel are available during the monitoring visits and possible audits or inspections and that sufficient time is devoted to the process. 13.4 Study Termination and Site Closure BioCryst reserves the right to discontinue the trial prior to inclusion of the intended number of subjects but intends only to exercise this right for valid scientific or administrative reasons. After such a decision, the Investigator must contact all participating subjects immediately after notification. As directed by BioCryst, all study materials must be collected and all case report forms completed to the greatest extent possible. 13.5 Records Retention To enable evaluations and/or audits from regulatory authorities or BioCryst, the Investigator agrees to keep records, including the identity of all participating subjects (sufficient information to link records, case report forms and hospital records), all original signed informed consent forms, copies of all case report forms and detailed records of treatment disposition. The records should be retained by the Investigator according to local regulations or as specified in the Clinical Trial Agreement, whichever is longer. If the Investigator relocates, retires, or for any reason withdraws from the study, the study records may be transferred to an acceptable designee, such as another investigator, another institution, or to BioCryst. The Investigator must obtain BioCryst’s written permission before disposing of any records. 311 311 BCX1812-311 (V2.0: 05-October-2007) Page 51 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.6 Study Organization 13.6.1 Data Monitoring Committee BioCryst will assemble an independent Data Monitoring Committee (DMC) to assess safety parameters of the trial on a periodic, ongoing basis while the trial is in progress. The committee will include a statistician and three physicians, two of whom will be Infectious Disease / Clinical Virology specialists. Full details of the composition of the DMC and how the DMC is to operate will be described in a separate DMC charter. 13.7 Confidentiality of Information BioCryst affirms the subject’s right to protection against invasion of privacy. Only a subject identification number, initials and/or date of birth will identify subject data retrieved by BioCryst. However, in compliance with federal regulations, BioCryst requires the investigator to permit BioCryst’s representatives and, when necessary, representatives of the FDA or other regulatory authorities to review and/or copy any medical records relevant to the study. BioCryst will ensure that the use and disclosure of protected health information obtained during a research study complies with the HIPAA Privacy Rule, where this rule is applicable. The Rule provides federal protection for the privacy of protected health information by implementing standards to protect and guard against the misuse of individually identifiable health information of subjects participating in BioCryst-sponsored Clinical Trials. "Authorization" is required from each research subject, i.e., specified permission granted by an individual to a covered entity for the use or disclosure of an individual's protected health information. A valid authorization must meet the implementation specifications under the HIPAA Privacy Rule. Authorization may be combined in the Informed Consent document (approved by the IRB/IEC) or it may be a separate document, (approved by the IRB/IEC) or provided by the Investigator or Sponsor (without IRB/IEC approval). It is the responsibility of the investigator and institution to obtain such waiver/authorization in writing from the appropriate individual. HIPAA authorizations are required for U.S. sites only. 13.8 Study Publication All data generated from this study are the property of BioCryst and shall be held in strict confidence along with all information furnished by BioCryst. Independent analysis and/or publication of these data by the Investigator or any member of his/her staff are not permitted without prior written consent of BioCryst. Written permission to the Investigator will be contingent on the review by BioCryst of the statistical analysis and manuscript and will provide for nondisclosure of BioCryst confidential or proprietary information. In all cases, the parties agree to submit all manuscripts or abstracts to all other parties 30 days prior to submission. This will enable all parties to protect proprietary information and to provide comments based on information that may not yet be available to other parties. 312 312 BCX1812-311 (V2.0: 05-October-2007) Page 52 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 14 REFERENCES 1. Cox NJ, Subbarao K. Influenza. Lancet 1999;354(9186):1277–1282. 2. Thompson WW, Shay KD, Weintraub E, Branner L, Cox N, et al. Mortality associated with influenza and respiratory syncytial virus in the United States. JAMA 2003;289(2):179–186. 3. Kaiser L, Wat C, Mills T, Mahoney P, Ward P, et al. Impact of oseltamivir treatment on influenza-related lower respiratory tract complications and hospitalizations. Arch Intern Med 2003;163(14):1667–1672. 4. Hayden FG, Treanor JJ, Fritz RS, Lobo M, Betts RF, et al. Use of the oral neuraminidase inhibitor oseltamivir in experimental human influenza: randomized controlled trials for prevention and treatment. JAMA 1999;282(13):1240–1246. 5. Kiso M, Mitamura K, Sakai-Tagawa Y, Shiraishi K, Kawakami C, et al. Resistant influenza A viruses in children treated with oseltamivir: descriptive study. Lancet 2004;364(9436):759– 765. 6. Bantia S, Parker CD, Ananth SL, Horn LL, Andries K, et al. Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir. Antimicrob Agents Chemother 2001;45(4):1162–1167. 7. Boivin G, Goyette N. Susceptibility of recent Canadian influenza A and B virus isolates to different neuraminidase inhibitors. Antiviral Res 2002;54(3):143–147. 8. Gubareva LV, Webster RG, Hayden FG. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother 2001;45(12):3403–3408. 9. Govorkova EA, Fang HB, Tan M, Webster RG. Neuraminidase inhibitor-rimantadine combinations exert additive and synergistic anti-influenza virus effects in MDCK cells. Antimicrob Agents Chemother 2004;48(12):4855–4863. 10. BioCryst Pharmaceuticals. Unpublished data. 11. Arnold CS, Zacks MA, Dziuba N, Yun N, Linde N, Smith J, Babu YS, Paessler S. Injectable peramivir promotes survival in mice and ferrets infected with highly pathogenic avian influenza A/Vietnam/1203/04 (H5N1). V-2041B, ICAAC 2006, San Francisco 12. Boltz, DA, Ilyushina NA, Arnold CS, Babu, YS, Webster RG and Govorkova EA. Intramuscular administration of neuraminidase inhibitor peramivir promotes survival against lethal H5N1 influenza infection in mice. Antiviral Research,2007; 74 (3): A32 13. BioCryst Pharmaceuticals unpublished clinical study report BC-01-03. 14. Tamiflu® Package Insert. Roche Pharmaceuticals. Rev. December 2005. 15. Quidel QuickVue Influenza A+B and Binax NOW Influenza A&B Test Kit product information sheets 16. Treanor JJ, Hayden FG, Vrooman PS, Barbarash R et al. Efficacy and safety of the oral neuraminidase inhibitor oseltamivir in treating acute influenza. JAMA 2000; 283(8): 1016- 1024. 17. Nicholson KG, Aoki FY, Osterhaus AD, Trottier S et al. Efficacy and safety of oseltamivir in treatment of influenza: a randomised controlled trial. Lancet 2000; 355(9218): 1845-1850. 313 313 BCX1812-311 (V2.0: 05-October-2007) Page 53 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 18. US Department of Health and Human Services, Food and Drug Administration Center for Drug Evaluation and Reserach (CDER). Attachment to Guidance on Antiviral Product Development- Conducting and Submitting Virology Studies to the Agency: Guidance for Submitting Influenza Resistance Data. http://www.fda.gov/cder/guidance/7070fnlFLU.htm 314 314 BCX1812-311 (V2.0: 05-October-2007) Page 54 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15 APPENDICES 15.1 NYHA Functional Classification Criteria: Heart Failure and Angina NYHA Functional Classification of Heart Failure Class I No symptoms. Ordinary physical activity such as walking and climbing stairs does not cause fatigue or dyspnea. Class II Symptoms with ordinary physical activity. Walking or climbing stairs rapidly; walking uphill; walking or stair climbing after meals, in cold weather, in wind, or when under emotional stress causes undue fatigue or dyspnea. Class III Symptoms w ith less than ordinary phy sical activity. Walking one to two blocks on t he level and clim bing m ore th an one flight of stai rs in norm al conditions causes undue fatigue or dyspnea. Class IV Symptoms at rest. Inability to carry on any physical activity without fatigue or dyspnea. NYHA Functional Classification of Angina Class I Angina only with unusually strenuous activity. Class II Angina with slightl y more prolonged o r slightly more vigorous activit y than usual. Class III Angina with usual daily activity. Class IV Angina at rest. 315 315 BCX1812-311 (V2.0: 05-October-2007) Page 55 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15.2 Criteria for Severe COPD and Severe Asthma The following guidelines are provided to assist in the evaluation of subjects who have a medical history for Chronic Obstructive Pulmonary Disease (COPD) and/or Asthma. Subjects with severe COPD or severe persistent Asthma are to be excluded from this study. (See section 8.1.2, exclusion criteria number 3). Classification of Asthma from National Asthma and Education and Prevention Program For Adults and Children (> 5 yrs) who can use a spirometer or peak flow meter Classification Days with Symptoms Nights with Symptoms FEV1 or PEF % Predicted Normal PEF Variability (%) Severe persistent Continual Frequent ≤ 60 > 30 Moderate Persistent Daily > 1/ week > 60 - < 80 > 30 Mild Persistent > 2 / week but < 1 times / day > 2/ month ≥ 80 20 – 30 Mild Intermittent ≤ 2 / week < 2 / month ≥ 80 < 20 FEV1: percentage predicted value for forced expiratory volume in 1 second. PEF: percentage of personal best for peak expiratory flow. Extracted from: Expert Panel Report 3: Guidelines for the Diagnosis and Management of Asthma. National Heart, Lung, and Blood Institute, National Asthma Education and Prevention Program. HHS/NIH 2007 Spirometric Classification of COPD Severity based upon Post-Bronchodilator FEV1 (GOLD Criteria) Stage Characteristics Mild COPD FEV1/FVC < 70% FEV1 ≥ 80% predicted Moderate COPD FEV1/FVC < 70% 50 % ≤ FEV1 < 80% predicted Severe COPD FEV1/FVC < 70% 30 % ≤ FEV1 < 50% predicted Very Severe COPD FEV1/FVC < 70% FEV1 < 30% predicted or FEV1 < 50% predicted plus chronic respiratory failure FEV1: percentage predicted value for forced expiratory volume in one second. FVC: forced vital capacity Extracted from: Rabe KF, et al. Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease (GOLD Executive Summary). Am. J. Respir. Crit. Care Med. 2007:176;532-555. 316 316 CLINICAL STUDY PROTOCOL Protocol No. BCX1812-311 IND No. 76,350 A PHASE 3 MULTICENTER, RANDOMIZED, DOUBLE BLIND, PLACEBO- CONTROLLED STUDY TO EVALUATE THE EFFICACY AND SAFETY OF INTRAMUSCULAR PERAMIVIR IN SUBJECTS WITH UNCOMPLICATED ACUTE INFLUENZA THE IMPROVE I STUDY (IntraMuscular Peramivir for the Relief Of symptoms and Virologic Efficacy) Short title: Intramuscular Peramivir for the Treatment of Uncomplicated Influenza Protocol Date(s): Version 1.0: 04 September 2007 Version 2.0: 05 October 2007 Version 3.0 20 November 2007 BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35244, USA Phone: +1 919 859 1302 Fax: +1 919 851 1416 The document contains trade secrets and proprietary information of BioCryst Pharmaceuticals, Inc. This information is confidential property of BioCryst Pharmaceuticals, Inc., and is subject to confidentiality agreements entered into with BioCryst Pharmaceuticals, Inc. No information contained herein should be disclosed without prior written approval. CONFIDENTIAL 317 317 BCX1812-311 (V3.0: 20-November-2007) Page 2 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1 TITLE PAGE Protocol Number: BCX1812-311 Study Title: A phase 3 multicenter, randomized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza. IND Number: 76, 350 Investigational Product: Peramivir (BCX1812) Indication Studied: Uncomplicated acute influenza Sponsor: BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35233 Development Phase: 3 Sponsor Medical Officer: W. James Alexander, M.D., M.P.H. Senior Vice President, Clinical Development Chief Medical Officer Phone: +1 919 859 1302 Fax: +1 919 851 1416 Email Address: jalexander@biocryst.com Compliance Statement: This study will be conducted in accordance with the ethical principles that have their origin in the Declaration of Helsinki and clinical research guidelines established by the Code of Federal Regulations (Title 21, CFR Parts 50, 56, and 312) and ICH Guidelines. Essential study documents will be archived in accordance with applicable regulations. Final Protocol Date: Version 1.0: 04 September 2007 Amendment(s) Date(s): Version 2.0: 05 October 2007 Version 3.0: 20 November 2007 318 318 319 319 BCX1812-311 (V3.0: 20-November-2007) Page 4 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1.2 Clinical Study Protocol Agreement Protocol No. BCX1812-311 Protocol Title: A phase 3 multicenter, random ized, double-blind, placebo-controlled study to evaluate the effic acy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza I have carefully read this protocol and agree that it contains all of the necessary information required to conduct this study. I agree to c onduct this study as described and according t o the Decl aration of Helsinki, Internationa l Conference on Har monization Guidelines for Good Clinical Practices, and all applicable regulatory requirements. Investigator’s Signature Date Name (Print) 320 320 BCX1812-311 (V3.0: 20-November-2007) Page 5 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 2 SYNOPSIS Protocol No. BCX1812-311 Protocol Title: A phase 3, multicenter, randomized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza. Sponsor: BioCryst Pharmaceuticals, Inc. Investigators/Study Sites: Multinational Development Phase: 3 Objectives: Primary: To evaluate the efficacy of peramivir administered intramuscularly compared to placebo on the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza A. Secondary: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly 2. To evaluate secondary clinical outcomes in response to treatment 3. To evaluate changes in influenza virus titer in nasopharyngeal samples (viral shedding) in response to treatment Exploratory: 1. To assess pharmacoeconomic measures as response to treatment 2. To assess changes in influenza viral susceptibility to neuraminidase inhibitors following treatment Number of Subjects: Total enrollment: up to a total of 750 evaluable subjects will be randomized to treatment (150 subjects in the placebo treatment group, 300 subjects in the peramivir 300mg treatment group and 300 subjects in the peramivir 600mg treatment group). An evaluable subject is one who is randomized, receives study drug, and has confirmed acute influenza A by primary viral culture or PCR. A positive Rapid Antigen Test (RAT) for influenza A at screening will be required for enrollment. Because results of clinic-based RAT tests may not precisely indicate presence of influenza infection, it is expected that at least 850 subjects will be randomized to treatment to ensure that 750 evaluable subjects are treated. Study Design: This is a multinational, randomized, double-blind study comparing the efficacy and safety of two single dose regimens of peramivir administered intramuscularly versus placebo in 321 321 BCX1812-311 (V3.0: 20-November-2007) Page 6 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL adults with uncomplicated acute influenza. Each subject’s assignment to treatment will be stratified according to smoking status. All subjects will be centrally randomized to one of three treatment groups according to smoking status strata in a ratio of 2:2:1 such that 80% of subjects are randomized to one of the two single dose regimens of peramivir. Treatment Group 1: Peramivir 300mg Treatment Group 2: Peramivir 600mg Treatment Group 3: Placebo Study drug will be administered as bilateral 4mL intramuscular injections (total of 8mL injected in equally divided doses). Procedures for gluteal intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. Subjects eligible for screening will have an anterior nasal swab collected for testing by rapid antigen testing (RAT) for influenza A, in accordance with the commercially available RAT kit instructions. If the initial RAT is negative, the test should be repeated within one hour. Subjects meeting the inclusion/exclusion criteria may be enrolled into the study. All enrolled subjects will record the following information in a Study Diary: • Assessment of the presence and severity of each of seven symptoms of influenza on a 4-point scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatment, then once daily (AM) through Day 14 • Oral temperature measurements taken with an electronic thermometer every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol) or other anti-pyretic medications. • Assessment of subject’s time lost from work or usual activities and rating of productivity compared to normal (rated as 0-10 on a visual analog scale) once daily through Day 14 • Doses of antipyretic, expectorant, and/or throat lozenges taken for symptomatic relief each day through Day 14 Anterior nose (bilateral) and posterior pharynx specimens (swabs) will be collected at Day 1 (pre-treatment) and at Days 3, 322 322 BCX1812-311 (V3.0: 20-November-2007) Page 7 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5, and 9, for quantitative virologic assessments. Specimens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result on culture) as well as other virologic assessments (e.g. PCR, genotypic testing) All virologic assessments will be performed by a central laboratory. Two samples for pharmacokinetic (PK) testing for plasma levels of peramivir will be obtained from all subjects randomized. The first PK sample will be obtained between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be obtained at the day 3 visit in all subjects. The data from these PK samples will be utilized in a population exposure-response analysis. At selected sites a separate sub-study will be conducted to collect additional PK samples between treatment and Day 3 for the purpose of conducting a separate exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Study Population: Male and female subjects, 18 years of age and older, with symptoms consistent with a diagnosis of uncomplicated acute influenza infection may be screened for enrollment. Subject eligibility will require the presence of two or more symptoms of at least moderate severity consistent with acute influenza as well as positive results obtained from a rapid antigen test (RAT) for influenza A at screening. Inclusion Criteria: 1. Male and non-pregnant female subjects age ≥18 years. 2. A positive Influenza A Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate anterior nasal specimen, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated within one-hour. Subjects with a positive influenza B or mixed A and B RAT will be excluded. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. A subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at the time of screening. 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of at least moderate severity. 5. Presence of at least one constitutional symptom (myalgia [aches and pains], headache, feverishness, or fatigue) of at least moderate severity. 323 323 BCX1812-311 (V3.0: 20-November-2007) Page 8 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6. Onset of symptoms no more than 48 hours before presentation for screening. 7. Written informed consent. Exclusion Criteria: 1. Women who are pregnant or breast-feeding. 2. Presence of clinically significant signs of acute respiratory distress. 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma. 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class III or IV functional status within the past 12 months. 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 6. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min). 7. Clinical evidence of worsening of any chronic medical condition (temporally associated with the onset of symptoms of influenza) which, in the investigator’s opinion, indicates that such finding(s) could represent complications of influenza. 8. Current clinical evidence, including clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis and/or pneumonia, or active bacterial infection at any body site that requires therapy with oral or systemic antibiotics. 9. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy which would include oral or systemic treatment with > 10 mg prednisone or equivalent on a daily basis within 30 days of screening. 10. Currently receiving treatment for viral hepatitis B or viral hepatitis C. 11. Presence of known HIV infection with a CD4 count <350 cell/mm3. 12. Current therapy with oral warfarin or other systemic anticoagulant. 13. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening. 14. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days. 15. Immunized against influenza with inactivated virus vaccine within the previous 14 days. 16. Receipt of any intramuscular injection within the previous 14 days. 17. History of alcohol abuse or drug addiction within 1 year prior to admission in the study. 324 324 BCX1812-311 (V3.0: 20-November-2007) Page 9 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 18. Participation in a previous study of intramuscular or intravenous peramivir or previous participation in this study 19. Participation in a study of any investigational drug or device within the last 30 days. Study Endpoints: Primary Endpoint: Clinical: Time to alleviation of clinical symptoms of influenza. Secondary Endpoint(s): Safety: Incidence of treatment-emergent adverse events and treatment- emergent changes in clinical laboratory tests. Clinical: Time to resolution of fever. Incidence of influenza related complications. Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID50). Exploratory Endpoint(s): Pharmacoeconomic: Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. Virologic: Quantitative change in influenza virus shedding, measured by PCR. Change in influenza virus susceptibility to neuraminidase inhibitors. Investigational Product, Dose, and Mode of Administration: Peramivir (BCX-1812), 7 5mg/mL, 4mL (300m g) per injection, adm inistered as bilateral injections. Reference Therapy, Dose, and Mode of Administration: Matching Placebo (buffered diluent), 4mL per injection administered as bilateral injections. Duration of Treatment: Following treatment on day 1, study duration for all subjects is expected to be up to 14 days (including all visits). Presence of unresolved adverse events and/or treatment-emergent laboratory findings at the Day 14 visit, or persistent or recurrent symptoms of influenza (of the seven symptoms assessed) of either moderate or severe intensity at the Day 14 visit, will require additional follow up. Statistical Methods: Study Hypothesis: The null hypothesis (H0) for this study is that the time to alleviation of influenza symptoms is the same for subjects treated with placebo and for subjects treated with peramivir 325 325 BCX1812-311 (V3.0: 20-November-2007) Page 10 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 300mg (H01) or peramivir 600mg (H02). The alternative hypothesis (H1) is that subjects treated with peramivir 300mg (H11) or peramivir 600mg (H12) have an improvement in time to alleviation of influenza symptoms over those treated with placebo. Sample Size: From preliminary results of a phase 2 study evaluating peramivir treatment of uncomplicated influenza, it is expected that the median time to alleviation of symptoms will be 137.0 hours (95% CI: 115.9, 165.8) for subjects receiving placebo treatment. Additionally, it is expected that the median time to alleviation for the 150 mg dose peramivir arm will be reduced by 30% compared to placebo (see table below) yielding a hazard ratio of 0.70. Median Time To Alleviation of Symptoms (Hours) Placebo Peramivir 150mg Difference (hours) 145.0 101.5 43.5 140.0 98.0 42.0 135.0 94.5 40.5 130.0 91.0 39.0 125.0 87.5 37.5 120.0 84.0 36.0 115.0 80.5 34.5 110.0 77.0 33.0 105.0 73.5 31.5 100.0 70.0 30.0 Using these assumptions, a sample size of 300 evaluable subjects per active treatment group and 150 evaluable subjects in the placebo group (a total of 750 evaluable subjects) is sufficient to provide at least 90% power to detect a hazard ratio of 0.70 using a log-rank statistic and α = 0.025 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). Efficacy: The intent-to-treat infected population (ITTI) will include all subjects who are randomized, received study drug, and have confirmed influenza A by primary viral culture or PCR. The primary efficacy variable is the time to alleviation of symptoms, defined as the time from injection of study drug to the start of the time period when each of seven symptoms of influenza are either absent or are present at no more than mild severity level and remain at no worse than this severity status for a 21.5 hour (24 hours – 10%) period. Descriptive statistics for the primary efficacy variable will be 326 326 BCX1812-311 (V3.0: 20-November-2007) Page 11 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL tabulated by treatment group. Alleviation of symptoms will be determined by assessment of symptoms as reported on each subject’s diary card. Time to alleviation of symptoms will be summarized for each treatment group. Treatment differences between each active group and placebo will be assessed using a Wilcoxon-Gehan statistic stratified by smoking status at screening. Subjects who do not experience alleviation of symptoms will be censored at the date of their last non-missing assessment. The overall significance level will be maintained by utilization of Hochberg’s method for the planned comparisons between the two active treatments and placebo. Time to resolution of fever will be analyzed in a similar manner without the adjustment for multiple comparisons. Efficacy analyses will be repeated for a Per-Protocol Infected population (PPI). This population will include those subjects in the ITTI population who received an adequate intramuscular injection. Details of this population will be described in the statistical analysis plan. The PPI population analysis will be used as supportive to the primary analysis with the ITTI. Changes in influenza virus TCID50 (viral titers from nasopharyngeal specimens) will be compared using the van Elteren statistic controlling for smoking status at screening. Analyses of other continuous endpoints will be analyzed in a similar manner. The number and percentage of subjects experiencing influenza related complications (IRC) will be summarized by complication preferred term and treatment group. The difference between the treatment groups will be assessed using a logistic regression model with factors for treatment group and smoking status at screening. Pairwise differences between the treatment groups will be evaluated using contrasts from the final logistic regression model. Safety: Safety analyses will be presented for all subjects in the safety population, defined as all randomized subjects who receive at least one dose of study drug. Adverse events will be mapped to a Medical Dictionary for Regulatory Activities (MedDRA) preferred term and system organ classification. The occurrence of treatment-emergent AEs will be summarized using preferred terms, system organ classifications, and severity. Separate summaries of treatment-emergent SAEs and treatment- emergent AEs that are related to study medication will be generated. All AEs will be listed for individual subjects showing both verbatim and preferred terms. 327 327 BCX1812-311 (V3.0: 20-November-2007) Page 12 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Descriptive summaries of vital signs and quantitative clinical laboratory changes will be presented by study visit. Frequency and percentages of subjects with abnormal laboratory test results will be summarized by toxicity grade. Concomitant medications will be mapped to a WHO preferred term and drug classification. The number and percent of subjects taking concomitant medications will be summarized using preferred terms and drug classifications. The number and percent of subjects experiencing each abnormal physical examination finding will be presented. The number and percent of subjects discontinuing study as well as the reasons for discontinuation will be summarized by treatment group. Date of Protocol: Version 1.0: 04-September-2007 Amendment (Dates): Version 2.0: 05-October-2007 Version 3.0: 20-November-2007 328 328 BCX1812-311 (V3.0: 20-November-2007) Page 13 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 3 TABLE OF CONTENTS 1 TITLE PAGE...............................................................................................................................2 1.1 PROTOCOL APPROVAL SIGNATURE PAGE......................................................................................3 1.2 CLINICAL STUDY PROTOCOL AGREEMENT....................................................................................4 2 SYNOPSIS...................................................................................................................................5 3 TABLE OF CONTENTS...........................................................................................................13 3.1 LIST OF FIGURES .........................................................................................................................15 3.2 LIST OF TABLES ..........................................................................................................................15 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS.............................................16 5 INTRODUCTION......................................................................................................................18 5.1 BACKGROUND.............................................................................................................................18 5.2 RATIONALE FOR STUDY ..............................................................................................................18 5.3 NON-CLINICAL EXPERIENCE WITH PERAMIVIR...........................................................................19 5.3.1 In vitro Assays.......................................................................................................................19 5.3.2 Animal Models......................................................................................................................19 5.4 PREVIOUS PHASE 3 CLINICAL EXPERIENCE WITH ORAL PERAMIVIR...........................................20 5.5 PREVIOUS PHASE 1 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR.........................................20 5.6 PHASE 2 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR .........................................................22 5.7 DOSE RATIONALE................................................................................................................................25 6 STUDY OBJECTIVES..............................................................................................................26 6.1 OBJECTIVES ................................................................................................................................26 6.1.1 Primary Objective..................................................................................................................26 6.1.2 Secondary Objective(s) .........................................................................................................26 6.1.3 Exploratory Objective(s) .......................................................................................................26 6.2 STUDY ENDPOINTS......................................................................................................................26 6.2.1 Primary Endpoint...................................................................................................................26 6.2.2 Secondary Endpoint(s) ..........................................................................................................26 6.2.3 Exploratory Endpoints...........................................................................................................27 7 STUDY DESIGN.......................................................................................................................27 7.1 OVERALL STUDY DESIGN AND PLAN ..........................................................................................27 8 SELECTION AND WITHDRAWAL OF SUBJECTS..............................................................28 8.1.1 Inclusion Criteria...................................................................................................................28 8.1.2 Exclusion Criteria..................................................................................................................29 8.1.3 Removal of Subjects from Therapy or Assessment...............................................................30 9 TREATMENTS .........................................................................................................................30 9.1 TREATMENTS ADMINISTERED.....................................................................................................30 9.2 IDENTITY OF INVESTIGATIONAL PRODUCT(S) .............................................................................30 9.3 METHOD OF ASSIGNING SUBJECTS TO TREATMENT GROUPS ......................................................31 9.4 STUDY MEDICATION ACCOUNTABILITY......................................................................................31 9.5 BLINDING/UNBLINDING OF TREATMENTS...................................................................................31 9.6 PRIOR AND CONCOMITANT THERAPIES.......................................................................................32 9.7 OVERDOSE AND TOXICITY MANAGEMENT..................................................................................32 9.8 DOSE INTERRUPTION...................................................................................................................32 10 STUDY CONDUCT..................................................................................................................32 10.1 EVALUATIONS.............................................................................................................................32 10.1.1 Informed Consent .............................................................................................................32 10.1.2 Medical History ................................................................................................................32 10.1.3 Rapid Antigen Test for Influenza .....................................................................................32 10.1.4 Physical Examination and Influenza-related Complications Assessments .......................33 10.1.5 Vital Signs ........................................................................................................................33 10.1.6 Electrocardiogram Measurements ....................................................................................33 10.1.7 Clinical Laboratories ........................................................................................................33 10.1.8 Urine Pregnancy Test .......................................................................................................34 10.1.9 Serology for Influenza ......................................................................................................34 329 329 BCX1812-311 (V3.0: 20-November-2007) Page 14 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.10 Samples for Virologic Laboratory Assessments...............................................................34 10.1.11 Subject Self Assessments..................................................................................................34 10.1.12 Concomitant Medications.................................................................................................35 10.1.13 Adverse Events.................................................................................................................35 10.1.14 Pharmacokinetic Exposure Samples.................................................................................35 10.2 SCREENING PERIOD.....................................................................................................................35 10.2.1 Informed Consent .............................................................................................................35 10.2.2 Screening/Baseline Evaluation and Enrollment................................................................35 10.3 TREATMENT PERIOD—STUDY DAY 1 .........................................................................................36 10.3.1 Pre-dose Evaluations-Study Day 1 ...................................................................................36 10.3.2 Post-dose Evaluations-Study Day 1..................................................................................36 10.4 POST-TREATMENT ASSESSMENT PERIOD....................................................................................37 10.4.1 Days 2, 3, 5, 9 and 14 .......................................................................................................37 10.4.2 Adverse Events Reported at Post-treatment Visits ...........................................................38 11 ADVERSE EVENT MANAGEMENT......................................................................................41 11.1 DEFINITIONS ...............................................................................................................................41 11.1.1 Adverse Event...................................................................................................................41 11.1.2 Serious Adverse Event......................................................................................................41 11.2 METHOD, FREQUENCY, AND TIME PERIOD FOR DETECTING ADVERSE EVENTS AND REPORTING SERIOUS ADVERSE EVENTS ........................................................................................................42 11.2.1 Definition of Severity .......................................................................................................42 11.2.2 Definition of Relationship to Study Drug.........................................................................43 11.2.3 Reporting Serious Adverse Events ...................................................................................43 11.2.4 Emergency Procedures .....................................................................................................44 12 STATISTICAL METHODS ......................................................................................................44 12.1 DATA COLLECTION METHODS ....................................................................................................44 12.2 STATISTICAL ANALYSIS PLAN ....................................................................................................45 12.3 STUDY HYPOTHESIS....................................................................................................................45 12.4 SAMPLE SIZE ESTIMATES............................................................................................................45 12.5 ANALYSIS POPULATIONS ............................................................................................................46 12.6 INTERIM AND END OF STUDY ANALYSES....................................................................................47 12.7 EFFICACY ANALYSES..................................................................................................................47 12.7.1 Primary Efficacy Endpoint ...............................................................................................47 12.7.2 Secondary Efficacy Endpoints..........................................................................................47 12.7.3 Exploratory Endpoints......................................................................................................48 12.8 SAFETY ANALYSES .....................................................................................................................48 12.9 SUB-STUDY AND PHARMACOKINETIC ANALYSIS........................................................................49 12.10 GENERAL ISSUES FOR STATISTICAL ANALYSIS ...........................................................................49 12.10.1 Multiple Comparisons and Multiplicity............................................................................49 12.10.2 Covariates.........................................................................................................................49 12.10.3 Planned Sub-Groups.........................................................................................................49 12.10.4 Missing Data.....................................................................................................................50 13 STUDY ADMINISTRATION...................................................................................................50 13.1 REGULATORY AND ETHICAL CONSIDERATIONS ..........................................................................50 13.1.1 Regulatory Authority Approvals.......................................................................................50 13.1.2 Ethics Committee Approvals............................................................................................51 13.1.3 Subject Informed Consent ................................................................................................51 13.1.4 Payment to Subjects..........................................................................................................51 13.1.5 Investigator Reporting Requirements ...............................................................................51 13.2 STUDY MONITORING...................................................................................................................52 13.3 QUALITY ASSURANCE.................................................................................................................52 13.4 STUDY TERMINATION AND SITE CLOSURE..................................................................................52 13.5 RECORDS RETENTION .................................................................................................................52 13.6 STUDY ORGANIZATION...............................................................................................................52 13.6.1 Data Monitoring Committee.............................................................................................52 13.7 CONFIDENTIALITY OF INFORMATION ..........................................................................................53 330 330 BCX1812-311 (V3.0: 20-November-2007) Page 15 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.8 STUDY PUBLICATION ..................................................................................................................53 14 REFERENCES...........................................................................................................................54 15 APPENDICES ...........................................................................................................................56 15.1 NYHA FUNCTIONAL CLASSIFICATION CRITERIA: HEART FAILURE AND ANGINA ......................56 15.2 CRITERIA FOR SEVERE COPD AND SEVERE ASTHMA .................................................................57 3.1 List of Figures Figure 1 Study Measurements and Visit Schedule.................................................................39 3.2 List of Tables Table 1 Results of study BC-01-03.......................................................................................20 Table 2 Pharmacokinetic parameters from study Him-06-111. ............................................21 Table 3 Summary of Efficacy from BCX1812-211. .............................................................24 Table 4 Summary of Safety from BCX1812-211. ................................................................25 Table 5 Median time to alleviation of symptoms (30% reduction, 0.70 hazard ratio)..........46 331 331 BCX1812-311 (V3.0: 20-November-2007) Page 16 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS AE adverse event ALT alanine aminotransferase AST aspartate aminotransferase AUC area under the curve AUC0–72 area under the curve from time 0 to 72 hours AUC0–∞ area under the curve extrapolated from time 0 to infinity BMI Body Mass Index in kg/m2 CBC complete blood count CDC Centers for Disease Control and Prevention CIOMS Council for International Organizations of Medical sciences Cmax maximum plasma concentration CK creatine kinase CNS central nervous system COPD chronic obstructive pulmonary disease CRF Case Report Form CV coefficient of variation ECG Electrocardiogram GCP Good Clinical Practice HCG human chorionic gonadotropin HIV Human immunodeficiency virus IC50 median inhibitory concentration ICF informed consent form ICH International Conference on Harmonization IEC Independent Ethics Committee IRB Institutional Review Board IRC influenza related complications ITT intent-to-treat ITTI intent-to-treat infected IUD intrauterine device IVRS interactive voice response system LDH lactate dehydrogenase MedDRA Medical Dictionary for Regulatory Activities MRU medical resource utilization NSAID non-steroidal anti-inflammatory drug PCR polymerase chain reaction RAT Rapid Antigen Test RBC red blood cell SAE serious adverse event SAP statistical analysis plan 332 332 BCX1812-311 (V3.0: 20-November-2007) Page 17 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL SD standard deviation SUSAR Suspected Unexpected Serious Adverse Event t1/2 elimination half-life t1/2 λz terminal half-life TCID50 tissue-culture infective dose50 TEAEs treatment-emergent adverse events Tmax time to attain maximum plasma concentration UPEP Urine protein electrophoresis WBC white blood cell WHO World Health Organization 333 333 BCX1812-311 (V3.0: 20-November-2007) Page 18 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5 INTRODUCTION 5.1 Background Influenza virus is a member of the orthomyxovirus family and causes an acute viral disease of the respiratory tract. Typical influenza illness is characterized by abrupt onset of fever, headache, myalgia, sore throat, and nonproductive cough.1 The illness is usually self-limiting, with relief of symptoms occurring within 5 to 7 days. Nevertheless, it is an important disease for several reasons, including ease of communicability, short incubation time, rapid rate of viral mutation, morbidity with resultant loss of productivity, risk of complicating conditions, and increased risk of death, particularly in the elderly. During 19 of the 23 influenza seasons between 1972/1973 and 1994/1995, estimated influenza-associated deaths in the United States ranged from approximately 25 to more than 150 per 100,000 persons above 65 years of age, accounting for more than 90% of the deaths attributed to pneumonia and influenza.2 Presently, only a few measures are available that can reduce the impact of influenza: active immunoprophylaxis with an inactivated or live attenuated vaccine and chemoprophylaxis or therapy with an influenza-specific antiviral drug. Neuraminidase inhibitors are the current mainstay of antiviral treatment for influenza. Marketed neuraminidase inhibitors include zanamivir (Relenza®, GlaxoSmithKline) and oseltamivir (Tamiflu®, Roche-Gilead), an oral prodrug of the active agent, oseltamivir carboxylate. Influenza neuraminidase is a surface glycoprotein that cleaves sialic acid residues from glycoproteins and glycolipids. The enzyme is responsible for the release of new viral particles from infected cells and may also assist in the spreading of virus through the mucus within the respiratory tract. The neuraminidase inhibitors represent an important advance in the treatment of influenza with respect to activity against influenza A and B viruses, with proven therapeutic value in reducing influenza lower respiratory complications,3 and lower rates of antiviral drug resistance4. The use of currently available neuraminidase inhibitors has been limited by concerns including, the degree of effectiveness, the requirement for an inhaler device (zanamivir), and the emergence of resistant influenza virus variants in some treated populations.5 In addition, there are risks of bronchospasm with zanamivir; and gastrointestinal side effects, with oseltamivir. Peramivir is a neuraminidase inhibitor that represents a potentially promising addition to the armamentarium of drugs for the treatment of influenza infections due to its potential for parenteral administration and lower frequency of dosing. 5.2 Rationale for Study An oral formulation of peramivir has previously been evaluated in a full range of safety, tolerability, pharmacokinetic, and efficacy studies. In a multinational phase 3 clinical trial conducted in 1999-2001, oral peramivir demonstrated antiviral activity against influenza A and B infections, and improvement in the relief of clinical symptoms. Because of the limited bioavailability of peramivir following oral administration (<5%), it was determined that the parenteral route of administration is more appropriate for the delivery of peramivir. Subsequent phase 1 studies of intravenous and intramuscular formulations of peramivir have confirmed that parenteral routes of administration result in plasma levels of drug that are as much as 100 times those achieved via the oral route. In a phase 2 study of intramuscular peramivir in subjects with acute uncomplicated influenza, subjects who received a single injection of 150mg or 300mg 334 334 BCX1812-311 (V3.0: 20-November-2007) Page 19 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL peramivir had clinically meaningful reductions in the time to alleviation of symptoms of influenza, compared to subjects who received a placebo injection. Further details of these studies are provided below and in the Investigator Brochure. Because of the previous demonstration of clinical efficacy of intramuscular peramivir in acute influenza in the phase 2 study, and the encouraging pharmacokinetic and preliminary safety profile of the intramuscular formulation of peramivir demonstrated to date, this phase 3 study will be conducted to evaluate the efficacy and safety profile of intramuscular peramivir and to determine the optimal single dose regimen. 5.3 Non-Clinical Experience with Peramivir 5.3.1 In vitro Assays Peramivir is a selective inhibitor of viral neuraminidase, with 50% inhibitory concentrations (IC50) for bacterial and mammalian enzymes of >300µM.6 In an in vitro study, 42 influenza A and 23 influenza B isolates were collected from untreated subjects during the 1999–2000 influenza season in Canada.7 These isolates were tested for their susceptibility to the neuraminidase inhibitors zanamivir, oseltamivir carboxylate, and peramivir using a chemiluminescent neuraminidase assay. Inhibition of Type A influenza neuraminidase by peramivir was approximately an order of magnitude greater than inhibition of neuraminidase from Type B viruses. IC50 values for the Type A enzymes ranged from <0.1 to 1.4nM, whereas the Type B enzymes ranged from <0.1 to 11nM, with three out of four values in the 5- to 11nM range. Peramivir was the most potent drug against influenza A (H3N2) viruses with a mean IC50 of 0.60nM as well as most potent against influenza B with a mean IC50 of 0.87nM. In another in vitro comparison of peramivir, oseltamivir, and zanamivir, using a neuraminidase inhibition assay with influenza A viruses, the median IC50 of peramivir (approximately 0.34nM) was comparable to that of oseltamivir (0.45nM) and significantly lower than zanamivir (0.95nM). For influenza B virus clinical isolates, the median IC50 of peramivir (1.36nM) was comparable to that of zanamivir (2.7nM) and lower than that of oseltamivir (8.5nM).8 The potency of peramivir was evaluated against five zanamivir-resistant and six oseltamivir- resistant influenza viruses.9 Peramivir remained a potent inhibitor against all oseltamivir-resistant viruses including the mutations H274Y, R292K, E119V, and D198N, with IC50 values ≤40nM. Peramivir also potently inhibited (IC50 ≤ 26nM) the neuraminidase activity of zanamivir-resistant strains, which had the following mutations: R292K, E119G, E119A, and E119D. However, one zanamivir-resistant influenza B virus, B/Mem/96, with a mutation R152K isolated from cell culture, was relatively resistant to all neuraminidase inhibitors, including peramivir (IC50 = 400nM). 5.3.2 Animal Models In a mouse model of influenza infection, a single intramuscular injection of peramivir (10mg/kg) given 4 hours prior to inoculation with an A/NWS/33 (H1N1) influenza strain resulted in 100% survival in contrast to 100% mortality in a control group injected with saline.6 In the same mouse model, treatment of mice up to 72 hours after influenza infection using peramivir (20mg/kg) resulted in 100% survival, compared to 100% mortality in the control group injected with vehicle.10 Peramivir has also demonstrated activity in animal models utilizing a clinical H5N1 isolate as the 335 335 BCX1812-311 (V3.0: 20-November-2007) Page 20 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL infecting virus strain. In a mouse model, a single intramuscular dose of peramivir (30mg/kg) injected 1 hour after inoculation with the highly pathogenic (H5N1) A/Vietnam/1203/04 strain, resulted in a 70% survival rate that was similar to that seen in mice treated with oseltamivir given orally at 10mg/kg/day for 5 days11. In similar experiments, mice inoculated with the same strain of H5N1 virus that were then treated for up to 8 days with intramuscular peramivir exhibited 100% survival12. This longer duration of peramivir treatment also prevented viral replication in the lungs, brain and spleen at days 3, 6 and 9 post inoculation. 5.4 Previous Phase 3 Clinical Experience with Oral Peramivir An oral formulation of peramivir has previously demonstrated antiviral activity and preliminary clinical efficacy in challenge studies in human volunteers, as well as in treatment studies in patients with uncomplicated acute influenza infections during the influenza seasons of 1999- 2001. A Phase 3 multinational study (BC-01-03) of oral peramivir was conducted. Two dose regimens of oral peramivir, 800mg QD for 5 days, or 800mg QD on Day 1, followed by 400mg QD for 4 days, were compared to a matched placebo treatment group. A total of 1246 subjects were randomized to treatment at sites in the USA, Western and Eastern Europe, South America, Australia and New Zealand. As presented in the Table 1 below, the primary end-point of time to relief of influenza symptoms in 694 subjects with confirmed influenza was not found to be significantly different (p=0.17) between the three treatment groups.13 A sub-group analysis of the time to relief of symptoms by country or region demonstrated marked differences in the primary endpoint.. In the subset of influenza-infected subjects enrolled at sites in the US, clinically meaningful differences in time to relief of influenza symptoms between the placebo and the two peramivir arms were observed, however statistical significance (p=0.07) was not achieved. However, a number of secondary endpoints in this phase 3 study, such as time to overall well- being, time to normal activity, incidence of influenza related complications and quantity of viral shedding, achieved or approached statistically significant differences between the peramivir and placebo treatment groups (p=0.03-0.06). Table 1 Results of study BC-01-03 Median Time to Relief of Influenza Symptoms (Hours) Dose and Regimen Overall Results (n=694) US Sites (n=198) Peramivir 800mg po x 5d 89.0 70.8 Peramivir 800mg po x 1d and 400mg po x 4d 91.7 88.8 Placebo x 5 days 104.4 106.8 p value 0.17 0.07 5.5 Previous Phase 1 Experience with Intramuscular Peramivir Two phase 1studies evaluating the safety and pharmacokinetics of an intramuscular formulation of peramivir have been conducted in a total of 45 healthy volunteers receiving peramivir. An additional phase 1 study has recently been initiated to evaluate the pharmacokinetics and 336 336 BCX1812-311 (V3.0: 20-November-2007) Page 21 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL tolerability of higher single doses (up to 600 mg) of intramuscular peramivir. Study Peramivir-Him-06-111 evaluated the single dose pharmacokinetics and tolerability of 75mg, 150mg and 300mg doses of peramivir administered as intramuscular (i.m.) and intravenous (i.v.) injections in a crossover design (9 subjects per group). Peak plasma levels of i.m. peramivir generally occurred within 30 minutes following injection. Plasma pharmacokinetic parameters for i.m. peramivir are summarized in Table 2 below for the three intramuscular single dose regimens evaluated. Table 2 Pharmacokinetic parameters from study Him-06-111. Dose (mg) Cmax (ng/mL) AUC0-∞ (hr·ng/mL) t½a (hr) 75 i.m. 4296 ± 812 11659 ± 1123 19.8 ± 7.9 150 i.m. 7612 ± 884 23952 ± 3804 24.3 ± 4.1 300 i.m. 15150 ± 2367 49649 ± 5619 22.8 ± 2.5 aterminal half life In a second phase 1 study, Peramivir-Him-06-112, the same dose levels of peramivir were administered as single i.m. injections on two consecutive days (6 subjects per group). This double-blind study also included a placebo arm. The pharmacokinetic parameters of i.m. peramivir following the second day of dosing were consistent with those seen following single doses of the drug. An additional phase 1 study, BCX1812- 117, was initiated to evaluate the effect of needle length adjustment according to gender and bod y m ass index on the pharm acokinetics and s afety of peramivir fo llowing vent rogluteal int ramuscular injection, and dors ogluteal intram uscular injection in a subgroup o f subjects. Interim data are available for the first 40 subjects who received single peram ivir doses of 600 m g, co nsisting of directly obse rved tolerabilit y assessments, safety laboratory studies, reporte d adverse even ts, and pharmacokinetic data. Clinical laboratory results obtained 72 hours after dosing showed no abnorm alities with reg ards to hematology or urinary analytes and the only chemistry analytes outside normal ranges (CK and AST) were related to receipt of intramuscular injection. A majority of the first 40 subjects treated com plained of acute pain immediately after injection at the ventrogluteal site and a num ber of these subj ects reported that the pain w as also assoc iated with muscle cramping. Some subjects reported radiation of pain to the lower extremities. In most instances, these reactions abated after 15-30 minutes. This protocol also evaluated the acute tolerab ility of doses of 450 m g and 600 mg of perami vir administered at the dors ogluteal site. Direct observations deter mined that the use of the dorsogluteal injection site resulted in an acute tolerability profile of the 600 mg dose of peramivir that was i mproved com pared to that observed w ith ventrogl uteal site injections. However, a number of th ese subjects also experienced acute pain and discomfort and some reported muscle cramping in the gluteal area which persisted for up to 30 minutes. In summary, this study confirmed that the intram uscular injection of peram ivir results in acute pain and discomfort after gluteal injection in the majority of subjects in whom total doses of up to 600mg are adm inistered. In some subjects, the ac ute pain at the injection site may also b e 337 337 BCX1812-311 (V3.0: 20-November-2007) Page 22 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL associated with muscle cramping. Based on these findings, the dorsogluteal site will be util ized in future trials. The safety data for i.m. peramivir administered as single doses ranging from 75 mg to 600mg at the dorsogluteal injection site in each of the 3 phase 1 studies conducted to date have been unremarkable. No serious adverse events were reported. The most commonly observed adverse events or laboratory abnormalities were injection site pain or discomfort, headache, and transient increases in muscle enzymes (CK). There have been several reports of signs and symptoms of self-limited vasovagal reactions following injections.. No consistent differences in frequency of adverse events or laboratory toxicities were observed between the active and placebo treatment groups in the controlled phase 1studies, with the exception that CK elevations appeared to be dose related in the peramivir treatment groups. 5.6 Phase 2 Experience with Intramuscular Peramivir A phase 2 study BCX1812-211 was completed in 2007. This study was a randomized, double- blind placebo- controlled study to evaluate the efficacy and safety of two single dose regimens of peramivir. A total of 344 subjects were enrolled into this study with 115 subjects randomized to Placebo; 114 subjects randomized to peramivir 150 mg; and 114 subjects randomized to peramivir 300 mg. The primary endpoint of the study was the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. Based on preliminary data, the primary endpoint of time to alleviation of clinical symptoms in BCX1812-211 did not achieve statistical significance in the pre-planned ITTI study population (Table 3).. Based on pre-planned and post hoc analyses, it appeared that a majority of subjects within this phase 2 study did not receive an adequate intramuscular injection. In phase 1 studies (Hi m-06-111 and Him-06-112) of i.m . per amivir, significant increases in creatine kinase (CK) were observed at Day 3 compared with Baseline (Day 1) in all subjects who received active study drug or placebo. CK is a well established marker of muscle damage, and it was hypothesized that CK increase may act as a surrogate marker of an adequate i.m. injection. Within the phase 2 study, an increase in CK between Baseline (Day 1) and Day 3 was not observed in a majority of subjects. In the phase 1 studies study drug was administered with a 1½ inch needle. In the phase 2 study a shorter needle (1 inch) was supplied with the study drug, with guidance that a longer needle (1½ inch) should be used for larger subjects. Based on the observed lack of CK increases at Day 3 compared to baseline, the Sponsor hypothesized that the needle used for injection failed to penetrate muscle and deliver intramuscular study medication in many subjects. A sub group of subjects was identified in which a Day 3 CK increase of at least 50U/L was observed over baseline. Within this adequate intramuscular injection sub-group, notable improvements in the time to alleviation of symptoms were observed for both peramivir dose groups: 44.6 hours for peramivir 150 mg treatment and 64.8 hours for the peramivir 300 mg treatment 338 338 BCX1812-311 (V3.0: 20-November-2007) Page 23 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 3). A further sub-group analysis suggested that in subjects with an influenza B infection confirmed by PCR a single dose of peramivir had marginal activity (Table 3). These efficacy data support the further development of peramivir as a single dose, intramuscular treatment for acute influenza. 339 339 BCX1812-311 (V3.0: 20-November-2007) Page 24 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 3 Summary of Efficacy from BCX1812-211. Placebo Peramivir 150mg Peramivir 300mg Intent-to-Treat Infected Population1 (n=313) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=107 137.0 115.9-163.8 n=104 114.1 95.2-145.5 22.9 n=102 115.9 77.8-136.6 21.1 Adequate Injection Population2 (n=101) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=40 152.2 103.8-183.9 n=32 107.6 76.8-175.1 44.6 n=29 87.4 40.8-163.8 64.8 ITTI Influenza A infected population (n=247) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=83 138.4 117.0-173.4 n=85 115.7 92.2-145.5 22.7 n=79 115.9 51.1-195.9 22.5 ITTI Influenza B infected population (n=66) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=24 117.1 100.3-162.3 n=19 100.8 68.2-162.0 16.3 n=23 123.3 67.5-178.7 -6.2 1: Intent-to-Treat Infected Population: PCR+ for either Influenza A and/or Influenza B at baseline/screening visit. 2: Adequate Injection Population: ITTI subjects in who study drug reached target muscle tissue, as evidenced by an increase in serum CK levels of ≥ 50 U/L over baseline at the Day 3 study visit. An independent data monitoring committee reviewed grouped blinded safety data throughout study BCX1812-211. In the overall safety population (n=342), doses of peramivir 150 mg and 300 mg were both found to be well tolerated and no safety concerns were identified by the DMC. The three treatment groups were similar with respect to the frequency and severity of adverse events. Two serious adverse events were reported in the study, and neither was considered by the investigator to be related to treatment. One SAE (pyelonephritis) occurred 5-days after study treatment in a subject who received placebo, and one SAE (meningitis, resulting in death) occurred 10-days after study treatment in a subject who received 300 mg of peramivir. There were no meaningful differences among the three treatment groups with respect to the frequency or severity of graded laboratory toxicities. A summary of the adverse events and graded toxicities, together with a list of the most frequently reported adverse events, is presented in Table 4. 340 340 BCX1812-311 (V3.0: 20-November-2007) Page 25 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 4 Summary of Safety from BCX1812-211. Safety Parameters Placebo (N=114) Peramivir 150 mg (N=113) Peramivir 300 mg (N=115) Any Clinical Adverse Event 49 (43%) 43 (38%) 44 (38%) Any Graded Laboratory Toxicity 99 (87%) 93 (82%) 92 (80%) Any Serious Adverse Event 1 (<1%) 0 1 (<1%) Most Frequent Adverse Events Assessed as Study Drug-Related Diarrhea Nausea Vasovagal Reaction 5 (4%) 7 (6%) 4 (4%) 5 (4%) 7 (6%) 2 (2%) 6 (5%) 9 (8%) 0 5.7 Dose Rationale Oseltamivir is approved for the treatment of uncomplicated acute influenza at a dosage of 75mg twice daily in adults14. Oseltamivir was shown to be clinically effective in a phase 3 study of oral oseltamivir versus placebo in naturally occurring seasonal influenza, and these data were sufficient for regulatory approval for marketing of oseltamivir. At least 75% of an oral dose of oseltamivir reaches the systemic circulation as oseltamivir carboxylate. When oseltamivir is administered orally at a dose of 75mg twice daily, the serum Cmax of oseltamivir carboxylate is approximately 348ng/mL and the AUC0-48 is 10,876 h·ng/mL. The clinical data indicate that this level of exposure to oseltamivir was sufficient to provide clinical improvement in uncomplicated acute influenza. The serum pharmacokinetic data (Cmax and AUC0-∞, respectively) following intramuscular doses of peramivir are approximately 7600ng/mL and 24,000 h·ng/mL for the 150mg dose and are approximately 15,000ng/mL and 49,000 h·ng/mL for the 300mg dose. Previous studies have assessed the concentrations of the neuraminidase inhibitor zanamivir in nasal and pharyngeal secretions after parenteral administration of this drug. . Within several hours after administration, the concentrations in secretions were approximately 100-fold lower than in serum or plasma. In theory, relatively high levels of a neuraminidase inhibitor in respiratory secretions are desirable in order to rapidly inactivate influenza virus and to delay or prevent the development of resistance in infecting virus strains. Intramuscular doses of peramivir, including doses of 300mg and 600mg have been shown to be well tolerated in previous Phase 1 studies. In the completed Phase 2 study, both doses of peramivir (150 mg and 300 mg) were well tolerated and no safety concerns were apparent. As evidence of a dose response between the 150mg and 300mg doses was observed in the phase 2 study, it is possible that a higher dose of 600mg of peramivir may further improve the treatment response observed in study 211. Therefore, it is appropriate to evaluate two dose regimens of 300mg and 600mg to undergo further evaluation in this Phase 3 study. 341 341 BCX1812-311 (V3.0: 20-November-2007) Page 26 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6 STUDY OBJECTIVES 6.1 Objectives 6.1.1 Primary Objective To evaluate the efficacy of peramivir administered intramuscularly compared to placebo on the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. 6.1.2 Secondary Objective(s) The secondary objectives of this study are: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly, 2. To evaluate secondary clinical outcomes in response to treatment, 3. To evaluate changes in influenza virus titer in nasopharyngeal samples (viral shedding) in response to treatment. 6.1.3 Exploratory Objective(s) The following exploratory objectives have been identified for this study. 1. To assess pharmacoeconomic measures as response to treatment. 2. To assess changes in influenza viral susceptibility to neuraminidase inhibitors following treatment. 6.2 Study Endpoints 6.2.1 Primary Endpoint The primary clinical endpoint is the time to alleviation of clinical symptoms of influenza in subjects with influenza A. 6.2.2 Secondary Endpoint(s) Secondary safety, clinical, and virologic endpoints will include evaluations in each subject of: Safety: Incidence of treatment-emergent adverse events and treatment-emergent changes in clinical laboratory tests. Clinical: Time to resolution of fever; Incidence of influenza related complications. Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID50). 342 342 BCX1812-311 (V3.0: 20-November-2007) Page 27 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6.2.3 Exploratory Endpoints Pharmacoeconomic and virologic evaluations in each subject for exploratory endpoints will also be assessed and include: Pharmacoeconomic: Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. Virologic: Quantitative change in influenza virus shedding, measured by PCR; Change in influenza virus susceptibility to neuraminidase inhibitors. 7 STUDY DESIGN 7.1 Overall Study Design and Plan This is a multinational, randomized, double-blind study comparing the efficacy and safety of two single dose regimens of peramivir administered intramuscularly versus placebo in adults with uncomplicated acute influenza. Up to a total of 750 evaluable subjects will be randomized to treatment (150 subjects in the placebo treatment group, 300 subjects in the peramivir 300mg treatment group and 300 subjects in the peramivir 600mg treatment group). Each subject’s assignment to treatment will be stratified according to smoking status. All subjects will be centrally randomized to one of three treatment groups in a ratio of 2:2:1 such that 80% of subjects are randomized to one of the two single dose regimens of peramivir. Treatment Group 1: Peramivir 300mg Treatment Group 2: Peramivir 600mg Treatment Group 3: Placebo Study drug will be administered as bilateral 4mL intramuscular injections (total of 8mL injected in equally divided doses). Procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. Subjects eligible for screening will have an anterior nasal swab collected for testing by RAT for influenza A and B, in accordance with the commercially available RAT kit instructions. If the initial RAT is negative, the test should be repeated within one hour. Subjects meeting the inclusion/ exclusion criteria may be enrolled into the study. All enrolled subjects will record the following information in a Study Diary. • Assessment of the presence and severity of each of seven symptoms of influenza on a 4-point scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatment, then once daily (AM) through Day 14. 343 343 BCX1812-311 (V3.0: 20-November-2007) Page 28 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL • Oral temperature measurements will be taken with an electronic thermometer every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol) or other antipyretic medication. • Assessment of subject’s time lost from work or usual activities and rating of productivity compared to normal (rated as 0-10 on a visual analog scale) once daily through Day 14 • Doses of antipy retic, expectorant, and/or th roat lozenges taken for s ymptomatic relief each day through Day 14 Anterior nose (bilateral) and posterior pharynx specimens (swabs) will be collected at Day 1 (pre- treatment) and at Days 3, 5, and 9, for quantitative virologic assessments. Specimens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result) as well as other virologic assessments (e.g. PCR, genotypic testing). All virologic assessments will be performed by a central laboratory. Two samples for pharmacokinetic (PK) testing for plasma levels of peramivir will be obtained from all subjects randomized. The first PK sample will be obtained between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be obtained at the day 3 visit in all subjects. The data from these PK samples will be utilized in a population exposure-response analysis. At selected sites a separate sub-study will be conducted to collect additional PK samples between treatment and Day 3 for the purpose of conducting a separate exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Study drug will be administered as bilateral 2mL intramuscular injections (total of 4mL injected in divided doses). Procedures for intramuscular injection, with a recommended needle length appropriate to the size and weight of the subject, are provided in the study drug administration manual. 8 SELECTION AND WITHDRAWAL OF SUBJECTS 8.1.1 Inclusion Criteria Subjects must meet all of the following criteria for inclusion in this study: 1. Male and non-pregnant female subjects age ≥18 years. 2. A positive Influenza A Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate anterior nasal specimen, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated within one hour. Subjects with a positive influenza B or mixed A and B RAT will be excluded. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. A subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at the time of screening. 344 344 BCX1812-311 (V3.0: 20-November-2007) Page 29 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of at least moderate severity. 5. Presence of at least one constitutional symptom (myalgia [aches and pains], headache, feverishness, or fatigue) of at least moderate severity. 6. Onset of symptoms no more than 48 hours before presentation for screening. 7. Written informed consent. 8.1.2 Exclusion Criteria Subjects to whom any of the following criteria apply will be excluded from the study: 1. Women who are pregnant or breast-feeding. 2. Presence of clinically significant signs of acute respiratory distress 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma. (See Section 15.2). 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class III or IV functional status within the past 12 months. (See Section 15.1). 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 6. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min). 7. Clinical evidence of worsening of any chronic medical condition (temporally associated with the onset of symptoms of influenza) which, in the investigator’s opinion, indicates that such finding(s) could represent complications of influenza. 8. Current clinical evidence, including clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis and/or pneumonia, or active bacterial infection at any body site that requires therapy with oral or systemic antibiotics. 9. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy which would include oral or systemic treatment with > 10 mg prednisone or equivalent on a daily basis within 30 days of screening. 10. Currently receiving treatment for viral hepatitis B or viral hepatitis C. 11. Presence of known HIV infection with a CD4 count <350 cell/mm3. 12. Current therapy with oral warfarin or other systemic anticoagulant. 13. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening. 14. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days. 15. Immunized against influenza with inactivated virus vaccine within the previous 14 days. 16. Receipt of any intramuscular injection within the previous 14 days. 17. History of alcohol abuse or drug addiction within 1 year prior to admission in the study. 18. Participation in a previous study of intramuscular or intravenous peramivir or previous participation in this study. 19. Participation in a study of any investigational drug or device within the last 30 days. 345 345 BCX1812-311 (V3.0: 20-November-2007) Page 30 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 8.1.3 Removal of Subjects from Therapy or Assessment All subjects are permitted to withdraw fro m participation in this study at any ti me and for any reason, specified or unspecified, and without prejudice. T he Investigator or sp onsor m ay terminate the subject’s participation in the study at any time for reasons including the following: 1. Adverse event; 2. Intercurrent illness; 3. Non-compliance with study procedures; 4. Subject’s decision; 5. Administrative reasons; 6. Lack of efficacy; 7. Investigator’s opinion to protect the subject’s best interest. Any subject who withdraws because of an adve rse event will be followe d until the sign(s) or symptom(s) that constituted the adverse event has/ha ve resolved or is determ ined to represent a stable medical condition. A subject should be with drawn from the trial if, in the opinion of the Investigator, it is medically necessary, or if it is the desire of the subject. If a subject does not return for a scheduled visit, every effort should be made to contact the subject and determine the subject’s medical condition. In any circumstance, every effort should be made to document subject outcome, if possible. If the subject withdraws consent, no fu rther ev aluations should b e perfo rmed and no attempts should be made to collect additional data. 9 TREATMENTS 9.1 Treatments Administered Peramivir is an investigational drug. Peramivir for intramuscular injection is a small-volume parenteral and will be supplied as a 75mg/mL solution in sodium citrate/ citric acid buffer. The pH is approximately 3.0. A matched placebo solution of sodium citrate/ citric acid buffer with 1.2% sodium chloride at a pH of approximately 3.0 will be supplied. The gluteal site of injection and the syringe needle length are to be recorded in the subjects CRF. Procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. 9.2 Identity of Investigational Product(s) Peramivir and placebo peramivir will be supplied in clear 2mL vials. An individual study drug kit will contain 2 vials of blinded study drug (peramivir and/or placebo, depending upon the treatment group). Syringes and needles will be provided in which to draw up the solution for intramuscular injection. All study drug kits must be stored at 2-8oC. 346 346 BCX1812-311 (V3.0: 20-November-2007) Page 31 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Each individual study drug kit will be labeled with some or all of the following information as required by local regulations: • Sponsor name and contact information, study protocol number, kit number, description of the contents of the container, instructions for the preparation of the syringe and administration of the study drug, conditions for storage, statement regarding the investigational (clinical trial) use of the study drug and date for retest or expiry date. Each vial of study drug will be labeled with some or all of the following information as required by local regulations: • Sponsor name, study protocol number, description of the contents of the vial, instructions for the preparation of the syringe, statement regarding the investigational (clinical trial) use of the study drug and lot number. 9.3 Method of Assigning Subjects to Treatment Groups Subjects will be centrally randomized according in a ratio of 2:2:1 to one of three treatment groups: single dose peramivir 300mg, single dose peramivir 600mg or placebo, in accordance with a computer-generated randomization schedule prepared by a non-study statistician. Eighty percent (80%) of subjects will be randomized to treatment with one of the two single dose regimens of peramivir, 20% will be randomized to treatment with placebo. Each subject’s assignment to treatment will be stratified according to smoking status. Once a subject is eligible for randomization, he/she will be assigned two study drug kit numbers that will be obtained by study staff from the study interactive voice response system (IVRS). Once a study drug kit number has been assigned to a subject, it cannot be reassigned to any other subject. 9.4 Study Medication Accountability The Investigator/pharmacist must maintain accurate records of the disposition of all study drugs received from the sponsor, issued to the subject or directly administered to the subject (including date and time), and any drug accidentally destroyed. The sponsor will supply a specific drug- accountability form. At the end of the study, information describing study drug supplies (e.g., lot numbers) and disposition of supplies for each subject must be provided, signed by the Investigator or designee, and collected by the study monitor. If any errors or irregularities in any shipment of study medication to the site are discovered at any time, the Project Manager must be contacted immediately. At the end of the study, all medication not dispensed or administered and packaging materials will be collected with supervision of the monitor and returned to the sponsor or destroyed on site as dictated by the appropriate Standard Operating Procedure at the participating institution. 9.5 Blinding/Unblinding of Treatments This is a double-blind study. The treatment group assignment will not be known by the study subjects, the investigator, the clinical staff, the CRO or Sponsor staff during the conduct of the study. 347 347 BCX1812-311 (V3.0: 20-November-2007) Page 32 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Section 11.2.4 provides information regarding the process for unblinding the treatment assignment, if necessary, in the event of an SAE. 9.6 Prior and Concomitant Therapies All medications, by any route of administration, used during this study must be documented on the Case Report Form (CRF). Prescription as well as non-prescription medications should be recorded. Medication used for the treatment of influenza-related symptoms will be captured by the subject in the diary card provided by BioCryst. 9.7 Overdose and Toxicity Management To date there is no experience with overdose of intramuscular or intravenous peramivir. If overdose occurs, subjects should receive indicated supportive therapy and evaluation of hematologic and clinical chemistry laboratory tests should be conducted. The effect of hemodialysis on elimination of peramivir is unknown. 9.8 Dose Interruption As this is a study of a single dose of peramivir or placebo, guidelines for treatment interruption for drug related SAEs or toxicities are not applicable. 10 STUDY CONDUCT A study schedule of evaluations is presented in Figure 1. A detailed list of the evaluations and visits is also provided in the following sections. 10.1 Evaluations All subjects enrolled in this study will undergo the following evaluations: 10.1.1 Informed Consent Prior to any study-related procedure subjects will be administered informed consent. For further discussion of consent see section 10.2.1. 10.1.2 Medical History Medical history, influenza vaccination status within the previous 12 months and demographic data (including smoking behavior) will be recorded at Screening/Baseline. 10.1.3 Rapid Antigen Test for Influenza At Screening/Baseline, a commercially available, rapid antigen test (RAT) for influenza A will be performed on an adequate specimen collected by swabbing the anterior nose in accordance with the RAT manufacturer’ instructions. A negative initial RAT should be repeated within one hour. Subjects with a positive influenza B or mixed A and B RAT will be excluded. Refer to the Study Manual for instructions regarding the use of the RAT kits provided for this study. Sites may use the kits provided by the Sponsor or any other commercially approved RAT available at their site to document a confirmed influenza infection. 348 348 BCX1812-311 (V3.0: 20-November-2007) Page 33 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.4 Physical Examination and Influenza-related Complications Assessments The Investigator will perform a physical examination at Screening/Baseline. Subject’s height and weight, and BMI will be recorded at Screening/Baseline in the subjects CRF. Study personnel will be provided with an influenza-related complications (IRC) checklist in the CRF to evaluate the subject for the presence of clinical signs and/or symptoms of the following influenza-related complications: sinusitis, otitis, bronchitis and pneumonia. Note that subjects with clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis, and/or pneumonia at screening are not eligible for enrollment in this study (See Section 8.1.2: exclusion criteria number 8). A targeted physical examination will be conducted at each visit to record the presence/absence of influenza related complications (IRC). If the investigator determines that the subject experiences (or is presumed to experience) an IRC as noted above, he/she will record that assessment on the IRC CRF page and any medication used to treat the condition will be recorded on the concomitant medication page. The investigator will promptly provide appropriate treatment for any suspected or proven IRC. Such information describing IRC signs and/or symptoms should not be reported as adverse events. Any injection site reactions noted will be recorded in the CRFs as adverse events. 10.1.5 Vital Signs Vital signs evaluations will include blood pressure, pulse rate, and respiration rate. The investigator will record oral or rectal body temperature at baseline. Thereafter the subject will record oral temperature twice daily in the study diary card. Vital signs will be measured at Screening/Baseline, pre-dose, and at 15 minutes following the study drug injection on Day 1, then once daily on Days 3, 5, 9, and 14. 10.1.6 Electrocardiogram Measurements A 12-lead electrocardiogram (ECG) will be obtained at Screening/Baseline. The principal investigator will be responsible for interpretation of the Screening ECG. This interpretation may be performed by the investigator or he/she may delegate this action to another physician and the investigator will acknowledge the interpretation. If this baseline ECG is interpreted as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal but does not meet the exclusionary criteria, the subject may be enrolled unless other exclusion criteria apply. The principal investigator is responsible to ensure that such an enrolled subject be informed of the nature of the abnormal ECG and that any medically indicated repeat ECG examinations and/or referral of the subject for further evaluation is made either during subject's participation in the study or immediately after the subject's discharge from the study. 10.1.7 Clinical Laboratories Clinical chemistry profiles will include a Chemistry 20 panel (includes sodium, potassium, chloride, total CO2 [bicarbonate], creatinine, glucose, urea nitrogen, albumin, total calcium, total magnesium, phosphorus, alkaline phosphatase, alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin, direct bilirubin, lactate dehydrogenase [LDH], total protein, total creatine kinase, and uric acid). 349 349 BCX1812-311 (V3.0: 20-November-2007) Page 34 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Hematology will include complete blood count (CBC) with differential. Urinalysis will include dipstick tests for protein, glucose, ketones, blood, urobilinogen, nitrite, pH, and specific gravity and microscopic evaluation for RBCs and WBCs. For any subject with a Day 3 positive test for urine protein by dipstick test of 2+ or higher, who had a Baseline/ Day 1 protein dipstick of <2+, a 24 hour urine collection for assessment of protein and a simultaneous assessment by UPEP on the same specimen will be obtained. Clinical laboratory studies (clinical chemistries, hematology, and urinalysis) will be completed at Screening/Baseline, and on Days 3, 5 and 14. 10.1.8 Urine Pregnancy Test Females of childbearing potential will be evaluated for pregnancy at Screening/Baseline and Day 14 using a urine pregnancy test. 10.1.9 Serology for Influenza Paired blood samples for determination of antibody to influenza A and B (serology) will be obtained with the clinical laboratory tests at Screening/Enrollment and at Day 14. These specimens will be stored at the central laboratory and will be analyzed if needed to confirm the diagnosis of influenza. 10.1.10 Samples for Virologic Laboratory Assessments An adequate specimen will be collected by swabbing the anterior nose (bilateral) and posterior pharynx for virologic laboratory assessments including culture for the isolation of influenza virus and/or quantitative PCR assay at Screening/Baseline, and at Days 3, 5, and 9. Refer to the Laboratory Manual for instructions regarding the processing and shipment of these specimens. 10.1.11 Subject Self Assessments Subject self assessments will be performed beginning pre-dose on Day 1 and recorded in the subject’s Study Diary including the following: • Oral temperature measurements with an electronic thermometer (provided by the Sponsor for the study) every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol, provided) or other anti-pyretic medications. The times of each temperature determination will be recorded in the Study Diary. The baseline temperature will be recorded at the screening/Day 1 visit prior to dosing, regardless of whether the subject had recently taken an anti-pyretic; the time of anti-pyretic use pre- treatment will be recorded in the CRF, if applicable. • Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [aches and pains], headache, feverishness, and fatigue) on a 4-point severity scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily, beginning pre-dose on Day 1 and through Day 9, then once daily through Day 14. • Assessment of the subject’s time lost from work or usual activities and productivity compared to normal using a 0-10 visual analogue scale once daily through Day 14. The subject’s diary card will be reviewed by study staff at each visit for completion of the record 350 350 BCX1812-311 (V3.0: 20-November-2007) Page 35 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL of all required items, with particular emphasis on alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the recurrence of at least one respiratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours and the presence of fever (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Study staff will not attempt to ask subjects to retrospectively complete missing diary card data for any scheduled assessments that have not been completed prior to the clinic visit. Study staff should, however, remind the subject to complete the diary card at all scheduled times. 10.1.12 Concomitant Medications All concomitant medications used during this study, with the exception of those medications taken for symptomatic relief of influenza symptoms, which will be recorded by the subject in their diary card, must be documented on the Case Report Form (CRF). 10.1.13 Adverse Events AEs will be assessed from the time of administration of study medication through the final study visit. 10.1.14 Pharmacokinetic Exposure Samples All subjects will have two pharmacokinetic (PK) samples drawn to assess peramivir drug levels. The first PK sample will be drawn on day 1 between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be drawn at the day 3 visit in all subjects. The sample will be drawn at the same time as the blood draw is completed for clinical laboratory investigations. The 30-60 minute sample (treatment day 1) and the day 3 PK sample will be analyzed for plasma concentrations of peramivir (ng/mL) and evaluated in a population exposure response analysis. At selected sites a separate sub-study will also be conducted to collect additional PK samples for the purpose of conducting an exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Data from these two PK samples in all subjects will be combined with data from the PK sub-study (BCX1812-311PK) to perform a population based exposure-response analysis. This analysis will be described as part of the sub-study analysis plan. All PK samples will be processed at a central bioanalytical laboratory. Refer to the instructions provided regarding the processing and shipment of these PK samples. 10.2 Screening Period 10.2.1 Informed Consent The nature and purpose of the study and the expectations of a participating subject will be described to potential study subjects, their questions will be answered, and the subjects will then be asked to sign an informed consent document. Study subjects will then undergo the screening evaluation as noted in Section 10.2.2 10.2.2 Screening/Baseline Evaluation and Enrollment Screening/baseline evaluation may be conducted in the investigator’s office or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and 351 351 BCX1812-311 (V3.0: 20-November-2007) Page 36 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL qualified staff. Clinical laboratory assessments performed at Screening are for the purpose of establishing a baseline. Subjects may be enrolled and receive treatment with study drug prior to receiving results of the laboratory assessments (with the exception of urine pregnancy test result, which must be known). Eligible subjects will be enrolled and randomized to blinded study treatment. The randomization will be stratified by smoking status. The Investigator will prepare a request for blinded study drug assignment which includes the subject’s screening number. The Investigator or designee at the clinical study center will contact the central randomization Interactive Voice System (IVRS call center). The IVRS call center will advise the study center of the two investigational study drug kit numbers that are assigned to that subject at enrollment. Subjects that are determined to be ineligible will be advised accordingly, and the reason for ineligibility will be discussed. If desired by the subject the reason for ineligibility may be provided and/or discussed with their health-care provider by the Investigator or designee. Ineligible subjects who have been screened for the study will also be entered on the IVRS. For such subjects, the screening number assigned, subject’s date of birth and a reason for ineligibility will be entered on to the IVRS. All ineligible subjects must be entered onto the IVRS within 24 hours of screening, to assist with surveillance analysis during the course of the study. 10.3 Treatment Period—Study Day 1 Day 1 represents the only day of study drug dosing. Study drug administration should occur as soon as possible following informed consent, screening and randomization. Therefore, it is expected that the date of Screening/ Baseline and Day 1 will usually be the same date. 10.3.1 Pre-dose Evaluations-Study Day 1 Following an explanation of the Subject Self Assessment measures (Section 10.1.11), the subject shall complete the record of these assessments in their Study Diary prior to dosing. The subject will be counseled regarding the expectations for recording these assessments through Day 14. Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) and a 12 lead ECG will be obtained prior to dosing. A nasopharyngeal swab for influenza culture/ PCR assay will be obtained prior to dosing. 10.3.2 Post-dose Evaluations-Study Day 1 The blinded study drug will be administered (hour 0) as bilateral intramuscular injections within a period of ≤ 10 minutes. The calendar date and 24-hour clock time of the first and second injections will be recorded. The gluteal site of injection and the syringe needle length are also to be recorded in the subjects CRF. Sites are instructed to follow procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, provided in the study drug administration manual. The following evaluations will be performed post-dose on Study Day 1: 352 352 BCX1812-311 (V3.0: 20-November-2007) Page 37 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL • Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) 15 minutes following the second intramuscular injection of blinded study drug; record the exact 24-hour clock time of the vital sign measurements in the subjects CRF. • Draw a PK sample between 30 and 60 minutes following the second intramuscular injection of blinded study drug; record the exact 24-hour clock time of the blood draw. • Record any concomitant medications. • Record any AEs. 10.4 Post-Treatment Assessment Period 10.4.1 Days 2, 3, 5, 9 and 14 Study evaluations will be performed on Days 2, 3, 5, 9 and 14 in accordance with the schedule of evaluations (Figure 1). Subjects with persistent moderate or severe influenza symptoms at day 14 will also complete a Day 21 visit, and if required a Day 28 visit. Visits may be conducted in the investigator’s office or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and qualified staff. Study staff will attempt to contact the subjects on Day 2 by telephone to confirm their compliance with completion of the Subject Self Assessments, to note any concomitant medications and adverse events. Any adverse events reported by the subject during this telephone contact will be recorded on the adverse event form and verified during the visit on day 3. For any subject with a Day 3 positive test for urine protein by dipstick test of 2+ or higher, who had a Baseline/ Day 1 protein dipstick of <2+, a 24 hour urine collection for assessment of protein and a simultaneous assessment by UPEP on the same specimen will be obtained. At each visit it is important that the subject’s Study Diary record be reviewed for completion of daily Subject Self Assessments. The subjects should be counseled as necessary regarding self assessments and Study Diary record requirements. The subject’s diary card will be reviewed by study staff for alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the recurrence of at least one respiratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours and the presence of fever (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Day 3: The second PK sample for all subjects will be obtained on Day 3 at the same time as the clinical laboratory blood specimen is obtained. The exact 24-hour clock time of the blood draw will be recorded in the subjects CRF. Day 14: If a subject has one or more persistent or recurrent symptoms of influenza (of the seven symptoms assessed) of either moderate or severe intensity at the Day 14 visit then the subject must be evaluated in further follow-up visits, at day 21 (± 3 days), and if required at day 28 (± 3 days) If a subject reports moderate or severe influenza symptoms then the investigator will 353 353 BCX1812-311 (V3.0: 20-November-2007) Page 38 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL record the intensity of each of the influenza symptoms on a visit specific CRF page at the day 21 and day 28 visits. After day 14 the subject will not record symptoms in a diary. Day 21 (if applicable): The day 21 visit is to be completed only if the subject reports symptoms of influenza of moderate or severe intensity at day 14. The investigator will make a clinical judgment as to the appropriate medical course of action for such subjects at the Day 21 visit and such action(s) will be recorded on the Day 21 CRF page. The investigator will recall the subject for a further study visit at day 28 (± 3 days) if moderate or severe symptom(s) of influenza persist at Day 21. Day 28 (if applicable): The day 28 visit is to be completed only if the subject reports symptoms of influenza of moderate or severe intensity at day 21. The investigator will make a clinical judgment as to the appropriate medical course of action for such subjects at this visit and such action(s) will be recorded on the Day 28 CRF page. No further follow-up visits beyond day 28 are to be formally scheduled unless in the clinical judgment of the investigator further follow-up is required. The investigator will use his/her clinical judgment to manage the subject, referring the subject, if appropriate, for further medical care. 10.4.2 Adverse Events Reported at Post-treatment Visits In this study, symptoms of influenza will be considered separately from adverse events reported during the post-treatment period. Accordingly, adverse events that have onset in the post- treatment period will be assessed and followed as specified in 11.2. Specifically, the investigator should attempt to follow all unresolved AEs and/or SAEs observed during the study until they are resolved, or are judged medically stable, or are otherwise medically explained. 354 354 BCX1812-311 (V3.0: 20-November-2007) Page 39 Figure 1 Study Measurements and Visit Schedule Treatment Period Assessment Day End of Study Early Withdrawal Assessments Screening 1 (Baseline) Day 11 Day 22 Day 3 Day 5 (±1 day) Day 9 (±3 day) Day 14 (±3 day) 8 Informed Consent X Rapid Antigen test for Influenza A X Medical History/Physical Exam X Influenza-related complications checklist3 X X X X X Inclusion/Exclusion X Clinical Chemistries4 X X X X Hematology4 X X X X Exposure Pharmacokinetic Sample9 X X4 Serology (serum) Sample X X Urinalysis10 X X4 X X Urine Pregnancy Test X X Vital Signs5 X X X X X X ECG6 X Sample (nasopharyngeal swab) for Influenza Virus Culture/ PCR assay and for resistance studies X X X X Study Drug Administration X Subject Diary Review7 X X X X X X Concomitant Medications X X X X X X X Adverse Events X X X X X X Study Measurements and Visit Schedule Figure Legend on Next Page BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 355 355 BCX1812-311 (V3.0: 20-November-2007) Page 40 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Study Measurements and Visit Schedule Figure Legend 1 It is expected that the date of Screening and Day 1 (date of administration of study drug) will be the same. Visits at Screening and on subsequent study days may occur in subject’s home by the investigator (all visits) or appropriately trained study center staff (Day 3, 5, 9 visits). 2 Day 2 will be a telephone contact with the subject to ensure compliance with diary card completion, concomitant medication and adverse event review. 3 A targeted physical examination will be conducted at each visit to record the presence/absence of influenza related complications. 4 Clinical laboratory assessments performed at Screening are for the purpose of establishing a baseline. Subject may be enrolled and begin treatment with study drug prior to receiving results. A PK sample will be drawn 30-60 minutes following the second treatment administration injection. On Day 3 an extra tube will be included with the safety blood sample to collect the second PK sample for evaluation of peramivir concentrations. For any subject with a Day 3 positive test for urine protein by dipstick test of 2+ or higher, who had a Baseline/ Day 1 protein dipstick of <2+, a 24 hour urine collection for assessment of protein and a simultaneous assessment by UPEP on the same specimen will be obtained. 5 Vital sign measures will include blood pressure, pulse rate and respiration rate. Vital signs will be recorded at Screening, pre-dose and at 15 min following the study drug administration on Day 1, then once on remaining days as stipulated. The investigator will record oral temperature at baseline. Thereafter the subject will report oral temperature measurements twice daily in the Study Diary 6 If the baseline ECG is interpreted by the conducting physician as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal and does not meet the exclusionary criteria (e.g. acute ischemia, medically significant dysrhythmia) then this subject may be enrolled If the conditions highlighted in section 10.1.5 are met for the subject. 7 Subjects record symptom assessment in Study Diary, twice daily, beginning pre-dose on Day 1 through Day 9, then once daily through Day 14. Subjects record time lost from work or usual activities and rating of productivity compared to normal once daily through Day 14. Subjects record oral temperature twice daily throughout as well as all influenza related medications. 8 For any subject with unresolved moderate or severe intensity influenza symptoms a follow up assessment will be scheduled at Day 21 (± 3 days) and Day 28 (± 3 days) if required (See Section 10.4.1). 9 A PK sample will be drawn 30-60 minutes following the second treatment injection on Day 1, and on Day 3.. 10.For any subject with a Day 3 positive test for urine protein by dipstick test of 2+ or higher, who had a Baseline/ Day 1 protein dipstick of <2+, a 24 hour urine collection for assessment of protein and a simultaneous assessment by UPEP on the same specimen will be obtained. 356 356 BCX1812-311 (V3.0: 20-November-2007) Page 41 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11 ADVERSE EVENT MANAGEMENT 11.1 Definitions 11.1.1 Adverse Event An AE is any untoward medical occurrence in a clinical study subject. No causal relationship with the study drug or with the clinical study itself is implied. An AE may be an unfavorable and unintended sign, symptom, syndrome, or illness that develops or worsens during the clinical study. Clinically relevant abnormal results of diagnostic procedures including abnormal laboratory findings (e.g., requiring unscheduled diagnostic procedures or treatment measures, or resulting in withdrawal from the study) are considered to be AEs. AEs may be designated as “nonserious” or “serious” (see Section 11.1.2). Surgical procedures are not AEs but may constitute therapeutic measures for conditions that require surgery. The condition for which the surgery is required is an AE, if it occurs or is detected during the study period. Planned surgical measures permitted by the clinical study protocol and the conditions(s) leading to these measures are not AEs, if the condition(s) was (were) known before the start of study treatment. In the latter case the condition should be reported as medical history. Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [aches and pains], headache, feverishness, and fatigue) will be documented in a subject’s study diary and analyzed as a measure of efficacy of the study treatment. These symptoms will not be reported as AEs unless the symptom(s) worsen to the extent that the outcome fulfils the definition of an SAE, which then must be recorded as such (see Section 11.1.2). Likewise, a RAT for influenza is required at screening in order to determine eligibility for the study, and therefore a positive RAT is not considered an AE. 11.1.2 Serious Adverse Event A SAE is an adverse event that results in any of the following outcomes: • Death • Is life-threatening (subject is at immediate risk of death at the time of the event; it does not refer to an event that hypothetically might have caused death if it were more severe) • Requires in-subject hospitalization (formal admission to a hospital for medical reasons) or prolongation of existing hospitalization • Results in persistent or significant disability/incapacity (i.e., there is a substantial disruption of a person’s ability to carry out normal life functions) • Is a congenital anomaly/birth defect • Is an important medical event Important medical events that may not result in death, are not life-threatening, or do not require hospitalization may be considered an SAE when, based upon appropriate medical judgment, they may jeopardize the subject or may require medical or surgical intervention to prevent one of the 357 357 BCX1812-311 (V3.0: 20-November-2007) Page 42 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL outcomes listed in this definition. Examples of such events include allergic bronchospasm requiring intensive treatment in an emergency room or at home, blood dyscrasias or convulsions that do not result in subject hospitalization, or the development of drug dependency or drug abuse. In addition Suspected Unexpected Serious Adverse Reactions (SUSAR) may also be reported to competent authorities where this type of reporting is required (e.g. European Union Directives). See section 11.2.3. 11.2 Method, Frequency, and Time Period for Detecting Adverse Events and Reporting Serious Adverse Events Reports of AEs are to be collected from the time of study drug administration through the follow-up period ending on Day 14. The Investigator or designee must completely and promptly record each AE on the appropriate CRF. The Investigator should attempt, if possible, to establish a diagnosis based on the presenting signs and symptoms. In such cases, the diagnosis should be documented as the AE and not the individual sign/symptom. If a clear diagnosis cannot be established, each sign and symptom must be recorded individually. The Investigator should attempt to follow all unresolved AEs and/or SAEs observed during the study until they are resolved, or are judged medically stable, or are otherwise medically explained. 11.2.1 Definition of Severity All AEs will be assessed (graded) for severity and classified into one of four clearly defined categories as follows: • Mild: (Grade 1): Transient or mild symptoms; no limitation in activity; no intervention required. The AE does not interfere with the participant’s normal functioning level. It may be an annoyance. • Moderate: (Grade 2): Symptom results in mild to moderate limitation in activity; no or minimal intervention required. The AE produces some impairment of functioning, but it is not hazardous to health. It is uncomfortable or an embarrassment. • Severe: (Grade 3): Symptom results in significant limitation in activity; medical intervention may be required. The AE produces significant impairment of functioning or incapacitation. • Life-threatening: (Grade 4): Extreme limitation in activity, significant assistance required; significant medical intervention or therapy required; hospitalization. 358 358 BCX1812-311 (V3.0: 20-November-2007) Page 43 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11.2.2 Definition of Relationship to Study Drug The blinded Principal Investigator must review each AE and make the determination of relationship to study drug using the following guidelines: Not Related: The event can be readily explained by other factors such as the subject’s underlying medical condition, concomitant therapy, or accident, and no temporal relationship exists between the study drug and the event. Unlikely: The event does not follow a reasonable temporal sequence from drug administration and is readily explained by the subject’s clinical state or by other modes of therapy administered to the subject. Possibly Related: There is some temporal relationship between the event and the administration of the study drug and the event is unlikely to be explained by the subject’s medical condition, other therapies, or accident. Probably Related: The event follows a reasonable temporal sequence from drug administration, abates upon discontinuation of the drug, and cannot be reasonably explained by the known characteristics of the subject’s clinical state. Definitely Related: The event follows a reasonable temporal sequence from administration of the medication, follows a known or suspected response pattern to the medication, is confirmed by improvement upon stopping the medication (dechallenge), and reappears upon repeated exposure (rechallenge, if rechallenge is medically appropriate). 11.2.3 Reporting Serious Adverse Events Any SAE / SUSAR (Suspected Unexpected Serious Adverse Reaction) must be reported to BioCryst or its designee within 24 hours of the Investigator’s recognition of the SAE by first notifying the Medical Monitor at the number listed below: Telephone: Europe: +44 1628 548000; North America: 1-888-724-4908 Facsimile: Europe: +44 1628 540028; North America: 1-888-887-8097 or 1-609-734-9208 In addition to the telephone numbers listed above, local country-specific toll free numbers may be provided within the study reference manual. The site is required to fax a completed SAE / SUSAR Report Form (provided as a separate report form) within 24 hours. All additional follow-up evaluations of the SAE / SUSAR must be reported and sent by facsimile to BioCryst or its designee as soon as they are available. The Principal Investigator or designee at each site is responsible for submitting the IND safety report (initial and follow-up) or other safety information (e.g., revised Investigator’s Brochure) to the Institutional Review Board/Independent Ethics Committee (IRB/IEC) and for retaining a copy in their files. 359 359 BCX1812-311 (V3.0: 20-November-2007) Page 44 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL If the Investigator becomes aware of any SAE / SUSAR occurring within 30 days after a subject has completed or withdrawn from the study, he or she should notify BioCryst or its designee. Any SAEs / SUSARs considered possibly related to treatment will be reported to the FDA and other Regulatory Competent Authorities as applicable via the MedWatch / CIOMS reporting system in accordance with FDA and other applicable regulations. However, the Investigator is not obligated to actively seek reports of AEs in former study participants. While pregnancy is not considered an AE, all cases of fetal drug exposure via parent as study participant (see Section 4.4) are to be reported immediately to BioCryst or its designee. Information related to the pregnancy must be given on a “Pregnancy Confirmation and Outcome” form that will be provided by the Sponsor or its designee. 11.2.4 Emergency Procedures In the event of an SAE / SUSAR, the Principal Investigator may request the unblinding of the treatment assignment for the subject affected. If time allows (i.e., if appropriate treatment for the SAE is not impeded), the Principal Investigator will first consult with the Medical Monitor regarding the need to unblind the treatment assignment for the subject. At all times, the clinical well-being of any subject outweighs the need to consult with the Medical Monitor. The Principal Investigator may contact the IVRS central randomization center and request the unblinding of the treatment assignment that corresponds to the affected subject. The IVRS center will record the name of the Investigator making the request, the date and time of the request, the subject number and date of birth. The Sponsor will be informed within 24 hours if unblinding occurred. 12 STATISTICAL METHODS Descriptive statistical methods will be used to summarize the data from this study, with hypothesis testing performed for the primary and other selected efficacy endpoints. Unless stated otherwise, the term “descriptive statistics” refers to number of subjects (n), mean, median, standard deviation (SD), minimum, and maximum for continuous data and frequencies and percentages for categorical data. The term “treatment group” refers to randomized treatment assignment: peramivir 300 mg, peramivir 600 mg, or placebo. All data collected during the study will be included in data listings. Unless otherwise noted, the data will be sorted first by treatment assignment, subject number, and then by date within each subject number. Unless specified otherwise, all statistical testing will be two-sided and will be performed using a significance (alpha) level of 0.05. All statistical analyses will be conducted with the SAS® System, version 9.1.3 or higher. 12.1 Data Collection Methods The data will be recorded on the CRF approved by BioCryst. The Investigator must submit a completed CRF for each subject who signs an informed consent form (ICF), regardless of duration. All documentation supporting the CRF data, such as laboratory or hospital records, must be readily available to verify entries in the CRF. Documents (including laboratory reports, hospital records subsequent to SAEs, etc.) transmitted 360 360 BCX1812-311 (V3.0: 20-November-2007) Page 45 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL to BioCryst should not carry the subject’s name. This will help to ensure subject confidentiality. 12.2 Statistical Analysis Plan A statistical analysis plan (SAP) will be created and approved prior to the review of any data. This document will provide a more technical and detailed description of the proposed data analysis methods and procedures. 12.3 Study Hypothesis The primary hypothesis for evaluating the primary objective may be stated as follows: The null hypothesis (H0) is that the time to alleviation of influenza symptoms is the same for subjects treated with placebo and for subjects treated with peramivir 300mg (H01) or peramivir 600mg (H02). The alternative hypothesis (H1) is that subjects treated with peramivir 300mg (H11) or peramivir 600mg (H12) have an improvement in time to alleviation of influenza symptoms over those treated with placebo. 12.4 Sample Size Estimates Up to a total of 750 evaluable subjects randomized in a 2:2:1 (300 subjects treated with peramivir 300mg: 300 subjects treated with peramivir 600 mg: 150 subjects treated with placebo) are estimated for this phase 3 study. Because results of clinic-based RAT tests may not precisely indicate presence of influenza infection, it is expected that at least 850 subjects will be randomized to treatment to ensure that 750 evaluable subjects are treated. From preliminary results of a phase 2 study evaluating peramivir treatment of uncomplicated influenza, it is expected that the median time to alleviation of symptoms will be 137.0 hours (95% CI: 115.9, 165.8) for subjects receiving placebo treatment. Additionally, it is expected that the median time to alleviation for the 150 mg dose peramivir arm will be reduced by 30% compared to placebo (Table 5) yielding a hazard ratio of 0.70. 361 361 BCX1812-311 (V3.0: 20-November-2007) Page 46 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 5 Median time to alleviation of symptoms (30% reduction, 0.70 hazard ratio). Median Time To Alleviation of Symptoms (Hours) Placebo Peramivir 150mg Difference (hours) 145.0 101.5 43.5 140.0 98.0 42.0 135.0 94.5 40.5 130.0 91.0 39.0 125.0 87.5 37.5 120.0 84.0 36.0 115.0 80.5 34.5 110.0 77.0 33.0 105.0 73.5 31.5 100.0 70.0 30.0 Using these assumptions, a sample size of 300 evaluable subjects per active treatment group and 150 evaluable subjects in the placebo group (a total of 750 evaluable subjects) is sufficient to provide at least 90% power to detect a hazard ratio of 0.70 using a log-rank statistic and α = 0.025 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). 12.5 Analysis Populations The populations for analysis will include the intent-to-treat (ITT), intent-to-treat infected (ITTI), per-protocol infected (PPI), and safety populations. Additional analysis populations may be defined to evaluate study results. Any additional analysis populations will be defined in the SAP. Intent-To-Treat Population: The ITT population will include all subjects who are randomized. Subjects will be analyzed in the treatment group to which they were randomized. The ITT population will be used for analyses of accountability and demographics. Intent-To-Treat Infected Population: The ITTI population will include all subjects who are randomized, received study drug, and have confirmed influenza A by culture or PCR. Subjects will be analyzed according to the treatment randomized. If a discrepancy is noted in the final database for any subject, such that the drug differs from the randomized treatment assignment, efficacy analyses may be repeated with the subjects analyzed according to the treatment received. The ITTI population will be used for primary analyses of efficacy. Per-Protocol Infected: The PPI population includes all subjects in the ITTI population who receive an adequate intramuscular injection. The definition of an adequate intramuscular injection will be further described in the SAP. The PPI population will be used as supportive of the primary analyses for efficacy completed with the ITTI population. Safety Population: The safety population will include all subjects who received study drug. Subjects will be analyzed according to the treatment received. This population will be used for all safety analyses. 362 362 BCX1812-311 (V3.0: 20-November-2007) Page 47 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.6 Interim and End of Study Analyses Interim Analysis An independent DMC will review safety data on an ongoing basis. Safety analyses will be presented in a manner consistent with the presentations intended for the final analysis. End of Study Analysis A final analysis is planned after the last subject completes or discontinues the study, and the resulting clinical database has been cleaned, quality checked, and locked. 12.7 Efficacy Analyses 12.7.1 Primary Efficacy Endpoint The primary efficacy endpoint is the time to alleviation of symptoms of influenza in subjects diagnosed with influenza A, defined as the time from injection of study drug to the start of the time period when a subject has Alleviation of Symptoms. A subject has Alleviation of Symptoms if all of the seven symptoms of influenza (nasal congestion, sore throat, cough, aches and pains, fatigue (tiredness), headache, feeling feverish) assessed on his/her subject diary are either absent or are present at no more than mild severity level and at this status for at least 21.5 hours (24 hours - 10%). Descriptive statistics for the primary efficacy variable will be tabulated by treatment group. Alleviation of symptoms will be determined by assessment of symptoms as reported on each subject’s diary card. Time to alleviation of symptoms will be summarized for each treatment group. Treatment comparisons between each active group and placebo will be assessed using a Wilcoxon-Gehan19 statistic stratified by smoking status at screening Pairwise comparisons between each active group and placebo will be assessed using a Wilcoxon-Gehan test.. Subjects who do not experience alleviation of symptoms will be censored at the date of their last non- missing post-baseline assessment. For assessment of the primary efficacy endpoint, the overall significance level will be maintained by utilization of Hochberg’s20 method for the planned comparisons between the two active treatments and placebo. 12.7.2 Secondary Efficacy Endpoints All secondary endpoints will be summarized using descriptive statistics by treatment group, and study day/time, if appropriate. Statistical comparisons for each endpoint will be constructed without adjustment for multiple endpoints. The reduction in viral shedding will be assessed as the change in viral titers defined as the time- weighted change from baseline in log10 tissue culture infective dose50 (TCID50/mL) and will be summarized for each treatment group. The time-weighted average change from baseline will be calculated on a by-subject basis through Day 9 using the trapezoidal rule with all available post- baseline on-treatment data (data after initiation of study treatment) minus the baseline value. Specifically, the time-weighted area under the curve for time a (ta) to time b (tb) is given by the formula 363 363 BCX1812-311 (V3.0: 20-November-2007) Page 48 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL ) ( ) ( b a b a t t t t AUC TWAUC − − = , where ∑ − = − + − + = − 1 1 1 2 ) )( ( ) ( b a i i i i i b a t t y y t t AUC and ti represents the date of the ith viral titer assessment and yi represents the log10 value of the ith viral titer assessment. If there is a baseline value and only one follow-up value, yi then the time-weighted change from baseline is defined as the difference between yi and baseline. If there is a baseline value and no follow-up value, the subject is excluded from analysis. The differences between each of the peramivir treatment groups and placebo will be evaluated using a van Elteren Test adjusting for smoking status at screening. Analyses of the PCR results will be analyzed in a similar manner. Subject’s oral temperature will be summarized by study visit and treatment group. Differences between the treatment groups will be assessed using the van Elteren test controlling for smoking status at screening. A subject has Resolution of Fever if he/she has a temperature < 37.2°C (99.0°F) and no antipyretic medications have been taken for at least 12 hours. The time to resolution of fever will be estimated using the method of Kaplan-Meier using temperature and symptom relief medication information obtained from the subject diary data. Differences between the treatment groups will be assessed using the Wilcoxon-Gehan statistic controlling for smoking status at screening. Subjects who do not have resolution of fever will be censored at the time of their last non-missing post-baseline temperature assessment. The number and percentage of subjects experiencing influenza related complications will be summarized by complication preferred term and treatment group. The difference between the treatment groups will be assessed a logistic regression model with factors for treatment group and smoking status at screening. Pairwise differences between the treatment groups will be evaluated using contrasts from the final logistic regression model. 12.7.3 Exploratory Endpoints The MRU, MRU-related direct costs, and indirect costs attributable to days missed of work and work productivity and/or performance losses will be summarized by treatment group and smoking status. Methods for describing differences between treatment groups will be presented in the SAP. Genotypic (including Hemagglutinin and Neuraminidase), phenotypic, viral culture and PCR data will be listed for each subject. These listings will be constructed in a manner consistent with the FDA June 2006 Guidance Document: “Guidance for Submitting Influenza Resistance Data”.18 Additionally, the number and percentage of genotypic changes from wild-type amino acid will be summarized separately for treatment group, protein type, and study visit. 12.8 Safety Analyses AEs will be mapped to a MedDRA-preferred term and system organ classification. The occurrence of TEAEs will be summarized by treatment group using MedDRA-preferred terms, system organ classifications, and severity. If a subject experiences multiple events that map to a single preferred term, the greatest severity and strongest Investigator assessment of relation to study drug will be assigned to the preferred term for the appropriate summaries. All AEs will be 364 364 BCX1812-311 (V3.0: 20-November-2007) Page 49 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL listed for individual subjects showing both verbatim and preferred terms. Separate summaries of treatment-emergent SAEs and AEs related to study drug will be generated. Descriptive summaries of vital signs and clinical laboratory results will be presented by study visit. Laboratory abnormalities will be graded according to the DAIDS Table for Grading Adverse Events for Adults and Pediatrics (Publish Date: December 2004). The number and percentage of subjects experiencing treatment-emergent graded toxicities will be summarized by treatment group. Laboratory toxicity shifts from baseline to Day 3, Day 5, and Day 14 will be summarized by treatment group. Abnormal physical examination findings will be presented by treatment group. The number and percent of subjects experiencing each abnormal physical examination finding will be included. Concomitant medications will be coded using the WHO dictionary. These data will be summarized by treatment group. Subject disposition will be presented for all subjects. The number of subjects who completed the study and discontinued from the study will be provided. The reasons for early discontinuation also will be presented. 12.9 Sub-Study and Pharmacokinetic Analysis A sub-study to collect pharmacokinetic samples in up to 60 peramivir treated subjects to examine exposure response will be conducted at selected sites. The data from the sub-study will be combined with the two PK samples (collected on all subjects at 30-60 minutes following administration of study drug and on study day 3) to perform a population exposure-response analysis. All analyses related to exposure-response will be completed as part of the sub-study. All statistical methods will be outlined as part of the sub-study protocol and exposure-response analysis plan. All sub-study analyses, and exposure-response analyses from PK samples obtained in this study and a companion study BCX1812-312, will be reported in a separate sub-study report. 12.10 General Issues for Statistical Analysis 12.10.1 Multiple Comparisons and Multiplicity In order to maintain the overall type I error in the presence of the planned comparisons between the two peramivir treatments and placebo, Hochberg’s method will be applied to the primary efficacy endpoint analysis. No other adjustments for multiple comparisons are planned. 12.10.2 Covariates Primary and secondary efficacy analyses will be adjusted for smoking status at screening. 12.10.3 Planned Sub-Groups The primary efficacy endpoint will be summarized separately by smoking status at screening using descriptive statistics by treatment group and study day, if appropriate. No formal statistical testing will be utilized. 365 365 BCX1812-311 (V3.0: 20-November-2007) Page 50 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Additional analyses may be performed by country, if necessary, for submission to local regulatory authorities. 12.10.4 Missing Data Every effort will be made to obtain required data at each scheduled evaluation from all subjects who have been randomized. No attempt will be made retrospectively to obtain missing subject reported data (including influenza symptom severity assessments, temperature, ability to perform usual activities, missed days of work and impact of influenza on subject’s work performance and/or productivity) that has not been completed by the subject at the time of return of the subject diary to the investigative site. In situations where it is not possible to obtain all data, it may be necessary to impute missing data. In assessing the primary efficacy endpoint, for subjects who withdraw or who do not experience alleviation of symptoms, missing data will be censored using the date of subject’s last non- missing assessment of influenza symptoms. Missing assessments of influenza symptoms conservatively will be imputed as having severity above absent or mild (as failures). For the subject diary data, the following data conventions will be utilized. Missing diary completion will be imputed as 11:59 for diary entries designated as morning and 23:59 for evening and daily reported values. Select exploratory sensitivity analyses may be conducted to ascertain the effect, if any, of these methods. These sensitivity analyses are further described in the SAP. Secondary efficacy endpoints with time to event data will be censored using the date of subject’s last non- missing assessment of the given endpoint. 13 STUDY ADMINISTRATION 13.1 Regulatory and Ethical Considerations 13.1.1 Regulatory Authority Approvals This study will be conducted in compliance with the protocol; GCPs, including International Conference on Harmonization (ICH) of Technical Requirements for Registration of Pharmaceuticals for Human Use Guidelines; FDA regulatory requirements and in accordance with the ethical principles of the Declaration of Helsinki. In addition, all applicable local laws and regulatory requirements relevant to the use of new therapeutic agents in the countries involved will be adhered to. The Investigator should submit written reports of clinical study status to their Institutional Review Board (IRB)/ Independent Ethics Committee (IEC) annually or more frequently if requested by the IRB/ IEC. A final study notification will also be forwarded to the IRB/IEC after the study is completed or in the event of premature termination of the study in accordance with the applicable regulations. Copies of all contact with the IRB/ IEC should be maintained in the study documents file. Copies of clinical study status reports (including termination) should be provided to BioCryst. 366 366 BCX1812-311 (V3.0: 20-November-2007) Page 51 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.1.2 Ethics Committee Approvals Before initiation of the study at each investigational site, the protocol, the informed consent form, the subject information sheet, and any other relevant study documentation will be submitted to the appropriate IRB/IEC. Written approval of the study must be obtained before the study center can be initiated or the investigational medicinal product is released to the Investigator. Any necessary extensions or renewals of IRB/IEC approval must be obtained, in particular, for changes to the study such as modification of the protocol, the informed consent form, the written information provided to subjects and/or other procedures. The Investigator will report promptly to the IRB/IEC any new information that may adversely affect the safety of the subjects or the conduct of the study. On completion of the study, the Investigator will provide the IRB/IEC with a report of the outcome of the study. 13.1.3 Subject Informed Consent Signed informed consent must be obtained from each subject prior to performing any study- related procedures. Each subject should be given both verbal and written information describing the nature and duration of the clinical study. The informed consent process should take place under conditions where the subject has adequate time to consider the risks and benefits associated with his/her participation in the study. Subjects will not be screened or treated until the subject has signed an approved ICF written in a language in which the subject is fluent. The ICF that is used must be approved both by BioCryst and by the reviewing IRB/ IEC. The informed consent should be in accordance with the current revision of the Declaration of Helsinki, current ICH and GCP guidelines, and BioCryst policy. The Investigator must explain to potential subjects or their legal representatives the aims, methods, reasonably anticipated benefits, and potential hazards of the trial and any discomfort it may entail. Subjects will be informed that they are free not to participate in the trial and that they may withdraw consent to participate at any time. They will be told that refusal to participate in the study will not prejudice future treatment. They will also be told that their records may be examined by competent authorities and authorized persons but that personal information will be treated as strictly confidential and will not be publicly available. Subjects must be given the opportunity to ask questions. After this explanation and before entry into the trial, consent should be appropriately recorded by means of the subject’s dated signature. The subject should receive a signed and dated copy of the ICF. The original signed informed consent should be retained in the study files. The Investigator shall maintain a log of all subjects who sign the ICF and indicate if the subject was enrolled into the study or reason for non-enrollment. 13.1.4 Payment to Subjects Reasonable compensation to study subjects may be provided if approved by the IRB/IEC responsible for the study at the Investigator’s site. 13.1.5 Investigator Reporting Requirements The Investigator will provide timely reports regarding safety to his/her IRB/IEC as required. 367 367 BCX1812-311 (V3.0: 20-November-2007) Page 52 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.2 Study Monitoring During trial conduct, BioCryst or its designee will conduct periodic monitoring visits to ensure that the protocol and GCPs are being followed. The monitors may review source documents to confirm that the data recorded on CRFs is accurate. The investigator and institution will allow BioCryst monitors or its designees and appropriate regulatory authorities direct access to source documents to perform this verification. 13.3 Quality Assurance The trial site may be subject to review by the IRB/IEC, and/or to quality assurance audits performed by BioCryst, and/or to inspection by appropriate regulatory authorities. It is important that the investigator(s) and their relevant personnel are available during the monitoring visits and possible audits or inspections and that sufficient time is devoted to the process. 13.4 Study Termination and Site Closure BioCryst reserves the right to discontinue the trial prior to inclusion of the intended number of subjects but intends only to exercise this right for valid scientific or administrative reasons. After such a decision, the Investigator must contact all participating subjects immediately after notification. As directed by BioCryst, all study materials must be collected and all case report forms completed to the greatest extent possible. 13.5 Records Retention To enable evaluations and/or audits from regulatory authorities or BioCryst, the Investigator agrees to keep records, including the identity of all participating subjects (sufficient information to link records, case report forms and hospital records), all original signed informed consent forms, copies of all case report forms and detailed records of treatment disposition. The records should be retained by the Investigator according to local regulations or as specified in the Clinical Trial Agreement, whichever is longer. If the Investigator relocates, retires, or for any reason withdraws from the study, the study records may be transferred to an acceptable designee, such as another investigator, another institution, or to BioCryst. The Investigator must obtain BioCryst’s written permission before disposing of any records. 13.6 Study Organization 13.6.1 Data Monitoring Committee BioCryst will assemble an independent Data Monitoring Committee (DMC) to assess safety parameters of the trial on a periodic, ongoing basis while the trial is in progress. The committee will include a statistician and three physicians, two of whom will be Infectious Disease / Clinical Virology specialists. Full details of the composition of the DMC and how the DMC is to operate will be described in a separate DMC charter. 368 368 BCX1812-311 (V3.0: 20-November-2007) Page 53 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.7 Confidentiality of Information BioCryst affirms the subject’s right to protection against invasion of privacy. Only a subject identification number, initials and/or date of birth will identify subject data retrieved by BioCryst. However, in compliance with federal regulations, BioCryst requires the investigator to permit BioCryst’s representatives and, when necessary, representatives of the FDA or other regulatory authorities to review and/or copy any medical records relevant to the study. BioCryst will ensure that the use and disclosure of protected health information obtained during a research study complies with the HIPAA Privacy Rule, where this rule is applicable. The Rule provides federal protection for the privacy of protected health information by implementing standards to protect and guard against the misuse of individually identifiable health information of subjects participating in BioCryst-sponsored Clinical Trials. "Authorization" is required from each research subject, i.e., specified permission granted by an individual to a covered entity for the use or disclosure of an individual's protected health information. A valid authorization must meet the implementation specifications under the HIPAA Privacy Rule. Authorization may be combined in the Informed Consent document (approved by the IRB/IEC) or it may be a separate document, (approved by the IRB/IEC) or provided by the Investigator or Sponsor (without IRB/IEC approval). It is the responsibility of the investigator and institution to obtain such waiver/authorization in writing from the appropriate individual. HIPAA authorizations are required for U.S. sites only. 13.8 Study Publication All data generated from this study are the property of BioCryst and shall be held in strict confidence along with all information furnished by BioCryst. Independent analysis and/or publication of these data by the Investigator or any member of his/her staff are not permitted without prior written consent of BioCryst. Written permission to the Investigator will be contingent on the review by BioCryst of the statistical analysis and manuscript and will provide for nondisclosure of BioCryst confidential or proprietary information. In all cases, the parties agree to submit all manuscripts or abstracts to all other parties 30 days prior to submission. This will enable all parties to protect proprietary information and to provide comments based on information that may not yet be available to other parties. 369 369 BCX1812-311 (V3.0: 20-November-2007) Page 54 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 14 REFERENCES 1. Cox NJ, Subbarao K. Influenza. Lancet 1999;354(9186):1277–1282. 2. Thompson WW, Shay KD, Weintraub E, Branner L, Cox N, et al. Mortality associated with influenza and respiratory syncytial virus in the United States. JAMA 2003;289(2):179–186. 3. Kaiser L, Wat C, Mills T, Mahoney P, Ward P, et al. Impact of oseltamivir treatment on influenza-related lower respiratory tract complications and hospitalizations. Arch Intern Med 2003;163(14):1667–1672. 4. Hayden FG, Treanor JJ, Fritz RS, Lobo M, Betts RF, et al. Use of the oral neuraminidase inhibitor oseltamivir in experimental human influenza: randomized controlled trials for prevention and treatment. JAMA 1999;282(13):1240–1246. 5. Kiso M, Mitamura K, Sakai-Tagawa Y, Shiraishi K, Kawakami C, et al. Resistant influenza A viruses in children treated with oseltamivir: descriptive study. Lancet 2004;364(9436):759– 765. 6. Bantia S, Parker CD, Ananth SL, Horn LL, Andries K, et al. Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir. Antimicrob Agents Chemother 2001;45(4):1162–1167. 7. Boivin G, Goyette N. Susceptibility of recent Canadian influenza A and B virus isolates to different neuraminidase inhibitors. Antiviral Res 2002;54(3):143–147. 8. Gubareva LV, Webster RG, Hayden FG. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother 2001;45(12):3403–3408. 9. Govorkova EA, Fang HB, Tan M, Webster RG. Neuraminidase inhibitor-rimantadine combinations exert additive and synergistic anti-influenza virus effects in MDCK cells. Antimicrob Agents Chemother 2004;48(12):4855–4863. 10. BioCryst Pharmaceuticals. Unpublished data. 11. Arnold CS, Zacks MA, Dziuba N, Yun N, Linde N, Smith J, Babu YS, Paessler S. Injectable peramivir promotes survival in mice and ferrets infected with highly pathogenic avian influenza A/Vietnam/1203/04 (H5N1). V-2041B, ICAAC 2006, San Francisco 12. Boltz, DA, Ilyushina NA, Arnold CS, Babu, YS, Webster RG and Govorkova EA. Intramuscular administration of neuraminidase inhibitor peramivir promotes survival against lethal H5N1 influenza infection in mice. Antiviral Research,2007; 74 (3): A32 13. BioCryst Pharmaceuticals unpublished clinical study report BC-01-03. 14. Tamiflu® Package Insert. Roche Pharmaceuticals. Rev. December 2005. 15. Quidel QuickVue Influenza A+B and Binax NOW Influenza A&B Test Kit product information sheets 16. Treanor JJ, Hayden FG, Vrooman PS, Barbarash R et al. Efficacy and safety of the oral neuraminidase inhibitor oseltamivir in treating acute influenza. JAMA 2000; 283(8): 1016- 1024. 17. Nicholson KG, Aoki FY, Osterhaus AD, Trottier S et al. Efficacy and safety of oseltamivir in treatment of influenza: a randomised controlled trial. Lancet 2000; 355(9218): 1845-1850. 370 370 BCX1812-311 (V3.0: 20-November-2007) Page 55 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 18. US Department of Health and Human Services, Food and Drug Administration Center for Drug Evaluation and Reserach (CDER). Attachment to Guidance on Antiviral Product Development- Conducting and Submitting Virology Studies to the Agency: Guidance for Submitting Influenza Resistance Data. http://www.fda.gov/cder/guidance/7070fnlFLU.htm 19. Gehan EA (1965): A generalized Wilcoxon test for co mparing arbitrarily singl y censored samples. Biometrika 52:203-223 20. Hochberg, Y. A sharper Bonferroni pr ocedure for multiple tests of significance. Biometrika. 1988;75:800-2 371 371 BCX1812-311 (V3.0: 20-November-2007) Page 56 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15 APPENDICES 15.1 NYHA Functional Classification Criteria: Heart Failure and Angina NYHA Functional Classification of Heart Failure Class I No symptoms. Ordinary physical activity such as walking and climbing stairs does not cause fatigue or dyspnea. Class II Symptoms with ordinary physical activity. Walking or climbing stairs rapidly; walking uphill; walking or stair climbing after meals, in cold weather, in wind, or when under emotional stress causes undue fatigue or dyspnea. Class III Symptoms w ith less than ordinary phy sical activity. Walking one to two blocks on t he level and clim bing m ore th an one flight of stai rs in norm al conditions causes undue fatigue or dyspnea. Class IV Symptoms at rest. Inability to carry on any physical activity without fatigue or dyspnea. NYHA Functional Classification of Angina Class I Angina only with unusually strenuous activity. Class II Angina with slightl y more prolonged o r slightly more vigorous activit y than usual. Class III Angina with usual daily activity. Class IV Angina at rest. 372 372 BCX1812-311 (V3.0: 20-November-2007) Page 57 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15.2 Criteria for Severe COPD and Severe Asthma The following guidelines are provided to assist in the evaluation of subjects who have a medical history for Chronic Obstructive Pulmonary Disease (COPD) and/or Asthma. Subjects with severe COPD or severe persistent Asthma are to be excluded from this study. (See section 8.1.2, exclusion criteria number 3). Classification of Asthma from National Asthma and Education and Prevention Program For Adults and Children (> 5 yrs) who can use a spirometer or peak flow meter Classification Days with Symptoms Nights with Symptoms FEV1 or PEF % Predicted Normal PEF Variability (%) Severe persistent Continual Frequent ≤ 60 > 30 Moderate Persistent Daily > 1/ week > 60 - < 80 > 30 Mild Persistent > 2 / week but < 1 times / day > 2/ month ≥ 80 20 – 30 Mild Intermittent ≤ 2 / week < 2 / month ≥ 80 < 20 FEV1: percentage predicted value for forced expiratory volume in 1 second. PEF: percentage of personal best for peak expiratory flow. Extracted from: Expert Panel Report 3: Guidelines for the Diagnosis and Management of Asthma. National Heart, Lung, and Blood Institute, National Asthma Education and Prevention Program. HHS/NIH 2007 Spirometric Classification of COPD Severity based upon Post-Bronchodilator FEV1 (GOLD Criteria) Stage Characteristics Mild COPD FEV1/FVC < 70% FEV1 ≥ 80% predicted Moderate COPD FEV1/FVC < 70% 50 % ≤ FEV1 < 80% predicted Severe COPD FEV1/FVC < 70% 30 % ≤ FEV1 < 50% predicted Very Severe COPD FEV1/FVC < 70% FEV1 < 30% predicted or FEV1 < 50% predicted plus chronic respiratory failure FEV1: percentage predicted value for forced expiratory volume in one second. FVC: forced vital capacity Extracted from: Rabe KF, et al. Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease (GOLD Executive Summary). Am. J. Respir. Crit. Care Med. 2007:176;532-555. 373 373 CLINICAL STUDY PROTOCOL Protocol No. BCX1812-311 IND No. 76,350 A PHASE 3 MULTICENTER, RANDOMIZED, DOUBLE BLIND, PLACEBO- CONTROLLED STUDY TO EVALUATE THE EFFICACY AND SAFETY OF INTRAMUSCULAR PERAMIVIR IN SUBJECTS WITH UNCOMPLICATED ACUTE INFLUENZA THE IMPROVE I STUDY (IntraMuscular Peramivir for the Relief Of symptoms and Virologic Efficacy) Short title: Intramuscular Peramivir for the Treatment of Uncomplicated Influenza Protocol Date(s): Version 1.0: 04 September 2007 Version 2.0: 05 October 2007 Version 3.0: 20 November 2007 Version 4.0: 18 December 2007 BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35244, USA Phone: +1 919 859 1302 Fax: +1 919 851 1416 The document contains trade secrets and proprietary information of BioCryst Pharmaceuticals, Inc. This information is confidential property of BioCryst Pharmaceuticals, Inc., and is subject to confidentiality agreements entered into with BioCryst Pharmaceuticals, Inc. No information contained herein should be disclosed without prior written approval. CONFIDENTIAL 374 374 BCX1812-311 (V4.0: 18-December-2007) Page 2 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1 TITLE PAGE Protocol Number: BCX1812-311 Study Title: A phase 3 multicenter, randomized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza. IND Number: 76, 350 Investigational Product: Peramivir (BCX1812) Indication Studied: Uncomplicated acute influenza Sponsor: BioCryst Pharmaceuticals, Inc. 2190 Parkway Lake Drive Birmingham, AL 35233 Development Phase: 3 Sponsor Medical Officer: W. James Alexander, M.D., M.P.H. Senior Vice President, Clinical Development Chief Medical Officer Phone: +1 919 859 1302 Fax: +1 919 851 1416 Email Address: jalexander@biocryst.com Compliance Statement: This study will be conducted in accordance with the ethical principles that have their origin in the Declaration of Helsinki and clinical research guidelines established by the Code of Federal Regulations (Title 21, CFR Parts 50, 56, and 312) and ICH Guidelines. Essential study documents will be archived in accordance with applicable regulations. Final Protocol Date: Version 1.0: 04 September 2007 Amendment(s) Date(s): Version 2.0: 05 October 2007 Version 3.0: 20 November 2007 Version 4.0: 18 December 2007 375 375 376 376 BCX1812-311 (V4.0: 18-December-2007) Page 4 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 1.2 Clinical Study Protocol Agreement Protocol No. BCX1812-311 Protocol Title: A phase 3 multicenter, random ized, double-blind, placebo-controlled study to evaluate the effic acy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza I have carefully read this protocol and agree that it contains all of the necessary information required to conduct this study. I agree to c onduct this study as described and according t o the Decl aration of Helsinki, Internationa l Conference on Har monization Guidelines for Good Clinical Practices, and all applicable regulatory requirements. Investigator’s Signature Date Name (Print) 377 377 BCX1812-311 (V4.0: 18-December-2007) Page 5 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 2 SYNOPSIS Protocol No. BCX1812-311 Protocol Title: A phase 3, multicenter, randomized, double-blind, placebo- controlled study to evaluate the efficacy and safety of intramuscular peramivir in subjects with uncomplicated acute influenza. Sponsor: BioCryst Pharmaceuticals, Inc. Investigators/Study Sites: Multinational Development Phase: 3 Objectives: Primary: To evaluate the efficacy of peramivir administered intramuscularly compared to placebo on the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. Secondary: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly 2. To evaluate secondary clinical outcomes in response to treatment 3. To evaluate changes in influenza virus titer in nasopharyngeal samples (viral shedding) in response to treatment Exploratory: 1. To assess pharmacoeconomic measures as response to treatment 2. To assess changes in influenza viral susceptibility to neuraminidase inhibitors following treatment Number of Subjects: Total enrollment: approximately 600 subjects will be randomized. Subjects will be allocated to treatment using a 2:1 randomization schema. An evaluable subject is one who is randomized, receives study drug, and has confirmed acute influenza A or B by primary viral culture or PCR. A positive Rapid Antigen Test (RAT) for influenza A and B at screening will be required for enrollment. Because results of clinic-based RAT tests may not precisely indicate presence of influenza infection, it is expected that approximately 600 subjects will be randomized to treatment to ensure enrollment of approximately 450 subjects that are positive for influenza A. Study Design: This is a multinational, randomized, double-blind study comparing the efficacy and safety of a 300 mg dose of peramivir administered intramuscularly versus placebo in adults with 378 378 BCX1812-311 (V4.0: 18-December-2007) Page 6 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL uncomplicated acute influenza. All subjects will be centrally randomized to treatment with 300 mg of peramivir or placebo in a ratio of 2:1, and will be stratified according to smoking status and RAT test for influenza A or B. Study drug will be administered as bilateral 2mL intramuscular injections (total of 4mL injected in equally divided doses). Procedures for gluteal intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. Subjects eligible for screening will have an anterior nasal swab collected for testing by rapid antigen testing (RAT) for influenza A and B in accordance with the commercially available RAT kit instructions. If the initial RAT is negative, the test should be repeated within one hour. Subjects meeting the inclusion/exclusion criteria may be enrolled into the study. All enrolled subjects will record the following information in a Study Diary: • Assessment of the presence and severity of each of seven symptoms of influenza on a 4-point scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatment, then once daily (AM) through Day 14. • Oral temperature measurements taken with an electronic thermometer every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (Tylenol or paracetamol) or other anti-pyretic medications. • Assessment of subject’s time lost from work or usual activities and rating of productivity compared to normal (rated as 0-10 on a visual analog scale) once daily through Day 14. • Doses of antipyretic, expectorant, and/or throat lozenges taken for symptomatic relief each day through Day 14. Anterior nose (bilateral) and posterior pharynx specimens (swabs) will be collected at Day 1 (pre-treatment) and at Days 3, 5, and 9, for quantitative virologic assessments. Specimens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result on culture) as well as other virologic assessments (e.g. PCR, genotypic testing). All virologic assessments will be performed by a central laboratory. Two samples for pharmacokinetic (PK) testing for plasma levels of peramivir will be obtained from all subjects randomized. The 379 379 BCX1812-311 (V4.0: 18-December-2007) Page 7 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL first PK sample will be obtained between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be obtained at the day 3 visit in all subjects. The data from these PK samples will be utilized in a population exposure-response analysis. At selected sites a separate sub-study will be conducted to collect additional PK samples between treatment and Day 3 for the purpose of conducting a separate exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Study Population: Male and female subjects, 18 years of age and older, with symptoms consistent with a diagnosis of uncomplicated acute influenza infection may be screened for enrollment. Subject eligibility will require the presence of two or more symptoms of at least moderate severity consistent with acute influenza as well as positive results obtained from a rapid antigen test (RAT) for influenza A and/or B at screening. Inclusion Criteria: 1. Male and non-pregnant female subjects age ≥18 years. 2. A positive Influenza A and/or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate anterior nasal specimen, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated within one-hour. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. A subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at the time of screening. 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of at least moderate severity. 5. Presence of at least one constitutional symptom (myalgia [aches and pains], headache, feverishness, or fatigue) of at least moderate severity. 6. Onset of symptoms no more than 48 hours before presentation for screening. 7. Written informed consent. Exclusion Criteria: 1. Women who are pregnant or breast-feeding. 2. Presence of clinically significant signs of acute respiratory distress. 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma (See section 15.2). 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class III or IV functional status within the 380 380 BCX1812-311 (V4.0: 18-December-2007) Page 8 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL past 12 months. 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 6. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min). 7. Clinical evidence of worsening of any chronic medical condition (temporally associated with the onset of symptoms of influenza) which, in the investigator’s opinion, indicates that such finding(s) could represent complications of influenza. 8. Current clinical evidence, including clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis and/or pneumonia, or active bacterial infection at any body site that requires therapy with oral or systemic antibiotics. 9. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy which would include oral or systemic treatment with > 10 mg prednisone or equivalent on a daily basis within 30 days of screening. 10. Currently receiving treatment for viral hepatitis B or viral hepatitis C. 11. Presence of known HIV infection with a CD4 count <350 cell/mm3. 12. Current therapy with oral warfarin or other systemic anticoagulant. 13. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening. 14. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days. 15. Immunized against influenza with inactivated virus vaccine within the previous 14 days. 16. Receipt of any intramuscular injection within the previous 14 days. 17. History of alcohol abuse or drug addiction within 1 year prior to admission in the study. 18. Participation in a previous study of intramuscular or intravenous peramivir or previous participation in this study. 19. Participation in a study of any investigational drug or device within the last 30 days. Study Endpoints: Primary Endpoint: Clinical: Time to alleviation of clinical symptoms of influenza. Secondary Endpoint(s): Safety: Incidence of treatment-emergent adverse events and treatment- emergent changes in clinical laboratory tests. 381 381 BCX1812-311 (V4.0: 18-December-2007) Page 9 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Clinical: Time to resolution of fever. Incidence of influenza related complications. Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID50). Exploratory Endpoint(s): Pharmacoeconomic: Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. Virologic: Quantitative change in influenza virus shedding, measured by PCR. Change in influenza virus susceptibility to neuraminidase inhibitors. Investigational Product, Dose, and Mode of Administration: Peramivir (BCX-1812), 75mg/mL, 2mL (150mg) per injection, administered as bilateral intramuscular injections. Reference Therapy, Dose, and Mode of Administration: Matching Placebo (buffered diluent), 2mL per injection administered as bilateral intramuscular injections. Duration of Treatment: Following treatment on day 1, study duration for all subjects is expected to be up to 14 days (including all visits). Presence of unresolved adverse events and/or treatment-emergent laboratory findings at the Day 14 visit, or persistent or recurrent symptoms of influenza (of the seven symptoms assessed) of either moderate or severe intensity at the Day 14 visit, will require additional follow up. Statistical Methods: Study Hypothesis: The null hypothesis (H0) for this study is that the time to alleviation of influenza symptoms is the same for subjects treated with placebo and for subjects treated with peramivir 300mg. The alternative hypothesis (H1) is that subjects treated with peramivir 300mg have an improvement in time to alleviation of influenza symptoms over those treated with placebo. Sample Size: From preliminary results of a phase 2 study evaluating peramivir treatment of uncomplicated influenza, it is expected that the median time to alleviation of symptoms will be 137.0 hours (95% CI: 115.9, 165.8) for subjects receiving placebo treatment. Additionally, it is expected that the median time to alleviation 382 382 BCX1812-311 (V4.0: 18-December-2007) Page 10 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL for the 300 mg dose peramivir arm will be reduced by 30% compared to placebo yielding a hazard ratio of 0.70. Data from the phase 2 study suggested that the activity of peramivir against influenza B was limited. Therefore, this study will be sized to ensure that a minimum number of influenza A subjects is enrolled to achieve study power. Using these assumptions, a sample size of 450 evaluable subjects with influenza A (300 in the 300 mg treatment group and 150 evaluable subjects in the placebo group) is sufficient to provide at least 90% power to detect a hazard ratio of 0.70 using a log-rank statistic and α = 0.05 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). Efficacy: The primary efficacy analysis will be completed with the intent- to-treat infected population (ITTI). The ITTI population will include all subjects who are randomized, received study drug, and have confirmed influenza A and/or B by primary viral culture or PCR. The primary efficacy variable is the time to alleviation of symptoms, defined as the time from injection of study drug to the start of the time period when each of seven symptoms of influenza are either absent or are present at no more than mild severity level and remain at no worse than this severity status for a 21.5 hour (24 hours – 10%) period. Descriptive statistics for the primary efficacy variable will be tabulated by treatment group. Alleviation of symptoms will be determined by assessment of symptoms as reported on each subject’s diary card. Time to alleviation of symptoms will be summarized for each treatment group. Treatment differences between the 300 mg peramivir dose and placebo will be assessed using a Wilcoxon-Gehan statistic stratified by smoking status and positive PCR or viral culture for influenza A or B at screening. Subjects who do not experience alleviation of symptoms will be censored at the date of their last non-missing assessment. Efficacy analyses will be repeated for Intent To Treat Infected with influenza A (ITTI-A) population and Per-Protocol Infected population (PPI). The ITTI-A population includes all subjects who are randomized, received study drug, and have confirmed influenza A by primary viral culture or PCR. The PPI population will include those subjects in the ITTI population who received an adequate intramuscular injection. Details of this population will be described in the statistical analysis plan. Changes in influenza virus TCID50 (viral titers from nasopharyngeal specimens) will be compared using the van Elteren statistic controlling for smoking status and positive PCR or viral culture for influenza A or B at screening. Analyses of other continuous endpoints will be analyzed in a similar manner. 383 383 BCX1812-311 (V4.0: 18-December-2007) Page 11 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL The number and percentage of subjects experiencing influenza related complications (IRC) will be summarized by complication preferred term and treatment group. The difference between the treatment groups (300 mg peramivir and placebo) will be assessed using a Cochran-Mantel-Haenszel (CMH) test statistic controlling for smoking status, and positive PCR or viral culture for influenza A or B at screening. Safety: Safety analyses will be presented for all subjects in the safety population, defined as all randomized subjects who receive at least one dose of study drug. Adverse events will be mapped to a Medical Dictionary for Regulatory Activities (MedDRA) preferred term and system organ classification. The occurrence of treatment-emergent AEs will be summarized using preferred terms, system organ classifications, and severity. Separate summaries of treatment-emergent SAEs and treatment- emergent AEs that are related to study medication will be generated. All AEs will be listed for individual subjects showing both verbatim and preferred terms. Descriptive summaries of vital signs and quantitative clinical laboratory changes will be presented by study visit. Frequency and percentages of subjects with abnormal laboratory test results will be summarized by toxicity grade. Concomitant medications will be mapped to a WHO preferred term and drug classification. The number and percent of subjects taking concomitant medications will be summarized using preferred terms and drug classifications. The number and percent of subjects experiencing each abnormal physical examination finding will be presented. The number and percent of subjects discontinuing study as well as the reasons for discontinuation will be summarized by treatment group. Date of Protocol: Version 1.0: 04-September-2007 Amendment (Dates): Version 2.0: 05-October-2007 Version 3.0: 20-November-2007 Version 4.0: 18-December-2007 384 384 BCX1812-311 (V4.0: 18-December-2007) Page 12 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 3 TABLE OF CONTENTS 1 TITLE PAGE...............................................................................................................................2 1.1 PROTOCOL APPROVAL SIGNATURE PAGE......................................................................................3 1.2 CLINICAL STUDY PROTOCOL AGREEMENT....................................................................................4 2 SYNOPSIS...................................................................................................................................5 3 TABLE OF CONTENTS...........................................................................................................12 3.1 LIST OF FIGURES .........................................................................................................................14 3.2 LIST OF TABLES ..........................................................................................................................14 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS.............................................15 5 INTRODUCTION......................................................................................................................17 5.1 BACKGROUND.............................................................................................................................17 5.2 RATIONALE FOR STUDY ..............................................................................................................17 5.3 NON-CLINICAL EXPERIENCE WITH PERAMIVIR...........................................................................18 5.3.1 In vitro Assays.......................................................................................................................18 5.3.2 Animal Models......................................................................................................................18 5.4 PREVIOUS PHASE 3 CLINICAL EXPERIENCE WITH ORAL PERAMIVIR...........................................19 5.5 PREVIOUS PHASE 1 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR.........................................19 5.6 PHASE 2 EXPERIENCE WITH INTRAMUSCULAR PERAMIVIR .........................................................21 5.7 DOSE RATIONALE................................................................................................................................23 6 STUDY OBJECTIVES..............................................................................................................24 6.1 OBJECTIVES ................................................................................................................................24 6.1.1 Primary Objective..................................................................................................................24 6.1.2 Secondary Objective(s) .........................................................................................................24 6.1.3 Exploratory Objective(s) .......................................................................................................24 6.2 STUDY ENDPOINTS......................................................................................................................24 6.2.1 Primary Endpoint...................................................................................................................24 6.2.2 Secondary Endpoint(s) ..........................................................................................................24 6.2.3 Exploratory Endpoints...........................................................................................................24 7 STUDY DESIGN.......................................................................................................................25 7.1 OVERALL STUDY DESIGN AND PLAN ..........................................................................................25 8 SELECTION AND WITHDRAWAL OF SUBJECTS..............................................................26 8.1.1 Inclusion Criteria...................................................................................................................26 8.1.2 Exclusion Criteria..................................................................................................................26 8.1.3 Removal of Subjects from Therapy or Assessment...............................................................27 9 TREATMENTS .........................................................................................................................28 9.1 TREATMENTS ADMINISTERED.....................................................................................................28 9.2 IDENTITY OF INVESTIGATIONAL PRODUCT(S) .............................................................................28 9.3 METHOD OF ASSIGNING SUBJECTS TO TREATMENT GROUPS ......................................................28 9.4 STUDY MEDICATION ACCOUNTABILITY......................................................................................29 9.5 BLINDING/UNBLINDING OF TREATMENTS...................................................................................29 9.6 PRIOR AND CONCOMITANT THERAPIES.......................................................................................29 9.7 OVERDOSE AND TOXICITY MANAGEMENT..................................................................................29 9.8 DOSE INTERRUPTION...................................................................................................................29 10 STUDY CONDUCT..................................................................................................................30 10.1 EVALUATIONS.............................................................................................................................30 10.1.1 Informed Consent .............................................................................................................30 10.1.2 Medical History ................................................................................................................30 10.1.3 Rapid Antigen Test for Influenza .....................................................................................30 10.1.4 Physical Examination and Influenza-related Complications Assessments .......................30 10.1.5 Vital Signs ........................................................................................................................30 10.1.6 Electrocardiogram Measurements ....................................................................................31 10.1.7 Clinical Laboratories ........................................................................................................31 10.1.8 Urine Pregnancy Test .......................................................................................................31 10.1.9 Serology for Influenza ......................................................................................................31 385 385 BCX1812-311 (V4.0: 18-December-2007) Page 13 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10.1.10 Samples for Virologic Laboratory Assessments...............................................................31 10.1.11 Subject Self Assessments..................................................................................................32 10.1.12 Concomitant Medications.................................................................................................32 10.1.13 Adverse Events.................................................................................................................32 10.1.14 Pharmacokinetic Exposure Samples.................................................................................32 10.2 SCREENING PERIOD.....................................................................................................................33 10.2.1 Informed Consent .............................................................................................................33 10.2.2 Screening/Baseline Evaluation and Enrollment................................................................33 10.3 TREATMENT PERIOD—STUDY DAY 1 .........................................................................................33 10.3.1 Pre-dose Evaluations-Study Day 1 ...................................................................................34 10.3.2 Post-dose Evaluations-Study Day 1..................................................................................34 10.4 POST-TREATMENT ASSESSMENT PERIOD....................................................................................34 10.4.1 Days 2, 3, 5, 9 and 14 .......................................................................................................34 10.4.2 Adverse Events Reported at Post-treatment Visits ...........................................................35 11 ADVERSE EVENT MANAGEMENT......................................................................................38 11.1 DEFINITIONS ...............................................................................................................................38 11.1.1 Adverse Event...................................................................................................................38 11.1.2 Serious Adverse Event......................................................................................................38 11.2 METHOD, FREQUENCY, AND TIME PERIOD FOR DETECTING ADVERSE EVENTS AND REPORTING SERIOUS ADVERSE EVENTS ........................................................................................................39 11.2.1 Definition of Severity .......................................................................................................39 11.2.2 Definition of Relationship to Study Drug.........................................................................40 11.2.3 Reporting Serious Adverse Events ...................................................................................40 11.2.4 Emergency Procedures .....................................................................................................41 12 STATISTICAL METHODS ......................................................................................................41 12.1 DATA COLLECTION METHODS ....................................................................................................41 12.2 STATISTICAL ANALYSIS PLAN ....................................................................................................42 12.3 STUDY HYPOTHESIS....................................................................................................................42 12.4 SAMPLE SIZE ESTIMATES............................................................................................................42 12.5 ANALYSIS POPULATIONS ............................................................................................................42 12.6 INTERIM AND END OF STUDY ANALYSES....................................................................................43 12.7 EFFICACY ANALYSES..................................................................................................................43 12.7.1 Primary Efficacy Endpoint ...............................................................................................43 12.7.2 Secondary Efficacy Endpoints..........................................................................................44 12.7.3 Exploratory Endpoints......................................................................................................44 12.8 SAFETY ANALYSES .....................................................................................................................45 12.9 SUB-STUDY AND PHARMACOKINETIC ANALYSIS........................................................................45 12.10 GENERAL ISSUES FOR STATISTICAL ANALYSIS ...........................................................................46 12.10.1 Multiple Comparisons and Multiplicity............................................................................46 12.10.2 Covariates.........................................................................................................................46 12.10.3 Planned Sub-Groups .........................................................................................................46 12.10.4 Missing Data.....................................................................................................................46 13 STUDY ADMINISTRATION...................................................................................................47 13.1 REGULATORY AND ETHICAL CONSIDERATIONS ..........................................................................47 13.1.1 Regulatory Authority Approvals.......................................................................................47 13.1.2 Ethics Committee Approvals............................................................................................47 13.1.3 Subject Informed Consent ................................................................................................47 13.1.4 Payment to Subjects..........................................................................................................48 13.1.5 Investigator Reporting Requirements ...............................................................................48 13.2 STUDY MONITORING...................................................................................................................48 13.3 QUALITY ASSURANCE.................................................................................................................48 13.4 STUDY TERMINATION AND SITE CLOSURE..................................................................................48 13.5 RECORDS RETENTION .................................................................................................................49 13.6 STUDY ORGANIZATION...............................................................................................................49 13.6.1 Data Monitoring Committee.............................................................................................49 13.7 CONFIDENTIALITY OF INFORMATION ..........................................................................................49 386 386 BCX1812-311 (V4.0: 18-December-2007) Page 14 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.8 STUDY PUBLICATION ..................................................................................................................49 14 REFERENCES...........................................................................................................................51 15 APPENDICES ...........................................................................................................................53 15.1 NYHA FUNCTIONAL CLASSIFICATION CRITERIA: HEART FAILURE AND ANGINA ......................53 15.2 CRITERIA FOR SEVERE COPD AND SEVERE ASTHMA .................................................................54 3.1 List of Figures Figure 1 Study Measurements and Visit Schedule.................................................................36 3.2 List of Tables Table 1 Results of study BC-01-03.......................................................................................19 Table 2 Pharmacokinetic parameters from study Him-06-111. ............................................20 Table 3 Summary of Efficacy from BCX1812-211. .............................................................22 Table 4 Summary of Safety from BCX1812-211. ................................................................23 387 387 BCX1812-311 (V4.0: 18-December-2007) Page 15 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 4 LIST OF ABBREVIATIONS AND DEFINITIONS OF TERMS AE adverse event ALT alanine aminotransferase AST aspartate aminotransferase AUC area under the curve AUC0–72 area under the curve from time 0 to 72 hours AUC0–∞ area under the curve extrapolated from time 0 to infinity BMI Body Mass Index in kg/m2 CBC complete blood count CDC Centers for Disease Control and Prevention CIOMS Council for International Organizations of Medical sciences Cmax maximum plasma concentration CK creatine kinase CMH Cochran-Mantel-Haenszel CNS central nervous system COPD chronic obstructive pulmonary disease CRF Case Report Form CV coefficient of variation ECG Electrocardiogram GCP Good Clinical Practice HCG human chorionic gonadotropin HIV Human immunodeficiency virus IC50 median inhibitory concentration ICF informed consent form ICH International Conference on Harmonization IEC Independent Ethics Committee IRB Institutional Review Board IRC influenza related complications ITT intent-to-treat ITTI intent-to-treat infected (Includes ITTI and ITTI-A) IUD intrauterine device IVRS interactive voice response system LDH lactate dehydrogenase MedDRA Medical Dictionary for Regulatory Activities MRU medical resource utilization NSAID non-steroidal anti-inflammatory drug PCR polymerase chain reaction PPI per-protocol infected RAT Rapid Antigen Test RBC red blood cell 388 388 BCX1812-311 (V4.0: 18-December-2007) Page 16 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL SAE serious adverse event SAP statistical analysis plan SD standard deviation SUSAR Suspected Unexpected Serious Adverse Event t1/2 elimination half-life t1/2 λz terminal half-life TCID50 tissue-culture infective dose50 TEAEs treatment-emergent adverse events Tmax time to attain maximum plasma concentration UPEP Urine protein electrophoresis WBC white blood cell WHO World Health Organization 389 389 BCX1812-311 (V4.0: 18-December-2007) Page 17 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 5 INTRODUCTION 5.1 Background Influenza virus is a member of the orthomyxovirus family and causes an acute viral disease of the respiratory tract. Typical influenza illness is characterized by abrupt onset of fever, headache, myalgia, sore throat, and nonproductive cough.1 The illness is usually self-limiting, with relief of symptoms occurring within 5 to 7 days. Nevertheless, it is an important disease for several reasons, including ease of communicability, short incubation time, rapid rate of viral mutation, morbidity with resultant loss of productivity, risk of complicating conditions, and increased risk of death, particularly in the elderly. During 19 of the 23 influenza seasons between 1972/1973 and 1994/1995, estimated influenza-associated deaths in the United States ranged from approximately 25 to more than 150 per 100,000 persons above 65 years of age, accounting for more than 90% of the deaths attributed to pneumonia and influenza.2 Presently, only a few measures are available that can reduce the impact of influenza: active immunoprophylaxis with an inactivated or live attenuated vaccine and chemoprophylaxis or therapy with an influenza-specific antiviral drug. Neuraminidase inhibitors are the current mainstay of antiviral treatment for influenza. Marketed neuraminidase inhibitors include zanamivir (Relenza®, GlaxoSmithKline) and oseltamivir (Tamiflu®, Roche-Gilead), an oral prodrug of the active agent, oseltamivir carboxylate. Influenza neuraminidase is a surface glycoprotein that cleaves sialic acid residues from glycoproteins and glycolipids. The enzyme is responsible for the release of new viral particles from infected cells and may also assist in the spreading of virus through the mucus within the respiratory tract. The neuraminidase inhibitors represent an important advance in the treatment of influenza with respect to activity against influenza A and B viruses, with proven therapeutic value in reducing influenza lower respiratory complications,3 and lower rates of antiviral drug resistance4. The use of currently available neuraminidase inhibitors has been limited by concerns including, the degree of effectiveness, the requirement for an inhaler device (zanamivir), and the emergence of resistant influenza virus variants in some treated populations.5 In addition, there are risks of bronchospasm with zanamivir; and gastrointestinal side effects, with oseltamivir. Peramivir is a neuraminidase inhibitor that represents a potentially promising addition to the armamentarium of drugs for the treatment of influenza infections due to its potential for parenteral administration and lower frequency of dosing. 5.2 Rationale for Study An oral formulation of peramivir has previously been evaluated in a full range of safety, tolerability, pharmacokinetic, and efficacy studies. In a multinational phase 3 clinical trial conducted in 1999-2001, oral peramivir demonstrated antiviral activity against influenza A and B infections, and improvement in the relief of clinical symptoms. Because of the limited bioavailability of peramivir following oral administration (<5%), it was determined that the parenteral route of administration is more appropriate for the delivery of peramivir. Subsequent phase 1 studies of intravenous and intramuscular formulations of peramivir have confirmed that parenteral routes of administration result in plasma levels of drug that are as much as 100 times those achieved via the oral route. In a phase 2 study of intramuscular peramivir in subjects with acute uncomplicated influenza, subjects who received a single injection of 150mg or 300mg 390 390 BCX1812-311 (V4.0: 18-December-2007) Page 18 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL peramivir had clinically meaningful reductions in the time to alleviation of symptoms of influenza, compared to subjects who received a placebo injection. Further details of these studies are provided below and in the Investigator Brochure. Because of the previous demonstration of clinical efficacy of intramuscular peramivir in acute influenza in the phase 2 study, and the encouraging pharmacokinetic and preliminary safety profile of the intramuscular formulation of peramivir demonstrated to date, this phase 3 study will be conducted to evaluate the efficacy and safety profile of an intramuscular 300 mg peramivir dose compared to placebo. 5.3 Non-Clinical Experience with Peramivir 5.3.1 In vitro Assays Peramivir is a selective inhibitor of viral neuraminidase, with 50% inhibitory concentrations (IC50) for bacterial and mammalian enzymes of >300µM.6 In an in vitro study, 42 influenza A and 23 influenza B isolates were collected from untreated subjects during the 1999–2000 influenza season in Canada.7 These isolates were tested for their susceptibility to the neuraminidase inhibitors zanamivir, oseltamivir carboxylate, and peramivir using a chemiluminescent neuraminidase assay. Inhibition of Type A influenza neuraminidase by peramivir was approximately an order of magnitude greater than inhibition of neuraminidase from Type B viruses. IC50 values for the Type A enzymes ranged from <0.1 to 1.4nM, whereas the Type B enzymes ranged from <0.1 to 11nM, with three out of four values in the 5- to 11nM range. Peramivir was the most potent drug against influenza A (H3N2) viruses with a mean IC50 of 0.60nM as well as most potent against influenza B with a mean IC50 of 0.87nM. In another in vitro comparison of peramivir, oseltamivir, and zanamivir, using a neuraminidase inhibition assay with influenza A viruses, the median IC50 of peramivir (approximately 0.34nM) was comparable to that of oseltamivir (0.45nM) and significantly lower than zanamivir (0.95nM). For influenza B virus clinical isolates, the median IC50 of peramivir (1.36nM) was comparable to that of zanamivir (2.7nM) and lower than that of oseltamivir (8.5nM).8 The potency of peramivir was evaluated against five zanamivir-resistant and six oseltamivir- resistant influenza viruses.9 Peramivir remained a potent inhibitor against all oseltamivir-resistant viruses including the mutations H274Y, R292K, E119V, and D198N, with IC50 values ≤40nM. Peramivir also potently inhibited (IC50 ≤ 26nM) the neuraminidase activity of zanamivir-resistant strains, which had the following mutations: R292K, E119G, E119A, and E119D. However, one zanamivir-resistant influenza B virus, B/Mem/96, with a mutation R152K isolated from cell culture, was relatively resistant to all neuraminidase inhibitors, including peramivir (IC50 = 400nM). 5.3.2 Animal Models In a mouse model of influenza infection, a single intramuscular injection of peramivir (10mg/kg) given 4 hours prior to inoculation with an A/NWS/33 (H1N1) influenza strain resulted in 100% survival in contrast to 100% mortality in a control group injected with saline.6 In the same mouse model, treatment of mice up to 72 hours after influenza infection using peramivir (20mg/kg) resulted in 100% survival, compared to 100% mortality in the control group injected with vehicle.10 Peramivir has also demonstrated activity in animal models utilizing a clinical H5N1 isolate as the 391 391 BCX1812-311 (V4.0: 18-December-2007) Page 19 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL infecting virus strain. In a mouse model, a single intramuscular dose of peramivir (30mg/kg) injected 1 hour after inoculation with the highly pathogenic (H5N1) A/Vietnam/1203/04 strain, resulted in a 70% survival rate that was similar to that seen in mice treated with oseltamivir given orally at 10mg/kg/day for 5 days11. In similar experiments, mice inoculated with the same strain of H5N1 virus that were then treated for up to 8 days with intramuscular peramivir exhibited 100% survival12. This longer duration of peramivir treatment also prevented viral replication in the lungs, brain and spleen at days 3, 6 and 9 post inoculations. 5.4 Previous Phase 3 Clinical Experience with Oral Peramivir An oral formulation of peramivir has previously demonstrated antiviral activity and preliminary clinical efficacy in challenge studies in human volunteers, as well as in treatment studies in patients with uncomplicated acute influenza infections during the influenza seasons of 1999- 2001. A Phase 3 multinational study (BC-01-03) of oral peramivir was conducted. Two dose regimens of oral peramivir, 800mg QD for 5 days, or 800mg QD on Day 1, followed by 400mg QD for 4 days, were compared to a matched placebo treatment group. A total of 1246 subjects were randomized to treatment at sites in the USA, Western and Eastern Europe, South America, Australia and New Zealand. As presented in the Table 1 below, the primary end-point of time to relief of influenza symptoms in 694 subjects with confirmed influenza was not found to be significantly different (p=0.17) between the three treatment groups.13 A sub-group analysis of the time to relief of symptoms by country or region demonstrated marked differences in the primary endpoint.. In the subset of influenza-infected subjects enrolled at sites in the US, clinically meaningful differences in time to relief of influenza symptoms between the placebo and the two peramivir arms were observed, however statistical significance (p=0.07) was not achieved. However, a number of secondary endpoints in this phase 3 study, such as time to overall well- being, time to normal activity, incidence of influenza related complications and quantity of viral shedding, achieved or approached statistically significant differences between the peramivir and placebo treatment groups (p=0.03-0.06). Table 1 Results of study BC-01-03 Median Time to Relief of Influenza Symptoms (Hours) Dose and Regimen Overall Results (n=694) US Sites (n=198) Peramivir 800mg po x 5d 89.0 70.8 Peramivir 800mg po x 1d and 400mg po x 4d 91.7 88.8 Placebo x 5 days 104.4 106.8 p value 0.17 0.07 5.5 Previous Phase 1 Experience with Intramuscular Peramivir Two phase 1 studies evaluating the safety and pharmacokinetics of an intramuscular formulation of peramivir have been conducted in a total of 45 healthy volunteers receiving peramivir. An additional phase 1 study has recently been initiated to evaluate the pharmacokinetics and 392 392 BCX1812-311 (V4.0: 18-December-2007) Page 20 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL tolerability of higher single doses (up to 600 mg) of intramuscular peramivir. Study Peramivir-Him-06-111 evaluated the single dose pharmacokinetics and tolerability of 75mg, 150mg and 300mg doses of peramivir administered as intramuscular (i.m.) and intravenous (i.v.) injections in a crossover design (9 subjects per group). Peak plasma levels of i.m. peramivir generally occurred within 30 minutes following injection. Plasma pharmacokinetic parameters for i.m. peramivir are summarized in Table 2 below for the three intramuscular single dose regimens evaluated. Table 2 Pharmacokinetic parameters from study Him-06-111. Dose (mg) Cmax (ng/mL) AUC0-∞ (hr·ng/mL) t½a (hr) 75 i.m. 4296 ± 812 11659 ± 1123 19.8 ± 7.9 150 i.m. 7612 ± 884 23952 ± 3804 24.3 ± 4.1 300 i.m. 15150 ± 2367 49649 ± 5619 22.8 ± 2.5 aterminal half life In a second phase 1 study, Peramivir-Him-06-112, the same dose levels of peramivir were administered as single i.m. injections on two consecutive days (6 subjects per group). This double-blind study also included a placebo arm. The pharmacokinetic parameters of i.m. peramivir following the second day of dosing were consistent with those seen following single doses of the drug. An additional phase 1 study, BCX1812-117, was initiated to evaluate the effect of needle length adjustment according to gender and body mass index on the pharmacokinetics and safety of peramivir following ventrogluteal intramuscular injection, and dorsogluteal intramuscular injection in a subgroup of subjects. Interim data are available for the first 40 subjects who received single peramivir doses of 600 mg, consisting of directly observed tolerability assessments, safety laboratory studies, reported adverse events, and pharmacokinetic data. Clinical laboratory results obtained 72 hours after dosing showed no abnormalities with regards to hematology or urinary analytes and the only chemistry analytes outside normal ranges (CK and AST) were related to receipt of intramuscular injection. A majority of the first 40 subjects treated complained of acute pain immediately after injection at the ventrogluteal site and a number of these subjects reported that the pain was also associated with muscle cramping. Some subjects reported radiation of pain to the lower extremities. In most instances, these reactions abated after 15-30 minutes. This protocol also evaluated the acute tolerability of doses of 450 mg and 600 mg of peramivir administered at the dorsogluteal site. Direct observations determined that the use of the dorsogluteal injection site resulted in an acute tolerability profile of the 600 mg dose of peramivir that was improved compared to that observed with ventrogluteal site injections. However, a number of these subjects also experienced acute pain and discomfort and some reported muscle cramping in the gluteal area which persisted for up to 30 minutes. In summary, this study confirmed that the intramuscular injection of peramivir results in acute pain and discomfort after gluteal injection in the majority of subjects in whom total doses of up to 600mg are administered. In some subjects, the acute pain at the injection site may also be 393 393 BCX1812-311 (V4.0: 18-December-2007) Page 21 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL associated with muscle cramping. Based on these findings, the dorsogluteal site will be utilized in future trials. The safety data for i.m. peramivir administered as single doses ranging from 75 mg to 600mg at the dorsogluteal injection site in each of the 3 phase 1 studies conducted to date have been unremarkable. No serious adverse events were reported. The most commonly observed adverse events or laboratory abnormalities were injection site pain or discomfort, headache, and transient increases in muscle enzymes (CK). There have been several reports of signs and symptoms of self-limited vasovagal reactions following injections. No consistent differences in frequency of adverse events or laboratory toxicities were observed between the active and placebo treatment groups in the controlled phase 1 studies, with the exception that CK elevations appeared to be dose related in the peramivir treatment groups. 5.6 Phase 2 Experience with Intramuscular Peramivir A phase 2 study BCX1812-211 was completed in 2007. This study was a randomized, double- blind placebo- controlled study to evaluate the efficacy and safety of two single dose regimens of peramivir. A total of 344 subjects were enrolled into this study with 115 subjects randomized to Placebo; 114 subjects randomized to peramivir 150 mg; and 114 subjects randomized to peramivir 300 mg. The primary endpoint of the study was the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. Based on preliminary data, the primary endpoint of time to alleviation of clinical symptoms in BCX1812-211 did not achieve statistical significance in the pre-planned ITTI study population (Table 3). Based on pre-planned and post hoc analyses, it appeared that a majority of subjects within this phase 2 study did not receive an adequate intramuscular injection. In phase 1 studies (Him-06-111 and Him-06-112) of i.m. peramivir, significant increases in creatine kinase (CK) were observed at Day 3 compared with Baseline (Day 1) in all subjects who received active study drug or placebo. CK is a well established marker of muscle damage, and it was hypothesized that CK increase may act as a surrogate marker of an adequate i.m. injection. Within the phase 2 study, an increase in CK between Baseline (Day 1) and Day 3 was not observed in a majority of subjects. In the phase 1 studies study drug was administered with a 1½ inch needle. In the phase 2 study a shorter needle (1 inch) was supplied with the study drug, with guidance that a longer needle (1½ inch) should be used for larger subjects. Based on the observed lack of CK increases at Day 3 compared to baseline, the Sponsor hypothesized that the needle used for injection failed to penetrate muscle and deliver intramuscular study medication in many subjects. A sub group of subjects was identified in which a Day 3 CK increase of at least 50U/L was observed over baseline. Within this adequate intramuscular injection sub-group, notable improvements in the time to alleviation of symptoms were observed for both peramivir dose groups: 44.6 hours for peramivir 150 mg treatment and 64.8 hours for the peramivir 300 mg treatment (Table 3). A further sub-group analysis suggested that in subjects with an influenza B infection confirmed by PCR a single dose of peramivir had limited activity (Table 3). These efficacy data support the further development of peramivir as a single dose, intramuscular treatment for acute influenza. 394 394 BCX1812-311 (V4.0: 18-December-2007) Page 22 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 3 Summary of Efficacy from BCX1812-211. Placebo Peramivir 150mg Peramivir 300mg Intent-to-Treat Infected Population1 (n=313) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=107 137.0 115.9-163.8 n=104 114.1 95.2-145.5 22.9 n=102 115.9 77.8-136.6 21.1 Adequate Injection Population2 (n=101) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=40 152.2 103.8-183.9 n=32 107.6 76.8-175.1 44.6 n=29 87.4 40.8-163.8 64.8 ITTI Influenza A infected population (n=247) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=83 138.4 117.0-173.4 n=85 115.7 92.2-145.5 22.7 n=79 115.9 51.1-195.9 22.5 ITTI Influenza B infected population (n=66) Median time to alleviation of symptoms (hrs) (95% Confidence Interval) Improvement over Placebo (hrs) n=24 117.1 100.3-162.3 n=19 100.8 68.2-162.0 16.3 n=23 123.3 67.5-178.7 -6.2 1: Intent-to-Treat Infected Population: PCR+ for either Influenza A and/or Influenza B at baseline/screening visit. 2: Adequate Injection Population: ITTI subjects in who study drug reached target muscle tissue, as evidenced by an increase in serum CK levels of ≥ 50 U/L over baseline at the Day 3 study visit. An independent data monitoring committee reviewed grouped blinded safety data throughout study BCX1812-211. In the overall safety population (n=342), doses of peramivir 150 mg and 300 mg were both found to be well tolerated and no safety concerns were identified by the DMC. The three treatment groups were similar with respect to the frequency and severity of adverse events. Two serious adverse events were reported in the study, and neither was considered by the investigator to be related to treatment. One SAE (pyelonephritis) occurred 5-days after study treatment in a subject who received placebo, and one SAE (meningitis, resulting in death) occurred 10-days after study treatment in a subject who received 300 mg of peramivir. There were no meaningful differences among the three treatment groups with respect to the frequency or severity of graded laboratory toxicities. A summary of the adverse events and graded toxicities, together with a list of the most frequently reported adverse events, is presented in Table 4. 395 395 BCX1812-311 (V4.0: 18-December-2007) Page 23 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Table 4 Summary of Safety from BCX1812-211. Safety Parameters Placebo (n=114) Peramivir 150 mg (n=113) Peramivir 300 mg (n=115) Any Clinical Adverse Event 49 (43%) 43 (38%) 44 (38%) Any Graded Laboratory Toxicity 99 (87%) 93 (82%) 92 (80%) Any Serious Adverse Event 1 (<1%) 0 1 (<1%) Most Frequent Adverse Events Assessed as Study Drug-Related Diarrhea Nausea Vasovagal Reaction 5 (4%) 7 (6%) 4 (4%) 5 (4%) 7 (6%) 2 (2%) 6 (5%) 9 (8%) 0 5.7 Dose Rationale Oseltamivir is approved for the treatment of uncomplicated acute influenza at a dosage of 75mg twice daily in adults14. Oseltamivir was shown to be clinically effective in a phase 3 study of oral oseltamivir versus placebo in naturally occurring seasonal influenza, and these data were sufficient for regulatory approval for marketing of oseltamivir. At least 75% of an oral dose of oseltamivir reaches the systemic circulation as oseltamivir carboxylate. When oseltamivir is administered orally at a dose of 75mg twice daily, the serum Cmax of oseltamivir carboxylate is approximately 348ng/mL and the AUC0-48 is 10,876 h·ng/mL. The clinical data indicate that this level of exposure to oseltamivir was sufficient to provide clinical improvement in uncomplicated acute influenza. The serum pharmacokinetic data (Cmax and AUC0-∞, respectively) following intramuscular doses of peramivir are approximately 7600ng/mL and 24,000 h·ng/mL for the 150mg dose and are approximately 15,000ng/mL and 49,000 h·ng/mL for the 300mg dose. Previous studies have assessed the concentrations of the neuraminidase inhibitor zanamivir in nasal and pharyngeal secretions after parenteral administration of this drug. . Within several hours after administration, the concentrations in secretions were approximately 100-fold lower than in serum or plasma. In theory, relatively high levels of a neuraminidase inhibitor in respiratory secretions are desirable in order to rapidly inactivate influenza virus and to delay or prevent the development of resistance in infecting virus strains. Intramuscular doses of peramivir, including doses of 300mg and 600mg have been shown to be tolerated in previous Phase 1 studies. In the completed Phase 2 study, both doses of peramivir (150 mg and 300 mg) were well tolerated and no safety concerns were apparent. The evidence of a dose response between the 150mg and 300mg doses observed in study BCX1812-211 indicates that the 300 mg dose should be studied further. The results of study BCX1812-211 support advancing the 300 mg dose to undergo further evaluation in this Phase 3 study. 396 396 BCX1812-311 (V4.0: 18-December-2007) Page 24 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6 STUDY OBJECTIVES 6.1 Objectives 6.1.1 Primary Objective To evaluate the efficacy of peramivir administered intramuscularly compared to placebo on the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. 6.1.2 Secondary Objective(s) The secondary objectives of this study are: 1. To evaluate the safety and tolerability of peramivir administered intramuscularly. 2. To evaluate secondary clinical outcomes in response to treatment. 3. To evaluate changes in influenza virus titer in nasopharyngeal samples (viral shedding) in response to treatment. 6.1.3 Exploratory Objective(s) The following exploratory objectives have been identified for this study. 1. To assess pharmacoeconomic measures as response to treatment. 2. To assess changes in influenza viral susceptibility to neuraminidase inhibitors following treatment. 6.2 Study Endpoints 6.2.1 Primary Endpoint The primary clinical endpoint is the time to alleviation of clinical symptoms of influenza. 6.2.2 Secondary Endpoint(s) Secondary safety, clinical, and virologic endpoints will include evaluations in each subject of: Safety: Incidence of treatment-emergent adverse events and treatment-emergent changes in clinical laboratory tests. Clinical: Time to resolution of fever; Incidence of influenza related complications. Virologic: Quantitative change in influenza virus shedding, measured by viral titer assay (TCID50). 6.2.3 Exploratory Endpoints Pharmacoeconomic and virologic evaluations in each subject for exploratory endpoints will also be assessed and include: 397 397 BCX1812-311 (V4.0: 18-December-2007) Page 25 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Pharmacoeconomic: Medical resource utilization (MRU), missed days of work, and impact of influenza illness on subject’s work performance and/or productivity. Virologic: Quantitative change in influenza virus shedding, measured by PCR; Change in influenza virus susceptibility to neuraminidase inhibitors. 7 STUDY DESIGN 7.1 Overall Study Design and Plan This is a multinational, randomized, double-blind study comparing the efficacy and safety of a 300 mg dose of peramivir administered intramuscularly versus placebo in adults with uncomplicated acute influenza. Approximately 600 subjects will be randomized to treatment to ensure enrollment of approximately 450 subjects that are positive for influenza A. All subjects will be centrally randomized to 300 mg of peramivir or placebo in a ratio of 2:1 and will be stratified according to smoking status and RAT test for influenza A or B. Study drug will be administered as bilateral 2mL intramuscular injections (total of 4mL injected in equally divided doses). Procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. Subjects eligible for screening will have an anterior nasal swab collected for testing by RAT for influenza A and B, in accordance with the commercially available RAT kit instructions. If the initial RAT is negative, the test should be repeated within one hour. Subjects meeting the inclusion/ exclusion criteria may be enrolled into the study. All enrolled subjects will record the following information in a Study Diary. • Assessment of the presence and severity of each of seven symptoms of influenza on a 4-point scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily (AM, PM) through Day 9 following treatment, then once daily (AM) through Day 14. • Oral temperature measurements will be taken with an electronic thermometer every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol) or other antipyretic medication. • Assessment of subject’s time lost from work or usual activities and rating of productivity compared to normal (rated as 0-10 on a visual analog scale) once daily through Day 14 • Doses of antipy retic, expectorant, and/or th roat lozenges taken for s ymptomatic relief each day through Day 14 Anterior nose (bilateral) and posterior pharynx specimens (swabs) will be collected at Day 1 (pre- treatment) and at Days 3, 5, and 9, for quantitative virologic assessments. Specimens from all subjects yielding influenza virus will also be assessed for susceptibility to neuraminidase inhibitors (Day 1 and last specimen yielding positive result) as well as other virologic 398 398 BCX1812-311 (V4.0: 18-December-2007) Page 26 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL assessments (e.g. PCR, genotypic testing). All virologic assessments will be performed by a central laboratory. Two samples for pharmacokinetic (PK) testing for plasma levels of peramivir will be obtained from all subjects randomized. The first PK sample will be obtained between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be obtained at the day 3 visit in all subjects. The data from these PK samples will be utilized in a population exposure-response analysis. At selected sites a separate sub-study will be conducted to collect additional PK samples between treatment and Day 3 for the purpose of conducting a separate exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. 8 SELECTION AND WITHDRAWAL OF SUBJECTS 8.1.1 Inclusion Criteria Subjects must meet all of the following criteria for inclusion in this study: 1. Male and non-pregnant female subjects age ≥18 years. 2. A positive Influenza A and/or B Rapid Antigen Test (RAT) performed with a commercially available test kit on an adequate anterior nasal specimen, in accordance with the manufacturer’s instructions. A negative initial RAT should be repeated within one hour. 3. Presence of fever at time of screening of ≥38.0 ºC (≥100.4 ºF) taken orally, or ≥38.5 ºC (≥101.2 ºF) taken rectally. A subject self-report of a history of fever or feverishness within the 24 hours prior to screening will also qualify for enrollment in the absence of documented fever at the time of screening. 4. Presence of at least one respiratory symptom (cough, sore throat, or nasal symptoms) of at least moderate severity. 5. Presence of at least one constitutional symptom (myalgia [aches and pains], headache, feverishness, or fatigue) of at least moderate severity. 6. Onset of symptoms no more than 48 hours before presentation for screening. 7. Written informed consent. 8.1.2 Exclusion Criteria Subjects to whom any of the following criteria apply will be excluded from the study: 1. Women who are pregnant or breast-feeding. 2. Presence of clinically significant signs of acute respiratory distress 3. History of severe chronic obstructive pulmonary disease (COPD) or severe persistent asthma. (See Section 15.2). 4. History of congestive heart failure requiring daily pharmacotherapy with symptoms consistent with New York Heart Association Class III or IV functional status within the past 12 months. (See Section 15.1). 5. Screening ECG which suggests acute ischemia or presence of medically significant dysrhythmia. 399 399 BCX1812-311 (V4.0: 18-December-2007) Page 27 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 6. History of chronic renal impairment requiring hemodialysis and/or known or suspected to have moderate or severe renal impairment (actual or estimated creatinine clearance <50 mL/min). 7. Clinical evidence of worsening of any chronic medical condition (temporally associated with the onset of symptoms of influenza) which, in the investigator’s opinion, indicates that such finding(s) could represent complications of influenza. 8. Current clinical evidence, including clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis and/or pneumonia, or active bacterial infection at any body site that requires therapy with oral or systemic antibiotics. 9. Presence of immunocompromised status due to chronic illness, previous organ transplant, or use of immunosuppressive medical therapy which would include oral or systemic treatment with > 10 mg prednisone or equivalent on a daily basis within 30 days of screening. 10. Currently receiving treatment for viral hepatitis B or viral hepatitis C. 11. Presence of known HIV infection with a CD4 count <350 cell/mm3. 12. Current therapy with oral warfarin or other systemic anticoagulant. 13. Receipt of any doses of rimantadine, amantadine, zanamivir, or oseltamivir in the 7 days prior to screening. 14. Immunized against influenza with live attenuated virus vaccine (FluMist®) in the previous 21 days. 15. Immunized against influenza with inactivated virus vaccine within the previous 14 days. 16. Receipt of any intramuscular injection within the previous 14 days. 17. History of alcohol abuse or drug addiction within 1 year prior to admission in the study. 18. Participation in a previous study of intramuscular or intravenous peramivir or previous participation in this study. 19. Participation in a study of any investigational drug or device within the last 30 days. 8.1.3 Removal of Subjects from Therapy or Assessment All subjects are permitted to withdraw from participation in this study at any time and for any reason, specified or unspecified, and without prejudice. The Investigator or sponsor may terminate the subject’s participation in the study at any time for reasons including the following: 1. Adverse event; 2. Intercurrent illness; 3. Non-compliance with study procedures; 4. Subject’s decision; 5. Administrative reasons; 6. Lack of efficacy; 7. Investigator’s opinion to protect the subject’s best interest. Any subject who withdraws because of an adverse event will be followed until the sign(s) or symptom(s) that constituted the adverse event has/have resolved or is determined to represent a stable medical condition. A subject should be withdrawn from the trial if, in the opinion of the Investigator, it is medically necessary, or if it is the desire of the subject. If a subject does not return for a scheduled visit, every effort should be made to contact the subject and determine the subject’s medical condition. In any circumstance, every effort should be made to document subject outcome, if possible. 400 400 BCX1812-311 (V4.0: 18-December-2007) Page 28 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL If the subject withdraws consent, no further evaluations should be performed and no attempts should be made to collect additional data. 9 TREATMENTS 9.1 Treatments Administered Peramivir is an investigational drug. Peramivir for intramuscular injection is a small-volume parenteral and will be supplied as a 75mg/mL solution in sodium citrate/ citric acid buffer. The pH is approximately 3.0. A matched placebo solution of sodium citrate/ citric acid buffer with 1.2% sodium chloride at a pH of approximately 3.0 will be supplied. The gluteal site of injection and the syringe needle length are to be recorded in the subjects CRF. Procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, are provided in the study drug administration manual. 9.2 Identity of Investigational Product(s) Peramivir and placebo peramivir will be supplied in clear 2mL vials. An individual study drug kit will contain 2 vials of blinded study drug (peramivir and/or placebo, depending upon the treatment group). Syringes and needles will be provided in which to draw up the solution for intramuscular injection. All study drug kits must be stored at 2-8oC. Each individual study drug kit will be labeled with some or all of the following information as required by local regulations: • Sponsor name and contact information, study protocol number, kit number, description of the contents of the container, instructions for the preparation of the syringe and administration of the study drug, conditions for storage, statement regarding the investigational (clinical trial) use of the study drug and date for retest or expiry date. Each vial of study drug will be labeled with some or all of the following information as required by local regulations: • Sponsor name, study protocol number, description of the contents of the vial, instructions for the preparation of the syringe, statement regarding the investigational (clinical trial) use of the study drug and lot number. 9.3 Method of Assigning Subjects to Treatment Groups Subjects will be centrally randomized in a ratio of 2:1 to a single dose peramivir 300mg or placebo, in accordance with a computer-generated randomization schedule prepared by a non- study statistician. Each subject’s assignment to treatment will be stratified according to smoking status and RAT test for influenza A or B. 401 401 BCX1812-311 (V4.0: 18-December-2007) Page 29 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Once a subject is eligible for randomization, he/she will be assigned a study drug kit number that will be obtained by study staff from the study interactive voice response system (IVRS). Once a study drug kit number has been assigned to a subject, it cannot be reassigned to any other subject. 9.4 Study Medication Accountability The Investigator/pharmacist must maintain accurate records of the disposition of all study drugs received from the sponsor, issued to the subject or directly administered to the subject (including date and time), and any drug accidentally destroyed. The sponsor will supply a specific drug- accountability form. At the end of the study, information describing study drug supplies (e.g., lot numbers) and disposition of supplies for each subject must be provided, signed by the Investigator or designee, and collected by the study monitor. If any errors or irregularities in any shipment of study medication to the site are discovered at any time, the Project Manager must be contacted immediately. At the end of the study, all medication not dispensed or administered and packaging materials will be collected with supervision of the monitor and returned to the sponsor or destroyed on site as dictated by the appropriate Standard Operating Procedure at the participating institution. 9.5 Blinding/Unblinding of Treatments This is a double-blind study. The treatment group assignment will not be known by the study subjects, the investigator, the clinical staff, the CRO, or Sponsor staff during the conduct of the study. Section 11.2.4 provides information regarding the process for unblinding the treatment assignment, if necessary, in the event of an SAE. 9.6 Prior and Concomitant Therapies All medications, by any route of administration, used during this study must be documented on the Case Report Form (CRF). Prescription as well as non-prescription medications should be recorded. Medication used for the treatment of influenza-related symptoms will be captured by the subject in the diary card provided by BioCryst. 9.7 Overdose and Toxicity Management To date there is no experience with overdose of intramuscular or intravenous peramivir. If overdose occurs, subjects should receive indicated supportive therapy and evaluation of hematologic and clinical chemistry laboratory tests should be conducted. The effect of hemodialysis on elimination of peramivir is unknown. 9.8 Dose Interruption As this is a study of a single dose of peramivir or placebo, guidelines for treatment interruption for drug related SAEs or toxicities are not applicable. 402 402 BCX1812-311 (V4.0: 18-December-2007) Page 30 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 10 STUDY CONDUCT A study schedule of evaluations is presented in Figure 1. A detailed list of the evaluations and visits is also provided in the following sections. 10.1 Evaluations All subjects enrolled in this study will undergo the following evaluations: 10.1.1 Informed Consent Prior to any study-related procedure subjects will be administered informed consent. For further discussion of consent see section 10.2.1. 10.1.2 Medical History Medical history, influenza vaccination status within the previous 12 months and demographic data (including smoking behavior) will be recorded at Screening/Baseline. 10.1.3 Rapid Antigen Test for Influenza At Screening/Baseline, a commercially available, rapid antigen test (RAT) for influenza A and B will be performed on an adequate specimen collected by swabbing the anterior nose in accordance with the RAT manufacturer’ instructions. A negative initial RAT should be repeated within one hour. Refer to the Study Manual [or RAT test package insert(s)] for instructions regarding the use of the RAT kits provided for this study. Sites may use the kits provided by the Sponsor or any other commercially approved RAT available at their site to document a confirmed influenza infection. 10.1.4 Physical Examination and Influenza-related Complications Assessments The Investigator will perform a physical examination at Screening/Baseline. Subject’s height and weight, and BMI will be recorded at Screening/Baseline in the subjects CRF. Study personnel will be provided with an influenza-related complications (IRC) checklist in the CRF to evaluate the subject for the presence of clinical signs and/or symptoms of the following influenza-related complications: sinusitis, otitis, bronchitis and pneumonia. Note that subjects with clinical signs and/or symptoms consistent with otitis, bronchitis, sinusitis, and/or pneumonia at screening are not eligible for enrollment in this study (See Section 8.1.2: exclusion criteria number 8). If an IRC is suspected then a targeted physical examination will be conducted to record the presence/absence of the IRC. If the investigator determines that the subject experiences (or is presumed to experience) an IRC as noted above, he/she will record that assessment on the IRC CRF page and any medication used to treat the condition will be recorded on the concomitant medication page. The investigator will promptly provide appropriate treatment for any suspected or proven IRC. Such information describing IRC signs and/or symptoms should not be reported as adverse events. Any injection site reactions noted will be recorded in the CRFs as adverse events. 10.1.5 Vital Signs Vital signs evaluations will include blood pressure, pulse rate, and respiration rate. The investigator will record oral or rectal body temperature at baseline. Thereafter the subject will 403 403 BCX1812-311 (V4.0: 18-December-2007) Page 31 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL record oral temperature twice daily in the study diary card. Vital signs will be measured at Screening/Baseline, pre-dose, and at 15 minutes following the study drug injection on Day 1, then once daily on Days 3, 5, 9, and 14. 10.1.6 Electrocardiogram Measurements A 12-lead electrocardiogram (ECG) will be obtained at Screening/Baseline. The principal investigator will be responsible for interpretation of the Screening ECG. This interpretation may be performed by the investigator or he/she may delegate this action to another physician and the investigator will acknowledge the interpretation. If this baseline ECG is interpreted as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal but does not meet the exclusionary criteria, the subject may be enrolled unless other exclusion criteria apply. The principal investigator is responsible to ensure that such an enrolled subject be informed of the nature of the abnormal ECG and that any medically indicated repeat ECG examinations and/or referral of the subject for further evaluation is made either during subject's participation in the study or immediately after the subject's discharge from the study. 10.1.7 Clinical Laboratories Clinical chemistry profiles will include a Chemistry 20 panel (includes sodium, potassium, chloride, total CO2 [bicarbonate], creatinine, glucose, urea nitrogen, albumin, total calcium, total magnesium, phosphorus, alkaline phosphatase, alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin, direct bilirubin, lactate dehydrogenase [LDH], total protein, total creatine kinase, and uric acid). Hematology will include complete blood count (CBC) with differential. Urinalysis will include tests for protein, glucose, ketones, blood, urobilinogen, nitrite, pH, and specific gravity and microscopic evaluation for RBCs and WBCs. For any subject with a Day 3 positive test for urine protein of 2+ or higher, who had a Baseline/ Day 1 protein of <2+, a 24 hour urine collection for assessment of protein will be completed. All urinalysis tests will be completed by the central laboratory. Clinical laboratory studies (clinical chemistries, hematology, and urinalysis) will be completed at Screening/Baseline, and on Days 3, 5 and 14. 10.1.8 Urine Pregnancy Test Females of childbearing potential will be evaluated for pregnancy at Screening/Baseline and Day 14 using a urine pregnancy test. 10.1.9 Serology for Influenza Paired blood samples for determination of antibody to influenza A and B (serology) will be obtained with the clinical laboratory tests at Screening/Enrollment and at Day 14. These specimens will be stored at the central laboratory and will be analyzed if needed to confirm the diagnosis of influenza. 10.1.10 Samples for Virologic Laboratory Assessments An adequate specimen will be collected by swabbing the anterior nose (bilateral) and posterior pharynx for virologic laboratory assessments including culture for the isolation of influenza virus 404 404 BCX1812-311 (V4.0: 18-December-2007) Page 32 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL and/or quantitative PCR assay at Screening/Baseline, and at Days 3, 5, and 9. Refer to the Laboratory Manual for instructions regarding the processing and shipment of these specimens. 10.1.11 Subject Self Assessments Subject self assessments will be performed beginning pre-dose on Day 1 and recorded in the subject’s Study Diary including the following: • Oral temperature measurements with an electronic thermometer (provided by the Sponsor for the study) every 12 hours. With the exception of the baseline measurement, all temperature measurements will be obtained at least 4 hours after, or immediately before, administration of oral acetaminophen (paracetamol, provided) or other anti-pyretic medications. The times of each temperature determination will be recorded in the Study Diary. The baseline temperature will be recorded at the screening/Day 1 visit prior to dosing, regardless of whether the subject had recently taken an anti-pyretic. • Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [aches and pains], headache, feverishness, and fatigue) on a 4-point severity scale (0, absent; 1, mild; 2, moderate; 3, severe) twice daily, beginning pre-dose on Day 1 and through Day 9, then once daily through Day 14. • Assessment of the subject’s time lost from work or usual activities and productivity compared to normal using a 0-10 visual analogue scale once daily through Day 14. The subject’s diary card will be reviewed by study staff at each visit for completion of the record of all required items, with particular emphasis on alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the recurrence of at least one respiratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours and the presence of fever (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Study staff will not attempt to ask subjects to retrospectively complete missing diary card data for any scheduled assessments that have not been completed prior to the clinic visit. Study staff should, however, remind the subject to complete the diary card at all scheduled times. 10.1.12 Concomitant Medications All concomitant medications used during this study, with the exception of those medications taken for symptomatic relief of influenza symptoms, which will be recorded by the subject in their diary card, must be documented on the Case Report Form (CRF). 10.1.13 Adverse Events AEs will be assessed from the time of administration of study medication through the final study visit. 10.1.14 Pharmacokinetic Exposure Samples All subjects will have two pharmacokinetic (PK) samples drawn to assess peramivir drug levels. The first PK sample will be drawn on day 1 between 30 and 60 minutes following study drug administration in all subjects. The second PK sample will be drawn at the day 3 visit in all subjects. The sample will be drawn at the same time as the blood draw is completed for clinical laboratory investigations. The 30-60 minute sample (treatment day 1) and the day 3 PK sample will be analyzed for plasma concentrations of peramivir (ng/mL) and evaluated in a population 405 405 BCX1812-311 (V4.0: 18-December-2007) Page 33 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL exposure response analysis. At selected sites a separate sub-study will also be conducted to collect additional PK samples for the purpose of conducting an exposure-response analysis. This sub-study will be conducted under a separate protocol, BCX1812-311PK. Data from these two PK samples in all subjects will be combined with data from the PK sub-study (BCX1812-311PK) to perform a population based exposure-response analysis. This analysis will be described as part of the sub-study analysis plan. All PK samples will be processed at a central bioanalytical laboratory. Refer to the instructions provided regarding the processing and shipment of these PK samples. 10.2 Screening Period 10.2.1 Informed Consent The nature and purpose of the study and the expectations of a participating subject will be described to potential study subjects, their questions will be answered, and the subjects will then be asked to sign an informed consent document. Study subjects will then undergo the screening evaluation as noted in Section 10.2.2 10.2.2 Screening/Baseline Evaluation and Enrollment Screening/baseline evaluation may be conducted in the investigator’s office or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and qualified staff. Clinical laboratory assessments performed at Screening are for the purpose of establishing a baseline. Subjects may be enrolled and receive treatment with study drug prior to receiving results of the laboratory assessments (with the exception of urine pregnancy test result, which must be known). Eligible subjects will be enrolled and randomized to blinded study treatment. The randomization will be stratified by smoking status and RAT test for influenza A or B. The Investigator will prepare a request for blinded study drug assignment which includes the subject’s screening number. The Investigator or designee at the clinical study center will contact the central randomization Interactive Voice System (IVRS call center). The IVRS call center will advise the study center of the investigational study drug kit number that is assigned to that subject at enrollment. Subjects that are determined to be ineligible will be advised accordingly, and the reason for ineligibility will be discussed. If desired by the subject the reason for ineligibility may be provided and/or discussed with their health-care provider by the Investigator or designee. Ineligible subjects who have been screened for the study will also be entered on the IVRS. For such subjects, the screening number assigned, subject’s date of birth and a reason for ineligibility will be entered on to the IVRS. All ineligible subjects must be entered onto the IVRS within 24 hours of screening, to assist with surveillance analysis during the course of the study. 10.3 Treatment Period—Study Day 1 Day 1 represents the only day of study drug dosing. Study drug administration should occur as soon as possible following informed consent, screening and randomization. Therefore, it is 406 406 BCX1812-311 (V4.0: 18-December-2007) Page 34 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL expected that the date of Screening/ Baseline and Day 1 will usually be the same date. 10.3.1 Pre-dose Evaluations-Study Day 1 Following an explanation of the Subject Self Assessment measures (Section 10.1.11), the subject shall complete the record of these assessments in their Study Diary prior to dosing. The subject will be counseled regarding the expectations for recording these assessments through Day 14. Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) and a 12 lead ECG will be obtained prior to dosing. A nasopharyngeal swab for influenza culture/ PCR assay will be obtained prior to dosing. 10.3.2 Post-dose Evaluations-Study Day 1 The blinded study drug will be administered (hour 0) as bilateral intramuscular injections within a period of ≤ 10 minutes. The calendar date and 24-hour clock time of the first and second injections will be recorded. The gluteal site of injection and the syringe needle length are also to be recorded in the subjects CRF. Sites are instructed to follow procedures for intramuscular injection, with a recommended needle length appropriate to the physical characteristics of the subject, provided in the study drug administration manual. The following evaluations will be performed post-dose on Study Day 1: • Vital sign measurements (blood pressure, pulse rate, respiration rate, and oral temperature) 15 minutes following the second intramuscular injection of blinded study drug; record the exact 24-hour clock time of the vital sign measurements in the subjects CRF. • Draw a PK sample between 30 and 60 minutes following the second intramuscular injection of blinded study drug; record the exact 24-hour clock time of the blood draw. • Record any concomitant medications. • Record any AEs. 10.4 Post-Treatment Assessment Period 10.4.1 Days 2, 3, 5, 9 and 14 Study evaluations will be performed on Days 2, 3, 5, 9 and 14 in accordance with the schedule of evaluations (Figure 1). Subjects with persistent moderate or severe influenza symptoms at day 14 will also complete a Day 21 visit, and if required a Day 28 visit. Visits may be conducted in the investigator’s office or clinic, or in the subject’s home, in which case all evaluations must be conducted by appropriately trained and qualified staff. Study staff will attempt to contact the subjects on Day 2 by telephone to confirm their compliance with completion of the Subject Self Assessments, to note any concomitant medications and adverse events. Any adverse events reported by the subject during this telephone contact will be recorded on the adverse event form and verified during the visit on day 3. For any subject with a Day 3 positive test for urine protein of 2+ or higher, who had a Baseline/ 407 407 BCX1812-311 (V4.0: 18-December-2007) Page 35 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Day 1 protein of <2+, a 24 hour urine collection for assessment of protein will be completed. At each visit it is important that the subject’s Study Diary record be reviewed for completion of daily Subject Self Assessments. The subjects should be counseled as necessary regarding self assessments and Study Diary record requirements. The subject’s diary card will be reviewed by study staff for alleviation of symptoms as well as relapse of symptoms. Relapse is defined as the recurrence of at least one respiratory symptom and one constitutional symptom (both greater than mild in severity) for 24 hours and the presence of fever (unless influenced by antipyretic use). Relapse can only occur after the subject has met the endpoint criteria for alleviation of symptoms. Day 3: The second PK sample for all subjects will be obtained on Day 3 at the same time as the clinical laboratory blood specimen is obtained. The exact 24-hour clock time of the blood draw will be recorded in the subjects CRF. Day 14: If a subject has one or more persistent or recurrent symptoms of influenza (of the seven symptoms assessed) of either moderate or severe intensity at the Day 14 visit then the subject must be evaluated in further follow-up visits, at day 21 (± 3 days), and if required at day 28 (± 3 days) If a subject reports moderate or severe influenza symptoms then the investigator will record the intensity of each of the influenza symptoms on a visit specific CRF page at the day 21 and day 28 visits. After day 14 the subject will not record symptoms in a diary. Day 21 (if applicable): The day 21 visit is to be completed only if the subject reports symptoms of influenza of moderate or severe intensity at day 14. The investigator will make a clinical judgment as to the appropriate medical course of action for such subjects at the Day 21 visit and such action(s) will be recorded on the Day 21 CRF page. The investigator will recall the subject for a further study visit at day 28 (± 3 days) if moderate or severe symptom(s) of influenza persist at Day 21. Day 28 (if applicable): The day 28 visit is to be completed only if the subject reports symptoms of influenza of moderate or severe intensity at day 21. The investigator will make a clinical judgment as to the appropriate medical course of action for such subjects at this visit and such action(s) will be recorded on the Day 28 CRF page. No further follow-up visits beyond day 28 are to be formally scheduled unless in the clinical judgment of the investigator further follow-up is required. The investigator will use his/her clinical judgment to manage the subject, referring the subject, if appropriate, for further medical care. 10.4.2 Adverse Events Reported at Post-treatment Visits In this study, symptoms of influenza will be considered separately from adverse events reported during the post-treatment period. Accordingly, adverse events that have onset in the post- treatment period will be assessed and followed as specified in 11.2. Specifically, the investigator should attempt to follow all unresolved AEs and/or SAEs observed during the study until they are resolved, or are judged medically stable, or are otherwise medically explained. 408 408 BCX1812-311 (V4.0: 18-December-2007) Page 36 Figure 1 Study Measurements and Visit Schedule Treatment Period Assessment Day End of Study Early Withdrawal Assessments Screening 1 (Baseline) Day 11 Day 22 Day 3 Day 5 (±1 day) Day 9 (±3 day) Day 14 (±3 day) 8 Informed Consent X Rapid Antigen test for Influenza A and B X Medical History/Physical Exam X Influenza-related complications (IRC) checklist3 X X X X X Inclusion/Exclusion X Clinical Chemistries4 X X X X Hematology4 X X X X Exposure Pharmacokinetic Sample9 X X4 Serology (serum) Sample X X Urinalysis10 X X X X Urine Pregnancy Test X X Vital Signs5 X X X X X X ECG6 X Sample (nasopharyngeal swab) for Influenza Virus Culture/ PCR assay and for resistance studies X X X X Study Drug Administration X Subject Diary Review7 X X X X X X Concomitant Medications X X X X X X X Adverse Events X X X X X X Study Measurements and Visit Schedule Figure Legend on Next Page BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 409 409 BCX1812-311 (V4.0: 18-December-2007) Page 37 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Study Measurements and Visit Schedule Figure Legend 1 It is expected that the date of Screening and Day 1 (date of administration of study drug) will be the same. Visits at Screening and on subsequent study days may occur in subject’s home by the investigator (all visits) or appropriately trained study center staff (Day 3, 5, 9 visits). 2 Day 2 will be a telephone contact with the subject to ensure compliance with diary card completion, concomitant medication and adverse event review. 3 If an IRC is suspected then a targeted physical examination will be conducted to record the presence/absence of the IRC. 4 Clinical laboratory assessments performed at Screening are for the purpose of establishing a baseline. Subject may be enrolled and begin treatment with study drug prior to receiving results. A PK sample will be drawn 30-60 minutes following the second treatment administration injection. On Day 3 an extra tube will be included with the safety blood sample to collect the second PK sample for evaluation of peramivir concentrations. 5 Vital sign measures will include blood pressure, pulse rate and respiration rate. Vital signs will be recorded at Screening, pre-dose and at 15 min following the study drug administration on Day 1, then once on remaining days as stipulated. The investigator will record oral temperature at baseline. Thereafter the subject will report oral temperature measurements twice daily in the Study Diary 6 If the baseline ECG is interpreted by the conducting physician as meeting the exclusionary criteria listed in section 8.1.2 the subject will not be enrolled in this study. If the ECG is interpreted as being abnormal and does not meet the exclusionary criteria (e.g. acute ischemia, medically significant dysrhythmia) then this subject may be enrolled If the conditions highlighted in section 10.1.5 are met for the subject. 7 Subjects record symptom assessment in Study Diary, twice daily, beginning pre-dose on Day 1 through Day 9, then once daily through Day 14. Subjects record time lost from work or usual activities and rating of productivity compared to normal once daily through Day 14. Subjects record oral temperature twice daily throughout as well as all influenza related medications. 8 For any subject with unresolved moderate or severe intensity influenza symptoms a follow up assessment will be scheduled at Day 21 (± 3 days) and Day 28 (± 3 days) if required (See Section 10.4.1). 9 A PK sample will be drawn 30-60 minutes following the second treatment injection on Day 1, and on Day 3. 10For any subject with a Day 3 positive test for urine protein of 2+ or higher, who had a Baseline/ Day 1 protein of <2+, a 24 hour urine collection for assessment of protein will be completed. 410 410 BCX1812-311 (V4.0: 18-December-2007) Page 38 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11 ADVERSE EVENT MANAGEMENT 11.1 Definitions 11.1.1 Adverse Event An AE is any untoward medical occurrence in a clinical study subject. No causal relationship with the study drug or with the clinical study itself is implied. An AE may be an unfavorable and unintended sign, symptom, syndrome, or illness that develops or worsens during the clinical study. Clinically relevant abnormal results of diagnostic procedures including abnormal laboratory findings (e.g., requiring unscheduled diagnostic procedures or treatment measures, or resulting in withdrawal from the study) are considered to be AEs. AEs may be designated as “nonserious” or “serious” (see Section 11.1.2). Surgical procedures are not AEs but may constitute therapeutic measures for conditions that require surgery. The condition for which the surgery is required is an AE, if it occurs or is detected during the study period. Planned surgical measures permitted by the clinical study protocol and the conditions(s) leading to these measures are not AEs, if the condition(s) was (were) known before the start of study treatment. In the latter case the condition should be reported as medical history. Assessment of seven influenza symptoms (cough, sore throat, nasal obstruction, myalgia [aches and pains], headache, feverishness, and fatigue) will be documented in a subject’s study diary and analyzed as a measure of efficacy of the study treatment. These symptoms will not be reported as AEs unless the symptom(s) worsen to the extent that the outcome fulfils the definition of an SAE, which then must be recorded as such (see Section 11.1.2). Likewise, a RAT for influenza is required at screening in order to determine eligibility for the study, and therefore a positive RAT is not considered an AE. 11.1.2 Serious Adverse Event A SAE is an adverse event that results in any of the following outcomes: • Death • Is life-threatening (subject is at immediate risk of death at the time of the event; it does not refer to an event that hypothetically might have caused death if it were more severe) • Requires in-subject hospitalization (formal admission to a hospital for medical reasons) or prolongation of existing hospitalization • Results in persistent or significant disability/incapacity (i.e., there is a substantial disruption of a person’s ability to carry out normal life functions) • Is a congenital anomaly/birth defect • Is an important medical event Important medical events that may not result in death, are not life-threatening, or do not require hospitalization may be considered an SAE when, based upon appropriate medical judgment, they may jeopardize the subject or may require medical or surgical intervention to prevent one of the 411 411 BCX1812-311 (V4.0: 18-December-2007) Page 39 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL outcomes listed in this definition. Examples of such events include allergic bronchospasm requiring intensive treatment in an emergency room or at home, blood dyscrasias or convulsions that do not result in subject hospitalization, or the development of drug dependency or drug abuse. In addition Suspected Unexpected Serious Adverse Reactions (SUSAR) may also be reported to competent authorities where this type of reporting is required (e.g. European Union Directives). See section 11.2.3. 11.2 Method, Frequency, and Time Period for Detecting Adverse Events and Reporting Serious Adverse Events Reports of AEs are to be collected from the time of study drug administration through the follow-up period ending on Day 14. The Investigator or designee must completely and promptly record each AE on the appropriate CRF. The Investigator should attempt, if possible, to establish a diagnosis based on the presenting signs and symptoms. In such cases, the diagnosis should be documented as the AE and not the individual sign/symptom. If a clear diagnosis cannot be established, each sign and symptom must be recorded individually. The Investigator should attempt to follow all unresolved AEs and/or SAEs observed during the study until they are resolved, or are judged medically stable, or are otherwise medically explained. 11.2.1 Definition of Severity All AEs will be assessed (graded) for severity and classified into one of four clearly defined categories as follows: • Mild: (Grade 1): Transient or mild symptoms; no limitation in activity; no intervention required. The AE does not interfere with the participant’s normal functioning level. It may be an annoyance. • Moderate: (Grade 2): Symptom results in mild to moderate limitation in activity; no or minimal intervention required. The AE produces some impairment of functioning, but it is not hazardous to health. It is uncomfortable or an embarrassment. • Severe: (Grade 3): Symptom results in significant limitation in activity; medical intervention may be required. The AE produces significant impairment of functioning or incapacitation. • Life-threatening: (Grade 4): Extreme limitation in activity, significant assistance required; significant medical intervention or therapy required; hospitalization. 412 412 BCX1812-311 (V4.0: 18-December-2007) Page 40 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 11.2.2 Definition of Relationship to Study Drug The blinded Principal Investigator must review each AE and make the determination of relationship to study drug using the following guidelines: Not Related: The event can be readily explained by other factors such as the subject’s underlying medical condition, concomitant therapy, or accident, and no temporal relationship exists between the study drug and the event. Unlikely: The event does not follow a reasonable temporal sequence from drug administration and is readily explained by the subject’s clinical state or by other modes of therapy administered to the subject. Possibly Related: There is some temporal relationship between the event and the administration of the study drug and the event is unlikely to be explained by the subject’s medical condition, other therapies, or accident. Probably Related: The event follows a reasonable temporal sequence from drug administration, abates upon discontinuation of the drug, and cannot be reasonably explained by the known characteristics of the subject’s clinical state. Definitely Related: The event follows a reasonable temporal sequence from administration of the medication, follows a known or suspected response pattern to the medication, is confirmed by improvement upon stopping the medication (dechallenge), and reappears upon repeated exposure (rechallenge, if rechallenge is medically appropriate). 11.2.3 Reporting Serious Adverse Events Any SAE / SUSAR (Suspected Unexpected Serious Adverse Reaction) must be reported to BioCryst or its designee within 24 hours of the Investigator’s recognition of the SAE by first notifying the Medical Monitor at the number listed below: Telephone: Europe: +44 1628 548000; North America: 1-888-724-4908 Facsimile: Europe: +44 1628 540028; North America: 1-888-887-8097 or 1-609-734-9208 In addition to the telephone numbers listed above, local country-specific toll free numbers may be provided within the study reference manual. The site is required to fax a completed SAE / SUSAR Report Form (provided as a separate report form) within 24 hours. All additional follow-up evaluations of the SAE / SUSAR must be reported and sent by facsimile to BioCryst or its designee as soon as they are available. The Principal Investigator or designee at each site is responsible for submitting the IND safety report (initial and follow-up) or other safety information (e.g., revised Investigator’s Brochure) to the Institutional Review Board/Independent Ethics Committee (IRB/IEC) and for retaining a copy in their files. 413 413 BCX1812-311 (V4.0: 18-December-2007) Page 41 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL If the Investigator becomes aware of any SAE / SUSAR occurring within 30 days after a subject has completed or withdrawn from the study, he or she should notify BioCryst or its designee. Any SAEs / SUSARs considered possibly related to treatment will be reported to the FDA and other Regulatory Competent Authorities as applicable via the MedWatch / CIOMS reporting system in accordance with FDA and other applicable regulations. However, the Investigator is not obligated to actively seek reports of AEs in former study participants. While pregnancy is not considered an AE, all cases of fetal drug exposure via parent as study participant (see Section 4.4) are to be reported immediately to BioCryst or its designee. Information related to the pregnancy must be given on a “Pregnancy Confirmation and Outcome” form that will be provided by the Sponsor or its designee. 11.2.4 Emergency Procedures In the event of an SAE / SUSAR, the Principal Investigator may request the unblinding of the treatment assignment for the subject affected. If time allows (i.e., if appropriate treatment for the SAE is not impeded), the Principal Investigator will first consult with the Medical Monitor regarding the need to unblind the treatment assignment for the subject. At all times, the clinical well-being of any subject outweighs the need to consult with the Medical Monitor. The Principal Investigator may contact the IVRS central randomization center and request the unblinding of the treatment assignment that corresponds to the affected subject. The IVRS center will record the name of the Investigator making the request, the date and time of the request, the subject number and date of birth. The Sponsor will be informed within 24 hours if unblinding occurred. 12 STATISTICAL METHODS Descriptive statistical methods will be used to summarize the data from this study, with hypothesis testing performed for the primary and other selected efficacy endpoints. Unless stated otherwise, the term “descriptive statistics” refers to number of subjects (n), mean, median, standard deviation (SD), minimum, and maximum for continuous data and frequencies and percentages for categorical data. The term “treatment group” refers to randomized treatment assignment: peramivir 300 mg or placebo. All data collected during the study will be included in data listings. Unless otherwise noted, the data will be sorted first by treatment assignment, subject number, and then by date within each subject number. Unless specified otherwise, all statistical testing will be two-sided and will be performed using a significance (alpha) level of 0.05. All statistical analyses will be conducted with the SAS® System, version 9.1.3 or higher. 12.1 Data Collection Methods The data will be recorded on the CRF approved by BioCryst. All documentation supporting the CRF data, such as laboratory or hospital records, must be readily available to verify entries in the CRF. Documents (including laboratory reports, hospital records subsequent to SAEs, etc.) transmitted to BioCryst should not carry the subject’s name. This will help to ensure subject confidentiality. 414 414 BCX1812-311 (V4.0: 18-December-2007) Page 42 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.2 Statistical Analysis Plan A statistical analysis plan (SAP) will be created and approved prior to the review of any data. This document will provide a more technical and detailed description of the proposed data analysis methods and procedures. 12.3 Study Hypothesis The primary hypothesis for evaluating the primary objective may be stated as follows: The null hypothesis (H0) is that the time to alleviation of influenza symptoms is the same for subjects treated with placebo and for subjects treated with peramivir 300mg. The alternative hypothesis (H1) is that subjects treated with peramivir 300mg have an improvement in time to alleviation of influenza symptoms over those treated with placebo. 12.4 Sample Size Estimates From preliminary results of a phase 2 study evaluating peramivir treatment of uncomplicated influenza, it is expected that the median time to alleviation of symptoms will be 137.0 hours (95% CI: 115.9, 165.8) for subjects receiving placebo treatment. Additionally, it is expected that the median time to alleviation for the 300 mg dose peramivir arm will be reduced by 30% compared to placebo yielding a hazard ratio of 0.70. Data from the phase 2 study suggested that the activity of peramivir against influenza B was limited. Therefore, this study will be sized to ensure that a minimum number of influenza A subjects is enrolled to achieve study power. Using these assumptions, a sample size of 450 evaluable subjects with influenza A (300 in the 300 mg treatment group and 150 evaluable subjects in the placebo group) is sufficient to provide at least 90% power to detect a hazard ratio of 0.70 using a log-rank statistic and α = 0.05 (SAS version 9.1.3; total accrual time 7 months; total enrollment time 6 months). 12.5 Analysis Populations The populations for analysis will include the intent-to-treat (ITT), intent-to-treat infected (ITTI and ITTI-A), per-protocol infected (PPI), and safety populations. Additional analysis populations may be defined to evaluate study results. Any additional analysis populations will be defined in the SAP. Intent-To-Treat Population: The ITT population will include all subjects who are randomized. Subjects will be analyzed in the treatment group to which they were randomized. The ITT population will be used for analyses of accountability and demographics. Intent-To-Treat Infected Population: The ITTI population will include all subjects who are randomized, received study drug, and have confirmed influenza by culture or PCR. Subjects will be analyzed according to the treatment randomized. If a discrepancy is noted in the final database for any subject, such that the drug differs from the randomized treatment assignment, efficacy analyses may be repeated with the subjects analyzed according to the treatment received. The ITTI population will be used for primary analyses of efficacy. Intent-To-Treat Infected Population-A: The ITTI-A population will include all subjects who 415 415 BCX1812-311 (V4.0: 18-December-2007) Page 43 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL are randomized, received study drug, and have confirmed influenza A by culture or PCR. Subjects will be analyzed according to the treatment randomized. If a discrepancy is noted in the final database for any subject, such that the drug differs from the randomized treatment assignment, efficacy analyses may be repeated with the subjects analyzed according to the treatment received. The ITTI-A population will be used for supportive analyses of efficacy. Per-Protocol Infected: The PPI population includes all subjects in the ITTI population who receive an adequate intramuscular injection. The definition of an adequate intramuscular injection will be further described in the SAP. The PPI population will be used for supportive analyses of efficacy. Safety Population: The safety population will include all subjects who received study drug. Subjects will be analyzed according to the treatment received. This population will be used for all safety analyses. 12.6 Interim and End of Study Analyses Interim Analysis An independent DMC will review safety data on an ongoing basis. Safety analyses will be presented in a manner consistent with the presentations intended for the final analysis. End of Study Analysis A final analysis is planned after the last subject completes or discontinues the study, and the resulting clinical database has been cleaned, quality checked, and locked. 12.7 Efficacy Analyses 12.7.1 Primary Efficacy Endpoint The primary efficacy endpoint is the time to alleviation of symptoms of influenza in subjects diagnosed with influenza, defined as the time from injection of study drug to the start of the time period when a subject has Alleviation of Symptoms. A subject has Alleviation of Symptoms if all of the seven symptoms of influenza (nasal congestion, sore throat, cough, aches and pains, fatigue (tiredness), headache, feeling feverish) assessed on his/her subject diary are either absent or are present at no more than mild severity level and at this status for at least 21.5 hours (24 hours - 10%). Descriptive statistics for the primary efficacy variable will be tabulated by treatment group. Alleviation of symptoms will be determined by assessment of symptoms as reported on each subject’s diary card. Time to alleviation of symptoms will be summarized for each treatment group (300 mg peramivir and placebo). Treatment comparisons between the 300 mg peramivir group and placebo will be assessed using a Wilcoxon-Gehan19 statistic stratified by smoking status and positive PCR or viral culture for influenza A or B at screening for the ITTI and PPI populations. Subjects who do not experience alleviation of symptoms will be censored at the date of their last non-missing post-baseline assessment. 416 416 BCX1812-311 (V4.0: 18-December-2007) Page 44 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.7.2 Secondary Efficacy Endpoints All secondary endpoints will be summarized using descriptive statistics by treatment group, and study day/time, if appropriate. Statistical comparisons for each endpoint will be constructed without adjustment for multiple endpoints. The reduction in viral shedding will be assessed as the change in viral titers defined as the time- weighted change from baseline in log10 tissue culture infective dose50 (TCID50/mL) and will be summarized for each treatment group. The time-weighted average change from baseline will be calculated on a by-subject basis through Day 9 using the trapezoidal rule with all available data (data after initiation of study treatment) minus the baseline value. Specifically, the time-weighted area under the curve for time a (ta) to time b (tb) is given by the formula ) ( ) ( b a b a t t t t AUC TWAUC − − = , where ∑ − = − + − + = − 1 1 1 2 ) )( ( ) ( b a i i i i i b a t t y y t t AUC and ti represents the date of the ith viral titer assessment and yi represents the log10 value of the ith viral titer assessment. If there is a baseline value and only one follow-up value, yi then the time-weighted change from baseline is defined as the difference between yi and baseline. If there is a baseline value and no follow-up value, the subject is excluded from analysis. The differences between the 300 mg peramivir treatment group and placebo will be evaluated using a van Elteren Test adjusting for smoking status and positive PCR or viral culture for influenza A or B at screening. Subject’s oral temperature will be summarized by study visit and treatment group. Differences between the 300 mg peramivir treatment group and placebo will be assessed using the van Elteren test controlling for smoking status and positive PCR or viral culture for influenza A or B at screening. A subject has Resolution of Fever if he/she has a temperature < 37.2°C (99.0°F) and no antipyretic medications have been taken for at least 12 hours. The time to resolution of fever will be estimated using the method of Kaplan-Meier using temperature and symptom relief medication information obtained from the subject diary data. Differences between the treatment groups will be assessed using the Wilcoxon-Gehan statistic controlling for smoking status and positive PCR or viral culture for influenza A or B at screening. Subjects who do not have resolution of fever will be censored at the time of their last non-missing post-baseline temperature assessment. The number and percentage of subjects experiencing influenza related complications will be summarized by complication preferred term and treatment group. The difference between the treatment groups (300 mg peramivir and placebo) will be assessed using a Cochran-Mantel- Haenszel (CMH) test statistic controlling for smoking status, and positive PCR or viral culture for influenza A or B at screening, if applicable. 12.7.3 Exploratory Endpoints The MRU, MRU-related direct costs, and indirect costs attributable to days missed of work and work productivity and/or performance losses will be summarized by treatment group, smoking status, and positive PCR or viral culture for influenza A or B at screening, if applicable. Methods for describing differences between treatment groups will be presented in the SAP. 417 417 BCX1812-311 (V4.0: 18-December-2007) Page 45 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL Genotypic (including Hemagglutinin and Neuraminidase), phenotypic, viral culture and PCR data will be listed for each subject. These listings will be constructed in a manner consistent with the FDA June 2006 Guidance Document: “Guidance for Submitting Influenza Resistance Data”.18 Additionally, the number and percentage of genotypic changes from wild-type amino acid will be summarized separately for treatment group, protein type, and study visit. 12.8 Safety Analyses AEs will be mapped to a MedDRA-preferred term and system organ classification. The occurrence of TEAEs will be summarized by treatment group using MedDRA-preferred terms, system organ classifications, and severity. If a subject experiences multiple events that map to a single preferred term, the greatest severity and strongest Investigator assessment of relation to study drug will be assigned to the preferred term for the appropriate summaries. All AEs will be listed for individual subjects showing both verbatim and preferred terms. Separate summaries of treatment-emergent SAEs and AEs related to study drug will be generated. Descriptive summaries of vital signs and clinical laboratory results will be presented by study visit. Laboratory abnormalities will be graded according to the DAIDS Table for Grading Adverse Events for Adults and Pediatrics (Publish Date: December 2004). The number and percentage of subjects experiencing treatment-emergent graded toxicities will be summarized by treatment group. Laboratory toxicity shifts from baseline to Day 3, Day 5, and Day 14 will be summarized by treatment group. Abnormal physical examination findings will be presented by treatment group. The number and percent of subjects experiencing each abnormal physical examination finding will be included. Concomitant medications will be coded using the WHO dictionary. These data will be summarized by treatment group. Subject disposition will be presented for all subjects. The number of subjects who completed the study and discontinued from the study will be provided. The reasons for early discontinuation also will be presented. 12.9 Sub-Study and Pharmacokinetic Analysis A sub-study to collect pharmacokinetic samples in up to 60 peramivir treated subjects to examine exposure response will be conducted at selected sites. The data from the sub-study will be combined with the two PK samples (collected on all subjects at 30-60 minutes following administration of study drug and on study day 3) to perform a population exposure-response analysis. All analyses related to exposure-response will be completed as part of the sub-study. All statistical methods will be outlined as part of the sub-study protocol and exposure-response analysis plan. All sub-study analyses, and exposure-response analyses from PK samples obtained in this study and a companion study BCX1812-312, will be reported in a separate sub-study report. 418 418 BCX1812-311 (V4.0: 18-December-2007) Page 46 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 12.10 General Issues for Statistical Analysis 12.10.1 Multiple Comparisons and Multiplicity No adjustments for multiple comparisons are currently planned. 12.10.2 Covariates Primary and secondary efficacy analyses will be adjusted for smoking status and positive PCR or viral culture for influenza A or B at screening, where appropriate. 12.10.3 Planned Sub-Groups The primary efficacy endpoint will be summarized separately by smoking status and positive PCR or viral culture for influenza A or B at screening using descriptive statistics by treatment group and study day, where appropriate. No formal statistical testing will be utilized. Additional analyses may be performed by country, if necessary, for submission to local regulatory authorities. 12.10.4 Missing Data Every effort will be made to obtain required data at each scheduled evaluation from all subjects who have been randomized. No attempt will be made retrospectively to obtain missing subject reported data (including influenza symptom severity assessments, temperature, ability to perform usual activities, missed days of work and impact of influenza on subject’s work performance and/or productivity) that has not been completed by the subject at the time of return of the subject diary to the investigative site. In situations where it is not possible to obtain all data, it may be necessary to impute missing data. In assessing the primary efficacy endpoint, for subjects who withdraw or who do not experience alleviation of symptoms, missing data will be censored using the date of subject’s last non- missing assessment of influenza symptoms. Missing assessments of influenza symptoms conservatively will be imputed as having severity above absent or mild (as failures). For the subject diary data, the following data conventions will be utilized. Missing diary completion will be imputed as 11:59 for diary entries designated as morning and 23:59 for evening and daily reported values. Select exploratory sensitivity analyses may be conducted to ascertain the effect, if any, of these methods. These sensitivity analyses are further described in the SAP. Secondary efficacy endpoints with time to event data will be censored using the date of subject’s last non- missing assessment of the given endpoint. 419 419 BCX1812-311 (V4.0: 18-December-2007) Page 47 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13 STUDY ADMINISTRATION 13.1 Regulatory and Ethical Considerations 13.1.1 Regulatory Authority Approvals This study will be conducted in compliance with the protocol; GCPs, including International Conference on Harmonization (ICH) of Technical Requirements for Registration of Pharmaceuticals for Human Use Guidelines; FDA regulatory requirements and in accordance with the ethical principles of the Declaration of Helsinki. In addition, all applicable local laws and regulatory requirements relevant to the use of new therapeutic agents in the countries involved will be adhered to. The Investigator should submit written reports of clinical study status to their Institutional Review Board (IRB)/ Independent Ethics Committee (IEC) annually or more frequently if requested by the IRB/ IEC. A final study notification will also be forwarded to the IRB/IEC after the study is completed or in the event of premature termination of the study in accordance with the applicable regulations. Copies of all contact with the IRB/ IEC should be maintained in the study documents file. Copies of clinical study status reports (including termination) should be provided to BioCryst. 13.1.2 Ethics Committee Approvals Before initiation of the study at each investigational site, the protocol, the informed consent form, the subject information sheet, and any other relevant study documentation will be submitted to the appropriate IRB/IEC. Written approval of the study must be obtained before the study center can be initiated or the investigational medicinal product is released to the Investigator. Any necessary extensions or renewals of IRB/IEC approval must be obtained, in particular, for changes to the study such as modification of the protocol, the informed consent form, the written information provided to subjects and/or other procedures. The Investigator will report promptly to the IRB/IEC any new information that may adversely affect the safety of the subjects or the conduct of the study. On completion of the study, the Investigator will provide the IRB/IEC with a report of the outcome of the study. 13.1.3 Subject Informed Consent Signed informed consent must be obtained from each subject prior to performing any study- related procedures. Each subject should be given both verbal and written information describing the nature and duration of the clinical study. The informed consent process should take place under conditions where the subject has adequate time to consider the risks and benefits associated with his/her participation in the study. Subjects will not be screened or treated until the subject has signed an approved ICF written in a language in which the subject is fluent. The ICF that is used must be approved both by BioCryst and by the reviewing IRB/ IEC. The informed consent should be in accordance with the current revision of the Declaration of Helsinki, current ICH and GCP guidelines, and BioCryst policy. The Investigator must explain to potential subjects or their legal representatives the aims, 420 420 BCX1812-311 (V4.0: 18-December-2007) Page 48 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL methods, reasonably anticipated benefits, and potential hazards of the trial and any discomfort it may entail. Subjects will be informed that they are free not to participate in the trial and that they may withdraw consent to participate at any time. They will be told that refusal to participate in the study will not prejudice future treatment. They will also be told that their records may be examined by competent authorities and authorized persons but that personal information will be treated as strictly confidential and will not be publicly available. Subjects must be given the opportunity to ask questions. After this explanation and before entry into the trial, consent should be appropriately recorded by means of the subject’s dated signature. The subject should receive a signed and dated copy of the ICF. The original signed informed consent should be retained in the study files. The Investigator shall maintain a log of all subjects who sign the ICF and indicate if the subject was enrolled into the study or reason for non-enrollment. 13.1.4 Payment to Subjects Reasonable compensation to study subjects may be provided if approved by the IRB/IEC responsible for the study at the Investigator’s site. 13.1.5 Investigator Reporting Requirements The Investigator will provide timely reports regarding safety to his/her IRB/IEC as required. 13.2 Study Monitoring During trial conduct, BioCryst or its designee will conduct periodic monitoring visits to ensure that the protocol and GCPs are being followed. The monitors may review source documents to confirm that the data recorded on CRFs is accurate. The investigator and institution will allow BioCryst monitors or its designees and appropriate regulatory authorities direct access to source documents to perform this verification. 13.3 Quality Assurance The trial site may be subject to review by the IRB/IEC, and/or to quality assurance audits performed by BioCryst, and/or to inspection by appropriate regulatory authorities. It is important that the investigator(s) and their relevant personnel are available during the monitoring visits and possible audits or inspections and that sufficient time is devoted to the process. 13.4 Study Termination and Site Closure BioCryst reserves the right to discontinue the trial prior to inclusion of the intended number of subjects but intends only to exercise this right for valid scientific or administrative reasons. After such a decision, the Investigator must contact all participating subjects immediately after notification. As directed by BioCryst, all study materials must be collected and all case report forms completed to the greatest extent possible. 421 421 BCX1812-311 (V4.0: 18-December-2007) Page 49 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 13.5 Records Retention To enable evaluations and/or audits from regulatory authorities or BioCryst, the Investigator agrees to keep records, including the identity of all participating subjects (sufficient information to link records, case report forms and hospital records), all original signed informed consent forms, copies of all case report forms and detailed records of treatment disposition. The records should be retained by the Investigator according to local regulations or as specified in the Clinical Trial Agreement, whichever is longer. If the Investigator relocates, retires, or for any reason withdraws from the study, the study records may be transferred to an acceptable designee, such as another investigator, another institution, or to BioCryst. The Investigator must obtain BioCryst’s written permission before disposing of any records. 13.6 Study Organization 13.6.1 Data Monitoring Committee BioCryst will assemble an independent Data Monitoring Committee (DMC) to assess safety parameters of the trial on a periodic, ongoing basis while the trial is in progress. The committee will include a statistician and three physicians, two of whom will be Infectious Disease / Clinical Virology specialists. Full details of the composition of the DMC and how the DMC is to operate will be described in a separate DMC charter. 13.7 Confidentiality of Information BioCryst affirms the subject’s right to protection against invasion of privacy. Only a subject identification number, initials and/or date of birth will identify subject data retrieved by BioCryst. However, in compliance with federal regulations, BioCryst requires the investigator to permit BioCryst’s representatives and, when necessary, representatives of the FDA or other regulatory authorities to review and/or copy any medical records relevant to the study. BioCryst will ensure that the use and disclosure of protected health information obtained during a research study complies with the HIPAA Privacy Rule, where this rule is applicable. The Rule provides federal protection for the privacy of protected health information by implementing standards to protect and guard against the misuse of individually identifiable health information of subjects participating in BioCryst-sponsored Clinical Trials. "Authorization" is required from each research subject, i.e., specified permission granted by an individual to a covered entity for the use or disclosure of an individual's protected health information. A valid authorization must meet the implementation specifications under the HIPAA Privacy Rule. Authorization may be combined in the Informed Consent document (approved by the IRB/IEC) or it may be a separate document, (approved by the IRB/IEC) or provided by the Investigator or Sponsor (without IRB/IEC approval). It is the responsibility of the investigator and institution to obtain such waiver/authorization in writing from the appropriate individual. HIPAA authorizations are required for U.S. sites only. 13.8 Study Publication All data generated from this study are the property of BioCryst and shall be held in strict 422 422 BCX1812-311 (V4.0: 18-December-2007) Page 50 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL confidence along with all information furnished by BioCryst. Independent analysis and/or publication of these data by the Investigator or any member of his/her staff are not permitted without prior written consent of BioCryst. Written permission to the Investigator will be contingent on the review by BioCryst of the statistical analysis and manuscript and will provide for nondisclosure of BioCryst confidential or proprietary information. In all cases, the parties agree to submit all manuscripts or abstracts to all other parties 30 days prior to submission. This will enable all parties to protect proprietary information and to provide comments based on information that may not yet be available to other parties. 423 423 BCX1812-311 (V4.0: 18-December-2007) Page 51 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 14 REFERENCES 1. Cox NJ, Subbarao K. Influenza. Lancet 1999;354(9186):1277–1282. 2. Thompson WW, Shay KD, Weintraub E, Branner L, Cox N, et al. Mortality associated with influenza and respiratory syncytial virus in the United States. JAMA 2003;289(2):179–186. 3. Kaiser L, Wat C, Mills T, Mahoney P, Ward P, et al. Impact of oseltamivir treatment on influenza-related lower respiratory tract complications and hospitalizations. Arch Intern Med 2003;163(14):1667–1672. 4. Hayden FG, Treanor JJ, Fritz RS, Lobo M, Betts RF, et al. Use of the oral neuraminidase inhibitor oseltamivir in experimental human influenza: randomized controlled trials for prevention and treatment. JAMA 1999;282(13):1240–1246. 5. Kiso M, Mitamura K, Sakai-Tagawa Y, Shiraishi K, Kawakami C, et al. Resistant influenza A viruses in children treated with oseltamivir: descriptive study. Lancet 2004;364(9436):759– 765. 6. Bantia S, Parker CD, Ananth SL, Horn LL, Andries K, et al. Comparison of the anti-influenza virus activity of RWJ-270201 with those of oseltamivir and zanamivir. Antimicrob Agents Chemother 2001;45(4):1162–1167. 7. Boivin G, Goyette N. Susceptibility of recent Canadian influenza A and B virus isolates to different neuraminidase inhibitors. Antiviral Res 2002;54(3):143–147. 8. Gubareva LV, Webster RG, Hayden FG. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother 2001;45(12):3403–3408. 9. Govorkova EA, Fang HB, Tan M, Webster RG. Neuraminidase inhibitor-rimantadine combinations exert additive and synergistic anti-influenza virus effects in MDCK cells. Antimicrob Agents Chemother 2004;48(12):4855–4863. 10. BioCryst Pharmaceuticals. Unpublished data. 11. Arnold CS, Zacks MA, Dziuba N, Yun N, Linde N, Smith J, Babu YS, Paessler S. Injectable peramivir promotes survival in mice and ferrets infected with highly pathogenic avian influenza A/Vietnam/1203/04 (H5N1). V-2041B, ICAAC 2006, San Francisco 12. Boltz, DA, Ilyushina NA, Arnold CS, Babu, YS, Webster RG and Govorkova EA. Intramuscular administration of neuraminidase inhibitor peramivir promotes survival against lethal H5N1 influenza infection in mice. Antiviral Research,2007; 74 (3): A32 13. BioCryst Pharmaceuticals unpublished clinical study report BC-01-03. 14. Tamiflu® Package Insert. Roche Pharmaceuticals. Rev. December 2005. 15. Quidel QuickVue Influenza A+B and Binax NOW Influenza A&B Test Kit product information sheets 16. Treanor JJ, Hayden FG, Vrooman PS, Barbarash R et al. Efficacy and safety of the oral neuraminidase inhibitor oseltamivir in treating acute influenza. JAMA 2000; 283(8): 1016- 1024. 17. Nicholson KG, Aoki FY, Osterhaus AD, Trottier S et al. Efficacy and safety of oseltamivir in treatment of influenza: a randomised controlled trial. Lancet 2000; 355(9218): 1845-1850. 424 424 BCX1812-311 (V4.0: 18-December-2007) Page 52 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 18. US Department of Health and Human Services, Food and Drug Administration Center for Drug Evaluation and Reserach (CDER). Attachment to Guidance on Antiviral Product Development- Conducting and Submitting Virology Studies to the Agency: Guidance for Submitting Influenza Resistance Data. http://www.fda.gov/cder/guidance/7070fnlFLU.htm 19. Gehan EA (1965): A generalized Wilcoxon test for co mparing arbitrarily singl y censored samples. Biometrika 52:203-223 425 425 BCX1812-311 (V4.0: 18-December-2007) Page 53 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15 APPENDICES 15.1 NYHA Functional Classification Criteria: Heart Failure and Angina NYHA Functional Classification of Heart Failure Class I No symptoms. Ordinary physical activity such as walking and climbing stairs does not cause fatigue or dyspnea. Class II Symptoms with ordinary physical activity. Walking or climbing stairs rapidly; walking uphill; walking or stair climbing after meals, in cold weather, in wind, or when under emotional stress causes undue fatigue or dyspnea. Class III Symptoms w ith less than ordinary phy sical activity. Walking one to two blocks on t he level and clim bing m ore th an one flight of stai rs in norm al conditions causes undue fatigue or dyspnea. Class IV Symptoms at rest. Inability to carry on any physical activity without fatigue or dyspnea. NYHA Functional Classification of Angina Class I Angina only with unusually strenuous activity. Class II Angina with slightl y more prolonged o r slightly more vigorous activit y than usual. Class III Angina with usual daily activity. Class IV Angina at rest. 426 426 BCX1812-311 (V4.0: 18-December-2007) Page 54 BioCryst Pharmaceuticals, Inc. CONFIDENTIAL 15.2 Criteria for Severe COPD and Severe Asthma The following guidelines are provided to assist in the evaluation of subjects who have a medical history for Chronic Obstructive Pulmonary Disease (COPD) and/or Asthma. Subjects with severe COPD or severe persistent Asthma are to be excluded from this study. (See section 8.1.2, exclusion criteria number 3). Classification of Asthma from National Asthma and Education and Prevention Program For Adults and Children (> 5 yrs) who can use a spirometer or peak flow meter Classification Days with Symptoms Nights with Symptoms FEV1 or PEF % Predicted Normal PEF Variability (%) Severe persistent Continual Frequent ≤ 60 > 30 Moderate Persistent Daily > 1/ week > 60 - < 80 > 30 Mild Persistent > 2 / week but < 1 times / day > 2/ month ≥ 80 20 – 30 Mild Intermittent ≤ 2 / week < 2 / month ≥ 80 < 20 FEV1: percentage predicted value for forced expiratory volume in 1 second. PEF: percentage of personal best for peak expiratory flow. Extracted from: Expert Panel Report 3: Guidelines for the Diagnosis and Management of Asthma. National Heart, Lung, and Blood Institute, National Asthma Education and Prevention Program. HHS/NIH 2007 Spirometric Classification of COPD Severity based upon Post-Bronchodilator FEV1 (GOLD Criteria) Stage Characteristics Mild COPD FEV1/FVC < 70% FEV1 ≥ 80% predicted Moderate COPD FEV1/FVC < 70% 50 % ≤ FEV1 < 80% predicted Severe COPD FEV1/FVC < 70% 30 % ≤ FEV1 < 50% predicted Very Severe COPD FEV1/FVC < 70% FEV1 < 30% predicted or FEV1 < 50% predicted plus chronic respiratory failure FEV1: percentage predicted value for forced expiratory volume in one second. FVC: forced vital capacity Extracted from: Rabe KF, et al. Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease (GOLD Executive Summary). Am. J. Respir. Crit. Care Med. 2007:176;532-555. 427 427
2
arm 1: Placebo intramuscular injection arm 2: Single intramuscular injection of 300mg peramivir
[ 2, 0 ]
2
[ 0, 0 ]
intervention 1: To evaluate the efficacy of peramivir administered intramuscularly compared to placebo on the time to alleviation of clinical symptoms in adult subjects with uncomplicated acute influenza. intervention 2: Single intramuscular injection
intervention 1: Peramivir intervention 2: Placebo
96
Millbrook | Alabama | United States | -86.36192 | 32.47986 Tuscaloosa | Alabama | United States | -87.56917 | 33.20984 Phoenix | Arizona | United States | -112.07404 | 33.44838 Jonesboro | Arkansas | United States | -90.70428 | 35.8423 Jonesboro | Arkansas | United States | -90.70428 | 35.8423 Mountain Home | Arkansas | United States | -92.38516 | 36.33534 Anaheim | California | United States | -117.9145 | 33.83529 Beverly Hills | California | United States | -118.40036 | 34.07362 Buena Park | California | United States | -117.99812 | 33.86751 Fair Oaks | California | United States | -121.27217 | 38.64463 Fresno | California | United States | -119.77237 | 36.74773 Fresno | California | United States | -119.77237 | 36.74773 Garden Grove | California | United States | -117.94145 | 33.77391 Long Beach | California | United States | -118.18923 | 33.76696 Los Angeles | California | United States | -118.24368 | 34.05223 Paramount | California | United States | -118.15979 | 33.88946 San Diego | California | United States | -117.16472 | 32.71571 San Luis Obispo | California | United States | -120.65962 | 35.28275 Boulder | Colorado | United States | -105.27055 | 40.01499 Colorado Springs | Colorado | United States | -104.82136 | 38.83388 Longmont | Colorado | United States | -105.10193 | 40.16721 Gainesville | Florida | United States | -82.32483 | 29.65163 Hialeah | Florida | United States | -80.27811 | 25.8576 Hialeah | Florida | United States | -80.27811 | 25.8576 Holly Hill | Florida | United States | -81.03756 | 29.24359 Jacksonville | Florida | United States | -81.65565 | 30.33218 Jacksonville | Florida | United States | -81.65565 | 30.33218 Jacksonville | Florida | United States | -81.65565 | 30.33218 Lake Worth | Florida | United States | -80.07231 | 26.61708 Largo | Florida | United States | -82.78842 | 27.90979 Miami | Florida | United States | -80.19366 | 25.77427 Orlando | Florida | United States | -81.37924 | 28.53834 Pembroke Pines | Florida | United States | -80.22394 | 26.00315 Saint Cloud | Florida | United States | -81.28118 | 28.2489 West Palm Beach | Florida | United States | -80.05337 | 26.71534 Sandersville | Georgia | United States | -82.81014 | 32.98154 Quincy | Illinois | United States | -91.40987 | 39.9356 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Newburgh | Indiana | United States | -87.40529 | 37.94449 Dubuque | Iowa | United States | -90.66457 | 42.50056 Shawnee Mission | Kansas | United States | -94.66583 | 39.02 Topeka | Kansas | United States | -95.67804 | 39.04833 Wichita | Kansas | United States | -97.33754 | 37.69224 Hazard | Kentucky | United States | -83.19323 | 37.24954 Whitley City | Kentucky | United States | -84.47049 | 36.72341 Baton Rouge | Louisiana | United States | -91.18747 | 30.44332 Lafayette | Louisiana | United States | -92.01984 | 30.22409 Shreveport | Louisiana | United States | -93.75018 | 32.52515 Benzonia | Michigan | United States | -86.09926 | 44.62139 Cadillac | Michigan | United States | -85.40116 | 44.25195 Interlochen | Michigan | United States | -85.7673 | 44.64472 Saint Clair Shores | Michigan | United States | -82.88881 | 42.49698 Olive Branch | Mississippi | United States | -89.82953 | 34.96176 Springfield | Missouri | United States | -93.29824 | 37.21533 Bozeman | Montana | United States | -111.03856 | 45.67965 Butte | Montana | United States | -112.53474 | 46.00382 Fremont | Nebraska | United States | -96.49808 | 41.43333 Hamilton | New Jersey | United States | -74.08125 | 40.20706 Elmira | New York | United States | -76.80773 | 42.0898 Ithaca | New York | United States | -76.49661 | 42.44063 Raleigh | North Carolina | United States | -78.63861 | 35.7721 Canfield | Ohio | United States | -80.76091 | 41.02506 Columbus | Ohio | United States | -82.99879 | 39.96118 Lyndhurst | Ohio | United States | -81.48873 | 41.52005 Edmond | Oklahoma | United States | -97.4781 | 35.65283 Owasso | Oklahoma | United States | -95.85471 | 36.26954 Ashland | Oregon | United States | -122.70948 | 42.19458 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Warminster | Pennsylvania | United States | -75.09962 | 40.20678 Cranston | Rhode Island | United States | -71.43728 | 41.77982 Johnston | Rhode Island | United States | -71.50675 | 41.82186 Greenville | South Carolina | United States | -82.39401 | 34.85262 Greenville | South Carolina | United States | -82.39401 | 34.85262 Simpsonville | South Carolina | United States | -82.25428 | 34.73706 Spartanburg | South Carolina | United States | -81.93205 | 34.94957 Bristol | Tennessee | United States | -82.18874 | 36.59511 Kingsport | Tennessee | United States | -82.56182 | 36.54843 Beaumont | Texas | United States | -94.10185 | 30.08605 Bryan | Texas | United States | -96.36996 | 30.67436 Corpus Christi | Texas | United States | -97.39638 | 27.80058 Dallas | Texas | United States | -96.80667 | 32.78306 Dallas | Texas | United States | -96.80667 | 32.78306 Houston | Texas | United States | -95.36327 | 29.76328 Houston | Texas | United States | -95.36327 | 29.76328 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Saratoga Springs | Utah | United States | -111.90466 | 40.34912 West Jordan | Utah | United States | -111.9391 | 40.60967 Richmond | Virginia | United States | -77.46026 | 37.55376 Weber City | Virginia | United States | -78.28389 | 37.75514 Bellevue | Washington | United States | -122.20068 | 47.61038
0
NCT00610935
[ 3 ]
126
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
false
1FEMALE
null
The purpose of the study is to assess the efficacy, safety and tolerability of Ospemifene 5 mg, 15 mg, and 30 mg in the treatment of VVA in postmenopausal women to find the minimum effective dose below the lowest dose of 30 mg tested earlier in Phase II.
null
Atrophy Vaginal Diseases
Menopausal symptoms Urogenital atrophy Vulvar and vaginal atrophy in postmenopausal women Vaginal atrophy
null
4
arm 1: Subjects will self-administer 1 placebo tablet daily (in the morning with food) for 12 weeks arm 2: Subjects will self-administer 1 ospemifene 5 mg tablet daily (in the morning with food) for 12 weeks arm 3: Subjects will self-administer 1 ospemifene 15 mg tablet daily (in the morning with food) for 12 weeks arm 4: Subjects will self-administer 1 ospemifene 30 mg tablet daily (in the morning with food) for 12 weeks
[ 2, 0, 0, 0 ]
4
[ 0, 0, 0, 0 ]
intervention 1: 1 tablet per day, orally, in the morning, with food for 12 weeks - from Visit 2 (Randomization, Day 1) to Visit 4 (End of therapy, Week 12). intervention 2: 1 tablet of ospemifene 5 mg (QD), orally, in the morning, with food for 12 weeks - from Visit 2 (Randomization, Day 1) to Visit 4 (End of therapy, Week 12). intervention 3: 1 tablet of ospemifene 15 mg (QD), orally, in the morning, with food for 12 weeks - from Visit 2 (Randomization, Day 1) to Visit 4 (End of therapy, Week 12). intervention 4: 1 tablet of ospemifene 30 mg (QD), orally, in the morning, with food for 12 weeks - from Visit 2 (Randomization, Day 1) to Visit 4 (End of therapy, Week 12).
intervention 1: Placebo intervention 2: Ospemifene 5 mg intervention 3: Ospemifene 15 mg intervention 4: Ospemifene 30 mg
0
null
0
NCT00630539
[ 0 ]
20
RANDOMIZED
FACTORIAL
0TREATMENT
3TRIPLE
false
0ALL
true
A total of 20 subjects will participate in this four week, between groups, double-blind, placebo controlled study. Subjects will participate in two experimental sessions separated by approximately one week. Subjects will be randomized to receive either 50 mg cycloserine or placebo combined with cue exposure. Several physiological and subjective outcome measures (e.g., heart rate, blood pressure, galvanic skin response) will be obtained during the sessions. Experimental sessions will last approximately 4.5 hours with follow-up sessions lasting approximately thirty minutes. Our aims are: 1. To examine the effect of cycloserine vs. placebo on extinction of smoking cue reactivity in overnight abstinent smokers. Reactivity to smoking cues will be captured with self-report smoking urges and physiological measures (heart rate, blood pressure, and skin conductance). We hypothesize that cycloserine, relative to placebo, will facilitate extinction of smoking cue reactivity. 2. To examine the effect of cycloserine vs. placebo when combined with two 4.5 hour laboratory cue exposure training sessions, on smoking behavior in smokers. Smoking behavior will be measured with self-report smoking and saliva cotinine levels. 3. To examine the effect of cycloserine vs. placebo on memory performance in nicotine dependent smokers. Memory performance will be measured with verbal learning, recognition and recall tasks. 4\) To examine the safety and tolerability of cycloserine treatment in smokers. We hypothesize that cycloserine will be well tolerated by smokers.
null
Smoking
null
2
arm 1: 50 mg cycloserine arm 2: Matched placebo
[ 0, 3 ]
2
[ 0, 0 ]
intervention 1: 50 mg Cycloserine given in two separate experimental sessions separated by approximately one week. intervention 2: Matched placebo for subjects randomized to placebo arm. Given in two experimental sessions separated by approximately one week.
intervention 1: Cycloserine intervention 2: Placebo
1
West Haven | Connecticut | United States | -72.94705 | 41.27065
0
NCT00633256
[ 0 ]
57
RANDOMIZED
CROSSOVER
1PREVENTION
2DOUBLE
true
0ALL
false
Question #1: Will glycine ameliorate cognitive deficits? Hypothesis #1: Based on positive findings conducted with glycine and milacemide, a glycine prodrug, in schizophrenia and dementia, we expect that glycine will ameliorate cognitive deficits. Question #2: Will alcoholic patients show enhanced endocrinal effects to glycine? Hypothesis #2: Based on the dose-related effects of glycine in healthy subjects, we expect that glycine will increase the endocrinal response to glycine in alcoholic patients with, supposedly, dysregulated NMDA receptor function. Question #3: Will D-cycloserine have ethanol-like effects? Hypothesis #3: If inhibition of NMDA receptor function is fundamental to the subjective effects of ethanol, then the NMDA antagonist properties of D-cycloserine should be recognized as ethanol-like (relative to placebo) in recently detoxified alcoholics and healthy subjects. Question #4: Will D-cycloserine reverse cognitive benefits of glycine? Hypothesis 4: Based on the dose related NMDA antagonist activity of D-cycloserine, we expect that D-cycloserine will compete with the agonist activity of glycine and therefore it will reverse the cognitive benefits of glycine. Question #5: Will D-cycloserine inhibit endocrinal effects of glycine? Hypothesis #5: If the agonist activity of glycine is necessary to determine endocrine response, then the dose-related NMDA antagonist properties of D-cycloserine should block these effects.
The purpose of this study is to investigate the interaction between glycine and D-cycloserine in alcoholic patients and healthy subjects. Preclinical studies have shown that compounds acting at the glycine site of the N-methyl-D-aspartate (NMDA) receptor complex, such as glycine, may reverse the effects of ethanol on the NMDA receptor function (Rabe et al., 1990). The amino acid glycine is a co-agonist of the NMDA receptor complex (Kemp et al., 1993). It binds to the strychnine-insensitive site and positively modulates the NMDA receptor (Mc Donald et al., 1990). Physiologically, the glycine site is not saturated, and administration of glycine can potentiate NMDA receptor mediated responses. In contrast, D-cycloserine (Hood et al., 1989) is a partial-agonist at the glycine site of the NMDA receptor, with dose-dependent NMDA antagonist properties. The NMDA antagonist activity of D-cycloserine should produce ethanol like-effects that can be reversed by the agonist glycine. This study is intended to evaluate possible contributions of the glycine site to the reduction of cognitive deficits of alcoholism and complements the current work at VA Connecticut Healthcare System on the NMDA antagonists in alcoholic and healthy subjects.
Alcohol Dependence
Alcohol Dependence, Alcoholism, Glycine, D-Cycloserine
null
2
arm 1: Alcohol dependent patients will receive 4 interventions arm 2: Healthy subjects will receive 4 interventions
[ 1, 1 ]
4
[ 0, 0, 0, 0 ]
intervention 1: Test days will involve administration of D-Cycloserine in the morning in pill form then 4 hours later a 30 minute infusion of Glycine. intervention 2: Placebo intervention 3: None intervention 4: None
intervention 1: D-Cycloserine PO and Glycine IV intervention 2: Placebo D-Cycloserine PO and placebo Glycine IV intervention 3: Placebo D-Cycloserine PO and Glycine IV intervention 4: D-Cycloserine PO and placebo Glycine IV
1
West Haven | Connecticut | United States | -72.94705 | 41.27065
0
NCT00635102
[ 2 ]
38
RANDOMIZED
SINGLE_GROUP
null
4QUADRUPLE
true
0ALL
false
The product is being tested to see if exposure to light causes toxic reactions on the skin.
null
Healthy
wound healing phototoxicity Healthy Subjects
null
3
arm 1: Drug arm 2: Placebo comparator arm 3: Subjects serve as own controls.
[ 0, 2, 4 ]
2
[ 0, 0 ]
intervention 1: 20mg under Finn chambers intervention 2: 20mg under Finn chambers
intervention 1: Xenaderm intervention 2: Placebo
0
null
0
NCT00644917
[ 5 ]
23
RANDOMIZED
CROSSOVER
7BASIC_SCIENCE
2DOUBLE
true
0ALL
false
A single center, double blind, randomized, placebo controlled, two-treatments, two-period crossover study conducted in adult smokers.
The main objective of this study is to use blood oxygen level-dependent (BOLD) functional Magnetic Resonance Imaging (fMRI) in abstinent smokers to directly evaluate the effect of the 4 milligrams (mg) nicotine lozenge on brain activation associated with visual attention. The experimental task featured 3 conditions: 1. a highly demanding cognitive/attention task, 2. a simple cognitive/attention task, and 3. simply look at a '+' symbol. During the experiment these conditions are each presented a number of times in an alternating manner while acquiring images.
Smoking
nicotine therapy fMRI/EEG replacement
null
2
arm 1: Nicotine lozenge containing 4 mg of nicotine to be placed in mouth and suck to dissolution. arm 2: Placebo lozenge to be placed in mouth and suck to dissolution.
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: Nicotine lozenge containing 4 mg of nicotine intervention 2: Placebo lozenge
intervention 1: Nicotine intervention 2: Placebo
0
null
0
NCT00657020
[ 3 ]
40
RANDOMIZED
SINGLE_GROUP
1PREVENTION
2DOUBLE
true
0ALL
false
To characterize features of metabolic syndrome in volunteers. To undertake a randomised trial to determine whether treatment with a statin improves muscle microvascular blood flow.
To characterise features of the metabolic syndrome, including body fat, insulin sensitivity, and liver fat together with muscle micorvascular blood flow. To undertake a randomised controlled trial of atorvastatin 40 mg. o.d for 6 months to determine whether any of the above measures change with treatment.
Metabolic Syndrome
metabolic syndrome Volunteers recruited from the community
null
2
arm 1: Active arm atorvastatin 40 mg. o.d. arm 2: Placebo arm dummy pill
[ 1, 2 ]
2
[ 0, 0 ]
intervention 1: 40 m.g. o.d. tablets for 6 months intervention 2: Placebo
intervention 1: atorvastatin intervention 2: placebo
0
null
0
NCT00666029
[ 5 ]
114
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
true
0ALL
true
The purpose of this study is to evaluate the amount of anxiety and pain felt by children during procedures that require a needle stick after using a topical anesthetic or placebo cream.
Pediatric patients frequently receive eutectic mixture of local anesthetics (EMLA) or other anesthetic medications prior to venipuncture. However, the time for the anesthetic to take affect is approximately 60 minutes. Another anesthetic medication besides EMLA is lidocaine 4% topical anesthetic cream (LMX4), which has a shorter acting time (30 minutes) compared to the EMLA, making it a more desirable medication when urgent labs are required. This medication is being evaluated to assess the anxiety and pain associated with venipuncture in 15 minutes versus the approved 30 minutes of pediatric patients treated as an inpatient or outpatient in the local Emergency Department, compared to standard care (no prior treatment).
Pain Anxiety
pediatric patients pain anxiety topical anesthetic randomized control trial
null
2
arm 1: This group received topical 4% lidocaine anesthetic cream under occlusive dressing for 15 minutes prior to needle stick. arm 2: This group received matching placebo cream under occlusive dressing for 15 minutes prior to needle stick.
[ 1, 2 ]
2
[ 0, 0 ]
intervention 1: A dollop of 4% lidocaine cream was applied under occlusive dressing for 15 mins prior to venipuncture intervention 2: A dollop of matching placebo cream was applied under occlusive dressing for 15 mins prior to venipuncture
intervention 1: 4% lidocaine topical anesthetic cream intervention 2: Placebo cream
1
Allentown | Pennsylvania | United States | -75.49018 | 40.60843
0
NCT00676364
[ 5 ]
20
RANDOMIZED
CROSSOVER
0TREATMENT
1SINGLE
false
0ALL
false
The purpose of this research study is to evaluate the use of Biafine Cream on wounds created by removal of actinic keratosis using cryotherapy in a clinical setting.
Subjects were randomized to apply Biafine® to wounds on one forearm and polysporin (standard of care) to wounds on the other. Medications were applied three times a day for 4 weeks to the areas that have been treated with cryotherapy at the baseline visit.
Actinic Keratosis
null
2
arm 1: Subjects were randomized to apply Biafine® to wounds on the left forearm and polysporin (standard of care) to wounds on the right forearm. Medications were applied three times a day for 4 weeks to the areas that have been treated with liquid nitrogen at the baseline visit. arm 2: Subjects were randomized to apply Biafine to wounds on the right forearm and Polysporin to wounds on the left forearm. Medications were applied three times a day for 4 weeks to the areas that have been treated with liquid nitrogen at the baseline visit.
[ 0, 0 ]
2
[ 0, 0 ]
intervention 1: Apply to wounds 3 times daily for 4 weeks: ingredients: purified water, liquid paraffin, glycol monostearate, stearic acid, propylene glycol, paraffin wax, squalene, avocado oil, trolamine sodium alginate, cetyl palmitate, methylparaben, sorbic acid, propyl paraben and fragrance. intervention 2: over the counter Polysporin ointment 3 times daily for 4 weeks to wounds
intervention 1: Biafine intervention 2: Polysporin
1
Winston-Salem | North Carolina | United States | -80.24422 | 36.09986
0
NCT00695578
[ 2 ]
26
RANDOMIZED
CROSSOVER
6HEALTH_SERVICES_RESEARCH
2DOUBLE
true
2MALE
false
The purpose of the study is to compare the pharmacokinetics (PK) and pharmacodynamics (PD) of Humalog (insulin lispro) or Humulin-R (recombinant human insulin) when administered as a single subcutaneous (SC) injection of 20 units (U) with or without coadministration of recombinant human hyaluronidase PH20 (rHuPH20). The study hypothesizes that the time required to reach maximum insulin concentration (tmax) when insulin is administered with rHuPH20 will be comparable or shorter than the time required without rHuPH20.
null
Diabetes Mellitus
rHuPH20 Hyaluronidase Insulin
null
4
arm 1: Humalog first, then Humalog + recombinant human hyaluronidase PH20 (rHuPH20) A single subcutaneous (SC) injection of 20 units (U) Humalog on Day 1 of the study, followed by a single SC injection of 20 U Humalog + 300 U rHuPH20 after a washout period of at least 6 days arm 2: Humalog + recombinant human hyaluronidase PH20 (rHuPH20) first, then Humalog A single subcutaneous (SC) injection of 20 units (U) Humalog + 300 U rHuPH20 on Day 1 of the study, followed by a single SC injection of 20 U Humalog after a washout period of at least 6 days arm 3: Humulin-R (recombinant human insulin) first, then Humulin-R + recombinant human hyaluronidase PH20 (rHuPH20) A single subcutaneous (SC) injection of 20 units (U) Humulin-R on Day 1 of the study, followed by a single SC injection of 20 U Humulin-R + 240 U rHuPH20 after a washout period of at least 6 days arm 4: Humulin-R (recombinant human insulin) + recombinant human hyaluronidase PH20 (rHuPH20) first, then Humulin-R A single subcutaneous (SC) injection of 20 units (U) Humulin-R + 240 U rHuPH20 on Day 1 of the study, followed by a single SC injection of 20 U Humulin-R after a washout period of at least 6 days
[ 1, 1, 1, 1 ]
3
[ 0, 0, 0 ]
intervention 1: None intervention 2: None intervention 3: None
intervention 1: Humalog intervention 2: Humulin-R intervention 3: Recombinant human hyaluronidase PH20 (rHuPH20)
1
San Antonio | Texas | United States | -98.49363 | 29.42412
0
NCT00705536
[ 5 ]
25
RANDOMIZED
SINGLE_GROUP
0TREATMENT
1SINGLE
true
1FEMALE
false
A study to compare the skin irritation potential of two marketed gels for acne treatment, each applied to half of the face of healthy volunteers.
At the Baseline Visit, following satisfaction of entry criteria and screening procedures, all subjects will be applying two products on their faces, each on half face. The side of face receiving each product is randomly assigned. One group will use tretinoin facial gel on the left side and adapalene facial gel on the right side of the face daily for two consecutive weeks after washing with study-supplied facial wash. The other group will use the same products, but on opposite sides of the face for two consecutive weeks after washing with the same study-supplied facial wash. Subjects will return to the study center every weekday morning for evaluation and for the morning application of both study products. Study personnel will monitor application on the weekdays. There will be a daily clinical evaluation of skin irritation by a blinded dermatologist and by subjects. At baseline and at the end of each week subjects will be photographed and have chromometer readings.
Acne Vulgaris
acne irritation objective sensory methods
null
1
arm 1: Adapalene facial gel and tretinoin facial gel applied daily for two weeks on opposite sides of the face (in a split-face model)
[ 0 ]
2
[ 0, 0 ]
intervention 1: adapalene gel 0.3% topically applied daily in a split-face model for two weeks intervention 2: Tretinoin 0.1% topically applied daily in a split face model for two weeks
intervention 1: Adapalene Gel intervention 2: Tretinoin Gel
1
Broomall | Pennsylvania | United States | -75.35658 | 39.9815
0
NCT00714714
[ 3 ]
45
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
The purpose of this study is to assess the efficacy of bortezomib in combination with melphalan and prednisone to achieve complete responses for patients with previously untreated multiple myeloma compared to an historical control group. This trial will also evaluate the safety and toxicity of this regimen as well as evaluate the duration of response of this regimen.
Based on the need to improve front-line therapy for patients less likely to undergo transplant, the promising recent in vitro and clinical work on melphalan and bortezomib, we propose a prospective trial with bortezomib added to standard melphalan and prednisone therapy for previously untreated patients with multiple myeloma. Bortezomib 1.3 mg/m2 will be given twice weekly for two weeks and will be added to standard melphalan and prednisone on a 4-week cycle. This three-drug combination will be compared to historical data. We have treated 2 patients with relapsed disease following \>2 prior regimens including high-dose therapy with autologous stem cell support. Each patient received melphalan, prednisone, and bortezomib as described below and both had marked declines in M-protein within 2 cycles. These responses have been sustained for at least 3 months and treatment was well tolerated. Eligible patients will have histologically confirmed Multiple Myeloma (MM) having not received prior systemic therapy given with the intent to induce remission, be adults, have life expectancy greater than 3 months, adequate performance status, organ and marrow function as described in the protocol, not be pregnant, HIV positive, or taking any investigational agents. Patients must not have history of allergic reactions to study drugs or similar compounds or have uncontrolled intercurrent illness or social situation that would limit compliance with study requirements. Patients must also have the ability to give informed consent. Study drugs will be administered on an inpatient or outpatient basis. Bortezomib 1.3 mg/m2 is administered intravenously in a 3-5 second bolus on days 1, 4, 8, and 11 of a 28 day cycle. Six cycles are planned. On days when both melphalan and bortezomib are given, melphalan is given at least one hour prior to bortezomib. Melphalan 6 mg/m2 is administered orally on an empty stomach daily on days 1-7 of each cycle. Prednisone 60 mg/m2 is administered orally daily on days 1-7 of each cycle. Supportive care measures such as antiemetics and growth factors may be given.
Multiple Myeloma
Multiple myeloma
null
1
arm 1: Bortezomib 1.3 mg/m2 is administered intravenously in a 3-5 second bolus on days 1, 4, 8, and 11 of a 28 day cycle. Six cycles are planned. On days when both melphalan and bortezomib are given, melphalan is given at least one hour prior to bortezomib. Melphalan 6 mg/m2 is administered orally on an empty stomach daily on days 1-7 of each cycle. Prednisone 60 mg/m2 is administered orally daily on days 1-7 of each cycle.
[ 0 ]
3
[ 0, 0, 0 ]
intervention 1: None intervention 2: None intervention 3: None
intervention 1: Bortezomib intervention 2: Melphalan intervention 3: Prednisone
1
Durham | North Carolina | United States | -78.89862 | 35.99403
0
NCT00734149
[ 5 ]
4
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
1FEMALE
null
Women with Systemic Lupus Erythematosus (SLE) are prone to cardiovascular disease. Early detection of improvement of endothelial function with simvastatin could be a clue for future intervention trials.
null
Systemic Lupus Erythematosus
null
2
arm 1: Arm 1: Drug arm 2: Arm 2: Placebo
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: simvastatin 20mg daily at nights for 12 weeks. Tablets intervention 2: placebo daily at nights for 12 weeks. Tablets
intervention 1: simvastatin intervention 2: Comparator: Placebo
0
null
0
NCT00739050
[ 3 ]
27
RANDOMIZED
CROSSOVER
7BASIC_SCIENCE
4QUADRUPLE
false
0ALL
false
The purpose of the study is to compare frequency and content of reflux episodes in patients with gastroesophageal reflux disease.
null
Reflux Episodes
GERD transient lower esophageal sphincter relaxations (TLESRs) reflux
null
2
arm 1: AZD3355 arm 2: None
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: 65 mg capsules, oral, 3 single doses intervention 2: capsules, oral, 3 single doses
intervention 1: AZD3355 intervention 2: Placebo
0
null
0
NCT00743444
[ 5 ]
30
RANDOMIZED
PARALLEL
0TREATMENT
1SINGLE
true
0ALL
false
Keloids are thought to result from derailments in the typical wound healing process following cutaneous injury. Current treatment options for keloids include intralesional corticosteroids, silicone gel sheeting, compression, surgery and adjuvants to surgery, including radiation and cryotherapy. 0.5% hydrocortisone, silicone, vitamin E lotion (HSE) and onion extract gel (OE) are widely used over-the-counter medications for the treatment of keloids and hypertrophic scars. However, their efficacy and safety have not been compared in a blinded, placebo-controlled, prospective fashion. This study is being undertaken to determine the efficacy and safety of HSE versus OE versus placebo (Cetearyl alcohol; CEA) in subjects with hypertrophic scars and keloids. This is an investigator-blinded study, which means that the doctor evaluating you will not know if you are receiving the study medication or not. Another doctor will be supplying you with the medication and discussing any problems that you may have with the medication. You will be assigned to one of the three treatment groups: HSE, OE, or CEA. The group will be assigned by chance and you will have two in three chances of receiving treatment with a study medication, HSE or OE. The no treatment group will receive CEA, a bland lotion, containing no active ingredients such as steroids, silicone, vitamin E, or onion extract.
This study will last up to 16 weeks, with a total of 5 visits to the clinic (Baseline visit, Week 4, 8, 12, and 16 ), excluding the Screening Visit. Screening Visit/Baseline Visit: Patients will read and be explained the informed consent. Patients who agree to participate will sign the informed consent and a copy will be given to them. Medical history and exclusion/inclusion criteria will be reviewed; if a patient qualifies he/she will be assigned a randomization number for the treatment. At the baseline visit, medical history and exclusion/inclusion criteria since the screening visit will be reviewed. Patients randomized to the HSE group will receive one tube and apply the first application to the keloid/hypertrophic scar during the baseline visit. Patients randomized to the OE group will be given a tube of OE gel and will apply the first application to the keloid/hypertrophic scar. Patients in the placebo group will be given a bottle of CEA lotion, the placebo medication, and will apply the first application to the keloid/hypertrophic scar. The medications will be given by the unblinded investigator and the blinded investigator will be evaluating the patients. Photographs of the patient's keloid/hypertrophic scar will be taken, and the keloid/hypertrophic scar will be measured/assessed according to Methods of Study Lesion Assessment (below). A urine pregnancy test will be obtained for all women of child-bearing potential. Week 4, 8, 12, and 16 Visit: Patients will be asked about side effects since last visit. Photographs of the patient's keloid/hypertrophic scar will be taken and the keloid/hypertrophic scar will be measured/assessed according to Methods of Study Lesion Assessment (below). A urine pregnancy test will be obtained at for all women of child-bearing potential. Methods of Study Lesion Assessment A. Volume B. Linear dimensions Investigator's Assessments w/ Visual Analog Scale (VAS): C. Cosmetic assessment D. Induration (hardness) \[compared to standardized hard discs with numerical ranking of increased induration\] E. Erythema (redness) F. Pigmentary alteration Patient's Assessments w/ VAS: G. Cosmetic assessment H. Pain I. Tenderness J. Pruritus (itching) K. Patient satisfaction L. Digital photographs
Keloid Hypertrophic Scar Cicatrix, Hypertrophic
Keloid Hypertrophic scar Hydrocortisone, silicone, vitamin E lotion HSE Onion extract gel OE Cetearyl alcohol lotion CEA
null
3
arm 1: 0.5% hydrocortisone, silicone, vitamin E lotion arm 2: Onion extract gel arm 3: Cetearyl alcohol lotion
[ 0, 0, 2 ]
3
[ 0, 0, 0 ]
intervention 1: 0.5% hydrocortisone, silicone, vitamin E lotion will be applied topically to cover the selected scar twice daily for 16 weeks. The lesion will be cleansed with soap and water and dried thoroughly. The medication will be applied with a brush and allow it to dry for one minute before contact with clothing. intervention 2: Onion extract gel is applied and massaged into the selected scar 3 to 4 times daily according to product instructions for 16 weeks. intervention 3: Placebo is cetearyl alcohol lotion with no steroids, silicone, vitamin E, or onion extract and will be applied 2 times a day to the lesion.
intervention 1: 0.5% hydrocortisone, silicone, vitamin E lotion intervention 2: Onion extract gel intervention 3: Cetearyl alcohol lotion
1
Miami | Florida | United States | -80.19366 | 25.77427
0
NCT00754247
[ 3 ]
10
RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
null
The purpose of this study is to provide decitabine to patients with Acute Myeloid Leukemia (AML) or Myelodysplastic Syndrome (MDS) who have completed participation per protocol in the DACO-018 study.
The objectives of this trial are: * To generate additional information about the overall safety profile, * To generate safety information of hepatically or renally impaired patients, as appropriate, and * To generate safety information when patients are also taking concomitant medications and/or therapies without trial restrictions when decitabine is administered at a dose of 20 mg/m² over a 1-hour intravenous infusion for 5 consecutive days every 4 weeks in patients with MDS or AML (≥ 30% blasts). The purpose of this open-label, expanded-access trial is to provide decitabine to patients with AML or MDS who have completed participation per protocol in the DACO-018 study and for whom continuation of treatment with decitabine is indicated, per the opinion of the investigator. In order to continue treatment with decitabine, at a minimum, there must be no disease progression while the patient was participating in the DACO-018 trial and during the period after the patient discontinued from the DACO-018 study and before entering this trial. Patients must enroll in this trial within 8 weeks of discontinuing from the DACO-018 study and not have received any other chemotherapy for their disease during this interim period. Decitabine will be administered at a dose of 20 mg/m² over a 1-hour intravenous infusion for 5 consecutive days every 4 weeks.
Acute Myelogenous Leukemia Myelodysplastic Syndrome
Acute Myelogenous Leukemia Myelodysplastic Syndrome Dacogen Decitabine
null
1
arm 1: Decitabine will be administered at a dose of 20 mg/m² over a 1-hour intravenous infusion for 5 consecutive days every 4 weeks.
[ 0 ]
1
[ 0 ]
intervention 1: Decitabine is administered at a dose of 20 mg/m² over a 1-hour intravenous infusion for 5 consecutive days every 4 weeks in patients with myelodysplastic syndrome (MDS) or acute myeloid leukemia (AML; ≥ 30% blasts).
intervention 1: Decitabine
1
St Louis | Missouri | United States | -90.19789 | 38.62727
0
NCT00760084
[ 3, 4 ]
17
RANDOMIZED
PARALLEL
0TREATMENT
1SINGLE
false
0ALL
true
This study is designed to compare the efficacy and safety of higher doses of Rituxan with a regimen combining standard doses of Rituxan + CVP in patients with chronic ITP who did not respond to or relapsed after standard doses of Rituxan. Patients eligible for this protocol will be stratified into two subgroups according to their initial response to Rituxan.
The rationale for using chemotherapy in combination with Rituximab: Since Rituximab is an anti-B cell therapy, in order to improve the rate of durable responses beyond the 32% (18 of 57) seen with Rituximab alone, it seems appropriate to combine it with a therapy that would also target T cells and/or macrophages. Our plan is therefore to combine Rituximab with a standard chemotherapy (CHOP)-like regimen as previously successfully tested in patients with follicular or diffuse large-B-cell lymphomas 13-15. The "CHOP" chemotherapy regimen is a combination of cyclophosphamide, doxorubicin, vincristine and prednisone (or prednisolone) that has been considered the "gold standard" for treating lymphomas for more than 20 years. This combination of medications was used in a Hodgkin's patient with refractory ITP and became the template for developing the use of cyclophosphamide, vincristine, and prednisone for ITP as initially reported in 1993. Since reports on doxorubicin efficacy by itself in ITP are only anecdotal 16 and this drug has a potential cardiac toxicity, a CVP regimen (namely a combination of cyclophosphamide + vincristine and prednisone) should be similar in efficacy to CHOP in patients with ITP and have less toxicity. Indeed, the efficacy of such a chemotherapy12 as well as pulses cyclophosphamide therapy alone11 have already been reported in patients with refractory ITP. Since attempts to increase the efficacy of CHOP by increasing the doses or adding other cytotoxic drugs have failed, a new therapeutic strategy combining CHOP with Rituxan has been successfully developed in the last few years in various types of B-cell lymphomas 13-15. In elderly patients with diffuse large-B-cell lymphoma, the addition of Rituxan to standard CHOP chemotherapy significantly reduced the risk of treatment failure and deaths without increasing toxicity 13. Moreover, in autoimmune disorders, there are few preliminary data suggesting that Rituxan and cyclophopshamide given in combination could be effective and relatively safe in patients with active rheumatoid arthritis 17. Therefore, the rationale for combining Rituxan with a CHOP-like regimen in ITP is threefold: Both Rituxan and CHOP or IV cyclophosphamide have efficacy in ITP The treatments have different mechanisms of action. They have minimally-overlapping toxicities. The rationale for using higher doses of Rituxan in patients who had no response, or relapsed, to the drug at the standard dose: The standard dose of Rituxan is arbitrary in that one dose of Rituxan has been used in the great majority of the clinical trials and virtually all patients since the FDA approval of Rituxan in 1997: 375 mg/m2 weekly x 4 weeks. To date, because Rituxan is a monoclonal antibody rather than a chemotherapeutic agent, it was recognized that a true maximum tolerated dose (MTD) might not be achieved. Among other factors that could influence the tolerance of higher doses of Rituxan are the rate of CD20 surface expression and the serum level of the antibody11. Limited trials of higher doses have been pursued in CLL18 (up to 2,250 mg/m2 per dose), but not in other types of lymphoma or in autoimmune diseases. In CLL, mild to severe toxicity was exclusively observed with the first dose (375 mg/m2) while toxicity on subsequent higher doses was minimal. In ITP, some of the few patients that have been retreated responded better to the second dose of rituximab than to the initial treatment (although the opposite is also true). Full depletion of the marrow and especially the lymph nodes is not achieved by the current dose regimen and B cells return in substantial number to the peripheral blood within 3-6 months in patients with ITP treated at the conventional dose. We therefore anticipate that in ITP patients who relapsed or did not respond after a previous course of rituximab, doubling the dose could lead to a deeper and more prolonged B cell depletion and to a better increase in the platelet count without enhancing toxicity.
Immune Thrombocytopenic Purpura
Pts w/ Chronic ITP who have fail/relap after Rituxan rx
null
2
arm 1: 'Standard Dose of Rituximab administered with C, V, P (CVP)' Interventions: Rituximab will be administered as an IV infusion at the standard dose of 375 mg/m2 for 4 doses at standard rates and use of premedication. The schedule will be to give the first rituximab infusion 5 days (± 3 days) prior to first administration of CVP, and the following 3 infusions will be given on the same day as the 3 cycles of C, V, P. On those days, the IV Cyclophosphamide and Vincristine will be given first so that the administration of fluids with the rituximab can be used as post-cyclophosphamide hydration, Cyclophosphamide dosing will be 750mg/m2 (maximum 2000mg), vincristine 1.4 mg/m2 (up to 1.6 mg), prednisone 100mg po daily for 5 days. arm 2: In this arm, Rituximab will be administered at a dose of 750 mg/m2 once a week x 4 consecutive weeks (4 infusions in total). We will perform EKG monitor tracings before, during and after Rituxan infusions. This will be a single-lead tracing that will allow us to look at the Q-T interval.
[ 1, 1 ]
2
[ 0, 0 ]
intervention 1: 'Rituximab, Cyclophosphamide, Vincristine, Prednisone interventions are as follows: Rituximab will be administered as an IV infusion at the standard dose of 375 mg/m2 for 4 doses. However, the schedule of the infusions will be different than the usual one: Rather than administrating the 4 doses once weekly, the first infusion will be given 5 days (± 3 days) prior to the first infusions of C and V and oral P, and the following 3 rituximab infusions will be given on the same day as the 3 cycles of C, V, and P. intervention 2: rituximab 750mg/m2 (twice the standard dose of 375mg/m2) will be given weekly for 4 weeks. Premedication and infusion rate escalation will be exactly the same as for standard dose rituximab. The additional dose will thus run at 400ml/hr.
intervention 1: Rituxan, Cyclophosphamide, Vincristine, Prednisone intervention 2: Higher Dose of Rituximab
1
New York | New York | United States | -74.00597 | 40.71427
0
NCT00774202
[ 0 ]
89
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
true
1FEMALE
true
The aim of this study is to estimate the efficacy of intracervical versus paracervical block on pain experienced during first trimester suction curettage without the use of preoperative cervical ripening. Because of the theoretical improved reliability of stromal block, the investigators hypothesize that intracervical block would produce lower pain scores than paracervical block at the time of cervical dilation.
null
Abortion, Induced Pain
Local anesthesia Paracervical Intracervical Abortion Pain Local anesthesia for elective first trimester abortion
null
2
arm 1: None arm 2: None
[ 1, 0 ]
3
[ 3, 3, 0 ]
intervention 1: The paracervical block was administered using 20 ml of buffered lidocaine and a 5/8 inch, 25-gauge needle. A small amount was injected at the tenaculum site, and the remainder equally distributed around the cervicovaginal junction at 3, 5, 7, and 9 o'clock. The depth was standardized at 5/8 inch by inserting the needle to the hub. intervention 2: The intracervical block was administered using 20 ml of buffered lidocaine and a 1-1/2 inch, 20 gauge needle in order to overcome the increased resistance to injection caused by the cervical stroma. A small amount was injected at the tenaculum site, and the remainder into the cervical stroma at 12, 3, 6, and 9 o'clock, at a depth of 1-1/2 inch by inserting the needle to the hub. intervention 3: The buffered lidocaine preparation for both block techniques consisted of 50 mL of 1% lidocaine, 5 units of vasopressin, and 5 mL 8% sodium bicarbonate.
intervention 1: Paracervical block intervention 2: Intracervical intervention 3: Buffered Lidocaine, vasopressin, sodium bicarbonate
1
San Diego | California | United States | -117.16472 | 32.71571
0
NCT00816751
[ 0 ]
40
RANDOMIZED
PARALLEL
4SUPPORTIVE_CARE
0NONE
true
1FEMALE
false
The purpose of this study to assess the safety of the etonogestrel-releasing subdermal implant (Implanon) inserted during the immediate puerperium of healthy women.
Many contraceptive methods are currently available. However, about 50% of all pregnancies in the world are not planned, most of them occurring in developing countries. Long-lasting reversible contraceptives such as the etonogestrel implant represent an option for the reduction of unwanted pregnancies, especially among patients at risk for a short intergestational period. In addition to preventing an undesired pregnancy, these methods have an impact on the reduction of the maternal-fetal morbidity-mortality known to be associated with these short intervals, also minimizing the malnutrition and the cycle of poverty caused by multiparity. On the basis of inclusion and exclusion criteria, we will selected 40 puerperae aged 18 to 35 years at the Low Risk Prenatal Care Program of the University Hospital of Ribeirão Preto, University of São Paulo (HC-FMRP). The subjects will be randomized to two types of treatment (etonogestrel-releasing implant to be inserted 24 to 48 hours after delivery or 150 mg medroxyprogesterone administered every three months starting 6 weeks after delivery). Blood samples (40 mL) will be collected in a single procedure from these patients and stored for later determination of multiple hemostatic and metabolic variables at 24-48 hours and at 6 and 12 weeks after delivery. Data on maternal and neonatal clinical parameter will be also collected.
Breastfeeding Contraception
Adverse Effects Etonogestrel Postpartum period Contraception Hemostasis Metabolism
null
2
arm 1: Etonogestrel releasing contraceptive implant (Implanon®, NV Organon, Oss, The Netherlands) inserted 24-48 h after delivery. It is compounded by 68mg of etonogestrel, 3years of duration. arm 2: At the 6th week postpartum, this group received intramuscular 150 mg of depot medroxyprogesterone acetate (Contracept®, EMS Sigma Pharma, Hortolandia, Brazil).
[ 0, 1 ]
2
[ 0, 0 ]
intervention 1: Etonogestrel-releasing subdermal implant (Implanon) inserted during the immediate postpartum period (from 24 to 48 hours postpartum) intervention 2: 150 mg medroxyprogesterone administered I.M. every three months starting 6 weeks after delivery
intervention 1: etonogestrel implant intervention 2: depot medroxyprogesterone acetate
1
Ribeirão Preto | São Paulo | Brazil | -47.81028 | -21.1775
0
NCT00828542
[ 0 ]
34
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
false
The investigators' primary specific aims are to demonstrate that: 1. Pediatric patients with normal airways, undergoing elective surgical procedures, can be successfully intubated when deeply sedated, without the use of muscle relaxants using the Shikani Optical Stylet. 2. Shikani intubation of pediatric patients is equally effective in children that are deeply sedated or paralyzed as evidenced by a non-significant difference in: * Time to intubation (defined as no more than a 30 second time difference between the two groups); * Incidence of adverse events.
null
Intubation,Endotracheal
Pediatric
null
2
arm 1: Normal saline volume calculated to be equal to the volume of cisatracurium 0.2mg/kg arm 2: Subjects in this arm will be given Cisatracurium 0.2mg/kg IV dose one time prior to intubation.
[ 2, 1 ]
2
[ 0, 0 ]
intervention 1: One intravenous dose: 0.2mg/kg/dose intervention 2: One Intravenous dose
intervention 1: Cisatracurium intervention 2: Normal saline
1
San Diego | California | United States | -117.16472 | 32.71571
0
NCT00912990
[ 2 ]
54
RANDOMIZED
CROSSOVER
7BASIC_SCIENCE
0NONE
true
0ALL
false
This study will evaluate the pharmacokinetic linearity of a single 35 mg fenofibric acid dose and demonstrate the bioequivalence of three 35 mg fenofibric acid tablets (105 mg total single dose) to a single 105 mg fenofibric acid tablet in healthy adult volunteers when each dose is administered under fasted conditions. Safety and tolerability of these regimens will also be evaluated.
This study will evaluate the pharmacokinetic linearity of a single 35 mg fenofibric acid dose and demonstrate the bioequivalence of three 35 mg fenofibric acid tablets (105 mg total single dose) to a single 105 mg fenofibric acid tablet in healthy adult volunteers when each dose is administered under fasted conditions. Fifty-four healthy, non-smoking, non-obese, 18-45 year old, male and female volunteers will be randomly assigned in a crossover fashion to receive each of three fenofibric acid dosing regimens in sequence with a 7 day washout period between dosing periods. On the morning of the first day of each dosing period, after an overnight fast of at least 10 hours, subjects will receive single doses of fenofibric acid (1 x 35 mg tablet), fenofibric acid (3 x 35 mg tablets - 105 mg total dose), or fenofibric acid (1 x 105 mg tablet). Fasting will continue for 4 hours after dose administration. Blood samples will be drawn from all participants prior to dosing and for 72 hours post-dose, at times sufficient to adequately define fenofibric acid pharmacokinetics. Subjects will be monitored throughout their participation for adverse reactions to the study drug and/or procedures. Seated blood pressure and pulse will be measured prior to each dose and approximately 2 hours after each dose to coincide with peak plasma concentrations. All adverse experiences, whether elicited by query, spontaneously reported, or observed by clinic staff, will be documented in the subject's case report form.
Healthy
healthy pharmacokinetics therapeutic equivalency fenofibric acid
null
3
arm 1: 1 x 35 mg tablet administered after an overnight fast of at least 10 hours arm 2: 3 x 35 mg tablets administered after an overnight fast of at least 10 hours arm 3: 1 x 105 mg tablet administered after an overnight fast of at least 10 hours
[ 0, 0, 0 ]
3
[ 0, 0, 0 ]
intervention 1: 1 x 35 mg tablet administered after an overnight fast of at least 10 hours intervention 2: 3 x 35 mg tablets administered after an overnight fast of at least 10 hours intervention 3: 105 mg tablet administered after an overnight fast of at least 10 hours
intervention 1: Fenofibric Acid 35 mg Tablet intervention 2: Fenofibric Acid 35 mg Tablet intervention 3: Fenofibric Acid 105 mg Tablet
0
null
0
NCT00961259
[ 5 ]
30
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
true
The purpose of this study is: * To identify the common factor for L5 prevalence in patients with Metabolic Syndrome. * To determine whether Ezetimibe, Simvastatin, and Vytorin can correct the L5- promoting factor and reduce L5 in Metabolic Syndrome patients.
Epidemiological evidence indicates that metabolic syndrome (MS) is a strong predisposing condition for atherosclerosis. Elevation of plasma low-density lipoprotein (LDL) cholesterol(LDL-C) concentration is the most important risk factor for atherosclerosis; however, LDL-C elevation is not a criterion for metabolic syndrome, raising the question of LDL's role in the syndrome's association with atherosclerosis. L5, a highly electronegative and mildly oxidized LDL subfraction that we recently isolated from hypercholesterolemic human plasma, may provide a key to answering this question. In cultured vascular endothelial cells (EC), L5 inhibits proliferation and induces apoptosis and monocyte-EC adhesion. In our preliminary studies, L5 could also be detected in patients with MS without elevated LDL-C. Because other LDL subfractions were harmless to EC, the presence of MS-L5 prompted us to hypothesize that the atherogenic role of LDL is not solely determined by plasma LDL-C concentration, but more importantly, by its composition. The proposed study is designed to test this hypothesis. The first question we will address is what lipid factor determines the prevalence of L5 in MS. Subsequently, we will examine whether treatment with selected medicines can effectively reduce L5 in MS patients by correcting the factor favorable for L5 formation. We are in the process of identifying the active components of L5 to fully characterize the atherogenic role of L5 in MS,. In the current proposal, we focus our interest on the efficacy of Ezetimibe, Simvastatin, and Vytorin in reducing L5 from the plasma of MS patients.
Metabolic Syndrome
Metabolic Syndrome LDL subfraction L5 The reduction of LDL in patients with Metabolic Syndrome The prevalence of L5 in patients with Metabolic Syndrome The reduction of L5 in patients with Metabolic Syndrome
null
4
arm 1: Randomly chosen participants will receive ezetimibe 10mg daily for 3 months. arm 2: Randomly chosen participants will receive Simvastatin 20mg daily for 3 months. arm 3: Randomly chosen participants will receive Vytorin 20/10mg daily for 3 months. arm 4: Randomly chosen participants will receive Placebo tab 1 daily for 3 months.
[ 1, 1, 1, 2 ]
4
[ 0, 0, 0, 0 ]
intervention 1: Simvastatin 20mg daily for 3 months. intervention 2: Vytorin 20/10mg daily for 3 months. intervention 3: Placebo one tablet daily times 3 months. intervention 4: Ezetimibe 10mg daily for 3 months.
intervention 1: Simvastatin intervention 2: Vytorin intervention 3: Placebo intervention 4: Ezetimibe
1
Houston | Texas | United States | -95.36327 | 29.76328
0
NCT00988364
[ 5 ]
162
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
false
0ALL
false
The objectives of the study are to evaluate the analgesic and hypnotic efficacy of naproxen sodium and diphenhydramine combination when compared to naproxen sodium, diphenhydramine, and an ibuprofen and diphenhydramine combination
null
Sleep
Naproxen sodium Diphenhydramine Drugs, Investigational
null
6
arm 1: None arm 2: None arm 3: None arm 4: None arm 5: None arm 6: None
[ 0, 1, 0, 1, 1, 1 ]
6
[ 0, 0, 0, 0, 0, 0 ]
intervention 1: Participants received 2 tablets of Naproxen Sodium 220 mg and 2 tablets of Diphenhydramine hydrochloride (DPH) 25 mg, single dose, orally. intervention 2: Participants received 2 tablets of Naproxen Sodium 220mg and 2 tablets of placebo, single dose, orally. intervention 3: One dose of naproxen sodium 220 mg plus diphenhydramine 50 mg intervention 4: Participants received 1 tablet of Naproxen Sodium 220 mg and 3 tablets of placebo, single dose, orally. intervention 5: Participants received 2 tablets of Diphenhydramine hydrochloride (DPH) 25 mg and 2 tablets of placebo, single dose, orally. intervention 6: Participants received 2 tablets of Advil PM (ibuprofen 200 mg and diphenhydramine citrate 38 mg) and 2 tablets of Placebo, single dose, orally.
intervention 1: Naproxen Sodium 440 mg (BAYH6689) / DPH 50mg intervention 2: Naproxen Sodium 440 mg (BAYH6689) intervention 3: Naproxen Sodium 220 mg (BAYH6689) / DPH 50mg intervention 4: Naproxen Sodium 220 mg (BAYH6689) intervention 5: DPH 50mg intervention 6: Ibuprofen 400 mg / Diphenhydramine citrate 76 mg
1
Salt Lake City | Utah | United States | -111.89105 | 40.76078
0
NCT01118273
[ 4 ]
301
RANDOMIZED
PARALLEL
1PREVENTION
1SINGLE
false
0ALL
null
The purpose of this study is to determine whether hydration with sodium bicarbonate is superior to hydration with saline to prevent contrast-induced nephropathy.
null
Renal Failure
contras-induced nephropathy
null
2
arm 1: hydration with sodium bicarbonate arm 2: hydration with saline 1ml/Kg/h for 6 hours
[ 0, 1 ]
2
[ 0, 0 ]
intervention 1: hydration with sodium bicarbonate 1ml/Kg/h for 6 hours intervention 2: hydration with saline 1ml/Kg/h for 6 hours
intervention 1: sodium bicarbonate intervention 2: saline
1
Porto Alegre | Rio Grande do Sul | Brazil | -51.23019 | -30.03283
0
NCT01172353
[ 4 ]
332
null
null
null
null
null
0ALL
null
To investigate that the efficacy of 3% DE-089 ophthalmic solution (one drop at a time, 6 times daily, 4 weeks topical administration), in comparison to 0.1% sodium hyaluronate ophthalmic solution (0.1% HA) (one drop at a time, 6 times daily, 4 weeks topical administration), is at least non-inferior in the change in fluorescein staining score, and is superior in the change in Rose bengal score, in a multicenter, double-masked, parallel-group comparison study. Safety profile will likewise be compared.
null
Dry Eye
null
2
arm 1: None arm 2: None
[ 0, 1 ]
2
[ 0, 0 ]
intervention 1: None intervention 2: None
intervention 1: 3% DE-089 ophthalmic solution intervention 2: 0.1% sodium hyaluronate ophthalmic solution
1
Osaka | Osaka | Japan | 135.50107 | 34.69379
0
NCT01240382
[ 3 ]
123
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
true
1FEMALE
false
Evaluate the adequacy of ovulation suppression, cycle control, and safety of three transdermal contraceptive delivery systems (TCDSs).
The primary objective was to evaluate the adequacy of ovulation suppression, cycle control, and safety of three transdermal contraceptive delivery systems (TCDSs) containing 2 different doses of levonorgestrel (LNG) and 3 different doses of ethinyl estradiol (EE) during 3 consecutive cycles of administration of each treatment.
Ovulation Suppression
contraception pregnancy prevention
null
3
arm 1: Drug intervention with levonorgestrel and ethinyl estradiol : AG200-15 a transdermal contraceptive system containing 2.60 mg of levonorgestrel and 2.30 mg of ethinyl estradiol. arm 2: Drug intervention with levonorgestrel and ethinyl estradiol: AG200 a transdermal contraceptive system containing 2.17 mg of levonorgestrel and 1.92 of ethinyl estradiol. arm 3: Drug intervention with levonorgestrel and ethinyl estradiol: AG200LE a transdermal contraceptive system containing 2.17 mg of levonorgestrel and 1.28 mg of ethinyl estradiol.
[ 0, 0, 0 ]
1
[ 0 ]
intervention 1: pregnancy prevention
intervention 1: levonorgestrel and ethinyl estradiol
11
Tucson | Arizona | United States | -110.92648 | 32.22174 San Diego | California | United States | -117.16472 | 32.71571 Denver | Colorado | United States | -104.9847 | 39.73915 Pembroke Pines | Florida | United States | -80.22394 | 26.00315 Tampa | Florida | United States | -82.45843 | 27.94752 Sandy Springs | Georgia | United States | -84.37854 | 33.92427 Cary | North Carolina | United States | -78.78112 | 35.79154 Winston-Salem | North Carolina | United States | -80.24422 | 36.09986 Jenkintown | Pennsylvania | United States | -75.12517 | 40.09594 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Bristol | Tennessee | United States | -82.18874 | 36.59511
0
NCT01250210
[ 2 ]
18
RANDOMIZED
PARALLEL
0TREATMENT
1SINGLE
false
0ALL
true
This Phase I/IIa, multi-center, randomized, placebo-controlled, single-blinded dose-escalation study evaluated TNX-832 (also referred to as ALT-836 and Sunol cH36) in subjects with suspected or proven bacteria-induced ALI/ARDS. Up to five cohorts of at least six subjects each were originally planned. Subjects were to be randomized in a 5:1 ratio to receive TNX-832 or placebo,respectively, administered as a single bolus infusion over 15 minutes. Three cohorts of subjects were enrolled to the study and safety and pharmacokinetics of the study treatment were evaluated.
Tissue factor (TF) is a transmembrane glycoprotein that acts as the principal initiator of the extrinsic coagulation pathway. TF is a key mediator between the immune system and coagulation and is the principal activator of coagulation. The TF-FVIIa complex activates FX and FIX, resulting in the cleavage of prothrombin to thrombin. Normally, localized activation of the coagulation cascade associated with inflammatory responses plays a role in controlling the spread of infectious agents; however, aberrant TF expression often leads to serious thrombotic disorders. TF-dependent thrombosis has been associated with many diseases including septic shock, coronary artery disease (CAD), cancer, and many inflammatory and autoimmune disorders such as lupus, rheumatoid arthritis, psoriasis, and inflammatory bowel disease. Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS) are forms of acute respiratory failure characterized by diffuse pulmonary infiltrates, pulmonary hypertension, refractory hypoxemia, loss of pulmonary compliance and normal hydrostatic pressures. ALI and ARDS commonly occur in patients with acute catastrophic events such as sepsis, trauma and severe pulmonary infections. The incidence of ALI and ARDS is extremely high in patients with sepsis. By blocking the initiating events of extrinsic coagulation activation, their effects on pro-inflammatory events in the lungs and disordered fibrin deposition may be corrected and the evolution of severe structural and functional injury may be averted during ALI/ARDS. TNX-832 (formerly known as Sunol-cH36), directed against human TF, which can block the pathological complications of TF-dependent thrombus formation. The blockage by TNX-832 of initiating events in the extrinsic coagulation pathway may attenuate the effects on pro-inflammatory events in ALI/ARDS patients, thereby averting or decreasing disordered fibrin deposition and averting the evolution of severe structural and functional injury.
Sepsis Acute Lung Injury Acute Respiratory Distress Syndrome
Sepsis Acute Lung Injury Acute Respiratory Distress Syndrome ALI/ARDS Lung Disease
Prot_SAP_000.pdf: CONFIDENTIAL The Safety, Pharmacokinetics, and Pharmacodynamic Effects of TNX- 832 (Sunol-cH36) in Subjects with Acute Lung Injury/Acute Respiratory Distress Syndrome TNX-832 Active Ingredient: TNX-832 (Sunol c-H36) Indication: Acute Lung Injury/Acute Respiratory Distress Syndrome Study TNX-832.201 Phase I/IIa Study Initiation Date: December 16, 2004 Date of Early Termination: July 26, 2006 Abbreviated Clinical Study Report Prepared for Genentech, Inc. by XTrials Research Services 265 Davidson Ave, Suite 202 Somerset, NJ 08873 Report Issue Date: 11 February, 2008 Sponsor Signatory: Alex Bajamonde Director, DATA Group, Genentech, Inc. Medical Director: Sean Bohen, M.D., Genentech, Inc. This study was performed in compliance with good clinical practice (GCP), including the archiving of essential documents. Page 1 of 3638 Page 2 of 3638 Page 3 of 3638 Page 4 of 3638 CONFIDENTIAL February 11, 2008 5 2. Synopsis Sponsor Name: Study Drug: Active Ingredient: Genentech TNX-832 TNX-832 (Sunol-cH36) Title: The Safety, Pharmacokinetics, and Pharmacodynamic Effects of TNX-832 (Sunol-cH36) in Subjects with Acute Lung Injury/Acute Respiratory Distress Syndrome Investigators/Study Centers: This study was conducted at 12 sites in the United States and 5 sites in Canada. Publications: None Study Period: 16 Dec 2004 to 30 July 2006 Phase of development: I/IIa Objectives: The objectives of this study were: x To evaluate the safety and pharmacokinetics of six dose levels of TNX-832 (0.06 mg/kg, 0.08 mg/kg, 0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg) in subjects with suspected or proven bacteria-induced ALI/ARDS. x To evaluate the pharmacodynamic effects of six dose levels of TNX-832 (0.06 mg/kg, 0.08 mg/kg, 0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, and 0.4 mg/kg) in subjects with suspected or proven bacteria-induced ALI/ARDS. Methodology: This multi-center, randomized, placebo-controlled, single-blinded dose-escalation study was to evaluate TNX-832 in subjects with suspected or proven bacteria-induced acute lung injury (ALI)/acute respiratory distress syndrome (ARDS). Five cohorts of at least six subjects each were originally planned. Subjects were to be randomized in a 5:1 ratio to receive TNX-832 or placebo, respectively, administered as a single bolus infusion over 15 minutes. In November, 2005, a Data Safety Monitoring Board (DSMB) review of adverse events in the 0.1 mg/kg in led to an observation of probably-related hematuria in all subjects who received TNX-832 at 0.1 mg/kg. This review required the studying of TNX-832 at a lower dose cohort than previously planned. One additional cohort (0.08 mg/kg) of at least 6 subjects was planned. Additionally, the DSMB recommended administering study drug through a slow IV infusion (over 2 hours; 50 cc/hr). In September, 2006, upon a subsequent DSMB review of adverse events in the 0.08 mg/kg dose group, a decision was made to prematurely discontinue the study. Subject Population: Eligible subjects were 18 years of age or older with a suspected or proven bacterial infection. Subjects were also required to: 1). Have a diagnosis of acute lung injury/acute respiratory distress syndrome ALI/ARDS; 2). be receiving positive pressure ventilation through an endotracheal tube; and 3). provide signed informed consent, authorization in accordance with the Health Inisurance Portability Accountability Act of 1996 (HIPAA) and agree to comply with all protocol-specified procedures and evaluations. Page 5 of 3638 CONFIDENTIAL February 11, 2008 6 Sponsor Name: Study Drug: Active Ingredient: Genentech TNX-832 TNX-832 (Sunol-cH36) Title: The Safety, Pharmacokinetics, and Pharmacodynamic Effects of TNX-832 (Sunol-cH36) in Subjects with Acute Lung Injury/Acute Respiratory Distress Syndrome Study Medication: Subjects were to be randomized in a 5:1 ratio to receive TNX-832 or placebo, respectively, administered as a single bolus infusion over 15 minutes. The TNX-832 dose for each cohort dosed was: x Cohort 1: 0.06 mg/kg TNX-832 x Cohort 2: 0.1 mg/kg TNX-832 x Cohort 3: 0.08 mg/kg TNX-832 The original planned dose in Cohort 3 was .2 mg/kg. This was lowered to 0.08 mg/kg following a recommendation by the DSMB upon a review of adverse events in Cohort 2. Criteria for Evaluation: Pharmacokinetics: The following PK parameters were to be determined: Cmax (maximum serum concentration), Tmax (time to maximum serum concentration), AUClast (area under the serum concentration-time curve from the time of dosing to the time of the last observed concentration), AUCf (area under the serum concentration-time curve from the time of dosing extrapolated to infinity), CL (serum clearance), Vd (apparent volume of distribution at elimination phase), Vss (apparent volume of distribution at steady state), t1/2 (terminal elimination phase half life). Pharmacodynamics: Sample for the following inflammatory markers were collected but not analyzed: C-reactive protein [CRP], IL-6, IL-8, IL-1ȕ, and TNF-Į. Safety: Safety assessments performed during this study included adverse events, clinical laboratory parameters (hematology, chemistry, coagulation, urinalysis, hematoccult), vital signs measurements (body temperature, heart rate, respiratory rate, blood pressure), physical examinations and electrocardiograms. Additional assessments included arterial blood gases, ventilation assessments, chest radiograph, hospital indices, and immunogenicity. Statistical Methods: Serum concentration and pharmacokinetic parameters were to be summarized by and compared among dosing cohorts using descriptive statistics. Parametric and/or non-parametric statistical comparisons were to be done if suggested by the data, but were not performed. Continuous data variables were summarized by sample size, mean and its standard error, median, standard deviation , minimum, and maximum values. PD samples were not analyzed as the data were not anticipated to provide any meaningful information about the action of the study drug. Safety evaluations were based on the incidence, intensity and type of AEs and clinically significant changes in the subject’s physical examination findings, vital signs, and Page 6 of 3638 CONFIDENTIAL February 11, 2008 7 Sponsor Name: Study Drug: Active Ingredient: Genentech TNX-832 TNX-832 (Sunol-cH36) Title: The Safety, Pharmacokinetics, and Pharmacodynamic Effects of TNX-832 (Sunol-cH36) in Subjects with Acute Lung Injury/Acute Respiratory Distress Syndrome clinical laboratory results. Safety variables were tabulated and presented for all subjects who received TNX-832 or placebo. Subjects who received TNX-832 were grouped by cohort. Subjects who received placebo were treated as one group. Summary: Number of Subjects: Eighteen subjects were assigned to study treatment. Two subjects were withdrawn from the study following administration of study drug. Subject 10-005 died during the study. The death occurred after removal of respiratory support for acute hypoxia; the death was determined by both the Investigator and the Sponsor to be not related to study drug administration. Subject 08-002 withdrew consent 48 days after administration of 0.06 mg/kg TNX-832. Demographics: Demographics and baseline characteristics are summarized in the table below. Placebo N=3 0.06 mg/kg TNX-832 N=5 0.1 mg/kg TNX-832 N=5 0.08 mg/kg TNX-832 N=5 Age, [Mean (SD)] 49.67 (24.3) 40.40 (18.2) 54.60 (13.7) 54.00 (16.9) Gender, [N (%)] -Male 1 (33.3) 1 (20.0) 0 (0.0) 2 (40.0) -Female 2 (66.7) 4 (80.0) 5 (100.0) 3 (60.0) Race, [N (%)] -Caucasian 1 (33.3) 4 (80.0) 3 (60.0) 2 (40.0) -Black 1 (33.3) 0 (0) 2 (40.0) 2 (40.0) -Hispanic 1 (33.3) 1 (20.0) 0 (0.0) 1 (20.0) Pharmacokinetic: Pharmacokinetic results are provided as an appendix to this report. Pharmacodynamic: Pharmacodynamic samples were not analyzed. Safety Results: There was one death during the study. Subject 10005 died after removal of respiratory support for acute hypoxia. The subject died 10 days after administration of 0.08 mg/kg TNX-832. The death was considered unrelated to study medication by the Investigator. Four subjects experienced non-fatal SAEs during the study, including bilateral pulmonary embolism, hypoxic respiratory failure secondary to hospital-acquired pneumonia, worsening acute renal failure, and worsening anemia and empyema. Of these SAEs, the hypoxic respiratory failure secondary to hospital- acquired pneumonia in one subject was considered possibly related to study medication. The worsening anemia and empyema in one subject were considered possibly related to study medication, with empyema considered unrelated at the time of resolution. Of the Page 7 of 3638 CONFIDENTIAL February 11, 2008 8 Sponsor Name: Study Drug: Active Ingredient: Genentech TNX-832 TNX-832 (Sunol-cH36) Title: The Safety, Pharmacokinetics, and Pharmacodynamic Effects of TNX-832 (Sunol-cH36) in Subjects with Acute Lung Injury/Acute Respiratory Distress Syndrome 18 subjects enrolled in this study, 16 subjects reported a total of 87 AEs during the study. Of the 87 treatment-emergent AEs in this study, 48 (55%) AEs were moderate in intensity, 35 (40%) AEs were mild in intensity, and 4 (5%) AEs were severe in intensity. Of the 87 treatment-emergent AEs, 16 AEs were considered by the Investigator to be related to study medication. Two AEs were considered related to placebo administration; 3 AEs were considered related to 0.06 mg/kg TNX-832 administration; 5 AEs were considered related to 0.1 mg/kg TNX-832 administration; 6 AEs were considered related to 0.08 mg/kg TNX-832 administration. A summary of treatment- emergent AEs is presented in the table below. Placebo 0.06 mg/kg TNX-832 0.1 mg/kg TNX-832 0.08 mg/kg TNX-832 Total Dosed 3 5 5 5 18 Number of AEs 20 18 20 29 87 Subjects with AEs 3 4 5 4 16 Subjects with SAEs 0 1 2 2 5 Subjects with severe AEs 2 0 1 0 3 Subjects who discontinued due to AEs 0 0 0 1 1 Seven subjects had 16 laboratory values that were reported as AEs. None of these laboratory values reported as Aes were assessed as related to study medication by the Investigator, with the exception of decreased hemoglobin which resolved one day after onset with red blood cell transfusion. There were no clinically significant trends in vital signs during the study. Three subjects had changes in vital signs that were reported as AEs during the study. None of these changes in vital signs reported as Aes were assessed as related to study medication by the Investigator. Four subjects had ECG findings reported as Aes, none of which were assessed as related to study medication by the Investigator. There were no clinically significant trends in any ventilation evaluation during the study. Two subjects had clinically significant findings on chest x-ray following administration of study medication. One subject experienced pulmonary oedema, which resolved 22 days after onset. One subject experienced empyema and right pleural effusion, which resolved 8 days and 2 days after onset, respectively. Conclusions: This study was prematurely discontinued due to the high incidence of hematuria (nine occurrences) during the study. All instances of hematuria were experienced by patients who received study drug. In this study, the most frequent AEs were hematuria (n=9) and anemia (n=6). At the highest dose level of TNX-832 administered during this study (0.1 mg/kg), all five subjects dosed had AEs of hematuria. Hematuria was considered Page 8 of 3638 CONFIDENTIAL February 11, 2008 9 Sponsor Name: Study Drug: Active Ingredient: Genentech TNX-832 TNX-832 (Sunol-cH36) Title: The Safety, Pharmacokinetics, and Pharmacodynamic Effects of TNX-832 (Sunol-cH36) in Subjects with Acute Lung Injury/Acute Respiratory Distress Syndrome related to study medication by the Investigator in four of the five subjects. After the dose level was reduced to 0.08 mg/kg in Cohort 3, 2 subjects experienced hematuria (1 related to study medication). Based upon the bleeding related AEs of hematuria, the DSMB decided to discontinue the study. In conclusion, the study was prematurely discontinued due to the high incidence of treatment-related hematuria reported during the study, and the continued observation of hematuria in spite of the lowered dose in the third cohort . x Although there was one death during the study, the death was considered unrelated to study medication and was not the cause for discontinuation of the study. Date of Report: 11 February 2008 Page 9 of 3638
2
arm 1: Anti-tissue factor antibody arm 2: Placebo control
[ 0, 2 ]
2
[ 2, 0 ]
intervention 1: Single intravenous dose of TNX-832 at 0.06, 0.08 or 0.10 mg/kg intervention 2: Single intravenous dose of saline control
intervention 1: TNX-832 intervention 2: Placebo
7
Miami | Florida | United States | -80.19366 | 25.77427 Boston | Massachusetts | United States | -71.05977 | 42.35843 St Louis | Missouri | United States | -90.19789 | 38.62727 Winston-Salem | North Carolina | United States | -80.24422 | 36.09986 Akron | Ohio | United States | -81.51901 | 41.08144 Houston | Texas | United States | -95.36327 | 29.76328 Halifax | Nova Scotia | Canada | -63.57688 | 44.64269
0
NCT01438853
[ 3 ]
38
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
null
This study will evaluate the efficacy and safety of MabThera/Rituxan in patients with relapsed low-grade centroblastic centrocytic non-Hodgkin's lymphoma. Patients will receive once-weekly intravenous MabThera/Rituxan for 4 weeks; responding patients will be treated a second time in case of relapse (defined as progression after complete or partial response). The anticipated time on study treatment is \<3 months.
null
Non-Hodgkin's Lymphoma
null
1
arm 1: None
[ 0 ]
1
[ 0 ]
intervention 1: 375 mg/m2 iv weekly for 4 weeks; for responders to first course of therapy a second course is possible after relapse
intervention 1: rituximab [MabThera/Rituxan]
11
Cologne | N/A | Germany | 6.95 | 50.93333 Erlangen | N/A | Germany | 11.00783 | 49.59099 Göttingen | N/A | Germany | 9.93228 | 51.53443 Grenzach-Wyhlen | N/A | Germany | 7.68333 | 47.55 Hanover | N/A | Germany | 9.73322 | 52.37052 Homburg/saar | N/A | Germany | N/A | N/A München | N/A | Germany | 13.31243 | 51.60698 München | N/A | Germany | 13.31243 | 51.60698 Münster | N/A | Germany | 7.62571 | 51.96236 Stuttgart | N/A | Germany | 9.17702 | 48.78232 Tübingen | N/A | Germany | 9.05222 | 48.52266
0
NCT01998893
[ 3 ]
6
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
null
This study will evaluate the efficacy and safety of Herceptin in patients with metastatic or advanced gastric cancer with disease progression during platinum-based or 5-fluoropyrimidine-based chemotherapy. The anticipated time on study treatment is until disease progression.
null
Gastric Cancer
null
1
arm 1: Initial dose of 4 milligrams (mg) per (/) kilogram (kg) by body weight (BW), followed by 2 mg/kg BW at each subsequent visit
[ 0 ]
1
[ 0 ]
intervention 1: 4 mg/kg initial dose, followed by 2 mg/kg
intervention 1: Trastuzumab
12
Vienna | N/A | Austria | 16.37208 | 48.20849 Dresden | N/A | Germany | 13.73832 | 51.05089 Erlangen | N/A | Germany | 11.00783 | 49.59099 Essen | N/A | Germany | 7.01228 | 51.45657 Grenzach-Wyhlen | N/A | Germany | 7.68333 | 47.55 Halle | N/A | Germany | 11.97947 | 51.48158 Kassel | N/A | Germany | 9.5 | 51.31667 Kiel | N/A | Germany | 10.13489 | 54.32133 Mannheim | N/A | Germany | 8.46694 | 49.4891 München | N/A | Germany | 13.31243 | 51.60698 München | N/A | Germany | 13.31243 | 51.60698 Oldenburg | N/A | Germany | 8.21467 | 53.14118
0
NCT02005484
[ 3 ]
24
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
false
0ALL
false
The objectives of this study are: * To assess the effect of ophthalmic phentolamine mesylate in mesopic conditions on the four endpoints: 1. Contrast sensitivity 2. Low contrast visual acuity 3. Wavefront aberrometry 4. Subjective questionnaire * To assess the safety of ophthalmic phentolamine mesylate
Double-masked, placebo-controlled, single-dose Phase 2 study in 24 patients experiencing severe night vision difficulties to evaluate ocular and systemic safety and efficacy following administration of one drop of phentolamine mesylate 1.0% QD in each eye for 1 day.
Decrease in Night Vision Disturbance; Vision, Loss
Night Vision Disturbances NVD Glare Halos Starbursts Nyxol
null
2
arm 1: 1 drop in each eye (QD) for one day. arm 2: 1 drop in each eye (QD) for one day.
[ 0, 2 ]
2
[ 0, 10 ]
intervention 1: Topical Sterile Ophthalmic Solution intervention 2: Topical Sterile Ophthalmic Solution
intervention 1: Phentolamine Mesylate Ophthalmic Solution 1% intervention 2: Phentolamine Mesylate Ophthalmic Solution Vehicle (Placebo)
1
Lynbrook | New York | United States | -73.6718 | 40.65483
0
NCT04004507
[ 4 ]
374
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
null
This study will evaluate the safety and efficacy of two different dose regimens (12 milligrams \[mg\] and 24 mg) of IV MOA-728 versus placebo in shortening the time to return of bowel function in participants receiving opioid analgesia administered via patient-controlled anesthesia (PCA), and who had undergone repair of large (greater than or equal to \[≥\]10 centimeters) ventral hernias with or without a mesh prosthesis via laparotomy or laparoscopy.
null
Ileus
POI Hernia Ventral Wall Hernia Repair Post Operative Ileus
null
3
arm 1: Participants will receive methylnaltrexone (MOA-728) 12 mg as an IV infusion over approximately 20 minutes for approximately every 6 hours for a total of 4 doses in 24-hour period. The first dose of study drug will be administered within approximately 90 minutes after completion of the surgical procedure (defined as the time when the last skin suture or staple is placed in the participant). Dose administration will be continued for a maximum of 10 days. arm 2: Participants will receive MOA-728 24 mg as an IV infusion over approximately 20 minutes for approximately every 6 hours for a total of 4 doses in 24-hour period. The first dose of study drug will be administered within approximately 90 minutes after completion of the surgical procedure (defined as the time when the last skin suture or staple is placed in the participant). Dose administration will be continued for a maximum of 10 days. arm 3: Participants will receive placebo matching to MOA-728 as an IV infusion over approximately 20 minutes for approximately every 6 hours for a total of 4 doses in 24-hour period. The first dose of study drug will be administered within approximately 90 minutes after completion of the surgical procedure (defined as the time when the last skin suture or staple is placed in the participant). Dose administration will be continued for a maximum of 10 days.
[ 0, 0, 2 ]
2
[ 0, 0 ]
intervention 1: MOA-728 will be administered per the dose and schedule specified in the arm. intervention 2: Placebo matching to MOA-728 will be administered per the schedule specified in the arm.
intervention 1: MOA-728 intervention 2: Placebo
106
Benton | Arkansas | United States | -92.58683 | 34.56454 Colton | California | United States | -117.31365 | 34.0739 Laguna Hills | California | United States | -117.71283 | 33.61252 Loma Linda | California | United States | -117.26115 | 34.04835 Long Beach | California | United States | -118.18923 | 33.76696 Los Angeles | California | United States | -118.24368 | 34.05223 Orange | California | United States | -117.85311 | 33.78779 San Jose | California | United States | -121.89496 | 37.33939 Santa Barbara | California | United States | -119.69819 | 34.42083 Denver | Colorado | United States | -104.9847 | 39.73915 Denver | Colorado | United States | -104.9847 | 39.73915 Inverness | Florida | United States | -82.33037 | 28.83582 Jacksonville | Florida | United States | -81.65565 | 30.33218 Jacksonville | Florida | United States | -81.65565 | 30.33218 Melbourne | Florida | United States | -80.60811 | 28.08363 Miami | Florida | United States | -80.19366 | 25.77427 Miami | Florida | United States | -80.19366 | 25.77427 Naples | Florida | United States | -81.79596 | 26.14234 Orlando | Florida | United States | -81.37924 | 28.53834 Pensacola | Florida | United States | -87.21691 | 30.42131 Tampa | Florida | United States | -82.45843 | 27.94752 Peoria | Illinois | United States | -89.58899 | 40.69365 Des Moines | Iowa | United States | -93.60911 | 41.60054 Kansas City | Kansas | United States | -94.62746 | 39.11417 Lexington | Kentucky | United States | -84.47772 | 37.98869 Baltimore | Maryland | United States | -76.61219 | 39.29038 Boston | Massachusetts | United States | -71.05977 | 42.35843 Boston | Massachusetts | United States | -71.05977 | 42.35843 Springfield | Massachusetts | United States | -72.58981 | 42.10148 Ann Arbor | Michigan | United States | -83.74088 | 42.27756 Detroit | Michigan | United States | -83.04575 | 42.33143 Flint | Michigan | United States | -83.68746 | 43.01253 Jackson | Mississippi | United States | -90.18481 | 32.29876 Columbia | Missouri | United States | -92.33407 | 38.95171 Omaha | Nebraska | United States | -95.94043 | 41.25626 Omaha | Nebraska | United States | -95.94043 | 41.25626 New Brunswick | New Jersey | United States | -74.45182 | 40.48622 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 Albany | New York | United States | -73.75623 | 42.65258 New York | New York | United States | -74.00597 | 40.71427 Stony Brook | New York | United States | -73.14094 | 40.92565 Syracuse | New York | United States | -76.14742 | 43.04812 The Bronx | New York | United States | -73.86641 | 40.84985 Chapel Hill | North Carolina | United States | -79.05584 | 35.9132 Durham | North Carolina | United States | -78.89862 | 35.99403 Winston-Salem | North Carolina | United States | -80.24422 | 36.09986 Winston-Salem | North Carolina | United States | -80.24422 | 36.09986 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Cleveland | Ohio | United States | -81.69541 | 41.4995 Columbus | Ohio | United States | -82.99879 | 39.96118 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Bend | Oregon | United States | -121.31531 | 44.05817 Portland | Oregon | United States | -122.67621 | 45.52345 Hershey | Pennsylvania | United States | -76.65025 | 40.28592 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Sellersville | Pennsylvania | United States | -75.3049 | 40.35399 Providence | Rhode Island | United States | -71.41283 | 41.82399 Sioux Falls | South Dakota | United States | -96.70033 | 43.54997 Knoxville | Tennessee | United States | -83.92074 | 35.96064 Memphis | Tennessee | United States | -90.04898 | 35.14953 Nashville | Tennessee | United States | -86.78444 | 36.16589 Fort Worth | Texas | United States | -97.32085 | 32.72541 San Antonio | Texas | United States | -98.49363 | 29.42412 Temple | Texas | United States | -97.34278 | 31.09823 Norfolk | Virginia | United States | -76.28522 | 36.84681 Winchester | Virginia | United States | -78.16333 | 39.18566 Bellevue | Washington | United States | -122.20068 | 47.61038 Tacoma | Washington | United States | -122.44429 | 47.25288 Morgantown | West Virginia | United States | -79.9559 | 39.62953 Milwaukee | Wisconsin | United States | -87.90647 | 43.0389 Adelaide SA | N/A | Australia | N/A | N/A Elizabeth Vale SA | N/A | Australia | N/A | N/A Wilrijkstraat 10 | Edegem | Belgium | N/A | N/A De Pintelaan 185 | Gent Belgium | Belgium | N/A | N/A Edmonton | Alberta | Canada | -113.46871 | 53.55014 Vancouver | British Columbia | Canada | -123.11934 | 49.24966 Montreal | Quebec | Canada | -73.58781 | 45.50884 Nussbaumstrasse 20 | Muenchen | Germany | N/A | N/A Augustenburger Platz 1 | State of Berlin | Germany | N/A | N/A Heidelberg | N/A | Germany | 8.69079 | 49.40768 Nyíregyháza | N/A | Hungary | 21.71671 | 47.95539 Pécs | N/A | Hungary | 18.23083 | 46.0725 Székesfehérvár | N/A | Hungary | 18.41034 | 47.18995 Veszprém | N/A | Hungary | 17.91149 | 47.09327 Corso Giovecca 203 | Ferrara | Italy | N/A | N/A Gemelli | Rome | Italy | N/A | N/A Padua | Via Giustiniani 2 | Italy | 11.88586 | 45.40797 Bergamo | N/A | Italy | 9.66721 | 45.69601 Jan Toorpstraat 164 | Amsterdam | Netherlands | N/A | N/A Roosendaal | N/A | Netherlands | 4.46528 | 51.53083 Powstancow Wielkopolskich 72 | Szczecin | Poland | N/A | N/A Bydgoszcz | N/A | Poland | 18.00762 | 53.1235 Polnocna 42 | Łódź Voivodeship | Poland | N/A | N/A Durban Kwa-Zulu | KwaZulu-Natal | South Africa | N/A | N/A Somerset West | Western Cape | South Africa | 18.82113 | -34.08401 Worcester | Western Cape | South Africa | 19.44852 | -33.64651 Moreletapark Pretoria | N/A | South Africa | N/A | N/A Pretoria | N/A | South Africa | 28.18783 | -25.74486 Pretoria Gauteng | N/A | South Africa | N/A | N/A Pretoria Gauteng | N/A | South Africa | N/A | N/A Seoul | N/A | South Korea | 126.9784 | 37.566
0
NCT00528970
[ 3 ]
6
NON_RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
1FEMALE
null
RATIONALE: Vaccines made from peptides may help the body build an effective immune response to kill tumor cells. Drugs used in chemotherapy, such as paclitaxel and carboplatin, work in different ways to stop the growth of tumor cells, either by killing the cells or by stopping them from dividing. Giving chemotherapy before surgery may make the tumor smaller and reduce the amount of normal tissue that needs to be removed. Giving vaccine therapy and chemotherapy after surgery may kill any tumor cells that remain after surgery. PURPOSE: This phase II trial is studying how well giving vaccine therapy together with paclitaxel and carboplatin works in treating patients who are undergoing surgery for stage III or stage IV ovarian cancer, primary peritoneal cancer, or fallopian tube cancer.
OBJECTIVES: * Determine the immunogenicity of vaccine therapy comprising synthetic ovarian cancer-associated peptides administered with a synthetic tetanus toxoid helper peptide emulsified in Montanide ISA-51 before or after paclitaxel and carboplatin in patients with stage III-IV ovarian epithelial, primary peritoneal cavity, or fallopian tube cancer undergoing optimal cytoreductive surgery. OUTLINE: This is an open-label study. Patients are assigned to 1 of 2 treatment groups. * Group 1: * Neoadjuvant chemotherapy:Patients receive paclitaxel IV over 3 hours and carboplatin IV over 30 minutes on day 1. Treatment repeats every 21 days for up to 4 courses in the absence of disease progression or unacceptable toxicity. Patients then proceed to surgical debulking. * Surgical debulking: Patients undergo primary optimal cytoreductive surgery. * Vaccine therapy: Within 14 days after surgery, patients receive vaccine therapy comprising synthetic ovarian cancer-associated peptides, MAGE-A1:161-169, FBP:1901-199, Her-2/neu:369-377, MAGE-A1:96-104, and Her-2/neu:754-762, and tetanus toxoid helper peptide emulsified in Montanide ISA-51 intradermally and subcutaneously on days 1, 8, and 15. Treatment repeats every 14 weeks for 2 courses. * Adjuvant chemotherapy: Patients receive 4 courses of paclitaxel and carboplatin as in neoadjuvant chemotherapy after completion of course 1 of vaccine therapy. * Group 2: * Surgical debulking: Patients undergo up-front optimal cytoreductive surgery. Patients with non-optimal primary debulking may undergo interval debulking surgery within 6 weeks after completing course 4 of adjuvant chemotherapy. If interval debulking surgery is performed, tumor and/or lymph node tissue is collected. * Vaccine therapy: Patients receive 2 courses of vaccine therapy as in group 1. * Adjuvant chemotherapy: Patients receive paclitaxel and carboplatin as in group 1, neoadjuvant chemotherapy. Treatment repeats every 21 days for up to 8 courses. Patients undergo periodic blood and tumor tissue collection during study for correlative immunological analysis. After completion of study treatment, patients with progressive disease are followed at 30 days and then every six months thereafter. All other patients are followed every 3 months for 36 months until disease progression or until another therapy is initiated, and then every six months thereafter. PROJECTED ACCRUAL: A total of 28 patients will be accrued for this study.
Fallopian Tube Cancer Ovarian Cancer Primary Peritoneal Cavity Cancer
fallopian tube cancer stage III ovarian epithelial cancer stage IV ovarian epithelial cancer primary peritoneal cavity cancer
null
2
arm 1: Patients in group one will receive a 3-hour infusion of paclitaxel and an infusion of carboplatin in week 1. Treatment may repeat every 3 weeks for up to four courses. They will then undergo surgery to remove as much of the tumor as possible. Within 2 weeks after surgery, patients will receive an injection of the vaccine once a week for 3 weeks. Treatment may repeat every 14 weeks for two courses. After finishing the first course of vaccine therapy, patients will receive a 3-hour infusion of paclitaxel and an infusion of carboplatin every 3 weeks for up to four courses. arm 2: Patients in group two will undergo surgery to remove as much of the tumor as possible. Within 2 weeks after surgery, patients will receive an injection of the vaccine once a week for 3 weeks. Treatment may repeat every 14 weeks for two courses. After finishing the first course of vaccine therapy, patients will receive a 3-hour infusion of paclitaxel and an infusion of carboplatin every 3 weeks for up to eight courses. Some patients may undergo a second surgery within 6 weeks after completing the fourth course of chemotherapy and undergo tumor and/or lymph node tissue collection.
[ 0, 0 ]
5
[ 2, 2, 0, 0, 3 ]
intervention 1: Given intradermally or subcutaneously intervention 2: Given intradermally or subcutaneously intervention 3: Given IV intervention 4: Given IV intervention 5: Patients undergo primary optimal cytoreductive surgery
intervention 1: MAGE-A1, Her-2/neu, FBP peptides ovarian cancer vaccine intervention 2: tetanus toxoid helper peptide intervention 3: carboplatin intervention 4: paclitaxel intervention 5: conventional surgery
1
Charlottesville | Virginia | United States | -78.47668 | 38.02931
0
NCT00373217
[ 2 ]
60
RANDOMIZED
CROSSOVER
9OTHER
4QUADRUPLE
true
0ALL
false
ICH E14 recommends that a thorough QT/QTc (TQT) study should be performed to determine whether intensive monitoring of QT interval in target patient populations is required during later stages of development. The current study is designed to ascertain whether CP-690,550 is associated with QTc prolongation.
The current study is designed to ascertain whether CP-690,550 is associated with QTc prolongation
Healthy
TQT study CP-690 550
null
3
arm 1: None arm 2: None arm 3: None
[ 0, 2, 1 ]
3
[ 0, 0, 0 ]
intervention 1: Single dose 100 mg (5 x 20 mg tablets) intervention 2: Single dose placebo tablets (5 tablets) intervention 3: Single dose Avelox 400 mg tablet
intervention 1: CP-690,550 intervention 2: Placebo intervention 3: Moxifloxacin
2
Brussels | N/A | Belgium | 4.34878 | 50.85045 Singapore | N/A | Singapore | 103.85007 | 1.28967
0
NCT01743677
[ 3 ]
287
NON_RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
false
Study RN624-CL007 is planned to be an open-label protocol to enroll subjects who have previously participated in Study No. RN624-CL006. In this study, subjects will receive RN624 on an open-label basis.
null
Osteoarthritis OA Knee Pain Arthritis
Monoclonal antibody
null
1
arm 1: None
[ 0 ]
1
[ 0 ]
intervention 1: 50 mcg/kg
intervention 1: RN624 (PF-04383119)
36
Birmingham | Alabama | United States | -86.80249 | 33.52066 Birmingham | Alabama | United States | -86.80249 | 33.52066 Phoenix | Arizona | United States | -112.07404 | 33.44838 Anaheim | California | United States | -117.9145 | 33.83529 Anaheim | California | United States | -117.9145 | 33.83529 National City | California | United States | -117.0992 | 32.67811 Stamford | Connecticut | United States | -73.53873 | 41.05343 Stamford | Connecticut | United States | -73.53873 | 41.05343 Daytona Beach | Florida | United States | -81.02283 | 29.21081 Ocala | Florida | United States | -82.14009 | 29.1872 Tampa | Florida | United States | -82.45843 | 27.94752 Tampa | Florida | United States | -82.45843 | 27.94752 Honolulu | Hawaii | United States | -157.85833 | 21.30694 Boise | Idaho | United States | -116.20345 | 43.6135 Merrillville | Indiana | United States | -87.33281 | 41.48281 Louisville | Kentucky | United States | -85.75941 | 38.25424 Wheaton | Maryland | United States | -77.05526 | 39.03983 Worcester | Massachusetts | United States | -71.80229 | 42.26259 Kansas City | Missouri | United States | -94.57857 | 39.09973 Omaha | Nebraska | United States | -95.94043 | 41.25626 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 Rochester | New York | United States | -77.61556 | 43.15478 Greensboro | North Carolina | United States | -79.79198 | 36.07264 Greensboro | North Carolina | United States | -79.79198 | 36.07264 Zanesville | Ohio | United States | -82.01319 | 39.94035 Duncansville | Pennsylvania | United States | -78.4339 | 40.42341 Knoxville | Tennessee | United States | -83.92074 | 35.96064 Knoxville | Tennessee | United States | -83.92074 | 35.96064 Austin | Texas | United States | -97.74306 | 30.26715 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 Midvale | Utah | United States | -111.89994 | 40.61106 Charlottesville | Virginia | United States | -78.47668 | 38.02931 Yakima | Washington | United States | -120.5059 | 46.60207
0
NCT00399490
[ 4 ]
419
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
false
The purpose of this trial is to investigate the efficacy, safety and tolerability of esmirtazapine (Org 50081) compared to placebo in patients with chronic primary insomnia.
Insomnia is a common complaint or disorder throughout the world. About one third of the population in the industrial countries reports difficulty initiating or maintaining sleep, resulting in a non-refreshing or non-restorative sleep. The majority of the insomniacs suffer chronically from their complaints. It has been reported that in patients with chronic insomnia lasting longer than six months, 50% had a past or current mental disorder. This raises the possibility that treatment of insomnia may reduce the risk for psychological conditions. This double-blind, placebo-controlled, parallel, randomized clinical trial is designed to assess the efficacy and safety of esmirtazapine in patients suffering from chronic primary insomnia.
Insomnia
Sleep Initiation and Maintenance Disorders, Sleep Disorders, Intrinsic Dyssomnias, Sleep Disorders, Nervous System Diseases, Mental Disorders
null
3
arm 1: Participants took placebo tablets on Days -7 and -6, esmirtazapine 3.0 mg tablets on Days 1-42, and placebo tablets on Days 43-50. Tablets were taken by mouth once daily in the evening. arm 2: Participants took placebo tablets on Days -7 and -6, esmirtazapine 4.5 mg tablets on Days 1-42, and placebo tablets on Days 43-50. Tablets were taken by mouth once daily in the evening. arm 3: Participants took placebo tablets on Days -7 and -6, placebo tablets on Days 1-42, and placebo tablets on Days 43-50. Tablets were taken by mouth once daily in the evening.
[ 0, 0, 2 ]
2
[ 0, 0 ]
intervention 1: Esmirtazapine maleate was provided as tablets for oral use containing 3.0 mg, or 4.5 mg of active compound. In addition, tablets contain the following excipients: hydroxypropyl cellulose, maize starch (United States Pharmacopeia \[USP\] name corn starch), magnesium stearate, and lactose monohydrate. intervention 2: The placebo tablets contained the following excipients: hydroxypropyl cellulose, maize starch (USP name corn starch), magnesium stearate, and lactose monohydrate.
intervention 1: Esmirtazapine intervention 2: Placebo
0
null
0
NCT00506389
[ 3 ]
334
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
false
This is a dose-ranging study that will evaluate the efficacy, safety and tolerability of a range of doses of investigational product and pioglitazone, compared to placebo, administered as monotherapy over 12 weeks in treatment naive patients with T2DM
null
Diabetes Mellitus, Type 2
Pioglitazone HbA1c Diabetes mellitus
null
3
arm 1: GSK189075 arm 2: Placebo arm 3: pioglitazone (active control)
[ 0, 2, 5 ]
3
[ 0, 0, 10 ]
intervention 1: Experimental Drug intervention 2: Active Control intervention 3: Placebo Comparator
intervention 1: GSK189075 intervention 2: pioglitazone intervention 3: Placebo
136
Mesa | Arizona | United States | -111.82264 | 33.42227 Hollywood | Florida | United States | -80.14949 | 26.0112 Miami | Florida | United States | -80.19366 | 25.77427 Saint Cloud | Florida | United States | -81.28118 | 28.2489 Sunset | Louisiana | United States | -92.06845 | 30.41131 Oxon Hill | Maryland | United States | -76.9897 | 38.80345 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 Canal Fulton | Ohio | United States | -81.59762 | 40.88978 Simpsonville | South Carolina | United States | -82.25428 | 34.73706 San Antonio | Texas | United States | -98.49363 | 29.42412 Burke | Virginia | United States | -77.27165 | 38.79345 Buenos Aries | Buenos Aires | Argentina | N/A | N/A Ciudad Autonoma de Buenos Aires | Buenos Aires | Argentina | N/A | N/A Ciudad Autónoma de Buenos Aires | Buenos Aires | Argentina | N/A | N/A Córdoba | Córdoba Province | Argentina | -64.18853 | -31.40648 Buenos Aires | N/A | Argentina | -58.37723 | -34.61315 Córdoba | N/A | Argentina | -64.18853 | -31.40648 Mendoza | N/A | Argentina | -68.84582 | -32.88946 Quilmes | N/A | Argentina | -58.25454 | -34.72065 San Miguel de Tucumán | N/A | Argentina | -65.21051 | -26.81601 Pleven | N/A | Bulgaria | 24.61667 | 43.41667 Plovdiv | N/A | Bulgaria | 24.75 | 42.15 Sofia | N/A | Bulgaria | 23.32415 | 42.69751 Sofia | N/A | Bulgaria | 23.32415 | 42.69751 Varna | N/A | Bulgaria | 27.91667 | 43.21667 Santiago | Región Metro de Santiago | Chile | -70.64827 | -33.45694 Santiago | Región Metro de Santiago | Chile | -70.64827 | -33.45694 San José | N/A | Costa Rica | -84.08489 | 9.93388 Brno | N/A | Czechia | 16.60796 | 49.19522 Brno | N/A | Czechia | 16.60796 | 49.19522 Brno | N/A | Czechia | 16.60796 | 49.19522 Cheb | N/A | Czechia | 12.37392 | 50.07963 České Budějovice | N/A | Czechia | 14.47434 | 48.97447 Havirov - Soumbrak | N/A | Czechia | N/A | N/A Olomouc | N/A | Czechia | 17.25175 | 49.59552 Prague | N/A | Czechia | 14.42076 | 50.08804 Prague | N/A | Czechia | 14.42076 | 50.08804 Prague | N/A | Czechia | 14.42076 | 50.08804 Prague | N/A | Czechia | 14.42076 | 50.08804 Semily | N/A | Czechia | 15.33552 | 50.60191 Šumperk | N/A | Czechia | 16.97061 | 49.96528 Ústí nad Labem | N/A | Czechia | 14.03227 | 50.6607 Znojmo | N/A | Czechia | 16.0488 | 48.8555 Bammental | Baden-Wurttemberg | Germany | 8.77944 | 49.35611 Kippenheim | Baden-Wurttemberg | Germany | 7.8251 | 48.29564 Mannheim | Baden-Wurttemberg | Germany | 8.46694 | 49.4891 Weinheim | Baden-Wurttemberg | Germany | 8.66697 | 49.54887 Haag | Bavaria | Germany | 12.07614 | 50.30379 Höhenkirchen-Siegertsbrunn | Bavaria | Germany | 11.71906 | 48.01932 Lampertheim | Hesse | Germany | 8.4725 | 49.59786 Damme | Lower Saxony | Germany | 8.19793 | 52.52157 Hanover | Lower Saxony | Germany | 9.73322 | 52.37052 Hildesheim | Lower Saxony | Germany | 9.95112 | 52.15077 Bergkamen | North Rhine-Westphalia | Germany | 7.64451 | 51.61633 Mainz | Rhineland-Palatinate | Germany | 8.2791 | 49.98419 Rhaunen | Rhineland-Palatinate | Germany | 7.34198 | 49.8638 Speyer | Rhineland-Palatinate | Germany | 8.43111 | 49.32083 Berlin | N/A | Germany | 13.41053 | 52.52437 Budapest | N/A | Hungary | 19.04045 | 47.49835 Budapest | N/A | Hungary | 19.04045 | 47.49835 Budapest | N/A | Hungary | 19.04045 | 47.49835 Budapest | N/A | Hungary | 19.04045 | 47.49835 Debrecen | N/A | Hungary | 21.62444 | 47.53167 Érd | N/A | Hungary | 18.91361 | 47.39489 Győr | N/A | Hungary | 17.63512 | 47.68333 Miskolc | N/A | Hungary | 20.77806 | 48.10306 Miskolc | N/A | Hungary | 20.77806 | 48.10306 Mosonmagyaróvár | N/A | Hungary | 17.26994 | 47.86789 Nyirtegyhaza | N/A | Hungary | N/A | N/A Pécs | N/A | Hungary | 18.23083 | 46.0725 Szentes | N/A | Hungary | 20.2608 | 46.65834 Szigetvár | N/A | Hungary | 17.80554 | 46.04865 Szombathely | N/A | Hungary | 16.62155 | 47.23088 Veszprém | N/A | Hungary | 17.91149 | 47.09327 Zalaegerszeg | N/A | Hungary | 16.84389 | 46.84 Bangalore | N/A | India | 77.59369 | 12.97194 Bangalore | N/A | India | 77.59369 | 12.97194 Bangalore | N/A | India | 77.59369 | 12.97194 Kochi | N/A | India | 76.26022 | 9.93988 Mumbai | N/A | India | 72.88261 | 19.07283 New Delhi | N/A | India | 77.2148 | 28.62137 Pune | N/A | India | 73.85535 | 18.51957 Jelgava | N/A | Latvia | 23.71278 | 56.65 Limbaži | N/A | Latvia | 24.71941 | 57.51287 Riga | N/A | Latvia | 24.10589 | 56.946 Riga | N/A | Latvia | 24.10589 | 56.946 Riga | N/A | Latvia | 24.10589 | 56.946 Riga | N/A | Latvia | 24.10589 | 56.946 Riga | N/A | Latvia | 24.10589 | 56.946 Talsi | N/A | Latvia | 22.58137 | 57.24562 Tukums | N/A | Latvia | 23.15554 | 56.96764 Kaunas | N/A | Lithuania | 23.90961 | 54.90272 Kaunas | N/A | Lithuania | 23.90961 | 54.90272 Kaunas | N/A | Lithuania | 23.90961 | 54.90272 Vilnius | N/A | Lithuania | 25.2798 | 54.68916 Vilnius | N/A | Lithuania | 25.2798 | 54.68916 Tijuana | Baja California Norte | Mexico | -117.00371 | 32.5027 Monterrey | Nuevo León | Mexico | -100.31721 | 25.68435 México | State of Mexico | Mexico | -99.12355 | 19.69237 Durango | N/A | Mexico | -104.65756 | 24.02032 Mexico | N/A | Mexico | -98.43784 | 18.88011 Mexico | N/A | Mexico | -98.43784 | 18.88011 Auckland | N/A | New Zealand | 174.76349 | -36.84853 Auckland | N/A | New Zealand | 174.76349 | -36.84853 Hamilton | N/A | New Zealand | 175.28333 | -37.78333 Rotorua | N/A | New Zealand | 176.24516 | -38.13874 Lima | N/A | Peru | -77.02824 | -12.04318 Lima | N/A | Peru | -77.02824 | -12.04318 Bydgoszcz | N/A | Poland | 18.00762 | 53.1235 Grudziądz | N/A | Poland | 18.75366 | 53.48411 Lodz | N/A | Poland | 19.47395 | 51.77058 Porąbka | N/A | Poland | 19.21835 | 49.81716 Siemianowice Śląskie | N/A | Poland | 19.02901 | 50.32738 Wroclaw | N/A | Poland | 17.03333 | 51.1 Ponce | N/A | Puerto Rico | -66.62398 | 18.01031 Brasov | N/A | Romania | 25.60613 | 45.64861 Bucharest | N/A | Romania | 26.10626 | 44.43225 Deva | N/A | Romania | 22.9 | 45.88333 Iași | N/A | Romania | 27.6 | 47.16667 Moscow | N/A | Russia | 37.61556 | 55.75222 Moscow | N/A | Russia | 37.61556 | 55.75222 Moscow | N/A | Russia | 37.61556 | 55.75222 Moscow | N/A | Russia | 37.61556 | 55.75222 Saint Petersburg | N/A | Russia | 30.31413 | 59.93863 Saint Petersburg | N/A | Russia | 30.31413 | 59.93863 Tomsk | N/A | Russia | 84.98204 | 56.50032 Tyumen | N/A | Russia | 65.52722 | 57.15222 Ufa | N/A | Russia | 55.96779 | 54.74306 Bellville | N/A | South Africa | 18.62847 | -33.90022 Gauteng | N/A | South Africa | N/A | N/A Orangegrove, Linksfield West | N/A | South Africa | N/A | N/A Parow | N/A | South Africa | 18.59992 | -33.89723 Roodepoort | N/A | South Africa | 27.8725 | -26.1625
0
NCT00500331
[ 4 ]
354
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
false
To assess the impact on glucose control by inhaled insulin in patients with type 2 diabetes who are not well controlled on 2 or more oral anti-diabetic agents
null
Diabetes Mellitus Type 2
Type 2 diabetes melllitus
null
2
arm 1: Inhaled insulin plus oral therapy arm 2: Standard of Care: All licensed diabetes drugs can be prescribed per discretion of investigators
[ 0, 5 ]
2
[ 0, 10 ]
intervention 1: Addition of inhaled insulin to pre-existing oral diabetes therapy. intervention 2: Standard of Care: All licensed diabetes drugs can be prescribed per discretion of investigators
intervention 1: Inhaled Insulin (Exubera) intervention 2: Standard of Care
64
Coquitlam | British Columbia | Canada | -122.78217 | 49.2846 Winnipeg | Manitoba | Canada | -97.14704 | 49.8844 Bathurst | New Brunswick | Canada | -65.65112 | 47.61814 London | Ontario | Canada | -81.23304 | 42.98339 Orillia | Ontario | Canada | -79.42068 | 44.60868 Charlottetown | Prince Edward Island | Canada | -63.1256 | 46.23459 Bonaventure | Quebec | Canada | -65.49259 | 48.04573 Chicoutimi | Quebec | Canada | -71.06369 | 48.41963 Drummondville | Quebec | Canada | -72.48241 | 45.88336 Gatineau | Quebec | Canada | -75.70164 | 45.47723 Greenfield Park | Quebec | Canada | -73.46223 | 45.48649 Saint-Foy | Quebec | Canada | N/A | N/A Saint-Marc-des-Carrieres | Quebec | Canada | -72.0491 | 46.68335 Trois-Rivières | Quebec | Canada | -72.5477 | 46.34515 Nantes | Cedex 01 | France | -1.55336 | 47.21725 Amiens | N/A | France | 2.3 | 49.9 Armentières | N/A | France | 2.88214 | 50.68568 Bondy | N/A | France | 2.48931 | 48.9018 Brest | N/A | France | -4.48628 | 48.39029 Cean Cedex | N/A | France | N/A | N/A Chartres | N/A | France | 1.48925 | 48.44685 Lille | N/A | France | 3.05858 | 50.63297 Lorient | N/A | France | -3.37177 | 47.74817 Montpellier | N/A | France | 3.87635 | 43.61093 Paris | N/A | France | 2.3488 | 48.85341 Paris | N/A | France | 2.3488 | 48.85341 Reims | N/A | France | 4.02853 | 49.26526 Rennes | N/A | France | -1.67429 | 48.11198 Roubaix | N/A | France | 3.17456 | 50.69421 Toul | N/A | France | 5.89115 | 48.68075 Athens | N/A | Greece | 23.72784 | 37.98376 Athens | N/A | Greece | 23.72784 | 37.98376 Haidari | N/A | Greece | N/A | N/A Pireaus | N/A | Greece | N/A | N/A Thessaloniki | N/A | Greece | 22.93086 | 40.64361 Aveiro | N/A | Portugal | -8.64554 | 40.64427 Coimbra | N/A | Portugal | -8.41955 | 40.20564 Lisbon | N/A | Portugal | -9.1498 | 38.72509 Lisbon | N/A | Portugal | -9.1498 | 38.72509 Porto | N/A | Portugal | -8.61099 | 41.14961 Torres Vedras | N/A | Portugal | -9.2586 | 39.09109 Santiago de Compostela | A Coruña | Spain | -8.54569 | 42.88052 Santiago de Compostela | A Coruña | Spain | -8.54569 | 42.88052 L'Hospitalet de Llobregat | Barcelona | Spain | 2.10028 | 41.35967 Terrassa | Barcelona | Spain | 2.01667 | 41.56667 Pamplona | Navarre | Spain | -1.64323 | 42.81687 Oviedo | Principality of Asturias | Spain | -5.84476 | 43.36029 Alicante | N/A | Spain | -0.48149 | 38.34517 Barcelona | N/A | Spain | 2.15899 | 41.38879 Barcelona | N/A | Spain | 2.15899 | 41.38879 Madrid | N/A | Spain | -3.70256 | 40.4165 Madrid | N/A | Spain | -3.70256 | 40.4165 Madrid | N/A | Spain | -3.70256 | 40.4165 Málaga | N/A | Spain | -4.42034 | 36.72016 Pontevedra | N/A | Spain | -8.64435 | 42.431 Valencia | N/A | Spain | -0.37966 | 39.47391 Valencia | N/A | Spain | -0.37966 | 39.47391 Zaragoza | N/A | Spain | -0.87734 | 41.65606 Ängelholm | N/A | Sweden | 12.86219 | 56.2428 Stockholm | N/A | Sweden | 18.06871 | 59.32938 Stockholm | N/A | Sweden | 18.06871 | 59.32938 Ankara | N/A | Turkey (Türkiye) | 32.85427 | 39.91987 Istanbul | N/A | Turkey (Türkiye) | 28.94966 | 41.01384 Izmir | N/A | Turkey (Türkiye) | 27.13838 | 38.41273
0
NCT00282971
[ 3 ]
30
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
false
This study was conducted to test the safety and tolerability of afegostat tartrate in participants with type 1 Gaucher disease already receiving enzyme replacement therapy.
This was a Phase 2, open-label study in participants with Gaucher disease, a lysosomal storage disorder. Afegostat tartrate (also known as AT2101 or isofagomine tartrate) is designed to act as a pharmacological chaperone by selectively binding to misfolded β-glucocerebrosidase (GCase) and helping it fold correctly, intended to restore GCase activity. The study consisted of a 14-day screening period, a 28-day treatment period, and a 7-day wash-out period. Participants received 1 of 4 dosing regimens for afegostat tartrate.
Gaucher Disease, Type 1 Type 1 Gaucher Disease Gaucher Disease
afegostat tartrate isofagomine tartrate AT2101 Amicus Therapeutics
null
4
arm 1: Afegostat tartrate was administered orally during the 4-week treatment period. arm 2: Afegostat tartrate was administered orally once per day during the 4-week treatment period. arm 3: Afegostat tartrate was administered orally once every 4 days during the 4-week treatment period. arm 4: Afegostat tartrate was administered orally once every 7 days during the 4-week treatment period.
[ 0, 0, 0, 0 ]
1
[ 0 ]
intervention 1: None
intervention 1: Afegostat tartrate
10
San Francisco | California | United States | -122.41942 | 37.77493 Coral Springs | Florida | United States | -80.2706 | 26.27119 Decatur | Georgia | United States | -84.29631 | 33.77483 Iowa City | Iowa | United States | -91.53017 | 41.66113 New York | New York | United States | -74.00597 | 40.71427 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Portland | Oregon | United States | -122.67621 | 45.52345 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Houston | Texas | United States | -95.36327 | 29.76328
0
NCT00433147
[ 2, 3 ]
66
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
true
A major factor in the respiratory health of cystic fibrosis (CF) subjects is acquisition of chronic Pseudomonas aeruginosa infections. The infection rate with P. aeruginosa increases with age and by age 18 years, 80% of CF subjects in the U.S. are infected. Liposomal Amikacin for Inhalation (Arikace™) is a sterile aqueous liposomal suspension consisting of amikacin sulfate encapsulated in liposomes. This formulation of amikacin maximizes the achievable dose and delivery to the lungs of subjects infected via a nebulizer. Because liposome particles are small enough to penetrate and diffuse through sputum into the bacterial biofilm, they deposit drug in close proximity to the bacterial colonies, thus improving the bioavailability of amikacin at the infection site. The clinically achievable doses of amikacin in the LAI formulation can effectively increase the half-life of the drug in the lungs, and decrease the potential for systemic toxicity. LAI offers several advantages over current therapies in treating CF subjects with chronic infection caused by P. aeruginosa.
Cystic fibrosis is a genetic disease resulting from mutations in a 230 kb gene on chromosome 7 known as the cystic fibrosis transmembrane conductance regulator (CFTR). Study subjects with CF manifest pathological changes in a variety of organs that express CFTR. The lungs are frequently affected, the sequelae being chronic infections and airway inflammation. The principal goal of treatment of subjects with CF is to slow the chronic deterioration of lung function. This is a Phase 2a study of safety, and tolerability of 28 days of daily dosing of two dose (280 mg, and 560 mg) cohorts of Arikace™ versus placebo. Study subjects will be randomized to receive either study drug or placebo (1.5% NaCl) by inhalation via a PARI eFlow® nebulizer. Cohort 1 (280mg) will complete 28 days of daily dosing with Arikace™ and 14 day post dosing safety evaluation by the Safety Committee (DSMB) before initiation of enrollment in Cohort 2 (560mg). Cohort 2 will complete 28 days of daily dosing, and a 14 day post dosing safety assessment by the DSMB to evaluate safety data. All study patients will be followed for safety, pharmacokinetics, clinical, and microbiologic activity for 28 days post completion of study treatment. The total study period will be up to 56 days, with screening visit occurring within the preceding 14 days prior to randomization. Patients will be clinically evaluated during the first 48 hours post-randomization, and weekly for the 28 days treatment period, and during the follow up visits at study days 35, 42, 49, and 56 days to determine safety, tolerability, pharmacokinetics (PK), and clinical, and microbiologic activity. Clinical laboratory parameters, audiology testing, clinical adverse events, and pulmonary function will be evaluated for all study subjects in order to determine the qualitative and quantitative safety and tolerability of Arikace™ compared to Placebo. Serum, urine, and sputum specimens will be collected at periodic intervals to assess PK. Additionally; sputum samples will be collected to determine changes in bacterial density. Pulmonary function testing and CFQ-R measurements will be assessed at selected time points throughout the study. DSMB has recommended the amendment of the main study to evaluate safety and efficacy of additional cycles of treatment with Arikace™. All patients who were randomized in the main study, were compliant with the study protocol, and continue meeting study eligibility criteria can be consented to participate in the open-label extension to evaluate the safety, tolerability and efficacy of 560 mg once daily dose of Arikace™ administered for six cycles over eighteen months. Each cycle will comprise of 28 days of treatment followed by 56 days off treatment. The total extension period will be up to 518 days (74 weeks, about 18 months). Clinical laboratory parameters, audiology testing, clinical adverse events, and pulmonary function will be evaluated for all study subjects in order to determine the longer term safety, tolerability, and efficacy of Arikace™. Serum specimens will be collected at periodic intervals to assess PK for safety. Additionally, sputum samples will be collected to determine changes in bacterial density. Pulmonary function testing and CFQ-R measurements will be assessed at selected time points throughout the study. Arikace™, Arikayce™, Liposomal Amikacin for Inhalation (LAI) and Amikacin Liposome Inhalation Suspension (ALIS) are all the same may be used interchangeably throughout the study and other studies evaluating amikacin liposome inhalation suspension.
Cystic Fibrosis
Cystic Fibrosis Respiratory Infections Pulmonary Cystic Fibrosis CFTR
null
4
arm 1: Subjects in this cohort will receive 280 mg of ARIKACE™ arm 2: Subjects in this arm of cohort 1 will receive matching placebo arm 3: Subjects in this cohort will receive 560 mg of ARIKACE™ arm 4: Subjects in this arm of cohort 2 will receive matching placebo
[ 0, 2, 0, 2 ]
2
[ 0, 0 ]
intervention 1: Study start date is before Jan 18, 2017. intervention 2: Study start date is before Jan 18, 2017.
intervention 1: ARIKACE™ intervention 2: Placebo
11
Leuven | N/A | Belgium | 4.70093 | 50.87959 Budapest | N/A | Hungary | 19.04045 | 47.49835 Kaposvár | N/A | Hungary | 17.8 | 46.36667 Skopje | N/A | North Macedonia | 21.43141 | 41.99646 Rabka-Zdrój | N/A | Poland | 19.96654 | 49.60889 Warsaw | N/A | Poland | 21.01178 | 52.22977 Belgrade | N/A | Serbia | 20.46513 | 44.80401 Bratislava | N/A | Slovakia | 17.10674 | 48.14816 Košice | N/A | Slovakia | 21.25808 | 48.71395 Kharkiv | N/A | Ukraine | 36.25475 | 49.98177 Kiev | N/A | Ukraine | 30.5238 | 50.45466
0
NCT00777296
[ 3 ]
28
RANDOMIZED
CROSSOVER
0TREATMENT
2DOUBLE
false
0ALL
false
A double-blind, placebo-controlled study to evaluate changes in pain, urgency and urinary frequency following administration of URG101 compared to placebo.
null
Painful Bladder Syndrome Interstitial Cystitis Bladder Pain Syndrome
bladder pain urgency frequency
null
2
arm 1: Placebo Treatment on Visit 1 followed by URG101 Treatment on Visit 2 arm 2: URG101 Treatment on Visit 1 followed by Placebo Treatment on Visit 2
[ 5, 5 ]
2
[ 0, 0 ]
intervention 1: Bladder instillation of URG101 or Placebo in random order on treatment 1 and treatment 2 followed by an open-label URG101 on treatment 3 within the same week. intervention 2: Liquid formulation without active URG101 drug components
intervention 1: URG101 intervention 2: Placebo
6
Glendora | California | United States | -117.86534 | 34.13612 San Diego | California | United States | -117.16472 | 32.71571 San Diego | California | United States | -117.16472 | 32.71571 San Diego | California | United States | -117.16472 | 32.71571 Cartersville | Georgia | United States | -84.80231 | 34.16533 San Antonio | Texas | United States | -98.49363 | 29.42412
0
NCT00517868
[ 4 ]
524
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
null
To evaluate the safety and efficacy of MNTX in participants who have undergone segmental colectomy and to assess if the time between the end of surgery and the first bowel movement is significantly shorter in the MNTX regimen than the equivalent assessment using a placebo regimen.
null
Post-Operative Ileus (POI)
null
3
arm 1: Participants will receive methylnaltrexone (MNTX) 12 milligrams (mg) as an intravenous (IV) infusion over approximately 20 minutes for every 6 hours until one of the following occurs: 1) 24 hours elapsed after the first bowel movement and the participant was tolerating clear liquids, 2) the participant was discharged from the hospital, or 3) a maximum of 10 days elapsed. The first dose of study drug will be administered within the first 90 minutes after the end of surgery (defined as the time when the last skin suture or staple is placed in the participant). arm 2: Participants will receive MNTX 24 mg as an IV infusion over approximately 20 minutes for every 6 hours until one of the following occurs: 1) 24 hours elapsed after the first bowel movement and the participant was tolerating clear liquids, 2) the participant was discharged from the hospital, or 3) a maximum of 10 days elapsed. The first dose of study drug will be administered within the first 90 minutes after the end of surgery (defined as the time when the last skin suture or staple is placed in the participant). arm 3: Participants will receive placebo matching to MNTX as an IV infusion over approximately 20 minutes for every 6 hours until one of the following occurs: 1) 24 hours elapsed after the first bowel movement and the participant was tolerating clear liquids, 2) the participant was discharged from the hospital, or 3) a maximum of 10 days elapsed. The first dose of study drug will be administered within the first 90 minutes after the end of surgery (defined as the time when the last skin suture or staple is placed in the participant).
[ 0, 0, 2 ]
2
[ 0, 0 ]
intervention 1: Methylnaltrexone will be administered as per the dose and schedule specified in the respective arms. intervention 2: Placebo matching to methylnaltrexone will be administered as per the schedule specified in the respective arm.
intervention 1: Methylnaltrexone intervention 2: Placebo
1
Tarrytown | New York | United States | -73.85875 | 41.07621
0
NCT00401375
[ 3 ]
30
RANDOMIZED
CROSSOVER
0TREATMENT
0NONE
false
0ALL
false
In some participants with cystic fibrosis (CF), the disease is caused by a nonsense mutation (premature stop codon) in the gene that makes the cystic fibrosis transmembrane regulator (CFTR) protein. Ataluren has been shown to partially restore CFTR production in animals with CF due to a nonsense mutation. The main purpose of this study is to understand whether ataluren can safely increase functional CFTR protein in the cells of participants with CF due to a nonsense mutation.
In this study, participants with CF due to a nonsense mutation will be treated with a new investigational drug called ataluren. Evaluation procedures (history, physical examination, blood and urine tests to assess organ function, electrocardiogram \[ECG\], chest x-ray, and CF-specific tests) to determine if a participant qualifies for the study will be performed within 21 days prior to the start of treatment. Eligible participants with nonsense-mutation-mediated CF will receive 2 repeated 28-day cycles, each comprising of 14 days on therapy and 14 days off therapy. In a crossover design, participants will be randomized to receive ataluren treatment in Cycle 1 by either of the following regimens: * Ataluren, given 3 times per day (TID) with a regimen of 4 milligrams/kilograms (mg/kg) at breakfast, 4 mg/kg at lunch, and 8 mg/kg at dinner, or * Ataluren, given 3 TID with a regimen of 10 mg/kg at breakfast, 10 mg/kg at lunch and 20 mg/kg at dinner. In Cycle 2, participants will then receive the drug according to the regimen opposite from that given in Cycle 1. There will be a 2-night stay at the clinical research center at the beginning and at the end of each 14 days of ataluren treatment, which means that there will be four 2-night stays at the clinical research center during the study. During the study, ataluren efficacy, safety, and pharmacokinetics (PK) will be evaluated periodically with measurements of transepithelial potential difference (TEPD), nasal mucosal brushing to assess for cellular CFTR messenger ribonucleic acid (mRNA) and protein, medical history, physical examinations, blood tests, sputum test, urinalysis, ECGs, chest x-ray, and pulmonary function tests. The measurement of TEPD, also known as nasal potential difference, provides a sensitive evaluation of sodium and chloride transport directly in secretory epithelial cells. TEPD assessments are made on the nasal epithelium cells lining the inferior turbinate because these cells are easier to access than the respiratory epithelial cells lining the lower airways and have been shown to have the same ion transport characteristics. As an endpoint, TEPD has the advantage that it can detect chloride transport changes that are a quantitative integration of the presence, functional activity, and apical location of the CFTR in airway cells. Furthermore, it is a direct measure of CFTR activity that is not likely to be affected by supportive or palliative treatments for CF (with the possible exception of systemically administered aminoglycoside antibiotics).
Cystic Fibrosis
Cystic fibrosis Nonsense mutation Premature stop codon
null
2
arm 1: During Cycle 1, participants will receive ataluren at 4 mg/kg in the morning, 4 mg/kg at midday, and 8 mg/kg in the evening for 14 days, followed by a 14-day follow-up period without treatment. Then, the participants will crossover to the other ataluren dose regimen (ataluren 10, 10, and 20 mg/kg) for Cycle 2. arm 2: During Cycle 1, participants will receive ataluren at 10 mg/kg in the morning, 10 mg/kg at midday, and 20 mg/kg in the evening for 14 days, followed by a 14-day follow-up period without treatment. Then, the participants will crossover to the other ataluren dose regimen (ataluren 4, 4, and 8 mg/kg) for Cycle 2.
[ 0, 0 ]
1
[ 0 ]
intervention 1: Ataluren will be provided as a vanilla-flavored powder to be mixed with water, milk, or apple juice. Participants are to receive a total of 42 doses of ataluren during each cycle, for a total of 84 doses of ataluren in both cycles.
intervention 1: Ataluren
3
Brussels | N/A | Belgium | 4.34878 | 50.85045 Leuven | N/A | Belgium | 4.70093 | 50.87959 Paris | N/A | France | 2.3488 | 48.85341
0
NCT00458341
[ 4 ]
752
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
1FEMALE
true
The purpose of this clinical research study is to learn if BMS-247550 added to the approved therapy of capecitabine is better than capecitabine alone in shrinking or slowing the growth of the cancer in women with metastatic breast cancer who are resistant to taxane and received anthracycline chemotherapy. The safety of this treatment will also be studied.
null
Breast Cancer Metastases
Metastatic Breast Cancer
null
2
arm 1: None arm 2: None
[ 0, 1 ]
2
[ 0, 0 ]
intervention 1: Ixabepilone - Intravenous Solution, IV 40mg/m², Day 1 every 21 days, Until progression/unacceptable toxicity Capecitabine (Active Comparator) - Tablet, Oral, 2000 mg/m², Bid Days 1-14 every 21 days, Until progression/unacceptable toxicity intervention 2: Tablet, Oral, 2500 mg/m², Bid Days 1-14 every 21 days, Until progression/unacceptable toxicity
intervention 1: Ixabepilone + Capecitabine intervention 2: Capecitabine
127
Little Rock | Arkansas | United States | -92.28959 | 34.74648 San Francisco | California | United States | -122.41942 | 37.77493 Vallejo | California | United States | -122.25664 | 38.10409 Denver | Colorado | United States | -104.9847 | 39.73915 Hartford | Connecticut | United States | -72.68509 | 41.76371 Washington D.C. | District of Columbia | United States | -77.03637 | 38.89511 Orlando | Florida | United States | -81.37924 | 28.53834 Baltimore | Maryland | United States | -76.61219 | 39.29038 Burlington | Massachusetts | United States | -71.19561 | 42.50482 Jackson | Mississippi | United States | -90.18481 | 32.29876 Columbia | Missouri | United States | -92.33407 | 38.95171 Kansas City | Missouri | United States | -94.57857 | 39.09973 St Louis | Missouri | United States | -90.19789 | 38.62727 Omaha | Nebraska | United States | -95.94043 | 41.25626 Livingston | New Jersey | United States | -74.31487 | 40.79593 New Brunswick | New Jersey | United States | -74.45182 | 40.48622 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 New York | New York | United States | -74.00597 | 40.71427 Columbus | Ohio | United States | -82.99879 | 39.96118 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Tulsa | Oklahoma | United States | -95.99277 | 36.15398 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Columbia | South Carolina | United States | -81.03481 | 34.00071 Greenville | South Carolina | United States | -82.39401 | 34.85262 Knoxville | Tennessee | United States | -83.92074 | 35.96064 Nashville | Tennessee | United States | -86.78444 | 36.16589 Austin | Texas | United States | -97.74306 | 30.26715 Houston | Texas | United States | -95.36327 | 29.76328 Ogden | Utah | United States | -111.97383 | 41.223 Burlington | Vermont | United States | -73.21207 | 44.47588 Tacoma | Washington | United States | -122.44429 | 47.25288 Morgantown | West Virginia | United States | -79.9559 | 39.62953 Capital Federal | Buenos Aires | Argentina | N/A | N/A Haedo | Buenos Aires | Argentina | -58.59212 | -34.64239 La Plata | Buenos Aires | Argentina | -57.95442 | -34.92126 Mar del Plata | Buenos Aires | Argentina | -57.5562 | -38.00042 Pilar | Buenos Aires | Argentina | -58.91398 | -34.45867 Quilmes | Buenos Aires | Argentina | -58.25454 | -34.72065 Lanús | BuenosAires | Argentina | -58.39132 | -34.70757 Rosario | Santa Fe Province | Argentina | -60.63932 | -32.94682 Córdoba | N/A | Argentina | -64.18853 | -31.40648 Neuquén | N/A | Argentina | -68.0592 | -38.95078 Santa Fe | N/A | Argentina | -60.70868 | -31.64881 Edegem | N/A | Belgium | 4.44504 | 51.15662 Ghent | N/A | Belgium | 3.71667 | 51.05 Leuven | N/A | Belgium | 4.70093 | 50.87959 Liège | N/A | Belgium | 5.56749 | 50.63373 Fortaleza | Ceará | Brazil | -38.54306 | -3.71722 Belo Horizonte | Mina Gerais | Brazil | -43.93778 | -19.92083 Curitiba | Paraná | Brazil | -49.27306 | -25.42778 Porto Alegre | Rio Grande do Sul | Brazil | -51.23019 | -30.03283 Jaú | São Paulo | Brazil | -48.55778 | -22.29639 Santo André | São Paulo | Brazil | -46.53833 | -23.66389 Sao Paulo - Sp | São Paulo | Brazil | N/A | N/A São Paulo | N/A | Brazil | -46.63611 | -23.5475 Vancouver | British Columbia | Canada | -123.11934 | 49.24966 Oshawa | Ontario | Canada | -78.84957 | 43.90012 Toronto | Ontario | Canada | -79.39864 | 43.70643 Montreal | Quebec | Canada | -73.58781 | 45.50884 Beijing | Beijing Municipality | China | 116.39723 | 39.9075 Guangzhou | Guangdong | China | 113.25 | 23.11667 Nanjing | Jiangsu | China | 118.77778 | 32.06167 Jinan | Shandong | China | 116.99722 | 36.66833 Beijing | Shanghai Municipality | China | N/A | N/A Xi’an | Shanxi | China | 113.52486 | 35.99785 Beijing | N/A | China | 116.39723 | 39.9075 Shanghai | N/A | China | 121.45806 | 31.22222 Angers | N/A | France | -0.55202 | 47.47156 Avignon | N/A | France | 4.80892 | 43.94834 Bayonne | N/A | France | -1.473 | 43.49316 Besançon | N/A | France | 6.01815 | 47.24878 Bobigny | N/A | France | 2.45012 | 48.90982 Bordeaux | N/A | France | -0.5805 | 44.84044 Clermont-Ferrand | N/A | France | 3.08682 | 45.77969 Lyon | N/A | France | 4.84671 | 45.74846 Nantes | N/A | France | -1.55336 | 47.21725 Nice | N/A | France | 7.26608 | 43.70313 Saint-Brieuc | N/A | France | -2.76838 | 48.51513 Saint-Cloud | N/A | France | 2.20289 | 48.84598 Saint-Herblain | N/A | France | -1.651 | 47.21154 Strasbourg | N/A | France | 7.74553 | 48.58392 Toulouse | N/A | France | 1.44367 | 43.60426 Berlin | N/A | Germany | 13.41053 | 52.52437 Duisburg | N/A | Germany | 6.76516 | 51.43247 Erlangen | N/A | Germany | 11.00783 | 49.59099 Athens | N/A | Greece | 23.72784 | 37.98376 Thessaloniki | N/A | Greece | 22.93086 | 40.64361 Budapest | N/A | Hungary | 19.04045 | 47.49835 Debrecen | N/A | Hungary | 21.62444 | 47.53167 Győr | N/A | Hungary | 17.63512 | 47.68333 Pécs | N/A | Hungary | 18.23083 | 46.0725 Brescia | N/A | Italy | 10.21472 | 45.53558 Candiolo (To) | N/A | Italy | 7.59812 | 44.95858 Forlì | N/A | Italy | 12.04144 | 44.22177 San Giovanni Rotondo | N/A | Italy | 15.7277 | 41.70643 Kampung Baharu Nilai | Negeri Sembilan | Malaysia | 101.7972 | 2.8033 Kuala Lumpur | N/A | Malaysia | 101.68653 | 3.1412 Acapulco de Juárez | Guerrero | Mexico | -99.90891 | 16.84942 Mérida | Yucatán | Mexico | -89.62318 | 20.967 Chihuahua City | N/A | Mexico | -106.08889 | 28.63528 Distrito Federal | N/A | Mexico | -93.02694 | 16.59 San Luis Potosí City | N/A | Mexico | -100.97135 | 22.15234 Lima | N/A | Peru | -77.02824 | -12.04318 Manila | N/A | Philippines | 120.9822 | 14.6042 Quezon | N/A | Philippines | 125.09889 | 7.73028 Quezon City | N/A | Philippines | 121.0509 | 14.6488 Gdansk | N/A | Poland | 18.64912 | 54.35227 Opole | N/A | Poland | 17.92533 | 50.67211 Incheon | N/A | South Korea | 126.70515 | 37.45646 Seoul | N/A | South Korea | 126.9784 | 37.566 Barcelona | N/A | Spain | 2.15899 | 41.38879 Girona | N/A | Spain | 2.82493 | 41.98311 Madrid | N/A | Spain | -3.70256 | 40.4165 Valencia | N/A | Spain | -0.37966 | 39.47391 Zaragoza | N/A | Spain | -0.87734 | 41.65606 Gothenburg | N/A | Sweden | 11.96679 | 57.70716 Stockholm | N/A | Sweden | 18.06871 | 59.32938 Tainan City | N/A | Taiwan | 120.21333 | 22.99083 Taipei | N/A | Taiwan | 121.52639 | 25.05306 Bangkok | N/A | Thailand | 100.50144 | 13.75398 Bristol | Avon | United Kingdom | -2.59665 | 51.45523 Chelmsford | Essex | United Kingdom | 0.46958 | 51.73575 London | Greater London | United Kingdom | -0.12574 | 51.50853 Manchester | Greater Manchester | United Kingdom | -2.23743 | 53.48095 Sheffield | South Yorkshire | United Kingdom | -1.4659 | 53.38297 Guildford | Surrey | United Kingdom | -0.57427 | 51.23536 Newcastle upon Tyne | Tyne and Wear | United Kingdom | -1.61396 | 54.97328
1
NCT00080301
[ 4 ]
1,221
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
1FEMALE
true
The purpose of this clinical research study is to learn if BMS-247550 added to the approved therapy of capecitabine (Xeloda) provides measurable clinical benefits over capecitabine alone in women with metastatic breast cancer. Patients should have previously received an anthracycline and a taxane. The safety of this treatment will also be studied.
null
Cancer Breast Cancer
null
2
arm 1: None arm 2: None
[ 0, 1 ]
2
[ 0, 0 ]
intervention 1: Ixabepilone lypholized powder/Diluent for solution for injection/Tablets, IV/Oral, 40 mg/m2 + Capecitabine 2000 mg/m2, Ixabepilone on Day 1 and Capecitabine twice daily Days 1-14 of 21 day cycle intervention 2: Tablet, Oral, 2500 mg/m2, Capecitabine twice daily Days 1-14 of 21 day cycle
intervention 1: Ixabepilone + Capecitabine intervention 2: Capecitabine
186
Tucson | Arizona | United States | -110.92648 | 32.22174 Beverly Hills | California | United States | -118.40036 | 34.07362 Corona | California | United States | -117.56644 | 33.87529 Hartford | Connecticut | United States | -72.68509 | 41.76371 Plantation | Florida | United States | -80.23184 | 26.13421 Boise | Idaho | United States | -116.20345 | 43.6135 Evanston | Illinois | United States | -87.69006 | 42.04114 Iowa City | Iowa | United States | -91.53017 | 41.66113 Louisville | Kentucky | United States | -85.75941 | 38.25424 Baton Rouge | Louisiana | United States | -91.18747 | 30.44332 Bethesda | Maryland | United States | -77.10026 | 38.98067 Boston | Massachusetts | United States | -71.05977 | 42.35843 Jackson | Mississippi | United States | -90.18481 | 32.29876 Columbia | Missouri | United States | -92.33407 | 38.95171 Voorhees Township | New Jersey | United States | -74.49062 | 40.4795 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 Latham | New York | United States | -73.75901 | 42.74702 Mineola | New York | United States | -73.64068 | 40.74927 New York | New York | United States | -74.00597 | 40.71427 The Bronx | New York | United States | -73.86641 | 40.84985 Durham | North Carolina | United States | -78.89862 | 35.99403 Goldsboro | North Carolina | United States | -77.99277 | 35.38488 Hickory | North Carolina | United States | -81.3412 | 35.73319 Kinston | North Carolina | United States | -77.58164 | 35.26266 Canton | Ohio | United States | -81.37845 | 40.79895 Columbus | Ohio | United States | -82.99879 | 39.96118 Langhorne | Pennsylvania | United States | -74.92267 | 40.17455 Knoxville | Tennessee | United States | -83.92074 | 35.96064 Memphis | Tennessee | United States | -90.04898 | 35.14953 Dallas | Texas | United States | -96.80667 | 32.78306 Charlottesville | Virginia | United States | -78.47668 | 38.02931 Norfolk | Virginia | United States | -76.28522 | 36.84681 Richmond | Virginia | United States | -77.46026 | 37.55376 Marshfield | Wisconsin | United States | -90.1718 | 44.66885 Avellaneda | Buenos Aires | Argentina | -58.36744 | -34.66018 Bahía Blanca | Buenos Aires | Argentina | -62.26545 | -38.7176 Belén de Escobar | Buenos Aires | Argentina | -58.79442 | -34.34602 Ciudad Autonoma de Buenos Aires | Buenos Aires | Argentina | N/A | N/A Resistencia | Chaco Province | Argentina | -58.98665 | -27.46363 Barrio Alto Verde | Córdoba Province | Argentina | N/A | N/A San Miguel de Tucumán | Tucumán Province | Argentina | -65.21051 | -26.81601 Buenos Aires | N/A | Argentina | -58.37723 | -34.61315 Mendoza | N/A | Argentina | -68.84582 | -32.88946 Salta | N/A | Argentina | -65.41999 | -24.80645 Santa Fe | N/A | Argentina | -60.70868 | -31.64881 Sydney | New South Wales | Australia | 151.20732 | -33.86785 Westmead | New South Wales | Australia | 150.98768 | -33.80383 Brisbane | Queensland | Australia | 153.02809 | -27.46794 Herston | Queensland | Australia | 153.01852 | -27.44453 South Brisbane | Queensland | Australia | 153.02049 | -27.48034 Toowoomba | Queensland | Australia | 151.95386 | -27.56056 Adelaide | South Australia | Australia | 138.59863 | -34.92866 Woodville | South Australia | Australia | 138.54291 | -34.877 East Melbourne | Victoria | Australia | 144.9879 | -37.81667 Parkville | Victoria | Australia | 144.95 | -37.78333 Perth | Western Australia | Australia | 115.8614 | -31.95224 Graz | N/A | Austria | 15.45 | 47.06667 Vienna | N/A | Austria | 16.37208 | 48.20849 Vöcklabruck | N/A | Austria | 13.65652 | 48.00279 Brussels | N/A | Belgium | 4.34878 | 50.85045 Charleroi | N/A | Belgium | 4.44448 | 50.41136 Ghent | N/A | Belgium | 3.71667 | 51.05 Hasselt | N/A | Belgium | 5.33781 | 50.93106 Kortrijk | N/A | Belgium | 3.26487 | 50.82803 Wilrijk | N/A | Belgium | 4.39513 | 51.16734 Centro-Porto Alegre | Rio Grande do Sul | Brazil | N/A | N/A Bela Vista | São Paulo | Brazil | -46.64758 | -23.56086 Higienopolis | São Paulo | Brazil | N/A | N/A São Paulo | São Paulo | Brazil | -46.63611 | -23.5475 Rio de Janeiro | N/A | Brazil | -43.18223 | -22.90642 Thunder Bay | Ontario | Canada | -89.25018 | 48.38202 Montreal | Quebec | Canada | -73.58781 | 45.50884 Santiago | Santiago Metropolitan | Chile | -70.64827 | -33.45694 Beijing | Beijing Municipality | China | 116.39723 | 39.9075 Guangzhou | Guangdong | China | 113.25 | 23.11667 Nanjing | Jiangsu | China | 118.77778 | 32.06167 Dalian | Liaoning | China | 121.60222 | 38.91222 Dilian | Liaoning | China | N/A | N/A Jinan | Shandong | China | 116.99722 | 36.66833 Shanghai | Shanghai Municipality | China | 121.45806 | 31.22222 Xi’an | Shanxi | China | 113.52486 | 35.99785 Hangzhou | Zhejiang | China | 120.16142 | 30.29365 Split | N/A | Croatia | 16.43915 | 43.50891 Zagreb | N/A | Croatia | 15.97798 | 45.81444 Brno | N/A | Czechia | 16.60796 | 49.19522 Hradec Králové | N/A | Czechia | 15.83277 | 50.20923 Prague | N/A | Czechia | 14.42076 | 50.08804 Aalborg | N/A | Denmark | 9.9187 | 57.048 Herlev | N/A | Denmark | 12.43998 | 55.72366 København Ø | N/A | Denmark | 12.56862 | 55.70968 Angers | N/A | France | -0.55202 | 47.47156 Bordeaux | N/A | France | -0.5805 | 44.84044 Caen | N/A | France | -0.35912 | 49.18585 Clermont-Ferrand | N/A | France | 3.08682 | 45.77969 Colmar | N/A | France | 7.35584 | 48.08078 Le Mans | N/A | France | 0.20251 | 48.0021 Metz | N/A | France | 6.17269 | 49.11911 Paris | N/A | France | 2.3488 | 48.85341 Pierre-Bénite | N/A | France | 4.82424 | 45.70359 Reims | N/A | France | 4.02853 | 49.26526 Saint-Brieuc | N/A | France | -2.76838 | 48.51513 Saint-Grégoire | N/A | France | -1.68579 | 48.15101 Saint-Herblain | N/A | France | -1.651 | 47.21154 Tours | N/A | France | 0.70398 | 47.39484 Villejuif | N/A | France | 2.35992 | 48.7939 Berlin | N/A | Germany | 13.41053 | 52.52437 Erlangen | N/A | Germany | 11.00783 | 49.59099 Essen | N/A | Germany | 7.01228 | 51.45657 Hanover | N/A | Germany | 9.73322 | 52.37052 Karlsruhe | N/A | Germany | 8.40444 | 49.00937 Kiel | N/A | Germany | 10.13489 | 54.32133 Marburg | N/A | Germany | 8.77069 | 50.80904 München | N/A | Germany | 13.31243 | 51.60698 Rehling | N/A | Germany | 10.93333 | 48.48333 Saarbrücken | N/A | Germany | 7.00982 | 49.23262 Tübingen | N/A | Germany | 9.05222 | 48.52266 Ulm | N/A | Germany | 9.99155 | 48.39841 Wiesbaden | N/A | Germany | 8.24932 | 50.08258 Athens | N/A | Greece | 23.72784 | 37.98376 Crete | N/A | Greece | N/A | N/A Pátrai | N/A | Greece | 21.73444 | 38.24444 Thessaloniki | N/A | Greece | 22.93086 | 40.64361 Wilton | Cork | Ireland | N/A | N/A Cork | N/A | Ireland | -8.47061 | 51.89797 Dublin | N/A | Ireland | -6.24889 | 53.33306 Galway | N/A | Ireland | -9.05095 | 53.27245 Haifa | N/A | Israel | 34.99928 | 32.81303 Jerusalem | N/A | Israel | 35.21633 | 31.76904 Ramat Gan | N/A | Israel | 34.81065 | 32.08227 Tel Aviv | N/A | Israel | 34.78057 | 32.08088 Rozzano | Milan | Italy | 9.1559 | 45.38193 Bari | N/A | Italy | 16.86982 | 41.12066 Florence | N/A | Italy | 11.24626 | 43.77925 Genova | N/A | Italy | 11.87211 | 45.21604 Milan | N/A | Italy | 12.59836 | 42.78235 Modena | N/A | Italy | 10.92539 | 44.64783 Perugia | N/A | Italy | 12.38878 | 43.1122 Potenza | N/A | Italy | 15.80794 | 40.64175 Roma | N/A | Italy | 11.10642 | 44.99364 San Giovanni Rotondo | N/A | Italy | 15.7277 | 41.70643 Sora | N/A | Italy | 13.61356 | 41.71829 Torino | N/A | Italy | 11.99138 | 44.88856 Arnhem | N/A | Netherlands | 5.91111 | 51.98 Enschede | N/A | Netherlands | 6.89583 | 52.21833 The Hague | N/A | Netherlands | 4.29861 | 52.07667 Zwolle | N/A | Netherlands | 6.09444 | 52.5125 Coimbra | N/A | Portugal | -8.41955 | 40.20564 Lisbon | N/A | Portugal | -9.1498 | 38.72509 Kazan' | N/A | Russia | 49.12214 | 55.78874 Moscow | N/A | Russia | 37.61556 | 55.75222 Saint Petersburg | N/A | Russia | 30.31413 | 59.93863 Singapore | N/A | Singapore | 103.85007 | 1.28967 Port Elizabeth | Eastern Cape | South Africa | 25.61494 | -33.96109 Johannesburg | Gauteng | South Africa | 28.04363 | -26.20227 Pretoria | Gauteng | South Africa | 28.18783 | -25.74486 Panorama | Western Cape | South Africa | N/A | N/A Gyeonggi-do | N/A | South Korea | 126.76917 | 37.58944 Incheon | N/A | South Korea | 126.70515 | 37.45646 Seoul | N/A | South Korea | 126.9784 | 37.566 Terassa | Barcelona | Spain | N/A | N/A Barcelona | N/A | Spain | 2.15899 | 41.38879 Cadiz | N/A | Spain | -6.2891 | 36.52672 Córdoba | N/A | Spain | -4.77275 | 37.89155 Elche (Alicante) | N/A | Spain | -0.70107 | 38.26218 Jaén | N/A | Spain | -3.79028 | 37.76922 L'Hospitalet de Llobregat | N/A | Spain | 2.10028 | 41.35967 Madrid | N/A | Spain | -3.70256 | 40.4165 Pontevedra | N/A | Spain | -8.64435 | 42.431 Reus | N/A | Spain | 1.10687 | 41.15612 Salamanca | N/A | Spain | -3.67975 | 40.42972 Santa Cruz de Tenerife | N/A | Spain | -16.25462 | 28.46824 Seville | N/A | Spain | -5.97317 | 37.38283 Valencia | N/A | Spain | -0.37966 | 39.47391 Zaragoza | N/A | Spain | -0.87734 | 41.65606 Bern | N/A | Switzerland | 7.44744 | 46.94809 Thun | N/A | Switzerland | 7.62166 | 46.75118 Zurich | N/A | Switzerland | 8.55 | 47.36667 Taipei | N/A | Taiwan | 121.52639 | 25.05306 Ankara | N/A | Turkey (Türkiye) | 32.85427 | 39.91987 Istanbul | N/A | Turkey (Türkiye) | 28.94966 | 41.01384 Izmir | N/A | Turkey (Türkiye) | 27.13838 | 38.41273 Belfast | Armagh | United Kingdom | -5.92541 | 54.59682 Glasgow | Central | United Kingdom | -4.25763 | 55.86515 London | Greater London | United Kingdom | -0.12574 | 51.50853 Shrewsbury | Shropshire | United Kingdom | -2.75208 | 52.71009 Birmingham | West Midlands | United Kingdom | -1.89983 | 52.48142
1
NCT00082433
[ 4 ]
200
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
true
The purpose of this study is to compare the safety and efficacy of XERECEPT® to dexamethasone (Decadron) a common treatment for symptoms of brain swelling (edema). This study is specifically aimed at patients who require chronic high doses of dexamethasone to manage symptoms.
XERECEPT® is not a potential treatment for cancer, but may reduce the edema associated with tumors and as a result, decrease neurological symptoms.
Brain Edema Brain Tumor
peritumoral brain edema edema malignant brain tumor astrocytoma brain tumor dexamethasone Decadron
null
2
arm 1: Patients will take hCRF (XERECEPT) 2mg/day and open label-dexamethasone they are currently taking. arm 2: Patient will receive placebo hCRF and any open-label dexamethasone that they are currently taking
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: hCRF ; open-label dexamethasone that the patient is currently taking intervention 2: placebo hCRF 2mg/day and open-label dexamethasone that they are taking
intervention 1: hCRF intervention 2: placebo hCRF
34
Phoenix | Arizona | United States | -112.07404 | 33.44838 Fresno | California | United States | -119.77237 | 36.74773 Newport Beach | California | United States | -117.92895 | 33.61891 Palo Alto | California | United States | -122.14302 | 37.44188 Sacramento | California | United States | -121.4944 | 38.58157 San Diego | California | United States | -117.16472 | 32.71571 Aurora | Colorado | United States | -104.83192 | 39.72943 Englewood | Colorado | United States | -104.98776 | 39.64777 Jacksonville | Florida | United States | -81.65565 | 30.33218 Orlando | Florida | United States | -81.37924 | 28.53834 Tampa | Florida | United States | -82.45843 | 27.94752 Atlanta | Georgia | United States | -84.38798 | 33.749 Chicago | Illinois | United States | -87.65005 | 41.85003 Evanston | Illinois | United States | -87.69006 | 42.04114 Boston | Massachusetts | United States | -71.05977 | 42.35843 Detroit | Michigan | United States | -83.04575 | 42.33143 Ridgewood | New Jersey | United States | -74.11653 | 40.97926 Amherst | New York | United States | -78.79976 | 42.97839 New York | New York | United States | -74.00597 | 40.71427 New York | New York | United States | -74.00597 | 40.71427 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Columbus | Ohio | United States | -82.99879 | 39.96118 Portland | Oregon | United States | -122.67621 | 45.52345 Seattle | Washington | United States | -122.33207 | 47.60621 Madison | Wisconsin | United States | -89.40123 | 43.07305 Milwaukee | Wisconsin | United States | -87.90647 | 43.0389 Edmonton | Alberta | Canada | -113.46871 | 53.55014 Winnipeg | Manitoba | Canada | -97.14704 | 49.8844 Moncton | New Brunswick | Canada | -64.7965 | 46.09454 Halifax | Nova Scotia | Canada | -63.57688 | 44.64269 Kingston | Ontario | Canada | -76.48098 | 44.22976 Ottawa | Ontario | Canada | -75.69812 | 45.41117 Toronto | Ontario | Canada | -79.39864 | 43.70643
1
NCT00088166
[ 3 ]
61
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
The purpose of this study is to test whether sunitinib (SU011248) has activity and is safe in patients with renal cell carcinoma (RCC) who have failed prior therapy with bevacizumab (Avastin) -based treatment.
null
Carcinoma, Renal Cell
null
1
arm 1: None
[ 0 ]
1
[ 0 ]
intervention 1: 50 mg orally daily for 4 weeks followed by 2 weeks off treatment for approximately 1 year or until disease progression/unacceptable toxicity; after completion of 1 year, pts with clinical benefit can continue the study treatment in a separate continuation protocol
intervention 1: Sunitinib
11
Duarte | California | United States | -117.97729 | 34.13945 Pasadena | California | United States | -118.14452 | 34.14778 San Francisco | California | United States | -122.41942 | 37.77493 Chicago | Illinois | United States | -87.65005 | 41.85003 Boston | Massachusetts | United States | -71.05977 | 42.35843 Boston | Massachusetts | United States | -71.05977 | 42.35843 Boston | Massachusetts | United States | -71.05977 | 42.35843 Durham | North Carolina | United States | -78.89862 | 35.99403 Cleveland | Ohio | United States | -81.69541 | 41.4995 Nashville | Tennessee | United States | -86.78444 | 36.16589 Dallas | Texas | United States | -96.80667 | 32.78306
1
NCT00089648
[ 4 ]
4,628
RANDOMIZED
PARALLEL
1PREVENTION
2DOUBLE
false
0ALL
true
To assess the efficacy of dronedarone in preventing cardiovascular hospitalization or death from any cause in a population of high-risk patients with atrial fibrillation/atrial flutter (AF/AFL). To assess that dronedarone is well tolerated in this population.
This is a prospective, multinational, double-blind, randomized, multi-center, placebo-controlled, parallel-group trial evaluating the effects of dronedarone versus placebo (ratio 1:1) over a minimum treatment duration of 12 months and a mean follow-up duration of 1.75 years (in AF/AFL patients). Patients can be included in the study while in atrial fibrillation/flutter or in sinus rhythm if conversion has occurred either spontaneously or following a procedure such as electrical cardioversion (or overdrive pacing) or administration of an antiarrhythmic drug.After randomization all patients will be followed until the common study end date; the last patient included in the study will be followed for 1 year. Visits will be at baseline, after 7 days, after 14 days, after one month, after three months and then every three months until end of the study. At each visit patients will be asked for the occurrence of hospitalizations or other events since the last visit. The study will be monitored by an independent Data Monitoring Committee (DMC) for safety, tolerability and efficacy.
Atrial Fibrillation Atrial Flutter
Mortality, Hospitalization
null
2
arm 1: Dronedarone 400mg tablets twice daily (bid) arm 2: matching placebo tablets
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: oral administration (tablets) intervention 2: oral administration (tablets)
intervention 1: dronedarone (SR33589) intervention 2: placebo
37
Bridgewater | New Jersey | United States | -74.64815 | 40.60079 Buenos Aires | N/A | Argentina | -58.37723 | -34.61315 New South Wales | N/A | Australia | N/A | N/A Vienna | N/A | Austria | 16.37208 | 48.20849 Diegem | N/A | Belgium | 4.43354 | 50.89727 Laval | N/A | Canada | -73.692 | 45.56995 Santiago | N/A | Chile | -70.64827 | -33.45694 Shangaï | N/A | China | N/A | N/A Prague | N/A | Czechia | 14.42076 | 50.08804 Helsinki | N/A | Finland | 24.93545 | 60.16952 Berlin | N/A | Germany | 13.41053 | 52.52437 Athens | N/A | Greece | 23.72784 | 37.98376 Causeway Bay | N/A | Hong Kong | 114.18515 | 22.28189 Budapest | N/A | Hungary | 19.04045 | 47.49835 Mumbai | N/A | India | 72.88261 | 19.07283 Netanya | N/A | Israel | 34.85992 | 32.33291 Milan | N/A | Italy | 12.59836 | 42.78235 Kuala Lumpur | N/A | Malaysia | 101.68653 | 3.1412 Mexico | N/A | Mexico | -98.43784 | 18.88011 Casablanca | N/A | Morocco | -7.61138 | 33.58831 Gouda | N/A | Netherlands | 4.70833 | 52.01667 Macquarie Park | N/A | New Zealand | N/A | N/A Lysaker | N/A | Norway | 10.63545 | 59.90994 Makati City | N/A | Philippines | 121.03269 | 14.55027 Warsaw | N/A | Poland | 21.01178 | 52.22977 Porto Salvo | N/A | Portugal | -9.30473 | 38.72293 Moscow | N/A | Russia | 37.61556 | 55.75222 Singapore | N/A | Singapore | 103.85007 | 1.28967 Midrand | N/A | South Africa | 28.118 | -25.976 Seoul | N/A | South Korea | 126.9784 | 37.566 Barcelona | N/A | Spain | 2.15899 | 41.38879 Bromma | N/A | Sweden | 17.94 | 59.34 Taipei | N/A | Taiwan | 121.52639 | 25.05306 Bangkok | N/A | Thailand | 100.50144 | 13.75398 Mégrine | N/A | Tunisia | 10.23639 | 36.76917 Istanbul | N/A | Turkey (Türkiye) | 28.94966 | 41.01384 Guildford Surrey | N/A | United Kingdom | N/A | N/A
1
NCT00174785
[ 3 ]
69
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
The purpose of the study is to determine if treatment of older patients indicated with untreated Acute Myeloid Leukemia (AML) who are not considered to be suitable for intensive chemotherapy, can effectively be treated with Clofarabine.
Note: This clinical trial was conducted by Bioenvision Ltd. Bioenvision Ltd. was acquired by Genzyme Corporation Oct 2007.
Acute Myeloid Leukemia
acute myelogenous leukemia acute myeloid leukemia clolar evoltra clofarabine untreated acute leukemia adult acute leukemia
null
1
arm 1: Clofarabine 30 mg/m\^2/day intravenously over 1 hour for 5 days every 28 to 42 days (one cycle), then 20mg/m\^2/day intravenously over 1 hour for 5 days every 29 to 43 days for the second and subsequent cycles, up to a maximum of 3 cycles.
[ 0 ]
1
[ 0 ]
intervention 1: None
intervention 1: clofarabine
15
Dublin | N/A | Ireland | -6.24889 | 53.33306 Bologna | N/A | Italy | 11.33875 | 44.49381 Rome | N/A | Italy | 12.51133 | 41.89193 Belfast | Northern Ireland | United Kingdom | -5.92541 | 54.59682 Aberdeen | N/A | United Kingdom | -2.09814 | 57.14369 Birmingham | N/A | United Kingdom | -1.89983 | 52.48142 Cardiff | N/A | United Kingdom | -3.18 | 51.48 Edinburgh | N/A | United Kingdom | -3.19648 | 55.95206 Leicester | N/A | United Kingdom | -1.13169 | 52.6386 Liverpool | N/A | United Kingdom | -2.97794 | 53.41058 London | N/A | United Kingdom | -0.12574 | 51.50853 Manchester | N/A | United Kingdom | -2.23743 | 53.48095 Nottingham | N/A | United Kingdom | -1.15047 | 52.9536 Somerset | N/A | United Kingdom | N/A | N/A Taunton | N/A | United Kingdom | -3.10293 | 51.01494
1
NCT00924443
[ 3 ]
42
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
true
This study will determine the safety and effectiveness of a combination of the immune-suppressing drugs antithymocyte globulin (ATG) and cyclosporine for treating myelodysplasia, a disorder of low blood cell counts. It will: evaluate whether this drug combination can increase blood counts in patients and reduce their need for transfusions; compare survival of patients who respond to ATG and cyclosporine treatment with those who do not respond; and determine the side effects of the treatment. Myelodysplasia is thought to result from an immune system abnormality in which cells called lymphocytes attack the marrow's blood-forming cells. The resulting deficiencies of platelets and red and white blood cells cause anemia, susceptibility to infections, and easy bruising and bleeding. Various therapies, such as blood transfusions for anemia and bleeding, antibiotics for infection, chemotherapy and bone marrow transplantation are used to treat myelodysplasia, but all have disadvantages and some carry serious risks. Patients 18 years of age and older with myelodysplasia may be eligible for this study. Candidates will be screened with a physical examination and medical history, blood tests, chest X-ray, electrocardiogram and bone marrow biopsy (removal of a marrow sample from the hipbone for microscopic examination).
Participants will be admitted to the NIH Clinical Center for the first 10 to 14 days of treatment and will then continue therapy on an outpatient basis. They will undergo the following tests and procedures: * Placement of central line-An intravenous (IV) catheter (flexible tube inserted into a vein) is placed in a large vein of the neck, chest or arm. Medicines are delivered through this line and blood samples are drawn from it. * ATG skin testing- ATG is injected under the skin to check for sensitization to horse serum, from which the drug is derived. * ATG treatment-Four doses of ATG are given through the IV line on each of 4 consecutive days. Prednisone is taken by mouth beginning the first day of ATG therapy and continuing for a total of 17 days. This drug is given to reduce the side effects of ATG, such as fever, skin rash and chills. * Cyclosporine treatment- Cyclosporine capsules are taken by mouth twice a day for at least 6 months. During hospitalization, blood will be drawn daily for blood counts and other tests. Upon the patient's discharge after 10 days, the referring physician will do blood tests weekly during the first month of treatment and then every 2 weeks for the rest of the time the patient is taking cyclosporine. Dosages of this drug may be adjusted depending on the test results. Patients will be evaluated at the NIH Clinical Center at 3-month intervals for the first year, then every 6 months for the next 3 years and then at yearly intervals. A blood sample will be drawn at each visit. Bone marrow biopsies will be done at 6-month intervals for the first 3 years after treatment. A growing body of laboratory and clinical evidence suggests that the cytopenia of MDS is at least partly a result of cytotoxic T cell activity. Treatments to abrogate T cell activity such as anti-thymocyte globulin alone and cyclosporine alone have demonstrated varying degrees of success in alleviating the cytopenia of MDS. A response to such therapy in MDS is associated with improved survival. Experience with aplastic anemia suggests that the combination of these two agents should be more effective in suppressing cytotoxic T cell activity and alleviating cytopenia. This protocol proposes using the combination of antithymocyte globulin (ATG) and cyclosporine (CSA) to treat the cytopenia of MDS, in an effort to improve the response rate to immunosuppressive therapy in this disease.
Myelodysplastic Syndrome
MDS Immunosuppression ATG Cyclosporine Myelodysplastic Syndrome
null
1
arm 1: Myelodysplastic syndromes (MDS) subjects will be treated with Anti-thymocyte Globulin (ATG) and cyclosporine (CsA). The subjects will receive ATG at a dose of 40mg/kg orally on days 1-4 in combination with oral prednisone at a dose of 1mg/kg/day on day one. The prednisone will be tapered on day 10. The taper schedule will be every two days over a total of eight days (days 10-17). Drug the ATG administration the subjects will receive at least 4 units of platelets daily for platelet counts less than 20,000/ microliters. Cyclosporine (CsA) will be started on day 14 at a dose of 5mg/kg twice daily with dose adjustments based on drug levels (target 200-400 ng/ml). Cyclosporine therapy will be continued for six months.
[ 0 ]
2
[ 0, 0 ]
intervention 1: Antithymocyte globulin (ATG) intravenous infusion: 40mg/kg/day. Infusion over 6 hours on day 1-4. intervention 2: Cyclosporine (CsA) intravenous infusion: 5mg/kg. Infusion on day 14 administered twice a day.
intervention 1: Antithymocyte globulin intervention 2: Cyclosporine
1
Bethesda | Maryland | United States | -77.10026 | 38.98067
0
NCT00005937
[ 4 ]
488
RANDOMIZED
FACTORIAL
0TREATMENT
4QUADRUPLE
true
0ALL
null
This randomized, controlled trial compared the efficacy of the medication sertraline (Zoloft®), cognitive-behavioral therapy, the combination of these treatments, and placebo for youth with anxiety disorders.
Anxiety disorders are among the most common conditions affecting children and adolescents. These disorders impair school, social, and family functioning. When left untreated, they also put children at risk for major depression and substance abuse in late adolescence and adulthood. Previous studies demonstrated the efficacy of cognitive behavioral therapy and selective serotonin-reuptake inhibitors for the treatment of child anxiety disorders. This study is testing the relative and combined efficacy of cognitive behavioral therapy and selective serotonin reuptake inhibitors as compared to each other and pill placebo. During Phase I of this two-phase study, 488 participants were randomly assigned to receive sertraline (Zoloft), cognitive behavioral therapy, a combination of these treatments, or a placebo for 12 weeks. Phase II involved a 6-month maintenance period for participants.
Anxiety Disorders Social Phobia Generalized Anxiety Disorder
Phobic Disorders Anxiety, Separation
null
4
arm 1: Participants received sertraline for 12 weeks. arm 2: Participants received cognitive behavioral therapy for 12 weeks arm 3: Participants received both sertraline and CBT for 12 weeks. arm 4: Participants received a placebo pill for 12 weeks.
[ 1, 1, 1, 2 ]
3
[ 0, 5, 0 ]
intervention 1: Participants were treated with sertraline. intervention 2: Participants received CBT. intervention 3: Participants were treated with a placebo pill.
intervention 1: Sertraline (SRT) intervention 2: Cognitive Behavioral Therapy (CBT) intervention 3: Placebo
6
Los Angeles | California | United States | -118.24368 | 34.05223 Baltimore | Maryland | United States | -76.61219 | 39.29038 New York | New York | United States | -74.00597 | 40.71427 Durham | North Carolina | United States | -78.89862 | 35.99403 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062
0
NCT00052078
[ 2, 3 ]
31
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
1FEMALE
null
This phase I/II trial studies the best dose of suramin when given together with paclitaxel in treating women with stage IIIB-IV breast cancer. Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. Suramin may increase the effectiveness of paclitaxel by making tumor cells more sensitive to the drug.
PRIMARY OBJECTIVES: I. Determine the dose of suramin in combination with paclitaxel (TXT) that results in suramin plasma concentrations approaching 10-50 uM over the duration, when TXT in the plasma is at therapeutically significant levels, in women with stage IIIB or IV breast cancer. (Phase I) II. Determine the objective response rate in patients treated with this regimen. (Phase II) SECONDARY OBJECTIVES: I. Determine the pharmacokinetics of low-dose suramin in these patients. (Phase I) II. Determine the time to tumor progression in patients treated with this regimen. (Phase II) III. Determine the 1-year survival of patients treated with this regimen. (Phase II) OUTLINE: This is a phase I, dose-escalation study of suramin followed by a phase II multicenter study. PHASE I: Patients receive low-dose suramin intravenously (IV) over 30 minutes and paclitaxel IV over 1 hour once weekly. Courses repeat every 4 weeks in the absence of disease progression or unacceptable toxicity. Cohorts of 3-6 patients receive adjusted doses of suramin until a target dose is determined. The suramin target dose is defined as the dose at which at least 5 of 6 patients achieve the target plasma concentration of 10-50 uM over the duration when paclitaxel levels are therapeutic. PHASE II: Patients receive paclitaxel in combination with the target dose of suramin as above. PROJECTED ACCRUAL: A total of 6-18 patients will be accrued for the phase I study within 9 months. A total of 28 patients will be accrued for the phase II study within 18-24 months.
Recurrent Breast Cancer Stage IIIB Breast Cancer Stage IV Breast Cancer
null
1
arm 1: PHASE I: Patients receive low-dose suramin IV over 30 minutes and paclitaxel IV over 1 hour once weekly. Courses repeat every 4 weeks in the absence of disease progression or unacceptable toxicity. Cohorts of 3-6 patients receive adjusted doses of suramin until a target dose is determined. The suramin target dose is defined as the dose at which at least 5 of 6 patients achieve the target plasma concentration of 10-50 uM over the duration when paclitaxel levels are therapeutic. PHASE II: Patients receive paclitaxel in combination with the target dose of suramin as above.
[ 0 ]
3
[ 0, 0, 10 ]
intervention 1: Given IV intervention 2: Given IV intervention 3: Correlative studies
intervention 1: suramin intervention 2: paclitaxel intervention 3: pharmacological study
1
Columbus | Ohio | United States | -82.99879 | 39.96118
0
NCT00054028
[ 3 ]
28
null
null
0TREATMENT
0NONE
false
0ALL
null
Nonalcoholic Steatohepatitis (NASH) is associated with progressive liver disease, fibrosis, and cirrhosis. Although the cause of NASH is unknown, it is often associated with obesity, type 2 diabetes, and insulin resistance. At present, there are no approved treatments for NASH patients, but an experimental approach has focused on improving their insulin sensitivity. Metformin is one of the most commonly used medications for the treatment of diabetes. The purpose of this study is to determine whether the medical problems of NASH patients, specifically liver damage, improves when their insulin sensitivity is enhanced with metformin. The study will last 3 to 5 years and will enroll up to 30 patients. Participants will undergo a complete medical examination, a series of lab tests, and a liver biopsy. They will then start taking a single 500-mg tablet of metformin once a day for 2 weeks, then the same dosage twice a day for 2 more weeks, if they tolerate the first dosage. The dosage will increase to 1,000 mg twice a day for the remaining 44 weeks of the study. After 1 year, participants will undergo a repeat medical examination and liver biopsy.
Nonalcoholic fatty liver disease (NAFLD) represents a spectrum of diseases ranging from simple fatty liver (steatosis) to steatosis with inflammation and necrosis to cirrhosis, that occurs in persons who drink little or no alcohol. Nonalcoholic steatohepatitis (NASH) represents the more severe end of this spectrum and is associated with progressive liver disease, fibrosis and cirrhosis. The etiology of NASH is unclear, but it is often associated with obesity, type 2 diabetes, hyperlipidemia and insulin resistance. We have recently conducted a study of a 48-week course of pioglitazone in 21 non-diabetic patients with NASH. Serum aminotransferase levels and liver histology improved in most patients and the improvements correlated with changes in insulin sensitivity. These results are promising, but pioglitazone is associated with significant weight gain, is quite expensive, and its long-term safety is yet to be proven. In contrast, metformin is inexpensive, extremely well tolerated, and of proven long-term safety in patients with diabetes and pre-diabetes. In this study, we propose to treat 20 non-diabetic patients with NASH with metformin for 48-weeks. After an initial evaluation for insulin sensitivity, fat distribution and liver biopsy, patients will receive gradually increasing doses of metformin orally to a maximum of 2000 mg daily. Patients will be monitored at regular intervals for symptoms of liver disease, side effects of metformin and serum biochemical and metabolic indices. At the end of 48-weeks, patients will have a repeat medical evaluation and liver biopsy. Pre and post treatment liver histology, fat distribution and insulin sensitivity will be compared. The primary end point of successful therapy will be improvement in hepatic histology as determined by reduction of at least three points in NASH activity score. Secondary end points will be improvement in insulin sensitivity, body fat distribution, and liver biochemistry.
Hepatitis
Insulin Obesity Fatty Liver Diabetes Cirrhosis Metformin Insulin Resistance Nonalcoholic Steatohepatitis Hepatitis NASH
null
0
null
null
1
[ 0 ]
intervention 1: After complete medical evaluation and liver biopsy, patients who qualified for therapy were started on metformin in an initial dose of 500 mg once daily. After 2 weeks, the dose was increased to 500 mg twice daily and after 4 weeks to the full dose of 1000 mg twice daily. Subsequent dose reductions were carried out based on tolerance, with particular attention to gastrointestinal upset and abdominal bloating. Patients were seen in the out-patient clinic, had a brief medical history and examination and routine blood tests at 2 and 4 weeks after enrolment and every 4 weeks thereafter. The oral and intravenous glucose tolerance tests were repeated after 40 and 44 weeks respectively and liver biopsy and imaging tests at 48 weeks. Metformin was discontinued after 48 weeks in patients without diabetes on the pre-treatment evaluation.
intervention 1: Metformin
1
Bethesda | Maryland | United States | -77.10026 | 38.98067
0
NCT00063232
[ 3 ]
7
NON_RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
true
RATIONALE: Drugs used in chemotherapy work in different ways to stop tumor cells from dividing so they stop growing or die. Giving combination chemotherapy before surgery may shrink the tumor so that it can be removed. Giving combination chemotherapy after surgery may kill any remaining tumor cells. PURPOSE: This phase II trial is studying how well surgery and/or combination chemotherapy work in treating children with fibrosarcoma.
OBJECTIVES: Primary * Determine the event-free and relapse-free survival of children with initially unresectable congenital, infantile, or childhood fibrosarcoma treated with neoadjuvant chemotherapy comprising vincristine, dactinomycin, and cyclophosphamide (VAC) before definitive local control. Secondary * Determine the event-free and relapse-free survival of patients initially treated with this regimen followed by observation after local control with positive microscopic margins. * Determine the event-free and relapse-free survival of patients initially treated with this regimen followed by additional chemotherapy comprising etoposide and ifosfamide after local control with gross positive margins. * Determine the event-free and relapse-free survival of patients treated with surgery alone. OUTLINE: This is a pilot, multicenter study. Patients begin treatment according to lesion resectability. Patients with resectable lesions proceed to surgery. * Surgery: Patients undergo resection of disease lesions. Patients with clear or microscopically positive margins undergo observation only. Patients with grossly positive margins undergo re-resection if feasible. Patients with grossly positive margins after re-resection or for whom re-resection is not feasible receive chemotherapy comprising vincristine, dactinomycin, and cyclophosphamide (VAC). Patients with unresectable lesions receive VAC chemotherapy. * VAC chemotherapy: Patients receive vincristine intravenously (IV) on days 1, 8, and 15 and dactinomycin IV and cyclophosphamide IV over 1 hour on day 1. Treatment repeats every 21 days for up to 6 courses in the absence of disease progression or unacceptable toxicity. Patients with disease progression after 2-4 courses of VAC chemotherapy proceed to chemotherapy comprising etoposide and ifosfamide (IE). Patients with stable disease after 4 courses of VAC chemotherapy proceed to IE chemotherapy. Patients with a partial response (PR) and unresectable lesions after 4 courses of VAC chemotherapy receive 2 additional courses of VAC and are then re-evaluated. Patients proceed to surgery if they continue to have a PR or achieve a complete response (CR) and lesions are now resectable. Patients with a CR or PR and resectable lesions after 4 courses of VAC chemotherapy proceed to surgery. Patients with stable disease, progressive disease, or a PR and unresectable lesions after 6 courses of VAC proceed to IE chemotherapy. * IE chemotherapy: Patients receive etoposide IV over 1 hour and ifosfamide IV over 1 hour on days 1-5. Treatment repeats every 21 days for 4 courses in the absence of disease progression or unacceptable toxicity. Patients with a CR or PR and resectable lesions after 2-4 courses of IE chemotherapy proceed to surgery. All patients are followed every 3 months for 6 months, every 6 months for 1 year, and then as clinically indicated. PROJECTED ACCRUAL: A total of 60-70 patients will be accrued for this study within 8 years.
Sarcoma
childhood fibrosarcoma nonmetastatic childhood soft tissue sarcoma
null
2
arm 1: Comprised of patients with disease lesions that are initially unresectable, or resected but with resulting grossly positive margins. All patients receive vincristine sulfate, dactinomycin, and cyclophosphamide (VAC), and mercaptoethane sulfonate (MESNA). Depending on response, patients may receive ifosfamide and etoposide (IE). Filgrastim may also be given, as needed. In addition to Chemotherapy, patients may receive Conventional Surgery. (See Interventions section for drug dosage and administration details.) arm 2: Comprised of patients with initially resectable disease lesions. All patients undergo Conventional Surgery. Those with a result of clear or microscopically positive margins remain on study in this arm, for observation with no further intervention.
[ 0, 0 ]
8
[ 2, 0, 0, 0, 0, 3, 2, 2 ]
intervention 1: Given Slow intravenous (IV) push over 1-5 minutes, dose \< 1yr 0.025 mg/kg \> or = 1 yr 0.045 mg/kg (max dose 2.5 mg) on days 1,22,43 and 64 intervention 2: Given IV over 60 minutes, dose 25 mg/kg on days 1,22,43 and 64. intervention 3: Given IV over 1 hour, dose 3.3 mg/kg in normal saline (NS) 10 cc/kg (or to equal 0.4 mg/mL concentration) on days 1-5 of IE cycle. intervention 4: Given IV over 1 hour, dose 60mg/kg in D5 1/4 NS 10 cc/kg IV on days 1-5 of IE Cycle intervention 5: Given IV Push over 1 minute, dose 0.05 mg/kg (max dose 2 mg) on days 1,8,15,22,29,36,43,50,57 and 64 intervention 6: Applied only when lesion is resectable. Surgery is the primary means of local control in this study and reasonable attempts at achieving clear margins with an "envelope" of normal tissue should be undertaken at the initial and/or subsequent resections. intervention 7: Given orally. Oral daily MESNA dose is equal to at least 60% of the daily cyclophosphamide dose. intervention 8: Given IV - Only use filgrastim if chemotherapy has been delayed or modified for hematologic toxicity, or if patient experiences a significant life-threatening toxicity due to bone marrow suppression
intervention 1: dactinomycin intervention 2: cyclophosphamide intervention 3: etoposide intervention 4: ifosfamide intervention 5: vincristine sulfate intervention 6: Conventional Surgery intervention 7: MESNA (mercaptoethane sulfonate) intervention 8: Filgrastim
74
Phoenix | Arizona | United States | -112.07404 | 33.44838 Little Rock | Arkansas | United States | -92.28959 | 34.74648 Downey | California | United States | -118.13257 | 33.94001 Loma Linda | California | United States | -117.26115 | 34.04835 Long Beach | California | United States | -118.18923 | 33.76696 Sacramento | California | United States | -121.4944 | 38.58157 San Francisco | California | United States | -122.41942 | 37.77493 Stanford | California | United States | -122.16608 | 37.42411 Farmington | Connecticut | United States | -72.83204 | 41.71982 Washington D.C. | District of Columbia | United States | -77.03637 | 38.89511 Fort Myers | Florida | United States | -81.84059 | 26.62168 Miami | Florida | United States | -80.19366 | 25.77427 Pensacola | Florida | United States | -87.21691 | 30.42131 St. Petersburg | Florida | United States | -82.67927 | 27.77086 Tampa | Florida | United States | -82.45843 | 27.94752 Atlanta | Georgia | United States | -84.38798 | 33.749 Augusta | Georgia | United States | -81.97484 | 33.47097 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Louisville | Kentucky | United States | -85.75941 | 38.25424 New Orleans | Louisiana | United States | -90.07507 | 29.95465 Bangor | Maine | United States | -68.77265 | 44.79884 Boston | Massachusetts | United States | -71.05977 | 42.35843 Flint | Michigan | United States | -83.68746 | 43.01253 Grand Rapids | Michigan | United States | -85.66809 | 42.96336 Grosse Pointe Woods | Michigan | United States | -82.90686 | 42.44365 Minneapolis | Minnesota | United States | -93.26384 | 44.97997 Minneapolis | Minnesota | United States | -93.26384 | 44.97997 Jackson | Mississippi | United States | -90.18481 | 32.29876 Kansas City | Missouri | United States | -94.57857 | 39.09973 Hackensack | New Jersey | United States | -74.04347 | 40.88593 Morristown | New Jersey | United States | -74.48154 | 40.79677 New York | New York | United States | -74.00597 | 40.71427 Syracuse | New York | United States | -76.14742 | 43.04812 Chapel Hill | North Carolina | United States | -79.05584 | 35.9132 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Durham | North Carolina | United States | -78.89862 | 35.99403 Akron | Ohio | United States | -81.51901 | 41.08144 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Cleveland | Ohio | United States | -81.69541 | 41.4995 Columbus | Ohio | United States | -82.99879 | 39.96118 Dayton | Ohio | United States | -84.19161 | 39.75895 Youngstown | Ohio | United States | -80.64952 | 41.09978 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Danville | Pennsylvania | United States | -76.61273 | 40.96342 Hershey | Pennsylvania | United States | -76.65025 | 40.28592 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Providence | Rhode Island | United States | -71.41283 | 41.82399 Charleston | South Carolina | United States | -79.93275 | 32.77632 Greenville | South Carolina | United States | -82.39401 | 34.85262 Knoxville | Tennessee | United States | -83.92074 | 35.96064 Memphis | Tennessee | United States | -90.04898 | 35.14953 Nashville | Tennessee | United States | -86.78444 | 36.16589 Dallas | Texas | United States | -96.80667 | 32.78306 Dallas | Texas | United States | -96.80667 | 32.78306 Houston | Texas | United States | -95.36327 | 29.76328 Lubbock | Texas | United States | -101.85517 | 33.57786 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Spokane | Washington | United States | -117.42908 | 47.65966 Green Bay | Wisconsin | United States | -88.01983 | 44.51916 Marshfield | Wisconsin | United States | -90.1718 | 44.66885 Milwaukee | Wisconsin | United States | -87.90647 | 43.0389 Westmead | New South Wales | Australia | 150.98768 | -33.80383 North Adelaide | South Australia | Australia | 138.59141 | -34.90733 Edmonton | Alberta | Canada | -113.46871 | 53.55014 Vancouver | British Columbia | Canada | -123.11934 | 49.24966 Halifax | Nova Scotia | Canada | -63.57688 | 44.64269 Toronto | Ontario | Canada | -79.39864 | 43.70643 Montreal | Quebec | Canada | -73.58781 | 45.50884 Montreal | Quebec | Canada | -73.58781 | 45.50884 Saskatoon | Saskatchewan | Canada | -106.66892 | 52.13238 Auckland | N/A | New Zealand | 174.76349 | -36.84853
0
NCT00072280
[ 3 ]
5
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
1FEMALE
true
RATIONALE: Giving chemotherapy, such as fludarabine and melphalan, before a donor peripheral blood stem cell transplant helps stop the growth of tumor cells. It also stops the patient's immune system from rejecting the donor's stem cells. The donated stem cells may replace the patient's immune system and help destroy any remaining tumor cells (graft-versus-tumor effect). Giving an infusion of the donor's T cells (donor lymphocyte infusion) after the transplant may help increase this effect. Sometimes the transplanted cells from a donor can also make an immune response against the body's normal cells. Giving antithymocyte globulin, cyclosporine, and methotrexate before or after the transplant may stop this from happening. PURPOSE: This phase II trial is studying how well antithymocyte globulin, high-dose melphalan, fludarabine, and allogeneic peripheral stem cell transplant work in treating patients with metastatic adenocarcinoma of the breast.
OBJECTIVES: Primary * Determine the toxicity and tolerability of allogeneic peripheral blood stem cell transplantation after a nonmyeloablative preparative regimen comprising anti-thymocyte globulin, high-dose melphalan, and fludarabine in women with chemotherapy-refractory or poor-prognosis metastatic adenocarcinoma of the breast. * Determine the ability of this preparative regimen to facilitate long-term engraftment of allogeneic stem cells and lymphocytes in these patients. * Determine the response in measurable/evaluable disease and its temporal relationship to the preparative chemotherapy used and to the onset of clinical graft-versus-host disease (GVHD) in patients treated with this regimen. Secondary * Determine the progression-free and overall survival of patients treated with this regimen. * Determine the tumor response and its temporal relationship to administration of high-dose chemotherapy and to the onset of GVHD in patients treated with this regimen. * Determine the frequency and durability of the induction of full donor chimerism of lymphocytes in patients treated with this regimen. OUTLINE: This is a nonrandomized, pilot study. * Nonmyeloablative preparative regimen: Patients receive fludarabine IV over 30 minutes on days -8 to -4, anti-thymocyte globulin IV over 4 hours on days -7 to -4, and high-dose melphalan IV over 30 minutes on days -3 and -2. * Graft-versus-host disease (GVHD) prophylaxis: Patients receive cyclosporine IV (and then orally when tolerated) every 12 hours beginning on day -4 and tapered after day 42 (if no GVHD occurs) or after day 90 (if grade I acute GVHD occurs). Patients also receive methotrexate IV on days 1, 3, and 6. * Allogeneic peripheral blood stem cell transplantation (PBSCT): Patients undergo allogeneic PBSCT on day 0. Patients also receive filgrastim (G-CSF) IV or subcutaneously beginning on day 0 and continuing until blood counts recover. * Donor lymphocyte infusion (DLI): Patients who show disease progression or fail to achieve full donor type T-cell chimerism (at least 90% donor derived T-cells) by the 90-day assessment posttransplantation, and have no evidence of active GVHD may receive DLI. Patients who have unresponsive disease with no active GVHD receive subsequent DLIs every 6-8 weeks. Patients are followed at 1, 3, 6, 12, 18, 24, 30, and 36 months. PROJECTED ACCRUAL: A total of 10 patients will be accrued for this study.
Breast Cancer
recurrent breast cancer stage IV breast cancer
null
1
arm 1: None
[ 0 ]
9
[ 2, 2, 2, 2, 0, 0, 0, 0, 3 ]
intervention 1: None intervention 2: None intervention 3: None intervention 4: None intervention 5: None intervention 6: None intervention 7: None intervention 8: None intervention 9: None
intervention 1: anti-thymocyte globulin intervention 2: filgrastim intervention 3: graft-versus-tumor induction therapy intervention 4: therapeutic allogeneic lymphocytes intervention 5: cyclosporine intervention 6: fludarabine phosphate intervention 7: melphalan intervention 8: methotrexate intervention 9: peripheral blood stem cell transplantation
1
La Jolla | California | United States | -117.2742 | 32.84727
0
NCT00074269
[ 4 ]
628
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
null
A substance called immunoglobulin E (IgE), which is naturally produced by our body, has a key role in generating asthma attacks. In patients with allergies, there is an exaggerated production of IgE in response to specific substances such as pollens. Omalizumab is a new drug that inactivates IgE. This study tested the safety and efficacy of omalizumab against asthma attacks in children with allergic asthma.
This study was designed to provide one year efficacy and safety data for subcutaneous (SC) omalizumab, compared to placebo in children (6 to \< 12 years) with moderate to severe persistent asthma who have inadequate asthma control despite treatment according to National Heart, Lung and Blood Institute (NHLBI) step 3 or 4 (at least medium dose inhaled corticosteroids with or without other controller asthma medications).
Asthma
allergic asthma atopic omalizumab immunoglobulin E IgE anti-IgE
null
2
arm 1: Participants received omalizumab administered by subcutaneous injection every 2 or 4 weeks for a duration of 52 weeks. The omalizumab dose was based on the patient's body weight and total serum IgE level at Screening. The first 24 weeks of the treatment period was a fixed steroid phase where the steroid dose was maintained constant; in the following 28 weeks the steroid dose was adjustable, depending on the patient's condition. Following the 52-week treatment period, patients were followed up for an additional 16 weeks. arm 2: Placebo was administered by subcutaneous injection every 2 or 4 weeks depending on the dosing schedule in the protocol for a total of 52 weeks. The first 24 weeks of the treatment period was a fixed steroid phase where the steroid dose was maintained constant; in the following 28 weeks the steroid dose was adjustable, depending on the patient's condition. Following the 52-week treatment period, patients were followed up for an additional 16 weeks.
[ 0, 2 ]
3
[ 0, 0, 0 ]
intervention 1: The omalizumab dose administered, based on the patient's body weight and total serum IgE level at Screening, and the number of injections and injection volume was determined from the dosing tables in the protocol. Omalizumab 75 to 375 mg was administered subcutaneous (SC) every 2 or 4 weeks depending on the dose. intervention 2: Placebo was administered subcutaneous (SC) every 2 or 4 weeks depending on the dosing schedule in the protocol. intervention 3: Patients entered the study using their current formulation of any inhaled steroid (proprietary drug and device) ≥ 200 μg/day equivalent of fluticasone administered with a dry-powder inhaler.
intervention 1: Omalizumab intervention 2: Placebo intervention 3: Fluticasone
56
Birmingham | Alabama | United States | -86.80249 | 33.52066 Little Rock | Arkansas | United States | -92.28959 | 34.74648 Little Rock | Arkansas | United States | -92.28959 | 34.74648 Huntington Beach | California | United States | -117.99923 | 33.6603 Huntington Beach | California | United States | -117.99923 | 33.6603 Long Beach | California | United States | -118.18923 | 33.76696 Mission Viejo | California | United States | -117.672 | 33.60002 Orange | California | United States | -117.85311 | 33.78779 Palmdale | California | United States | -118.11646 | 34.57943 Palo Alto | California | United States | -122.14302 | 37.44188 Riverside | California | United States | -117.39616 | 33.95335 San Diego | California | United States | -117.16472 | 32.71571 San Diego | California | United States | -117.16472 | 32.71571 San Jose | California | United States | -121.89496 | 37.33939 Santa Monica | California | United States | -118.49138 | 34.01949 Stockton | California | United States | -121.29078 | 37.9577 Walnut Creek | California | United States | -122.06496 | 37.90631 Denver | Colorado | United States | -104.9847 | 39.73915 Miami | Florida | United States | -80.19366 | 25.77427 Albany | Georgia | United States | -84.15574 | 31.57851 Atlanta | Georgia | United States | -84.38798 | 33.749 Savannah | Georgia | United States | -81.09983 | 32.08354 Chicago | Illinois | United States | -87.65005 | 41.85003 Elliott | Maryland | United States | -75.99632 | 38.31012 North Dartmouth | Massachusetts | United States | -70.97032 | 41.63899 St Louis | Missouri | United States | -90.19789 | 38.62727 Omaha | Nebraska | United States | -95.94043 | 41.25626 Brick | New Jersey | United States | -74.13708 | 40.05928 Newark | New Jersey | United States | -74.17237 | 40.73566 Buffalo | New York | United States | -78.87837 | 42.88645 Ithaca | New York | United States | -76.49661 | 42.44063 Liverpool | New York | United States | -76.2177 | 43.10646 Rockville Centre | New York | United States | -73.64124 | 40.65871 Durham | North Carolina | United States | -78.89862 | 35.99403 High Point | North Carolina | United States | -80.00532 | 35.95569 Cincinnati | Ohio | United States | -84.51439 | 39.12711 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Medford | Oregon | United States | -122.87559 | 42.32652 Altoona | Pennsylvania | United States | -78.39474 | 40.51868 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Upland | Pennsylvania | United States | -75.38269 | 39.85261 Lincoln | Rhode Island | United States | -71.435 | 41.92111 Knoxville | Tennessee | United States | -83.92074 | 35.96064 Nashville | Tennessee | United States | -86.78444 | 36.16589 Dallas | Texas | United States | -96.80667 | 32.78306 Dallas | Texas | United States | -96.80667 | 32.78306 Fort Worth | Texas | United States | -97.32085 | 32.72541 Houston | Texas | United States | -95.36327 | 29.76328 Houston | Texas | United States | -95.36327 | 29.76328 San Antonio | Texas | United States | -98.49363 | 29.42412 South Jordan | Utah | United States | -111.92966 | 40.56217 Norfolk | Virginia | United States | -76.28522 | 36.84681 Richmond | Virginia | United States | -77.46026 | 37.55376 Seattle | Washington | United States | -122.33207 | 47.60621 Spokane | Washington | United States | -117.42908 | 47.65966 Milwaukee | Wisconsin | United States | -87.90647 | 43.0389
0
NCT00079937
[ 3 ]
138
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
1FEMALE
false
This phase II study will evaluate and compare the efficacy and tolerability of two dose schedules (1500 mg QD and 500 mg BID) of oral Lapatinib as treatment for patients with advanced or metastatic breast cancer.
null
Neoplasms, Breast
lapatinib advanced metastatic breast cancer GW572016 ErbB2
null
0
null
null
1
[ 0 ]
intervention 1: None
intervention 1: Lapatinib
31
Hollywood | Florida | United States | -80.14949 | 26.0112 Santiago | Región Metro de Santiago | Chile | -70.64827 | -33.45694 Santiago | Región Metro de Santiago | Chile | -70.64827 | -33.45694 Santiago | Región Metro de Santiago | Chile | -70.64827 | -33.45694 Pokfulam | N/A | Hong Kong | N/A | N/A Delhi | N/A | India | 77.23149 | 28.65195 Hyderabad, Andhra Pradesh | N/A | India | 78.45636 | 17.38405 Pune | N/A | India | 73.85535 | 18.51957 Bandar Tun Razak, Cheras | N/A | Malaysia | N/A | N/A Kubang Kerian | N/A | Malaysia | 102.27938 | 6.09123 Tanjong Bungah | N/A | Malaysia | 100.29161 | 5.45828 Tanjong Bungah | N/A | Malaysia | 100.29161 | 5.45828 Ixtaltepec / Espinal | Oaxaca | Mexico | N/A | N/A Mérida | Yucatán | Mexico | -89.62318 | 20.967 Mexico | N/A | Mexico | -98.43784 | 18.88011 Karachi | N/A | Pakistan | 67.0104 | 24.8608 Karachi | N/A | Pakistan | 67.0104 | 24.8608 Karachi | N/A | Pakistan | 67.0104 | 24.8608 Lahore | N/A | Pakistan | 74.35071 | 31.558 Rawalpindi | N/A | Pakistan | 73.0479 | 33.59733 Lima | Lima Province | Peru | -77.02824 | -12.04318 Lima | Lima Province | Peru | -77.02824 | -12.04318 Lima | Lima Province | Peru | -77.02824 | -12.04318 Callao | N/A | Peru | -77.13452 | -12.05162 Bydogoszcz | N/A | Poland | N/A | N/A Krakow | N/A | Poland | 19.93658 | 50.06143 Olsztyn | N/A | Poland | 20.49416 | 53.77995 Singapore | N/A | Singapore | 103.85007 | 1.28967 Singapore | N/A | Singapore | 103.85007 | 1.28967 Taipei | N/A | Taiwan | 121.52639 | 25.05306 Taipei | N/A | Taiwan | 121.52639 | 25.05306
0
NCT00089999
[ 3 ]
197
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
The purpose of this clinical research study is to learn if BMS-354825 will have activity, defined by hematologic response, in subjects who have accelerated phase chronic myeloid leukemia (CML) who are resistant to or intolerant to imatinib mesylate. The safety of this treatment will also be studied.
null
Chronic Myelogenous Leukemia
Chronic myelogenous leukemia (CML): Accelerated phase
null
1
arm 1: None
[ 0 ]
1
[ 0 ]
intervention 1: Tablets, Oral, 70 mg, twice daily, until disease progression or intolerable toxicity, switch to the roll-over study or study closure
intervention 1: Dasatinib
70
Birmingham | Alabama | United States | -86.80249 | 33.52066 Anaheim | California | United States | -117.9145 | 33.83529 Los Angeles | California | United States | -118.24368 | 34.05223 Stanford | California | United States | -122.16608 | 37.42411 Vallejo | California | United States | -122.25664 | 38.10409 Jacksonville | Florida | United States | -81.65565 | 30.33218 Tampa | Florida | United States | -82.45843 | 27.94752 Atlanta | Georgia | United States | -84.38798 | 33.749 Chicago | Illinois | United States | -87.65005 | 41.85003 Kansas City | Kansas | United States | -94.62746 | 39.11417 Baltimore | Maryland | United States | -76.61219 | 39.29038 Boston | Massachusetts | United States | -71.05977 | 42.35843 Detroit | Michigan | United States | -83.04575 | 42.33143 St Louis | Missouri | United States | -90.19789 | 38.62727 Hackensack | New Jersey | United States | -74.04347 | 40.88593 New York | New York | United States | -74.00597 | 40.71427 Portland | Oregon | United States | -122.67621 | 45.52345 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Nashville | Tennessee | United States | -86.78444 | 36.16589 Dallas | Texas | United States | -96.80667 | 32.78306 Houston | Texas | United States | -95.36327 | 29.76328 Buenos Aires | Buenos Aires | Argentina | N/A | N/A Córdoba | Córdoba Province | Argentina | -64.18853 | -31.40648 St Leonards | New South Wales | Australia | 151.19836 | -33.82344 South Brisbane | Queensland | Australia | 153.02049 | -27.48034 East Melbourne | Victoria | Australia | 144.9879 | -37.81667 Parkville | Victoria | Australia | 144.95 | -37.78333 Wien | N/A | Australia | N/A | N/A B-Leuven | N/A | Belgium | N/A | N/A Edegem | N/A | Belgium | 4.44504 | 51.15662 Rio de Janeiro | Rio de Janeiro | Brazil | -43.18223 | -22.90642 São Paulo | São Paulo | Brazil | -46.63611 | -23.5475 Campinas | N/A | Brazil | -47.06083 | -22.90556 Toronto | Ontario | Canada | -79.39864 | 43.70643 Aarhus | N/A | Denmark | 10.21076 | 56.15674 Helsinki | N/A | Finland | 24.93545 | 60.16952 Lille | N/A | France | 3.05858 | 50.63297 Lyon | N/A | France | 4.84671 | 45.74846 Nantes | N/A | France | -1.55336 | 47.21725 Paris | N/A | France | 2.3488 | 48.85341 Pessac | N/A | France | -0.6324 | 44.80565 Poitiers | N/A | France | 0.34348 | 46.58261 Strasbourg | N/A | France | 7.74553 | 48.58392 Hamburg | N/A | Germany | 9.99302 | 53.55073 Mainz | N/A | Germany | 8.2791 | 49.98419 Mannheim | N/A | Germany | 8.46694 | 49.4891 Ramat Gan | N/A | Israel | 34.81065 | 32.08227 Bologna | N/A | Italy | 11.33875 | 44.49381 Napoli | N/A | Italy | 14.5195 | 40.87618 Orbassano | N/A | Italy | 7.53813 | 45.00547 Roma | N/A | Italy | 11.10642 | 44.99364 Nijmegen | N/A | Netherlands | 5.85278 | 51.8425 Rotterdam | N/A | Netherlands | 4.47917 | 51.9225 Trondheim | N/A | Norway | 10.39506 | 63.43049 Lima | Lima Province | Peru | -77.02824 | -12.04318 Quezon City | N/A | Philippines | 121.0509 | 14.6488 Singapore | N/A | Singapore | 103.85007 | 1.28967 Jeollanam-Do | N/A | South Korea | N/A | N/A Kyunggi-Do | N/A | South Korea | N/A | N/A Seoul | N/A | South Korea | 126.9784 | 37.566 Gothenburg | N/A | Sweden | 11.96679 | 57.70716 Lund | N/A | Sweden | 13.19321 | 55.70584 Umeå | N/A | Sweden | 20.25972 | 63.82842 Uppsala | N/A | Sweden | 17.63889 | 59.85882 Basel | N/A | Switzerland | 7.57327 | 47.55839 Taipei | N/A | Taiwan | 121.52639 | 25.05306 Taoyuan District | N/A | Taiwan | 121.3187 | 24.9896 Bangkok | N/A | Thailand | 100.50144 | 13.75398 Glasgow | Central | United Kingdom | -4.25763 | 55.86515 London | Greater London | United Kingdom | -0.12574 | 51.50853
0
NCT00101647
[ 3 ]
124
NON_RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
The purpose of this study is to see what effect an investigational drug (BMS-354825) has on subjects who are currently in the myeloid blast phase of chronic myeloid leukemia (CML) and who are either resistant to or intolerant of imatinib mesylate. Another purpose of the study is to see what side effects this drug may have on subjects.
null
Chronic Myeloid Leukemia Blast Crisis
Myeloid blast phase Chronic Myeloid Leukemia (CML)
null
1
arm 1: None
[ 0 ]
1
[ 0 ]
intervention 1: Tablets, Oral, 70 mg, twice daily, Until disease progression or intolerable toxicity, switch to the roll-over study or study closure.
intervention 1: Dasatinib
62
Birmingham | Alabama | United States | -86.80249 | 33.52066 Anaheim | California | United States | -117.9145 | 33.83529 Los Angeles | California | United States | -118.24368 | 34.05223 Stanford | California | United States | -122.16608 | 37.42411 Vallejo | California | United States | -122.25664 | 38.10409 Denver | Colorado | United States | -104.9847 | 39.73915 Jacksonville | Florida | United States | -81.65565 | 30.33218 Tampa | Florida | United States | -82.45843 | 27.94752 Atlanta | Georgia | United States | -84.38798 | 33.749 Chicago | Illinois | United States | -87.65005 | 41.85003 Kansas City | Kansas | United States | -94.62746 | 39.11417 Baltimore | Maryland | United States | -76.61219 | 39.29038 Boston | Massachusetts | United States | -71.05977 | 42.35843 Detroit | Michigan | United States | -83.04575 | 42.33143 St Louis | Missouri | United States | -90.19789 | 38.62727 Hackensack | New Jersey | United States | -74.04347 | 40.88593 New Brunswick | New Jersey | United States | -74.45182 | 40.48622 New York | New York | United States | -74.00597 | 40.71427 Portland | Oregon | United States | -122.67621 | 45.52345 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Nashville | Tennessee | United States | -86.78444 | 36.16589 Houston | Texas | United States | -95.36327 | 29.76328 Seattle | Washington | United States | -122.33207 | 47.60621 Adelaide | South Australia | Australia | 138.59863 | -34.92866 Vienna | N/A | Austria | 16.37208 | 48.20849 B-Leuven | N/A | Belgium | N/A | N/A Edegem | N/A | Belgium | 4.44504 | 51.15662 Montreal | Quebec | Canada | -73.58781 | 45.50884 Aarhus | N/A | Denmark | 10.21076 | 56.15674 Helsinki | N/A | Finland | 24.93545 | 60.16952 Lille | N/A | France | 3.05858 | 50.63297 Lyon | N/A | France | 4.84671 | 45.74846 Nantes | N/A | France | -1.55336 | 47.21725 Paris | N/A | France | 2.3488 | 48.85341 Pessac | N/A | France | -0.6324 | 44.80565 Poitiers | N/A | France | 0.34348 | 46.58261 Strasbourg | N/A | France | 7.74553 | 48.58392 Hamburg | N/A | Germany | 9.99302 | 53.55073 Mainz | N/A | Germany | 8.2791 | 49.98419 Mannheim | N/A | Germany | 8.46694 | 49.4891 Ramat Gan | N/A | Israel | 34.81065 | 32.08227 Bologna | N/A | Italy | 11.33875 | 44.49381 Napoli | N/A | Italy | 14.5195 | 40.87618 Orbassano | N/A | Italy | 7.53813 | 45.00547 Roma | N/A | Italy | 11.10642 | 44.99364 Nijmegen | N/A | Netherlands | 5.85278 | 51.8425 Rotterdam | N/A | Netherlands | 4.47917 | 51.9225 Trondheim | N/A | Norway | 10.39506 | 63.43049 Quezon City | N/A | Philippines | 121.0509 | 14.6488 Singapore | N/A | Singapore | 103.85007 | 1.28967 Jeollanam-Do | N/A | South Korea | N/A | N/A Kyunggi-Do | N/A | South Korea | N/A | N/A Seoul | N/A | South Korea | 126.9784 | 37.566 Gothenburg | N/A | Sweden | 11.96679 | 57.70716 Lund | N/A | Sweden | 13.19321 | 55.70584 Umeå | N/A | Sweden | 20.25972 | 63.82842 Uppsala | N/A | Sweden | 17.63889 | 59.85882 Basel | N/A | Switzerland | 7.57327 | 47.55839 Taipei | N/A | Taiwan | 121.52639 | 25.05306 Taoyuan District | N/A | Taiwan | 121.3187 | 24.9896 Glasgow | Central | United Kingdom | -4.25763 | 55.86515 London | Greater London | United Kingdom | -0.12574 | 51.50853
0
NCT00101816
[ 3 ]
150
RANDOMIZED
CROSSOVER
0TREATMENT
0NONE
false
0ALL
false
The primary purpose of this study is to estimate the major cytogenetic response rates of BMS-354825 and imatinib (800 mg/d) in subjects with chronic phase, Philadelphia chromosome positive, chronic myeloid leukemia (PH+ CML) with disease resistant to imatinib at a dose of 400-600 mg/d.
null
Chronic Myeloid Leukemia Philadelphia-Positive Myeloid Leukemia
Chronic Phase Philadelphia chromosome Positive (Ph+) chronic myeloid leukemia
null
2
arm 1: Active Comparator arm 2: Active Comparator
[ 0, 0 ]
2
[ 0, 0 ]
intervention 1: Tablets, oral, 20 mg and 50mg, twice daily, up to 96 weeks intervention 2: Tablets, Oral, 400mg and 100mg, twice daily, up to 96 weeks
intervention 1: Dasatinib intervention 2: Imatinib
131
Birmingham | Alabama | United States | -86.80249 | 33.52066 Anaheim | California | United States | -117.9145 | 33.83529 Bakersfield | California | United States | -119.01871 | 35.37329 Fullerton | California | United States | -117.92534 | 33.87029 Loma Linda | California | United States | -117.26115 | 34.04835 Los Angeles | California | United States | -118.24368 | 34.05223 Monterey Park | California | United States | -118.12285 | 34.06251 San Diego | California | United States | -117.16472 | 32.71571 Santa Barbara | California | United States | -119.69819 | 34.42083 Santa Maria | California | United States | -120.43572 | 34.95303 Stanford | California | United States | -122.16608 | 37.42411 Vallejo | California | United States | -122.25664 | 38.10409 Aurora | Colorado | United States | -104.83192 | 39.72943 Hartford | Connecticut | United States | -72.68509 | 41.76371 Washington D.C. | District of Columbia | United States | -77.03637 | 38.89511 Jacksonville | Florida | United States | -81.65565 | 30.33218 Tampa | Florida | United States | -82.45843 | 27.94752 Athens | Georgia | United States | -83.37794 | 33.96095 Atlanta | Georgia | United States | -84.38798 | 33.749 Lawrenceville | Georgia | United States | -83.98796 | 33.95621 Tucker | Georgia | United States | -84.21714 | 33.85455 Chicago | Illinois | United States | -87.65005 | 41.85003 Peoria | Illinois | United States | -89.58899 | 40.69365 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Kansas City | Kansas | United States | -94.62746 | 39.11417 Lexington | Kentucky | United States | -84.47772 | 37.98869 Boston | Massachusetts | United States | -71.05977 | 42.35843 Minneapolis | Minnesota | United States | -93.26384 | 44.97997 Rochester | Minnesota | United States | -92.4699 | 44.02163 Columbia | Missouri | United States | -92.33407 | 38.95171 Kansas City | Missouri | United States | -94.57857 | 39.09973 St Louis | Missouri | United States | -90.19789 | 38.62727 Omaha | Nebraska | United States | -95.94043 | 41.25626 Hackensack | New Jersey | United States | -74.04347 | 40.88593 Morristown | New Jersey | United States | -74.48154 | 40.79677 New Brunswick | New Jersey | United States | -74.45182 | 40.48622 Cary | North Carolina | United States | -78.78112 | 35.79154 Chapel Hill | North Carolina | United States | -79.05584 | 35.9132 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Tulsa | Oklahoma | United States | -95.99277 | 36.15398 Portland | Oregon | United States | -122.67621 | 45.52345 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Greenville | South Carolina | United States | -82.39401 | 34.85262 Nashville | Tennessee | United States | -86.78444 | 36.16589 Dallas | Texas | United States | -96.80667 | 32.78306 Fort Worth | Texas | United States | -97.32085 | 32.72541 Houston | Texas | United States | -95.36327 | 29.76328 San Antonio | Texas | United States | -98.49363 | 29.42412 Tyler | Texas | United States | -95.30106 | 32.35126 Norfolk | Virginia | United States | -76.28522 | 36.84681 Seattle | Washington | United States | -122.33207 | 47.60621 Spokane | Washington | United States | -117.42908 | 47.65966 Vancouver | Washington | United States | -122.66149 | 45.63873 Buenos Aires | Buenos Aires | Argentina | N/A | N/A Córdoba | Córdoba Province | Argentina | -64.18853 | -31.40648 Camperdown | New South Wales | Australia | 151.17642 | -33.88965 St Leonards | New South Wales | Australia | 151.19836 | -33.82344 South Brisbane | Queensland | Australia | 153.02049 | -27.48034 Adelaide | South Australia | Australia | 138.59863 | -34.92866 Perth | Western Australia | Australia | 115.8614 | -31.95224 Wein | N/A | Austria | N/A | N/A B-Leuven | N/A | Belgium | N/A | N/A Bruges | N/A | Belgium | 3.22424 | 51.20892 Brussels | N/A | Belgium | 4.34878 | 50.85045 Charleroi | N/A | Belgium | 4.44448 | 50.41136 Edegem | N/A | Belgium | 4.44504 | 51.15662 Yvoir | N/A | Belgium | 4.88059 | 50.3279 Curitiba | Paraná | Brazil | -49.27306 | -25.42778 Rio de Janeiro | Rio de Janeiro | Brazil | -43.18223 | -22.90642 São Paulo | São Paulo | Brazil | -46.63611 | -23.5475 Edmonton | Alberta | Canada | -113.46871 | 53.55014 Vancouver | British Columbia | Canada | -123.11934 | 49.24966 Toronto | Ontario | Canada | -79.39864 | 43.70643 Montreal | Quebec | Canada | -73.58781 | 45.50884 Beijing | N/A | China | 116.39723 | 39.9075 Shanghai | N/A | China | 121.45806 | 31.22222 Aarhus | N/A | Denmark | 10.21076 | 56.15674 Tallinn | N/A | Estonia | 24.75353 | 59.43696 Helsinki | N/A | Finland | 24.93545 | 60.16952 Lille | N/A | France | 3.05858 | 50.63297 Lyon | N/A | France | 4.84671 | 45.74846 Nantes | N/A | France | -1.55336 | 47.21725 Paris | N/A | France | 2.3488 | 48.85341 Pessac | N/A | France | -0.6324 | 44.80565 Poitiers | N/A | France | 0.34348 | 46.58261 Strasbourg | N/A | France | 7.74553 | 48.58392 Dresden | N/A | Germany | 13.73832 | 51.05089 Groenkloof | N/A | Germany | N/A | N/A Hamburg | N/A | Germany | 9.99302 | 53.55073 Leipzig | N/A | Germany | 12.37129 | 51.33962 Mainz | N/A | Germany | 8.2791 | 49.98419 Mannheim | N/A | Germany | 8.46694 | 49.4891 Budapest | N/A | Hungary | 19.04045 | 47.49835 Dublin | N/A | Ireland | -6.24889 | 53.33306 Ramat Gan | N/A | Israel | 34.81065 | 32.08227 Bari | N/A | Italy | 16.86982 | 41.12066 Bologna | N/A | Italy | 11.33875 | 44.49381 Milan | N/A | Italy | 12.59836 | 42.78235 Napoli | N/A | Italy | 14.5195 | 40.87618 Orbassano | N/A | Italy | 7.53813 | 45.00547 Roma | N/A | Italy | 11.10642 | 44.99364 Trondheim | N/A | Norway | 10.39506 | 63.43049 Lima | Lima Province | Peru | -77.02824 | -12.04318 Quezon City | N/A | Philippines | 121.0509 | 14.6488 Katowice | N/A | Poland | 19.02754 | 50.25841 Krakow | N/A | Poland | 19.93658 | 50.06143 Lublin | N/A | Poland | 22.56667 | 51.25 Warsaw | N/A | Poland | 21.01178 | 52.22977 San Juan | N/A | Puerto Rico | -66.10572 | 18.46633 Moscow | N/A | Russia | 37.61556 | 55.75222 Saint Petersburg | N/A | Russia | 30.31413 | 59.93863 Singapore | N/A | Singapore | 103.85007 | 1.28967 Bloemfontein | Free State | South Africa | 26.214 | -29.12107 Parktown | Gauteng | South Africa | 28.02671 | -26.18205 Soweto | Gauteng | South Africa | 27.85849 | -26.26781 Kyunggi-Do | N/A | South Korea | N/A | N/A Barcelona | N/A | Spain | 2.15899 | 41.38879 Madrid | N/A | Spain | -3.70256 | 40.4165 Gothenburg | N/A | Sweden | 11.96679 | 57.70716 Lund | N/A | Sweden | 13.19321 | 55.70584 Stockholm | N/A | Sweden | 18.06871 | 59.32938 Umeå | N/A | Sweden | 20.25972 | 63.82842 Uppsala | N/A | Sweden | 17.63889 | 59.85882 Basel | N/A | Switzerland | 7.57327 | 47.55839 Bellinzona | N/A | Switzerland | 9.01703 | 46.19278 Taipei | N/A | Taiwan | 121.52639 | 25.05306 Taoyuan District | N/A | Taiwan | 121.3187 | 24.9896 Bangkok | N/A | Thailand | 100.50144 | 13.75398 Glasglow | Central | United Kingdom | N/A | N/A London | Greater London | United Kingdom | -0.12574 | 51.50853 Newcastle | Tyne and Wear | United Kingdom | -5.88979 | 54.21804
0
NCT00103844
[ 4 ]
349
RANDOMIZED
PARALLEL
2DIAGNOSTIC
2DOUBLE
false
0ALL
false
The purpose of this 14 week, randomized, double-blind, placebo controlled study is to assess the safety and efficacy of aripiprazole to placebo as adjunctive treatment to an assigned open-label marketed antidepressant therapy (ADT) in patients with Major Depressive Disorder who demonstrate an incomplete response to a prospective eight week trial of the same assigned open-label marketed antidepressant therapy.
null
Major Depressive Disorder
Single or recurrent non-psychotic episode of Major Depressive Disorder
null
2
arm 1: None arm 2: None
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: Tablets, Oral, 2 - 20 mg variable dose once daily, 14 weeks intervention 2: Tablets, Oral, 2 - 20 mg variable dose once daily, 14 weeks
intervention 1: Aripiprazole+ ADT intervention 2: Placebo+ ADT
34
Birmingham | Alabama | United States | -86.80249 | 33.52066 San Diego | California | United States | -117.16472 | 32.71571 Washington D.C. | District of Columbia | United States | -77.03637 | 38.89511 Coral Springs | Florida | United States | -80.2706 | 26.27119 Augusta | Georgia | United States | -81.97484 | 33.47097 Smyrna | Georgia | United States | -84.51438 | 33.88399 Chicago | Illinois | United States | -87.65005 | 41.85003 Edwardsville | Illinois | United States | -89.95316 | 38.81144 Hoffman Estates | Illinois | United States | -88.0798 | 42.04281 Springfield | Illinois | United States | -89.64371 | 39.80172 Witchita | Kansas | United States | N/A | N/A New Orleans | Louisiana | United States | -90.07507 | 29.95465 Baltimore | Maryland | United States | -76.61219 | 39.29038 Farmington Hills | Michigan | United States | -83.37716 | 42.48531 Flint | Michigan | United States | -83.68746 | 43.01253 Minneapolis | Minnesota | United States | -93.26384 | 44.97997 Saint Paul | Minnesota | United States | -93.09327 | 44.94441 Las Vegas | Nevada | United States | -115.13722 | 36.17497 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Dayton | Ohio | United States | -84.19161 | 39.75895 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Portland | Oregon | United States | -122.67621 | 45.52345 Media | Pennsylvania | United States | -75.38769 | 39.91678 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Charleston | South Carolina | United States | -79.93275 | 32.77632 Columbia | South Carolina | United States | -81.03481 | 34.00071 Austin | Texas | United States | -97.74306 | 30.26715 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Charlottesville | Virginia | United States | -78.47668 | 38.02931 Bellevue | Washington | United States | -122.20068 | 47.61038 Brown Deer | Wisconsin | United States | -87.96453 | 43.16334 Middleton | Wisconsin | United States | -89.50429 | 43.09722
0
NCT00105196
[ 2 ]
48
NON_RANDOMIZED
SINGLE_GROUP
2DIAGNOSTIC
0NONE
false
0ALL
false
The purpose of this clinical research study is to establish the maximum tolerated dose and recommended Phase II dose of Erbitux™ in combination with Irinotecan in pediatric and adolescent patients with refractory solid tumors.
null
Cancer Refractory Solid Tumor
null
2
arm 1: 1-12 years old arm 2: 13-18 years old
[ 1, 1 ]
2
[ 0, 0 ]
intervention 1: Intravenous (IV) cetuximab 75 - 250 mg/m2 depending on dose escalation for MTD, weekly; irinotecan was administered at a dose of 16 or 20 mg/m2 or per dose escalation, administered x5 days x2 weeks, separated by 2 days off, every 21 days. intervention 2: Intravenous (IV) cetuximab 75 - 250 mg/m2 depending on dose escalation for MTD, weekly; irinotecan was administered at a dose of 20 mg/m2 or per dose escalation, administered x5 days x2 weeks, separated by 2 days off, every 21 days.
intervention 1: Cetuximab + Irinotecan intervention 2: Cetuximab + Irinotecan
9
Phoenix | Arizona | United States | -112.07404 | 33.44838 Tucson | Arizona | United States | -110.92648 | 32.22174 Denver | Colorado | United States | -104.9847 | 39.73915 Gainesville | Florida | United States | -82.32483 | 29.65163 Atlanta | Georgia | United States | -84.38798 | 33.749 Baltimore | Maryland | United States | -76.61219 | 39.29038 New York | New York | United States | -74.00597 | 40.71427 Nashville | Tennessee | United States | -86.78444 | 36.16589 Houston | Texas | United States | -95.36327 | 29.76328
0
NCT00110357
[ 3 ]
101
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
true
This is a randomized, double blind, placebo controlled, multicenter, phase II study to compare the anti-tumor activity as measured by progression-free survival (PFS) and the tolerability of Sorafenib in combination with Dacarbazine (DTIC) versus DTIC in combination with placebo in subjects with unresectable Stage III or Stage IV melanoma who have not received prior cytotoxic chemotherapy. A total of approximately 98 subjects will be randomized to receive DTIC + Sorafenib or DTIC + Placebo.
null
Cancer Melanoma
null
2
arm 1: Sorafenib, 2 tablets (200 mg each) orally twice daily (bid) on study days 1-21 + Dacarbazine, 1000 mg/m\^2 intravenous on study day 1 (21 days per cycle) for double-blind (DB) treatment. Subjects who discontinued DB treatment with complete response (CR), partial response (PR) or stable disease (SD) entered active follow up period. Subjects who discontinued DB treatment with disease progression (DP) entered long term follow up period. arm 2: Placebo, 2 tablets orally twice daily on study days 1-21 + Dacarbazine, 1000 mg/m\^2 intravenous on study day 1 (21 days per cycle) for double-blind (DB) treatment. Subjects who discontinued DB treatment with complete response (CR), partial response (PR) or stable disease (SD) entered active follow up period. Subjects who discontinued DB treatment with disease progression (DP) entered long term follow up period.
[ 0, 1 ]
3
[ 0, 0, 0 ]
intervention 1: Sorafenib, 400 mg, 2 tablets (200 mg each) po (per os) bid (twice daily) Study days 1-21 intervention 2: Placebo, 2 tablets, po (per os) bid (twice daily) Study days 1-21 intervention 3: Dacarbazine, 1000 mg/m\^2 intravenous on Study Day 1
intervention 1: Sorafenib (Nexavar, BAY43-9006) intervention 2: Placebo intervention 3: Dacarbazine
14
Tucson | Arizona | United States | -110.92648 | 32.22174 Aurora | Colorado | United States | -104.83192 | 39.72943 Lakeland | Florida | United States | -81.9498 | 28.03947 Park Ridge | Illinois | United States | -87.84062 | 42.01114 Boston | Massachusetts | United States | -71.05977 | 42.35843 Boston | Massachusetts | United States | -71.05977 | 42.35843 Boston | Massachusetts | United States | -71.05977 | 42.35843 St Louis | Missouri | United States | -90.19789 | 38.62727 Omaha | Nebraska | United States | -95.94043 | 41.25626 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Hilton Head Island | South Carolina | United States | -80.73816 | 32.19382 Nashville | Tennessee | United States | -86.78444 | 36.16589 San Antonio | Texas | United States | -98.49363 | 29.42412
0
NCT00110994
[ 3 ]
27
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
null
This phase II trial is studying how well sorafenib works in treating patients with progressive regional or metastatic cancer of the urothelium. Sorafenib may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth and by blocking blood flow to the tumor.
PRIMARY OBJECTIVES: I. To evaluate the 4-month progression-free survival rate, response rate and toxicity of BAY 43-9006 in patients with progressing regional or metastatic transitional cell carcinoma (or mixed histologies containing a component of TCC) of the urothelium who have progressed on one and only one prior systemic chemotherapy regimen for metastatic disease. SECONDARY OBJECTIVES: I. To determine the time to disease progression and overall survival with BAY 43-9006. II. To evaluate the frequency of polymorphisms in drug metabolizing enzymes and to correlate these polymorphisms with variations in BAY 43-9006 pharmacokinetics. III. To evaluate the frequency of raf kinase mutations in tumor specimens and correlate these with response rate. IV. To evaluate serum VEGF levels as potential markers of angiogenesis inhibition by BAY 43-9006. V. To evaluate markers of apoptosis and kinase inhibition in peripheral blood mononuclear cells as potential biomarkers of BAY 43-9006 activity. VI. To determine if there are proteins differentially translated from the genome in patients who respond to treatment with BAY 43-9006 versus patients who do not respond to BAY 43-9006. OUTLINE: This is a multicenter study. Patients receive oral sorafenib twice daily on days 1-56. Courses repeat every 56 days in the absence of disease progression or unacceptable toxicity. After completion of study treatment, patients are followed every 3 months until 2 years from study entry and then every 6 months until 3 years from study entry.
Adenocarcinoma of the Bladder Distal Urethral Cancer Metastatic Transitional Cell Cancer of the Renal Pelvis and Ureter Proximal Urethral Cancer Recurrent Bladder Cancer Recurrent Transitional Cell Cancer of the Renal Pelvis and Ureter Recurrent Urethral Cancer Regional Transitional Cell Cancer of the Renal Pelvis and Ureter Squamous Cell Carcinoma of the Bladder Stage III Bladder Cancer Stage IV Bladder Cancer Transitional Cell Carcinoma of the Bladder Urethral Cancer Associated With Invasive Bladder Cancer
null
1
arm 1: Patients receive oral sorafenib twice daily on days 1-56. Courses repeat every 56 days in the absence of disease progression or unacceptable toxicity.
[ 0 ]
2
[ 0, 10 ]
intervention 1: Given PO intervention 2: Optional correlative studies
intervention 1: sorafenib tosylate intervention 2: laboratory biomarker analysis
1
Boston | Massachusetts | United States | -71.05977 | 42.35843
0
NCT00112905
[ 2, 3 ]
6
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
The goals of this clinical research study are to see how individuals with advanced head and neck cancer respond to treatment with the new drug thrombospondin (ABT-510) and to learn how effective it is in destroying cancer cells. The safety of ABT-510 and the effect ABT-510 has on cells in the body will also be studied.
This is a phase Ib/II, single-center, open-label study designed to assess the safety, tolerability, pharmacokinetics, and biologic efficacy of ABT-510 (thrombospondin). Participants will be patients with incurable head and neck cancer. Patients will begin at a fixed dose level of thrombospondin subcutaneously twice daily. Cycles of treatment are 28 days (4 weeks). Patients will be treated with thrombospondin until progression of tumor or toxicity.
Head and Neck Cancer
Head and Neck Cancer Thrombospondin Analogue ABT-510 Antiangiogenic agent Lung Skin Thyroid
null
1
arm 1: Fixed dose level of thrombospondin 100 mg subcutaneously twice daily.
[ 0 ]
1
[ 0 ]
intervention 1: 100 mg subcutaneously twice daily
intervention 1: ABT-510
1
Houston | Texas | United States | -95.36327 | 29.76328
0
NCT00113334
[ 4 ]
18
RANDOMIZED
CROSSOVER
0TREATMENT
2DOUBLE
false
0ALL
null
Study Question: In premature infants with apnea and/or bradycardia attributed to gastroesophageal reflux disease (GERD), does treatment with medications (acid blockers and motility agents), compared to placebo, reduce the frequency of apnea and bradycardia? Background: Many clinicians believe that apnea and bradycardia in preterm infants may be caused by gastroesophageal reflux (GER), however, studies have failed to demonstrate even a temporal association between episodes of GER and apnea. There have been no prospective randomized trials of treatment for GERD in preterm infants with apnea or other symptoms attributed to GER. Methods: A randomized, cross-over study will be performed. This cross-over design will provide the patient's clinician with unbiased information about the patient's response to treatment. The clinician can use this information in deciding whether or not to continue treatment after the two-week study period.
Study Question: In premature infants with apnea and/or bradycardia attributed to GERD, does treatment with H2 blockers and prokinetic agents, compared to placebo, reduce the frequency of apnea and bradycardia? Background: The incidence of gastroesophageal reflux (GER) has been reported in as many as 50% of healthy term infants and 63% of preterm infants. Anecdotal observations of apnea and bradycardia clustered around feedings or with an episode of vomiting have suggested to clinicians that apnea and bradycardia in preterm infants may be caused by reflux, however, studies have failed to demonstrate even a temporal association between episodes of GER and apnea. One retrospective study concluded that anti-reflux medications did not reduce the frequency of apnea in premature infants. There have been no prospective randomized trials of treatment for GERD in preterm infants with apnea or other symptoms attributed to GER. Despite the lack of evidence supporting a causal relationship between GER and respiratory problems in preterm infants and the lack of data regarding the efficacy or safety of the treatments for GERD, many clinicians continue to believe that GER causes respiratory symptoms in preterm infants and these infants are commonly treated with medications for GERD. Specific aims: To determine whether medications for GER are effective in reducing respiratory symptoms attributed to GER. Methods: A randomized, controlled masked cross-over study will be performed. The cross-over design will prevent evaluation of long-term outcomes but will increase the power to evaluate short-term outcomes by using the patient as his/her own control. This cross-over design will also provide the patient's clinician with unbiased information about the patient's response to treatment. The clinician can use this information in deciding whether or not to continue treatment after the two-week study period. This approach for making therapeutic decisions in individual patients has been described as an "N of 1" trial.
Gastroesophageal Reflux
null
2
arm 1: 3-day course of anti-reflux medications, followed by 7-day course placebo, followed by 4-day course anti-reflux medications. All study medication administered via nipple or orogastric (OG) tube. Metaclopramide (anti-reflux) given in 0.1mg/kg/dose q6hrs, 30min. prior to feedings. Ranitidine, 3mg/kg/dose, q12hrs. Saline placebo at same respective volumes. arm 2: 3-day course placebo, followed by 7-day course anti-reflux medication, followed by 4-day course placebo. All study medication administered via nipple or OG tube. Metaclopramide (anti-reflux) given in 0.1mg/kg/dose q6hrs, 30min. prior to feedings. Ranitidine, 3mg/kg/dose, q12hrs. Saline placebo at same respective volumes.
[ 5, 5 ]
3
[ 0, 0, 0 ]
intervention 1: None intervention 2: None intervention 3: None
intervention 1: Metaclopramide intervention 2: Ranitidine intervention 3: placebo
1
Houston | Texas | United States | -95.36327 | 29.76328
0
NCT00131248
[ 4 ]
336
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
null
The purpose of this study is to evaluate long-term safety,tolerability and blood pressure effects of metoprolol versus nebivolol in patients with hypertension. These drugs may be given alone or in combination with other drugs that are commonly used in the treatment of hypertension
Approximately 50 million Americans have hypertension defined as a systolic blood pressure (SBP) greater then or equal to 140 mmHg and/or a diastolic blood pressure (DBP) greater then or equal to 90 mmHg. To control blood pressure, more than 2 agents are required in many patients. The current study is a randomized, titration-to-effect, open-label, multi center study. Patients will be randomized to either nebivolol or metoprolol. The dose of the randomized treatment can be titrated as needed to achieve blood pressure control. If necessary, additional antihypertensive agents (calcium antagonist, diuretic, etc.) can be added to achieve control. Patients will be seen every 1-3 months for approximately 18 months to assess long-term safety, tolerability and effectiveness of nebivolol versus metoprolol.
Hypertension
safety and tolerability study hypertension beta-blockers
null
2
arm 1: Nebivolol arm 2: Metoprolol
[ 0, 1 ]
2
[ 0, 0 ]
intervention 1: Patients randomized to nebivolol will initiate therapy with nebivolol 5 mg once daily for 4 weeks. intervention 2: Patients randomized to metoprolol will initiate therapy with 100 mg once daily for 4 weeks.
intervention 1: Nebivolol (NEB) intervention 2: Metoprolol (MET)
1
Morgantown | West Virginia | United States | -79.9559 | 39.62953
0
NCT00142584
[ 3 ]
114
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
true
1FEMALE
false
The purpose of this study is to determine if the combination therapy of lifestyle intervention and use of Metformin together will improve ovulation induction and hyperandrogenemia in women with polycystic ovary syndrome, by gathering data from adult and adolescent females.
PCOS is characterized by excess circulating androgen levels and chronic anovulation. PCOS is also characterized by insulin resistance and hyperinsulinemia. Several recent studies in a variety of non-hospital based populations have provided evidence that the incidence of hyperandrogenic chronic anovulation is in the range of 4-6% of the female population. Improvements in insulin sensitivity in women with PCOS, either through lifestyle changes or through pharmaceutical intervention, have consistently resulted in a marked improvement in the reproductive and metabolic abnormalities in PCOS. The primary objective in the adult female population is to determine that combination therapy will improve ovulatory frequency. Secondary objective is to improve circulating hyperandrogenemia and insulin sensitivity then single agent therapy. The primary objective of the adolescent population is to determine that the combination therapy will improve hyperandrogenemia. Secondary objective is to improve ovulatory frequency and insulin sensitivity than just the use of a single agent therapy.
Polycystic Ovary Syndrome
Polycystic Ovary Syndrome (PCOS) Anovulation Elevated Testosterone
null
2
arm 1: Metformin arm 2: Placebo
[ 0, 2 ]
3
[ 0, 0, 5 ]
intervention 1: Medication was initiated in a step-up fashion every five days, from one tablet per day to four (500 mg per tablet). intervention 2: Placebo intervention 3: A combined intervention of diet and exercise was employed with the goal of achieving an average weight loss of at least 7% of initial body weight over six months with a prescription of 150 min/week of exercise combined with a low-calorie diet.
intervention 1: Metformin intervention 2: Placebo intervention 3: Lifestyle Intervention
1
Hershey | Pennsylvania | United States | -76.65025 | 40.28592
0
NCT00151411
[ 2 ]
21
NON_RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
false
The purpose of the study was to assess the steady-state pharmacokinetics (PK) of efavirenz (EFV) in human immunodeficiency virus type 1 (HIV-1) infected subjects on stable antiretroviral regimens containing EFV, and having selected degrees of hepatic impairment or normal hepatic function.
null
HIV Infections Hepatic Impairment
null
4
arm 1: None arm 2: None arm 3: None arm 4: None
[ 0, 0, 0, 1 ]
4
[ 0, 0, 0, 0 ]
intervention 1: Capsule or Tablet, Oral, once daily for 2 days intervention 2: Capsule or Tablet, Oral, once daily for 2 days intervention 3: Capsule or Tablet, Oral, once daily for 2 days intervention 4: Capsule or Tablet, Oral, once daily for 2 days
intervention 1: efavirenz containing antiretroviral regimen intervention 2: efavirenz containing antiretroviral regimen intervention 3: efavirenz containing antiretroviral regimen intervention 4: efavirenz containing antiretroviral regimen
4
Baltimore | Maryland | United States | -76.61219 | 39.29038 San Antonio | Texas | United States | -98.49363 | 29.42412 Richmond | Virginia | United States | -77.46026 | 37.55376 Milan | N/A | Italy | 12.59836 | 42.78235
0
NCT00162097
[ 3 ]
28
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
false
Enzastaurin given daily to participants with colorectal cancer who have Stage 4 disease and have not received prior chemotherapy for advanced colorectal cancer
null
Colonic Neoplasms
null
1
arm 1: None
[ 0 ]
1
[ 0 ]
intervention 1: 1200 milligrams (mg) loading dose orally, then 500 mg, orally, daily, up to six 28-day cycles.
intervention 1: Enzastaurin HCl
3
Odense | N/A | Denmark | 10.38831 | 55.39594 Vejle | N/A | Denmark | 9.5357 | 55.70927 Uppsala | N/A | Sweden | 17.63889 | 59.85882
0
NCT00192114
[ 2, 3 ]
3
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
0ALL
true
Netherton syndrome is a genetic condition that can result in abnormal skin functioning. People with this condition often have red and scaling skin; sparse or short hair; and problems with absorption of medicines or chemicals that are applied to the skin. If these chemicals are absorbed at a high level, they may cause health problems. Elidel (pimecrolimus) is a new medicine that is available as a cream. It has been shown to help improve the appearance of the skin in patients with another skin condition known as atopic dermatitis, and is approved by the United States (US) Food and Drug Administration for use in children with mild to moderate atopic dermatitis. The purpose of this study is to determine if Elidel is safe, to see whether the medication is absorbed through the skin, and to see if side effects are associated with its use in children with Netherton syndrome.
Patients with Netherton syndrome, a rare genodermatosis, manifest a chronic, eczematous dermatitis with erythema and scaling that is often recalcitrant to conventional therapy with emollients and topical corticosteroids. These patients display an altered epidermal barrier with increased permeability to topical agents and are therefore susceptible to evaporative transepidermal water loss and infection. Topical therapy with the calcineurin inhibitors tacrolimus and pimecrolimus has been demonstrated to improve the skin integrity and the quality of life of patients with several chronic dermatoses, including atopic dermatitis. As a result of the underlying skin barrier dysfunction, however, the possibility of significant systemic absorption and resultant side effects is a concern when these agents are used in patients with Netherton syndrome. Experience with topical tacrolimus 0.1% ointment for patients with Netherton syndrome has demonstrated both marked efficacy as well as significant systemic absorption of the drug in this patient population. Use of topical pimecrolimus in patients with Netherton syndrome has not been reported to date. Investigation of the extent of systemic absorption and side effects will help to define the safety and efficacy profile of topical pimecrolimus in patients with Netherton syndrome.
Netherton Syndrome
null
1
arm 1: Treatment with drug/Elidel. Single arm-open-label treatment arm. A Pilot Study of the Efficacy and Safety of Pimecrolimus Cream 1% for the Treatment of Netherton Syndrome:
[ 0 ]
1
[ 0 ]
intervention 1: Open label single arm
intervention 1: Pimecrolimus 1% Cream
1
Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238
0
NCT00208026
[ 4 ]
63
RANDOMIZED
PARALLEL
1PREVENTION
2DOUBLE
false
2MALE
true
Risedronate is an orally administered pyridinyl bisphosphonate that is 36 times more potent than pamidronate and 72 times more potent than clodronate. Four randomized, double-blind trials have been carried out in patients with postmenopausal osteoporosis. In 2 of these studies, vertebral fracture incidence was reduced by a daily dose of 5 mg risedronate by up to 65% and 49% relative to placebo after 1 and 3 years, respectively. In these trials, risedronate improved lumbar spine, femoral neck, and femoral trochanter bone mineral density (BMD) at 6 months. In addition, preclinical studies have shown that risedronate is more potent than pamidronate and clodronate in inhibiting adhesion of prostate cancer cells to bone and preventing tumor cell invasion. The incidence of osteoporosis in prostate cancer patients has been well established; therefore, it is advantageous to assess the efficacy of oral bisphosphonate therapy.
OUTLINE: This is a randomized, placebo-controlled, double-blind, multicenter, 2 arm study. The study population will consist of prostate cancer patients with metastatic bone disease for whom androgen-deprivation therapy is planned. After stratification based on the patient's age, performance status, and severity of metastatic disease, the patients will be randomized at a 1:1 ratio to the following treatment arms: * Daily oral risedronate combined with androgen deprivation * Daily oral placebo combined with androgen deprivation Initial clinical evaluation will be performed during the 2-week screening period. While patients receive per-protocol treatment, study assessments will be performed every 4 weeks during the first 3 months, and every 12 weeks thereafter. Performance Status: Eastern Cooperative Oncology Group (ECOG) 0 to 2 Life Expectancy: At least 12 weeks Hematopoietic: * Absolute neutrophil count (ANC) \> 1,000/mm3 * Platelet count \> 100,000/mm3 * international normalized ratio (INR) \< 1.5 x upper limit of normal unless on therapeutic anticoagulation * Partial thromboplastin time (PTT) \< 1.5 x upper limit of normal unless on therapeutic anticoagulation Hepatic: * Bilirubin \< 1.5 mg/dL * Alanine transaminase (ALT) \< 2.5 x upper limit of normal Renal: * Creatinine clearance of \> 30 mL/min (by Cockcroft-Gault) Cardiovascular: * No significant history of uncontrolled cardiac disease (i.e., uncontrolled hypertension, unstable angina, and congestive heart failure). Pulmonary: * Not specified Calcium: * Corrected serum calcium = (4.0 g/dL - actual albumin g/dL)x 0.8 + serum calcium
Metastatic Prostate Cancer
null
2
arm 1: Daily oral risedronate combined with androgen deprivation arm 2: daily oral placebo combined with androgen deprivation
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: Daily oral risedronate combined with androgen deprivation intervention 2: Daily oral placebo combined with androgen deprivation
intervention 1: Risedronate intervention 2: Placebo
45
La Mesa | California | United States | -117.02308 | 32.76783 San Bernardino | California | United States | -117.28977 | 34.10834 New Britain | Connecticut | United States | -72.77954 | 41.66121 Tampa | Florida | United States | -82.45843 | 27.94752 Galesburg | Illinois | United States | -90.37124 | 40.94782 Peoria | Illinois | United States | -89.58899 | 40.69365 Evansville | Indiana | United States | -87.55585 | 37.97476 Goshen | Indiana | United States | -85.83444 | 41.58227 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Muncie | Indiana | United States | -85.38636 | 40.19338 South Bend | Indiana | United States | -86.25001 | 41.68338 Baltimore | Maryland | United States | -76.61219 | 39.29038 Greenbelt | Maryland | United States | -76.87553 | 39.00455 Rochester | Minnesota | United States | -92.4699 | 44.02163 Kansas City | Missouri | United States | -94.57857 | 39.09973 St Louis | Missouri | United States | -90.19789 | 38.62727 Reno | Nevada | United States | -119.8138 | 39.52963 New Brunswick | New Jersey | United States | -74.45182 | 40.48622 Trenton | New Jersey | United States | -74.74294 | 40.21705 Garden City | New York | United States | -73.6343 | 40.72677 Staten Island | New York | United States | -74.13986 | 40.56233 Cleveland | Ohio | United States | -81.69541 | 41.4995 Springfield | Oregon | United States | -123.02203 | 44.04624 Lancaster | Pennsylvania | United States | -76.30551 | 40.03788 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Seattle | Washington | United States | -122.33207 | 47.60621 Tacoma | Washington | United States | -122.44429 | 47.25288 La Crosse | Wisconsin | United States | -91.23958 | 43.80136 Kelowna | British Columbia | Canada | -119.48568 | 49.88307 Surrey | British Columbia | Canada | -122.82509 | 49.10635 Victoria | British Columbia | Canada | -123.35155 | 48.4359 Fredericton | New Brunswick | Canada | -66.66558 | 45.94541 Barrie | Ontario | Canada | -79.66634 | 44.40011 Burlington | Ontario | Canada | -79.83713 | 43.38621 Burlington | Ontario | Canada | -79.83713 | 43.38621 Hamilton | Ontario | Canada | -79.84963 | 43.25011 Kingston | Ontario | Canada | -76.48098 | 44.22976 London | Ontario | Canada | -81.23304 | 42.98339 Newmarket | Ontario | Canada | -79.46631 | 44.05011 Oakville | Ontario | Canada | -79.68292 | 43.45011 Scarborough Village | Ontario | Canada | -79.22124 | 43.73899 Toronto | Ontario | Canada | -79.39864 | 43.70643
0
NCT00216060
[ 4 ]
243
RANDOMIZED
PARALLEL
0TREATMENT
3TRIPLE
false
0ALL
true
In a previous phase II study, patients with pathological stage IIIb (without pleural effusion) NSCLC were treated with concurrent cisplatin and etoposide plus thoracic radiotherapy followed by 3 cycles of consolidation therapy with docetaxel. Docetaxel was selected based upon a survival benefit in patients with recurrent NSCLC. This trial will evaluate the role of consolidation therapy with docetaxel in patients with unresectable stage III disease. The purpose of the trial is to evaluate survival and toxicities of the regimens employed.
OUTLINE: This is a multi-center study. * Cisplatin 50 mg/m2 d1, 8, 29, 36 * Etoposide 50 mg/m2/day d1-5, 29-33 * Radiation 5940 cGy (180 cGy/day) Patients with CR, PR, SD Randomized to either:Docetaxel75 mg/m2 q3wk X 3 cycles or Observation Only Performance Status: ECOG 0 or 1 Life Expectancy: Not specified Hematopoietic: * ANC \> 1,500/mm3 * Platelet count \> 100,000/mm3 * Hemoglobin \> 8 g/dl. PRBC transfusions will be allowed to increase hemoglobin to \>8 g/dl Hepatic: * Serum bilirubin \< institutional upper limit of normal (ULN) * AST \< 2.5 X the upper limits of normal if alkaline phosphatase is \< ULN, or alkaline phosphatase may be up to 4 X ULN if AST are \< ULN Renal: * Serum creatinine of \< 2 mg/dl or calculated creatinine clearance \> 50 cc/min Cardiovascular: * No clinically significant history of cardiac disease, (i.e. uncontrolled hypertension, unstable angina, congestive heart failure, myocardial infarction within the past year, or cardiac ventricular arrhythmias requiring medication). Pulmonary: * Pre-registration FEV1 \> 1 liters by spirometry within 42 days prior to study treatment.
Non-Small Cell Lung Cancer
Non-Small Cell Lung Cancer
null
3
arm 1: Prior to randomization patients received Cisplatin 50 mg/m\^2 days 1,8,29,36 + Etoposide 50 mg/m\^2 days 1-5, 29-33 + Radiation 5940 cGy (180 cGy/day). Patients with CR, PR or SD with manageable toxicity were randomized to either Docetaxel arm or Observation only arm. arm 2: Docetaxel 75 mg/m\^2 q3wk X 3 cycles. arm 3: Patients were followed for Observation.
[ 5, 1, 4 ]
4
[ 0, 0, 4, 0 ]
intervention 1: Cisplatin 50 mg/m2 day 1, 8, 29, 36 intervention 2: Etoposide 50 mg/m2, days 1-5, 29-33 intervention 3: Radiation 5940 cGy (180 cGy/day) intervention 4: docetaxel 75mg/m2 q3wk x 3 cycles
intervention 1: Cisplatin intervention 2: Etoposide intervention 3: Radiation intervention 4: Docetaxel
15
Galesburg | Illinois | United States | -90.37124 | 40.94782 Elkhart | Indiana | United States | -85.97667 | 41.68199 Evansville | Indiana | United States | -87.55585 | 37.97476 Fort Wayne | Indiana | United States | -85.12886 | 41.1306 Goshen | Indiana | United States | -85.83444 | 41.58227 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Muncie | Indiana | United States | -85.38636 | 40.19338 New Albany | Indiana | United States | -85.82413 | 38.28562 South Bend | Indiana | United States | -86.25001 | 41.68338 Terre Haute | Indiana | United States | -87.41391 | 39.4667 St Louis | Missouri | United States | -90.19789 | 38.62727 Omaha | Nebraska | United States | -95.94043 | 41.25626 Houston | Texas | United States | -95.36327 | 29.76328
0
NCT00216125
[ 5 ]
134
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
null
This open, multi-center randomized controlled study is designed to investigate the quality of life in patients with mycophenolate mofetil (MMF)-induced gastrointestinal (GI) adverse events after converting to enteric-coated mycophenolate sodium (EC-MPS).
null
Renal Transplant
QoL GI Side Effects MPA
null
2
arm 1: 250 mg capsules or 500 mg tablets of mycophenolate mofetil. Daily dose decided by physician, was taken morning and evening. arm 2: Oral film-coated gastroresistant tablets containing 360mg or 180mg of mycophenolate sodium. Daily dose decided by the physician, was taken morning and evening.
[ 1, 0 ]
2
[ 0, 0 ]
intervention 1: None intervention 2: None
intervention 1: Enteric-Coated Mycophenolate Sodium (EC-MPS) intervention 2: Mycophenolate Mofetil (MMF)
1
Nottingham | N/A | United Kingdom | -1.15047 | 52.9536
0
NCT00239005
[ 3 ]
185
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
true
The purpose of this study is to determine the efficacy and preferred dose of CoQ10 in individuals with ALS for a possible future phase III study.
Amyotrophic lateral sclerosis (ALS) is a progressive and devastating neurodegenerative disorder. Available treatment for ALS remains scarce. Oxidative stress and mitochondrial dysfunction have been implicated in the pathophysiology of ALS. Oxidative stress refers to the effects of cell-damaging reactive oxygen species, also known as free radicals. Oxidative stress is thought to contribute to nerve cell loss in ALS. Mitochondria are organelles within each cell that are sometimes called "powerhouses of the cell" because cellular energy metabolism is located within the mitochondria. Coenzyme Q10 (CoQ10), a mitochondrial cofactor known for its antioxidant properties, has prolonged survival in the mouse model of ALS and has slowed functional decline in another neurodegenerative disorder, Parkinson's disease. The goals of this double-blind, placebo-controlled, two-dose comparison phase II study are to obtain preliminary efficacy data and to select the preferred dose for a larger phase III study. Participants were randomly assigned to CoQ10 (at two different dose levels) or placebo in the first stage, then the 2,700 mg dose was selected in the second stage. Duration of the trial was 9 months with a total of 7 visits.
Amyotrophic Lateral Sclerosis Lou Gehrig's Disease
amyotrophic lateral sclerosis ALS Lou Gehrig's disease CoQ10 coenzyme Q10 antioxidants free radicals mitochondrial dysfunction
null
3
arm 1: None arm 2: None arm 3: None
[ 0, 2, 0 ]
2
[ 0, 0 ]
intervention 1: antioxidant and mitochondrial cofactor, given in capsules three times daily intervention 2: Placebo capsules, indistinguishable from CoQ10 capsules, given three times daily
intervention 1: coenzyme Q10 intervention 2: Placebo
19
Little Rock | Arkansas | United States | -92.28959 | 34.74648 San Francisco | California | United States | -122.41942 | 37.77493 San Francisco | California | United States | -122.41942 | 37.77493 Denver | Colorado | United States | -104.9847 | 39.73915 New Haven | Connecticut | United States | -72.92816 | 41.30815 Chicago | Illinois | United States | -87.65005 | 41.85003 Chicago | Illinois | United States | -87.65005 | 41.85003 Kansas City | Kansas | United States | -94.62746 | 39.11417 Lexington | Kentucky | United States | -84.47772 | 37.98869 Boston | Massachusetts | United States | -71.05977 | 42.35843 Springfield | Massachusetts | United States | -72.58981 | 42.10148 Minneapolis | Minnesota | United States | -93.26384 | 44.97997 St Louis | Missouri | United States | -90.19789 | 38.62727 New York | New York | United States | -74.00597 | 40.71427 Syracuse | New York | United States | -76.14742 | 43.04812 Cleveland | Ohio | United States | -81.69541 | 41.4995 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 San Antonio | Texas | United States | -98.49363 | 29.42412 Burlington | Vermont | United States | -73.21207 | 44.47588
0
NCT00243932
[ 4 ]
255
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
true
The objective of this study is to evaluate whether Osmotic-Release Methylphenidate (OROS MPH), relative to placebo, increases the effectiveness of standard smoking treatment (i.e., nicotine patch and individual smoking cessation counseling) in obtaining prolonged abstinence for smokers with Attention Deficit Hyperactivity Disorder (ADHD).
The primary objective of this study is to evaluate whether OROS MPH (Concerta), relative to placebo, increases the effectiveness of standard smoking treatment (i.e., nicotine patch and individual smoking cessation counseling) in obtaining prolonged abstinence for smokers with ADHD. The study will involve an estimated 252 participants, recruited from approximately 6 sites.
ADHD Smoking
null
2
arm 1: None arm 2: None
[ 1, 2 ]
2
[ 0, 0 ]
intervention 1: OROS-MPH dosing strategy will start with 18 mg/day for 3 days, increasing to 36mg/day for the next three days; increasing to 54 mg/day in week two, and to 72 mg/day in week three through the remainder of the study (as tolerated). And, nicotine patch dosing schedule will be 21 mg/day during weeks 4-11; 14 mg/day during weeks 12-13; and 7 mg/day in week 14. intervention 2: OROS-MPH (placebo) dosing strategy will start with 18 mg/day for 3 days, increasing to 36mg/day for the next three days; increasing to 54 mg/day in week two, and to 72 mg/day in week three through the remainder of the study (as tolerated). And, nicotine patch dosing schedule will be 21 mg/day during weeks 4-11; 14 mg/day during weeks 12-13; and 7 mg/day in week 14.
intervention 1: Osmotic-Release Methylphenidate intervention 2: Placebo
6
Cambridge | Massachusetts | United States | -71.10561 | 42.3751 Rochester | Minnesota | United States | -92.4699 | 44.02163 New York | New York | United States | -74.00597 | 40.71427 New York | New York | United States | -74.00597 | 40.71427 Columbus | Ohio | United States | -82.99879 | 39.96118 Portland | Oregon | United States | -122.67621 | 45.52345
0
NCT00253747
[ 3, 4 ]
60
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
true
This is a placebo controlled trial (some people receive active and some people receive inactive medication) to evaluate the effectiveness of a new protocol to treat alcohol dependence. Two main medications (plus ancillary non-placebo controlled medications) and their placebos (inactive drugs) will be utilized to treat both alcohol withdrawal, promote abstinence, and reduce drinking over approximately a six-week treatment period. All participants will meet criteria for Alcohol Dependence and be drinking heavily up until 72 hours prior to receiving the first study drug. They will be injected one drug (flumazenil or placebo) over a two day period and receive the second one (gabapentin or placebo) by mouth for 39 days. The main hypothesis is that this protocol will reduce early alcohol withdrawal symptoms and will reduce relapse to drinking and promote abstinence compared to the placebo (inactive) drug group. Secondary outcomes that will be evaluated include reduction in craving, improvement in sleep, brain activity and mood.
Approximately 60 alcohol dependent individuals who are drinking heavily up until 72 hours, or less, prior to study participation will be randomized to receive either flumazenil (intravenously)on two successive days and gabapentin (orally)for 39 days or their matching placebos. They also will receive hydroxyzine and vitamins. Individuals will be evaluated for alcohol withdrawal, their response to acoustic startle, cognitive ability, craving, mood, sleep and drinking during the first week. They will then be seen weekly for about 6 weeks during which they take gabapentin or placebo and are provided with Combined Behavioral Intervention Therapy (counseling) once a week, or more, as required. Over this period they will be evaluated weekly for alcohol consumption, craving, sleep, mood, and biological markers of alcohol consumption ( percent carbohydrate deficient transferrin and gamma-glutamyl transferase). Blood will be obtained on week 3 and 6 for general health (liver, blood count etc.) screening. After the end of treatment, subjects will be followed-up at 4 weeks and again at 8 weeks after treatment to evaluate alcohol consumption, craving, sleep, mood. Subjects will undergo a functional magnetic resonance imaging (MRI) procedure sometime during the second or third week of study medication to assess cue induced regional brain activation to investigate the effect of medication on brain response to alcohol visual cues.
Alcohol Dependence
Alcoholism Alcohol Dependence Alcohol Withdrawal Treatment Pharmacotherapy
null
2
arm 1: 2 mg flumazenil given over 20 minutes on Day 1 and Day 2. Gabapentin 300 mg Day 1; gabapentin 600 mg Day 2; gabapentin 900 mg Day 3; gabapentin 1200 mg Day 4 to 30; gabapentin 900 mg day 31-33; gabapentin 600 mg day 34-36; gabapentin 300 mg day 37-39. arm 2: 20 mg Saline infused slowly over 20 minutes. Placebo 1 capsule Day 1, 2 capsules Day 2, 3 capsules Day 3, 4 capsules days 4 to 30; 3 capsules Day 31 to 33; 2 capsules day 34 to 36 and 1 capsule 37 to 39.
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: 2 mg flumazenil for infusion given slowly over 20 minutes given day 1 and day 2 gabapentin 300 mg increasing to 1200 mg over 4 days and continuing to day 30. Gabapentin 900 mg Day 31 to Day 33 gabapentin 600 mg Day 34 to 36 and gabapentin 300 mg Day 37 to 39. intervention 2: 20 mg Saline infused slowly over 20 minutes. Placebo 1 capsule Day 1, 2 capsules Day 2, 3 capsules Day 3, 4 capsules days 4 to 30; 3 capsules Day 31 to 33; 2 capsules day 34 to 36 and 1 capsule 37 to 39.
intervention 1: Flumazenil and Gabapentin intervention 2: Placebo
1
Charleston | South Carolina | United States | -79.93275 | 32.77632
0
NCT00262639
[ 3 ]
35
NA
SINGLE_GROUP
0TREATMENT
0NONE
false
2MALE
false
RATIONALE: Drugs used in chemotherapy, such as gemcitabine and docetaxel, work in different ways to stop the growth of tumor cells, either by killing the cells or by stopping them from dividing. Giving more than one drug (combination chemotherapy) may kill more tumor cells. PURPOSE: This phase II trial is studying how well giving gemcitabine together with docetaxel works in treating patients with metastatic prostate cancer.
OBJECTIVES: * Determine the objective response rate and toxicity in patients with androgen-independent metastatic prostate cancer treated with gemcitabine hydrochloride and docetaxel. OUTLINE: This is an open-label study. Patients receive gemcitabine hydrochloride IV over 30 minutes on days 1 and 8 followed by docetaxel IV over 60 minutes on day 8. Treatment repeats every 3 weeks for up to 6 courses in the absence of disease progression or unacceptable toxicity. After completion of study treatment, patients are followed periodically for at least 5 years. PROJECTED ACCRUAL: A total of 36 patients will be accrued for this study.
Prostate Cancer
adenocarcinoma of the prostate stage IV prostate cancer
null
1
arm 1: None
[ 0 ]
2
[ 0, 0 ]
intervention 1: docetaxel IV over 60 minutes on day 8. Treatment repeats every 3 weeks for up to 6 courses in the absence of disease progression or unacceptable toxicity. intervention 2: IV over 30 minutes on days 1 and 8 followed by docetaxel IV over 60 minutes on day 8. Treatment repeats every 3 weeks for up to 6 courses in the absence of disease progression or unacceptable toxicity.
intervention 1: docetaxel intervention 2: gemcitabine hydrochloride
1
Cleveland | Ohio | United States | -81.69541 | 41.4995
0
NCT00276549
[ 3 ]
200
NON_RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
true
RATIONALE: A peripheral stem cell transplant or an umbilical cord blood transplant from a donor may be able to replace blood-forming cells that were destroyed by chemotherapy or radiation therapy. Giving an infusion of the donor's white blood cells (donor lymphocyte infusion) after the transplant may help destroy any remaining cancer cells (graft-versus-tumor effect). Sometimes the transplanted cells can make an immune response against the body's normal cells. Methotrexate, cyclosporine, tacrolimus, or methylprednisolone may stop this from happening. PURPOSE: This clinical trial is studying how well a donor stem cell transplant or donor white blood cell infusions work in treating patients with hematologic cancer.
OBJECTIVES: Primary * Determine the effectiveness of unrelated donor allogeneic hematopoietic stem cells for transplantation after conditioning for the treatment of patients with high-risk hematologic malignancies. * Compare survival, disease-free survival (DFS), response rate, and toxicity rates in these patients with historical controls. * Compare the rate and severity of acute and chronic GVHD after allogeneic hematopoietic stem cell transplantation in patients with hematopoietic malignancies with historical controls transplanted with stem cells from related sibling donors * Assess engraftment, long-term hematopoietic recovery, relapse rate, and disease-free survival when allogeneic hematopoietic stem cells are used as a source of stem cells for transplantation in patients with high-risk hematological malignancies. * Assess engraftment, long-term hematopoietic recovery, and overall survival when allogeneic hematopoietic stem cells are used as a source of stem cells for transplantation in patients who have graft failure or graft rejection. * Compare engraftment, long-term hematopoietic recovery, rate of GVHD, rate of relapse, toxicity rates, overall disease-free survival and overall survival when donor leukocyte infusions (DLI) are given for patients who have disease recurrence, progression, or low donor chimerisms after unrelated stem cell transplantation or before DLI with historical controls of other donor leukocyte infusions. Secondary * Determine the quality of life of patients undergoing hematopoietic stem cell transplantation or donor leukocyte infusions from unrelated HLA genotypically-identical donors. OUTLINE: Patients are assigned to 1 of 8 treatment groups. * Group 1\*: Patients undergo total body irradiation (TBI) twice a day on days -7 to -4. Patients then receive cyclophosphamide IV over 1 hour on days -3 and -2. On day 0 patients undergo stem cell transplantation (SCT). Beginning on day 7, patients receive filgrastim (G-CSF) IV once daily until blood counts recover. * Group 2 (patients who have previously experienced dose-limiting radiotherapy): Patients receive oral busulfan 4 times daily on days -7 to -4 and cyclophosphamide IV over 1 hour on days -3 and -2. On day 0 patients undergo SCT. Beginning on day 7, patients receive G-CSF IV once daily until blood counts recover. * Group 3 (pediatric patients only): Patients receive busulfan IV 4 times daily on days -9 to -6 and cyclophosphamide IV over 1 hour and fludarabine IV over 30 minutes on days -5 to -2. On day 0 patients undergo SCT. Beginning on day 7, patients may receive G-CSF IV once daily until blood counts recover. * Group 4 (second SCT for patients who have experienced graft rejection or failure)\*: Patients receive low-dose fludarabine IV over 30 minutes on days -4 to -2. Patients then undergo low-dose TBI once followed by SCT on day 0. Beginning on day 7, patients may receive G-CSF IV once daily until blood counts recover. * Group 5 (patients who developed grade 3 cystitis after prior cyclophosphamide-containing therapy): Patients receive carmustine IV over 2 hours on day -6, etoposide IV over 2 hours and cytarabine IV over 30 minutes on days -5 to -2, and melphalan IV over 30 minutes on day -1 (BEAM). On day 0, patients undergo SCT. Beginning on day 7, patients receive G-CSF IV once daily until blood counts recover. * Group 6 (cord blood transplantation): Patients receive anti-thymocyte globulin IV once daily and methylprednisolone IV twice daily on days -3 to -1. On day 0, patients undergo an umbilical cord blood SCT. * Group 7 (patients with relapsing or progressive disease after prior transplants or low donor chimerisms)\*: Patients must not have existing graft-versus-host disease (GVHD). Patients receive donor lymphocyte infusions with conditioning chemotherapy and/or radiotherapy at the discretion of the investigator. * Group 8 (pediatric patients only)\*: Patients undergo TBI twice a day on days -7 to -5. Patients also receive etoposide IV over 24 hours on day -4 and cyclophosphamide IV over 1 hour on days -3 and -2. On day 0, patients undergo SCT. Beginning on day 7, patients may receive G-CSF IV once daily until blood counts recover. NOTE: \*Patients who have received \> 3000 cGy to the central nervous system or \> 2000 cGy to the lung or liver may not receive any regimen containing total body irradiation (TBI) All patients receive GVHD prophylaxis comprising methotrexate IV on days 1, 3, 6, and 11; cyclosporine and/or tacrolimus on days -2 to 100; and/or methylprednisolone IV on days 7 to 100. Patients with an unrelated donor who experience a relapse prior to transplantation, may proceed directly to transplantation. However, if immediate transplantation from the unrelated donor is not possible, the patient must be re-induced into a complete hematological remission. Patients who experience graft failure or graft rejection after allogeneic transplantation are eligible for a second stem cell infusion from the original donor. Quality of life is assessed at baseline and at 7 days, 3 months, and 1 year after transplantation. After completion of study treatment, patients are followed periodically for survival. PROJECTED ACCRUAL: A total of 43 patients will be accrued for this study.
Chronic Myeloproliferative Disorders Leukemia Lymphoma Multiple Myeloma and Plasma Cell Neoplasm Myelodysplastic Syndromes Myelodysplastic/Myeloproliferative Neoplasms Unusual Cancers of Childhood
adult acute lymphoblastic leukemia in remission L1 adult acute lymphoblastic leukemia L2 adult acute lymphoblastic leukemia L3 adult acute lymphoblastic leukemia recurrent adult acute lymphoblastic leukemia accelerated phase chronic myelogenous leukemia blastic phase chronic myelogenous leukemia chronic phase chronic myelogenous leukemia relapsing chronic myelogenous leukemia childhood acute lymphoblastic leukemia in remission L1 childhood acute lymphoblastic leukemia L2 childhood acute lymphoblastic leukemia L3 childhood acute lymphoblastic leukemia recurrent childhood acute lymphoblastic leukemia recurrent adult Hodgkin lymphoma recurrent/refractory childhood Hodgkin lymphoma stage IV adult Hodgkin lymphoma stage IV childhood Hodgkin lymphoma adult acute myeloid leukemia in remission adult acute myeloid leukemia with 11q23 (MLL) abnormalities adult acute myeloid leukemia with t(15;17)(q22;q12) adult acute myeloid leukemia with t(16;16)(p13;q22) childhood acute myeloid leukemia in remission recurrent adult acute myeloid leukemia recurrent childhood acute myeloid leukemia myelodysplastic/myeloproliferative neoplasm, unclassifiable previously treated myelodysplastic syndromes secondary myelodysplastic syndromes secondary acute myeloid leukemia refractory anemia with excess blasts in transformation refractory anemia with excess blasts refractory anemia chronic myelomonocytic leukemia childhood chronic myelogenous leukemia chronic eosinophilic leukemia primary myelofibrosis chronic neutrophilic leukemia de novo myelodysplastic syndromes atypical chronic myeloid leukemia, BCR-ABL negative extranodal marginal zone B-cell lymphoma of mucosa-associated lymphoid tissue juvenile myelomonocytic leukemia nodal marginal zone B-cell lymphoma noncontiguous stage II adult Burkitt lymphoma noncontiguous stage II adult diffuse large cell lymphoma noncontiguous stage II adult diffuse mixed cell lymphoma noncontiguous stage II adult diffuse small cleaved cell lymphoma noncontiguous stage II adult immunoblastic large cell lymphoma noncontiguous stage II adult lymphoblastic lymphoma noncontiguous stage II grade 1 follicular lymphoma noncontiguous stage II grade 2 follicular lymphoma noncontiguous stage II grade 3 follicular lymphoma noncontiguous stage II mantle cell lymphoma noncontiguous stage II marginal zone lymphoma noncontiguous stage II small lymphocytic lymphoma recurrent adult Burkitt lymphoma recurrent adult diffuse large cell lymphoma recurrent adult diffuse mixed cell lymphoma recurrent adult diffuse small cleaved cell lymphoma recurrent adult immunoblastic large cell lymphoma recurrent adult lymphoblastic lymphoma recurrent childhood large cell lymphoma recurrent childhood lymphoblastic lymphoma recurrent childhood small noncleaved cell lymphoma recurrent grade 1 follicular lymphoma recurrent grade 2 follicular lymphoma recurrent grade 3 follicular lymphoma recurrent mantle cell lymphoma recurrent marginal zone lymphoma recurrent small lymphocytic lymphoma refractory chronic lymphocytic leukemia refractory hairy cell leukemia refractory multiple myeloma splenic marginal zone lymphoma stage I multiple myeloma stage II multiple myeloma stage III adult Burkitt lymphoma stage III adult Hodgkin lymphoma stage III adult diffuse large cell lymphoma stage III adult diffuse mixed cell lymphoma stage III adult diffuse small cleaved cell lymphoma stage III adult immunoblastic large cell lymphoma stage III adult lymphoblastic lymphoma stage III chronic lymphocytic leukemia stage III grade 1 follicular lymphoma stage III grade 2 follicular lymphoma stage III grade 3 follicular lymphoma stage III mantle cell lymphoma stage III marginal zone lymphoma stage III multiple myeloma stage III small lymphocytic lymphoma stage IV adult Burkitt lymphoma stage IV adult diffuse large cell lymphoma stage IV adult diffuse mixed cell lymphoma stage IV adult diffuse small cleaved cell lymphoma stage IV adult immunoblastic large cell lymphoma stage IV adult lymphoblastic lymphoma stage IV chronic lymphocytic leukemia stage IV grade 1 follicular lymphoma stage IV grade 2 follicular lymphoma stage IV grade 3 follicular lymphoma stage IV mantle cell lymphoma stage IV marginal zone lymphoma stage IV small lymphocytic lymphoma stage III childhood Hodgkin lymphoma stage III childhood large cell lymphoma stage III childhood lymphoblastic lymphoma stage III childhood small noncleaved cell lymphoma stage IV childhood large cell lymphoma stage IV childhood lymphoblastic lymphoma stage IV childhood small noncleaved cell lymphoma unusual cancers of childhood childhood myelodysplastic syndromes
null
8
arm 1: None arm 2: None arm 3: On the day of your admission, you will start to take a drug called allopurinol which helps to protect your kidneys as your body works to discharge cells killed off by your chemotherapy and TBI. Chemotherapy will begin on Day -6 with carmustine (BCNU), followed by etoposide (VP-16), cytosine arabinoside (ARA-C), and melphalan. This conditioning regimen is known as the BEAM regimen. The dose of this therapy is high enough to kill cancer cells but will also kill all of your normal blood forming cells. Subjects undergoing the BEAM regimen will not have total body irradiation (TBI). arm 4: A conditioning regimen of low-dose fludarabine and TBI is used in the event that a second donation of hematopoietic stem cells is necessary. Chemotherapy with Fludarabine will begin 4 days prior to your transplant. This drug will be given through the catheter in your chest daily for 3 days. TBI (radiation) will be given to you on the day of your transplant. After your TBI, your donor's stem cells / bone marrow will be given to you through your catheter. The drugs cyclosporine and mycophenolate mofetil (MMF) will be given orally to help you accept your donor's cells. arm 5: On the day of your admission you will start to take a drug called Dilantin which is used to help prevent seizures while you receive your chemotherapy drugs. You will also start to take a drug called allopurinol which helps to protect your kidneys as your body works to discharge cells killed off by your chemotherapy and TBI. On the next day, you will then begin your conditioning therapy with a drug called busulfan. This medicine will be given to you by an infusion into your bloodstream through a small tube in the vein of your arm four times per day for four days. After the busulfan treatment, you will receive 4 doses each of two drugs, cyclophosphamide (also known as Cytoxan) and fludarabine, over 2 hours into your vein. arm 6: If you are undergoing a pre-transplant conditioning regimen prior to undergoing a cord blood transplant, you will receive a drug called ATG to improve your chances of engraftment and decrease your risk of graft versus host disease. You may receive ATG 3 times during your transplant regimen on days -3 through days -1 in addition to your pre-transplant conditioning therapy. Methylprednisolone will also be given during each dose of ATG to help reduce any reactions during infusion. arm 7: Donor Leukocyte Infusions: You will receive DLI from your original transplant donor. This will be given through a vein , usually in your arm. It will be similar to getting a platelet or blood transfusion. You may require more than one DLI. The decision to give you another infusion will be determined by your condition, relapse status, GVHD and how much DLI you were given before. You may need chemotherapy and/or radiation to improve your disease status prior to additional DLI's. arm 8: On the day after your admission, you will start receiving radiation therapy (TBI). Radiation will be given to you 2 times a day for 3 days. On the next day, you will then begin your chemotherapy with a drug called etoposide. This medicine will be given to you by an infusion into your bloodstream through a small tube in the vein of your arm for one day. After the etoposide treatment, on the next day you will receive cyclophosphamide (also known as Cytoxan) for 2 days. When you are given cyclophosphamide, you will also be given a medication called MESNA to help protect your bladder from damage. After you have completed the cyclophosphamide you will rest one day without any anti-cancer therapy. This allows your body time to remove and inactivate the chemotherapy. After a day of rest, you will be given your donor's cells.
[ 1, 1, 1, 1, 1, 1, 1, 1 ]
17
[ 2, 2, 0, 0, 0, 0, 0, 0, 0, 0, 0, 0, 0, 0, 3, 3, 4 ]
intervention 1: Intravenous, 1.5 mg/kg of body weight daily for 7 to 14 days The first dose should be administered over a minimum of 6 hours and over at least 4 hours on subsequent doses through a high-flow vein. intervention 2: Will be given IV at 5 µg/kg/day. The first injection will be administered on day +7, i.e. 7 days after the hematopoietic stem cells are infused. Will be administered until the ANC is 1500 / µl for 2 days. Dose and schedule of G-CSF administration is left to each center's discretion. intervention 3: Patients who take the drug PO, busulfan will be administered at 1 mg/kg/ dose given by mouth every 6 hours for 16 consecutive doses. Pediatric patients who receive busulfan IV continuous infusion will receive a dose of 3.0 mg/kg/IBW if under the age of 2.Pediatric patients over the age of 2 will receive busulfan at a dose of 0.8 mg/kg/dose. intervention 4: 300mg/m2 IV dissolved in 500 cc NS infused over 2 hours into right atrial catheter on day -6. intervention 5: For transplantation, the drug is diluted in 250 to 500 cc of NS or D5W and administered IV over 2 hours. intervention 6: Initial doses will be administered IV at a starting dose of 1.5 mg/kg BID. The infusion will vary from 2-24hr depending on the incidence of side-effects. intervention 7: 400 mg/m2 dissolved in 200cc D5W and infused over 30 minutes into right atrial catheter on days -5, -4, -3, -2. intervention 8: Etoposide administration 200 mg /m2 dissolved in 1 liter NS and infused over 2 hours into right atrial catheter. Infusion to begin after cytarabine administration on days -5, -4, -3, -2. Etoposide administration 50 mg/kg IV over 24 hours, divided into 3 doses. Dilute in normal saline at a concentration of 0.4 mg/ml (Observe for precipitation). Administered IV with continuous infusion over 24 hours. Diuretics may be given for fluid overload. intervention 9: Fludarabine administered at 30 mg/m2 IVPB infused over 30 minutes into right atrial catheter on days -4, -3, -2. Fludarabine administered at 40 mg/m2 IVPB infused over 30 into the right atrial catheter on days -5, -4, -3, and -2. intervention 10: 140 mg /m2 in concentration of 0.45 mg/ml of NS infused over 30 minutes into right atrial catheter on day -1. intervention 11: Administered on days +1, +3, and +7. intervention 12: Methyl-prednisolone is administered IV as a rapid infusion. intervention 13: Mycophenolate may be used as a substitute for Methotrexate intervention 14: A drug used to decrease the risk of graft versus host disease (GvHD). intervention 15: The stem cells will be given to you by intravenous injection (through your vein) using a catheter that was placed prior to beginning chemotherapy. The stem cell infusion takes 1-6 hours. intervention 16: The patient will receive ATG to improve the changes of engraftment and decrease their risk of graft versus host disease. The patient may receive ATG 3 times during their transplant regimen on days -3 through days -1 intervention 17: Radiation will be given to you 2 times a day for 3 or 4 days.
intervention 1: anti-thymocyte globulin intervention 2: filgrastim intervention 3: busulfan intervention 4: carmustine intervention 5: cyclophosphamide intervention 6: cyclosporine intervention 7: cytarabine intervention 8: etoposide intervention 9: fludarabine phosphate intervention 10: melphalan intervention 11: methotrexate intervention 12: methylprednisolone intervention 13: mycophenolate mofetil intervention 14: tacrolimus intervention 15: peripheral blood stem cell transplantation intervention 16: umbilical cord blood transplantation intervention 17: radiation therapy
1
Portland | Oregon | United States | -122.67621 | 45.52345
0
NCT00281879
[ 3 ]
66
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
0ALL
false
This study will determine whether the experimental drug LY686017 can reduce a person's desire for alcohol. A brain chemical called Substance P acts at places in the brain called NK1 receptors. Substance P is released in response to stress and gives rise to behaviors that are thought to represent anxiety. LY686017 blocks Substance P from acting at the NK1 receptors. People between 21 and 65 years of age who have been drinking on a regular basis for at least one month before entering the study, who meet the criteria for alcohol dependence and who have an elevated score on a general test of anxiety may be eligible for this study. Participants are admitted to the NIH Clinical Center for 35 days. They participate in an alcohol treatment program in addition to the research study. After having been withdrawn from alcohol for at least 2 days, participants receive either 50 mg of LY686017 or placebo (an inactive substance that looks like the study drug) every morning for 28 days. In addition to drug treatment, they undergo the following procedures: * Functional magnetic resonance imaging (fMRI): In the last week of the study, subjects undergo MRI to study the amount of blood going to brain structures thought to be involved in anxiety and craving. During the procedure, they look at pictures of faces exhibiting various emotions and pictures related to alcohol. * Cue reactivity: At the beginning and towards the end of the study, subjects are asked to rate their alcohol craving and their anxiety level while they sniff and handle their favorite alcoholic beverage or water. * Metyrapone test: During weeks 1 and 4 of the study, subjects are given metyrapone - a drug that interferes with the body's ability to make the stress hormone cortisol - to determine how LY686017 affects the body's hormonal response. The drop in cortisol from metyrapone administration causes the brain to release ACTH, a hormone that causes the adrenal gland to make cortisol. * Trier test: In the last week of the study, subjects give a 5-minute speech to three people and are then asked to subtract numbers in their head. Then they are asked to rate their feelings and desire for alcohol on two rating scales. Blood is drawn from a saline lock at the beginning and end of the test to measure hormone levels. * Rating scales: Subjects complete an Obsessive Drinking Scale weekly and an Alcohol Urge Questionnaire and Comprehensive Psychiatric Rating Scale twice a week. * Blood tests: Blood samples are collected periodically to check blood chemistries, clotting time, and the amount of LY686017 in the blood.
Background: Alcoholism is a chronic relapsing disorder characterized by cycles of intoxication interspersed with phases of withdrawal and abstinence. Co-morbidity with depression and anxiety disorders is high. Even in absence of independent psychiatric co-morbidity, anxiety symptoms are almost invariably present during early as well as protracted abstinence, sensitized over repeated cycles of intoxication and withdrawal, and are correlated with craving for alcohol upon exposure to alcohol associated cues. This psychopathology is likely to maintain the dependent state since it has been shown that stress and negative affective states are major relapse triggering factors. Substance P, released in the amygdala in response to stress, acts at NK1 receptors as an important mediator of behavioral stress effects in experimental animals. Blockade of this receptor subtype represents a novel principle for anxiolytic like actions, which is well documented in animal models and has some supportive data in humans. Furthermore, decreased opiate reward following NK1 receptor inaction is indicated by the reports that deletion of the NK1 receptor decreases both conditioned place preference and self-administration of opiates, while a similar reduction of alcohol reward is suggested by preliminary data showing decreased voluntary intake of alcohol in NK1 null-mutants. Aims: The present study is aimed at providing an initial, exploratory evaluation of whether the NK1 receptor is a candidate target for treatment of alcohol dependence that would merit further clinical development in conventional, full-scale clinical trial designs. To evaluate this, the aim of the present study is to determine whether NK1 antagonism can beneficially affect, in anxious alcohol dependent subjects during early abstinence, surrogate variables correlated with clinical outcomes, i.e. * reduce craving for alcohol, measured as baseline self-reported urges, or in response to presentation of alcohol associated cues * reduce negative affect * influence corresponding objective measures (brain fMRI responses to alcohol-associated cues and to fear stimuli, respectively; and endocrine stress responses). This study will address this aim using a novel, orally bioavailable and brain penetrant NK1 antagonist. Positive data in this exploratory study would be the first of their kind, and provide a rationale for evaluating the NK1 antagonist for anti-craving / anti-dipsotropic and anti-anxiety actions in alcohol dependent subjects in a longer term, suggesting that it might aid relapse prevention. Methods: The study will be carried out in 50 subjects aged 21-65 years, with alcohol dependence as their primary complaint, and without other serious medical or psychiatric conditions. An additional inclusion criterion will be the presence or history of significant anxiety symptoms on self report. Subjects will be admitted to the NIAAA research inpatient unit at the NIH Clinical Center through a platform training and natural history protocol which provides basic assessments and standard withdrawal treatment if needed. Patients will enter into the present protocol once such treatment, if needed, is completed. The present protocol will be started with a 1 week single blind placebo lead-in. During this phase, a baseline alcohol cue-reactivity session will be carried out according to established procedures, and urges to drink will be assessed. Cue-responsive subjects only, appr. 70% of alcohol dependent inpatients, will be randomized to active treatment or placebo, and enter the active treatment phase. The active treatment arm will receive 50 mg once daily of LY686017by oral intake, while the placebo group will continue to receive placebo in a double-blind fashion. The duration of active treatment will be 3 weeks. Patients will remain hospitalized throughout this protocol. During this period, no psychotropic medication will be allowed, and abstinence from alcohol and other drugs will be monitored. Measures of craving will be obtained using: 1) ratings completed twice a week on the established Alcohol Urge Questionnaire (AUQ); 2) assessments of urge to drink (at baseline and under medication) during an established cue reactivity paradigm during which each patient undergoes an invivo exposure to his or her preferred alcoholic beverage. The medicated cue reactivity session will follow immediately after the Trier Test, a social stress task that independently induces urges for alcohol (stress induced craving); and augments subsequent cue-induced urges (stress-potentiated cue induced craving); 3) weekly assessment of alcohol related cognitions using the Obsessive Drinking Scale (ODS), a pharmacologically validated subscale of the established Obsessive Compulsive Drinking Scale (OCDS). In addition, measures of anxiety and depression symptoms will be obtained twice-weekly using the Comprehensive Psychiatric Rating Scale (CPRS). During the last treatment week, subjects will undergo an fMRI scan using established paradigms to evoke emotional responses, and to evoke alcohol-cue associated responses, respectively. Psychophysiological measures will be obtained in conjunction with the scan. Blood draws will be carried out on the day of the scan to allow for analysis of plasma concentrations of the experimental drug. The neuroendocrine stress response will be probed, using the standard metyrapone challenge test, in unmedicated state following the baseline CR session, and then again under active treatment or placebo following the fMRI scan.
Alcohol Dependence Alcoholism
Anxiety Alcohol Dependence Alcoholism
null
2
arm 1: Subjects received 50 mg of the NK1 antagonist LY686017 orally on a daily basis. arm 2: Subjects received placebo orally on a daily basis
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: 50 mg administered orally on a daily basis intervention 2: Administered on a daily basis
intervention 1: LY686017 intervention 2: Placebo
1
Bethesda | Maryland | United States | -77.10026 | 38.98067
0
NCT00310427
[ 5 ]
90
RANDOMIZED
PARALLEL
0TREATMENT
4QUADRUPLE
false
1FEMALE
false
Preemptive analgesia is an intervention which provides an anesthetic prior to initiating a painful stimulus. This trial is examining the effects of a local anesthetic given at the point of innervation prior to performing a vaginal hysterectomy with suspension sutures.
null
Pain, Postoperative
preemptive analgesia paracervical block vaginal hysterectomy
null
2
arm 1: Active preemptive local analgesia. arm 2: Placebo for preemptive local analgesia.
[ 0, 2 ]
2
[ 0, 0 ]
intervention 1: 20 ml of 0.5% bupivacaine with 1:200,000 epinephrine paracervical injection. intervention 2: 20 ml normal saline injection.
intervention 1: bupivacaine and epinephrine intervention 2: Placebo
1
Scottsdale | Arizona | United States | -111.89903 | 33.50921
0
NCT00318292
[ 5 ]
92
RANDOMIZED
PARALLEL
0TREATMENT
0NONE
false
0ALL
false
This study looked at lipid changes in human immunodeficiency virus type 1 (HIV-1) infected patients when the nucleoside reverse transcriptase inhibitors (NRTIs) in their existing highly active antiretroviral therapy (HAART) regimen were switched to Truvada® (a fixed dose combination tablet of emtricitabine/tenofovir disoproxil fumarate 200 mg/300 mg \[FTC/TDF\]). Subjects continued their nonnucleoside reverse transcriptase inhibitor (NNRTI) or protease inhibitor (PI) at the same dose.
This was a Phase IV, multicenter (in France), open label study. The study was conducted in two phases: a comparative randomized phase, which served the primary objective of the study, and a follow-up phase. Study Phase 1, Day -14 to Week 12: patients were randomized on a 1:1 basis to one of two groups: * A. Truvada (substitution of their current NRTIs by Truvada \[FTC/TDF\] with continuation of their current NNRTI or PI at the same dose) * B. Maintain Baseline Regimen (continuation of previous HAART regimen, i.e., maintained baseline regimen). This phase of the study served the primary objective of the study. Study Phase 2, roll-over follow-up, Week 12 to Week 48: Patients in the Truvada group continued with Truvada + an NNRTI or PI. Patients in the control group could switch their NRTIs to Truvada in this phase of the study (Delayed Truvada group). Patients were assessed for efficacy and safety during both phases of the study.
HIV Infections
HIV 1 Infection
null
4
arm 1: Truvada once daily with continuation of the current NNRTI or PI at randomization arm 2: Maintain baseline regimen arm 3: Truvada once daily with NNRTI or PI (participants from the comparator group who switched to Truvada during Study Phase 2) arm 4: Truvada once daily with NNRTI or PI (all participants who received Truvada during the study, i.e., participants in the Truvada and Delayed Truvada groups)
[ 0, 1, 0, 0 ]
2
[ 0, 0 ]
intervention 1: Truvada + NNRTI or PI. intervention 2: Maintain baseline regimen
intervention 1: Truvada intervention 2: Current HAART regimen
1
Paris | N/A | France | 2.3488 | 48.85341
0
NCT00323492
[ 4 ]
1,554
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
false
The purpose of this study is to evaluate the safety and efficacy of alogliptin, once daily (QD), taken in combination with pioglitazone in adults with type 2 diabetes mellitus.
Over the past 30 years, the prevalence of diabetes has increased dramatically throughout the world due to population growth, aging, urbanization, increasing obesity, and physical inactivity. The total number of people with type 2 diabetes mellitus is projected to rise from 171 million in 2000 to 366 million in 2030. The incidence of type 2 diabetes mellitus in the United States alone is expected to increase from approximately 17 to 30.3 million by the year 2030. Type 2 diabetes mellitus is associated with a number of long-term microvascular and macrovascular complications associated with a reduced quality of life and increased morbidity and mortality. It is anticipated that the increasing incidence of type 2 diabetes mellitus will place an ever-increasing burden on families, increase national expenditures for health care services, and decrease worker productivity. Current pharmacologic interventions for type 2 diabetes mellitus include a diverse range of antidiabetic medications with different mechanisms of action including insulin and insulin analogues, sulfonylureas, metformin, meglitinides, thiazolidinediones, inhibitors of alpha-glucosidase, analogs of glucagon-like peptide-1 and synthetic analogues of human amylin. Despite the variety of medications, many have clinically important or potentially life-threatening side effects, restricted use in many subpopulations, concerns with long-term tolerability, and challenges related to compliance due to side effects and route of administration. All of these reasons contribute to the difficulties patients have achieving the target glycosylated hemoglobin level less than 7%. SYR-322 (alogliptin) is a selective, orally available inhibitor of the dipeptidyl peptidase-4 enzyme. Dipeptidyl peptidase-4 enzyme is thought to be primarily responsible for the in vivo degradation of 2 peptide hormones released in response to nutrient ingestion, namely glucagon-like peptide-1 and glucose-dependent insulinotropic peptide. Both peptides exert important effects on islet beta cells to stimulate glucose-dependent insulin secretion as well as regulating beta cell proliferation and cytoprotection. Glucagon-like peptide-1, but not glucose-dependent insulinotropic peptide, inhibits gastric emptying, glucagon secretion, and food intake. Glucose-dependent insulinotropic peptide has been shown to enhance insulin secretion by direct interaction with a glucose-dependent insulinotropic peptide -specific receptor on islet beta cells. The glucose-lowering actions of glucagon-like peptide-1, but not glucose-dependent insulinotropic peptide, are preserved in patients with type 2 diabetes mellitus. Pioglitazone (ACTOS®) is a thiazolidinedione developed by Takeda Chemical Industries, Ltd. (Osaka, Japan) that is approved for the treatment of type 2 diabetes mellitus. Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma agonist that decreases insulin resistance in the periphery and liver resulting in increased insulin-dependent glucose disposal and decreased hepatic glucose output. Given the complementary mechanisms of action of alogliptin (stimulation of insulin secretion) and pioglitazone (enhancement of insulin sensitivity), the goal of this study is to evaluate the efficacy of the combination of alogliptin with pioglitazone in patients who are inadequately controlled on metformin. Study participation is anticipated to be approximately 7 months.
Type 2 Diabetes Mellitus
Diabetes Mellitus, Type 2 Drug Therapy Diabetes Mellitus, Non Insulin Dependent Glucose Intolerance Hyperglycemia
null
12
arm 1: Alogliptin placebo-matching tablets, orally, once daily and pioglitazone placebo-matching tablets, orally, once daily for up to 26 weeks. arm 2: Alogliptin 12.5 mg, tablets, orally, once daily and pioglitazone placebo-matching tablets, orally, once daily for up to 26 weeks. arm 3: Alogliptin 25 mg, tablets, orally, once daily and pioglitazone placebo-matching tablets, orally, once daily for up to 26 weeks. arm 4: Alogliptin placebo-matching tablets, orally, once daily and pioglitazone 15 mg, tablets, orally, once daily for up to 26 weeks. arm 5: Alogliptin 12.5 mg, tablets, orally, once daily and pioglitazone 15 mg, tablets, orally, once daily for up to 26 weeks. arm 6: Alogliptin 25 mg, tablets, orally, once daily and pioglitazone 15 mg, tablets, orally, once daily for up to 26 weeks. arm 7: Alogliptin placebo-matching tablets, orally, once daily and pioglitazone 30 mg, tablets, orally, once daily for up to 26 weeks. arm 8: Alogliptin 12.5 mg, tablets, orally, once daily and pioglitazone 30 mg, tablets, orally, once daily for up to 26 weeks. arm 9: Alogliptin 25 mg, tablets, orally, once daily and pioglitazone 30 mg, tablets, orally, once daily for up to 26 weeks. arm 10: Alogliptin placebo-matching tablets, orally, once daily and pioglitazone 45 mg, tablets, orally, once daily for up to 26 weeks. arm 11: Alogliptin 12.5 mg, tablets, orally, once daily and pioglitazone 45 mg, tablets, orally, once daily for up to 26 weeks. arm 12: Alogliptin 25 mg, tablets, orally, once daily and pioglitazone 45 mg, tablets, orally, once daily for up to 26 weeks.
[ 2, 0, 0, 1, 0, 0, 1, 0, 0, 1, 0, 0 ]
4
[ 0, 0, 0, 0 ]
intervention 1: Alogliptin tablets. intervention 2: Alogliptin placebo-matching tablets. intervention 3: Pioglitazone tablets. intervention 4: Pioglitazone placebo-matching tablets.
intervention 1: Alogliptin intervention 2: Alogliptin placebo intervention 3: Pioglitazone intervention 4: Pioglitazone placebo
90
Birmingham | Alabama | United States | -86.80249 | 33.52066 Columbiana | Alabama | United States | -86.60721 | 33.17817 Huntsville | Alabama | United States | -86.58594 | 34.7304 Phoenix | Arizona | United States | -112.07404 | 33.44838 Little Rock | Arkansas | United States | -92.28959 | 34.74648 Searcy | Arkansas | United States | -91.73625 | 35.25064 Sherwood | Arkansas | United States | -92.22432 | 34.81509 Burbank | California | United States | -118.30897 | 34.18084 Foothill Ranch | California | United States | -117.66088 | 33.68641 Irvine | California | United States | -117.82311 | 33.66946 Sacramento | California | United States | -121.4944 | 38.58157 San Diego | California | United States | -117.16472 | 32.71571 Temecula | California | United States | -117.14836 | 33.49364 Tustin | California | United States | -117.82617 | 33.74585 Colorado Springs | Colorado | United States | -104.82136 | 38.83388 Washington D.C. | District of Columbia | United States | -77.03637 | 38.89511 Hollywood | Florida | United States | -80.14949 | 26.0112 Kissimmee | Florida | United States | -81.41667 | 28.30468 Miami | Florida | United States | -80.19366 | 25.77427 New Port Richey | Florida | United States | -82.71927 | 28.24418 Pembroke Pines | Florida | United States | -80.22394 | 26.00315 Pinellas Park | Florida | United States | -82.69954 | 27.8428 Sarasota | Florida | United States | -82.53065 | 27.33643 Vero Beach | Florida | United States | -80.39727 | 27.63864 Atlanta | Georgia | United States | -84.38798 | 33.749 Roswell | Georgia | United States | -84.36159 | 34.02316 Savannah | Georgia | United States | -81.09983 | 32.08354 Warner Robins | Georgia | United States | -83.62664 | 32.61574 Chicago | Illinois | United States | -87.65005 | 41.85003 Peoria | Illinois | United States | -89.58899 | 40.69365 Lafayette | Indiana | United States | -86.87529 | 40.4167 South Bend | Indiana | United States | -86.25001 | 41.68338 Waterloo | Iowa | United States | -92.34296 | 42.49276 Munfordville | Kentucky | United States | -85.89108 | 37.27228 Baton Rouge | Louisiana | United States | -91.18747 | 30.44332 Marrero | Louisiana | United States | -90.10035 | 29.89937 Elkridge | Maryland | United States | -76.71358 | 39.21261 Prince Frederick | Maryland | United States | -76.5844 | 38.5404 Towson | Maryland | United States | -76.60191 | 39.4015 Marlborough | Massachusetts | United States | -71.55229 | 42.34593 Ann Arbor | Michigan | United States | -83.74088 | 42.27756 Cadillac | Michigan | United States | -85.40116 | 44.25195 Detroit | Michigan | United States | -83.04575 | 42.33143 Livonia | Michigan | United States | -83.35271 | 42.36837 Kansas City | Missouri | United States | -94.57857 | 39.09973 North Las Vegas | Nevada | United States | -115.1175 | 36.19886 Blackwood | New Jersey | United States | -75.06406 | 39.80234 Trenton | New Jersey | United States | -74.74294 | 40.21705 New York | New York | United States | -74.00597 | 40.71427 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Statesville | North Carolina | United States | -80.8873 | 35.78264 Gallipolis | Ohio | United States | -82.20237 | 38.8098 Marion | Ohio | United States | -83.12852 | 40.58867 Clinton | Oklahoma | United States | -98.96731 | 35.51561 Oklahoma City | Oklahoma | United States | -97.51643 | 35.46756 Tulsa | Oklahoma | United States | -95.99277 | 36.15398 Allentown | Pennsylvania | United States | -75.49018 | 40.60843 Altoona | Pennsylvania | United States | -78.39474 | 40.51868 Philadelphia | Pennsylvania | United States | -75.16362 | 39.95238 Pittsburgh | Pennsylvania | United States | -79.99589 | 40.44062 Alcoa | Tennessee | United States | -83.97379 | 35.78953 Milan | Tennessee | United States | -88.75895 | 35.91979 Morristown | Tennessee | United States | -83.29489 | 36.21398 Arlington | Texas | United States | -97.10807 | 32.73569 Carrollton | Texas | United States | -96.89028 | 32.95373 Dallas | Texas | United States | -96.80667 | 32.78306 Fort Worth | Texas | United States | -97.32085 | 32.72541 Houston | Texas | United States | -95.36327 | 29.76328 San Antonio | Texas | United States | -98.49363 | 29.42412 Temple | Texas | United States | -97.34278 | 31.09823 Salt Lake City | Utah | United States | -111.89105 | 40.76078 Burlington | Vermont | United States | -73.21207 | 44.47588 Multiple Cities | N/A | Australia | N/A | N/A Multiple Cities | N/A | Brazil | N/A | N/A Multiple Cities | N/A | Bulgaria | N/A | N/A Multiple Cities | N/A | Chile | N/A | N/A Multiple Cities | N/A | Croatia | N/A | N/A Multiple Cities | N/A | Estonia | N/A | N/A Multiple Cities | N/A | Guatemala | N/A | N/A Multiple Cities | N/A | India | N/A | N/A Multiple Cities | N/A | Israel | N/A | N/A Multiple Cities | N/A | Latvia | N/A | N/A Multiple Cities | N/A | Mexico | N/A | N/A Multiple Cities | N/A | New Zealand | N/A | N/A Multiple Cities | N/A | Peru | N/A | N/A Multiple Cities | N/A | Romania | N/A | N/A Multiple Cities | N/A | Russia | N/A | N/A Multiple Cities | N/A | Serbia | N/A | N/A Multiple Cities | N/A | South Africa | N/A | N/A Multiple Cities | N/A | Ukraine | N/A | N/A
0
NCT00328627
[ 4 ]
547
RANDOMIZED
CROSSOVER
0TREATMENT
0NONE
false
0ALL
null
to demonstrate the efficacy of inhaled Technosphere/Insulin in combination with metformin versus combination metformin and a secretagogue
null
Diabetes Mellitus, Type 2
null
3
arm 1: Technosphere Insulin arm 2: Metformin \& Secretagogues arm 3: Technosphere \& Metformin
[ 0, 1, 0 ]
3
[ 0, 0, 0 ]
intervention 1: Inhalation, 15U/30U, prandial intervention 2: Metformin tablets,Secretagogues supplied as any of the currently marketed brands and formulations. intervention 3: Technosphere Insulin Inhalation Powder 15U/30U, Metformin tablets
intervention 1: Technosphere Insulin intervention 2: Metformin & Secretagogues intervention 3: Technosphere Insulin & Metformin
120
Birmingham | Alabama | United States | -86.80249 | 33.52066 Birmingham | Alabama | United States | -86.80249 | 33.52066 Phoenix | Arizona | United States | -112.07404 | 33.44838 Phoenix | Arizona | United States | -112.07404 | 33.44838 Chula Vista | California | United States | -117.0842 | 32.64005 Denver | Colorado | United States | -104.9847 | 39.73915 Denver | Colorado | United States | -104.9847 | 39.73915 Denver | Colorado | United States | -104.9847 | 39.73915 Waterbury | Connecticut | United States | -73.0515 | 41.55815 Hollywood | Florida | United States | -80.14949 | 26.0112 Miami | Florida | United States | -80.19366 | 25.77427 Chicago | Illinois | United States | -87.65005 | 41.85003 Chicago | Illinois | United States | -87.65005 | 41.85003 Skokie | Illinois | United States | -87.73339 | 42.03336 Towson | Maryland | United States | -76.60191 | 39.4015 Haverhill | Massachusetts | United States | -71.07728 | 42.7762 Detroit | Michigan | United States | -83.04575 | 42.33143 Livonia | Michigan | United States | -83.35271 | 42.36837 St Louis | Missouri | United States | -90.19789 | 38.62727 St Louis | Missouri | United States | -90.19789 | 38.62727 St Louis | Missouri | United States | -90.19789 | 38.62727 Omaha | Nebraska | United States | -95.94043 | 41.25626 Albuquerque | New Mexico | United States | -106.65114 | 35.08449 Mineola | New York | United States | -73.64068 | 40.74927 New Hyde Park | New York | United States | -73.68791 | 40.7351 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Charlotte | North Carolina | United States | -80.84313 | 35.22709 Durham | North Carolina | United States | -78.89862 | 35.99403 Dayton | Ohio | United States | -84.19161 | 39.75895 Dayton | Ohio | United States | -84.19161 | 39.75895 Portland | Oregon | United States | -122.67621 | 45.52345 Greenville | South Carolina | United States | -82.39401 | 34.85262 Collierville | Tennessee | United States | -89.66453 | 35.04204 Memphis | Tennessee | United States | -90.04898 | 35.14953 Memphis | Tennessee | United States | -90.04898 | 35.14953 Dallas | Texas | United States | -96.80667 | 32.78306 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 San Antonio | Texas | United States | -98.49363 | 29.42412 Tacoma | Washington | United States | -122.44429 | 47.25288 Avellaneda | Buenos Aires | Argentina | -58.36744 | -34.66018 Buenos Aires | N/A | Argentina | -58.37723 | -34.61315 Buenos Aires | N/A | Argentina | -58.37723 | -34.61315 Buenos Aires | N/A | Argentina | -58.37723 | -34.61315 Buenos Aires | N/A | Argentina | -58.37723 | -34.61315 Porto Alegre | Rio Grande do Sul | Brazil | -51.23019 | -30.03283 Porto Alegre | Rio Grande do Sul | Brazil | -51.23019 | -30.03283 Rio de Janeiro | N/A | Brazil | -43.18223 | -22.90642 Santos | N/A | Brazil | -46.33361 | -23.96083 São Paulo | N/A | Brazil | -46.63611 | -23.5475 São Paulo | N/A | Brazil | -46.63611 | -23.5475 São Paulo | N/A | Brazil | -46.63611 | -23.5475 São Paulo | N/A | Brazil | -46.63611 | -23.5475 Markham | Ontario | Canada | -79.2663 | 43.86682 Oakville | Ontario | Canada | -79.68292 | 43.45011 Thornhill | Ontario | Canada | -79.4163 | 43.80011 Toronto | Ontario | Canada | -79.39864 | 43.70643 Toronto | Ontario | Canada | -79.39864 | 43.70643 Richmond Hill | N/A | Canada | -79.43725 | 43.87111 Santiago | Santiago Metropolitan | Chile | -70.64827 | -33.45694 Santiago | N/A | Chile | -70.64827 | -33.45694 Santiago | N/A | Chile | -70.64827 | -33.45694 Santiago | N/A | Chile | -70.64827 | -33.45694 Ostrava-Kunčice | CZE | Czechia | 18.2919 | 49.7903 Prague | CZE | Czechia | 14.42076 | 50.08804 Prague | CZE | Czechia | 14.42076 | 50.08804 Ostrava | Ostrava | Czechia | 18.28204 | 49.83465 Ostrava | N/A | Czechia | 18.28204 | 49.83465 Prague | N/A | Czechia | 14.42076 | 50.08804 Prague | N/A | Czechia | 14.42076 | 50.08804 Prague | N/A | Czechia | 14.42076 | 50.08804 Mexico City | Durango | Mexico | N/A | N/A Monterrey | Nuevo León | Mexico | -100.31721 | 25.68435 Garza García | N/A | Mexico | -99.81754 | 25.18305 Mexico City | N/A | Mexico | -99.12766 | 19.42847 Mexico City | N/A | Mexico | -99.12766 | 19.42847 Monterrey | N/A | Mexico | -100.31721 | 25.68435 Bialystock | POL | Poland | N/A | N/A Bialystok | POL | Poland | 23.16433 | 53.13333 Krakow | POL | Poland | 19.93658 | 50.06143 Lodz | POL | Poland | 19.47395 | 51.77058 Pruszków | POL | Poland | 20.81214 | 52.17072 Lodz | N/A | Poland | 19.47395 | 51.77058 Warsaw | N/A | Poland | 21.01178 | 52.22977 Warsaw | N/A | Poland | 21.01178 | 52.22977 Kemerovo | RUS | Russia | 86.08333 | 55.33333 Moscow | RUS | Russia | 37.61556 | 55.75222 Moscow | RUS | Russia | 37.61556 | 55.75222 Moscow | RUS | Russia | 37.61556 | 55.75222 Moscow | RUS | Russia | 37.61556 | 55.75222 Saint Petersburg | RUS | Russia | 30.31413 | 59.93863 Saint Petersburg | RUS | Russia | 30.31413 | 59.93863 Saint Petersburg | RUS | Russia | 30.31413 | 59.93863 Saint Petersburg | RUS | Russia | 30.31413 | 59.93863 Smolensk | RUS | Russia | 32.04371 | 54.77944 Yaroslavl | RUS | Russia | 39.87368 | 57.62987 Yaroslavl | RUS | Russia | 39.87368 | 57.62987 Moscow | N/A | Russia | 37.61556 | 55.75222 Seville | Andalusia | Spain | -5.97317 | 37.38283 Barcelona | N/A | Spain | 2.15899 | 41.38879 Madrid | N/A | Spain | -3.70256 | 40.4165 Madrid | N/A | Spain | -3.70256 | 40.4165 Sabadell | N/A | Spain | 2.10942 | 41.54329 Chernivtsy | UKR | Ukraine | N/A | N/A Dniepropetrovsk | UKR | Ukraine | N/A | N/A Donetsk | UKR | Ukraine | 37.80224 | 48.023 Donetsk | UKR | Ukraine | 37.80224 | 48.023 Donetsk | UKR | Ukraine | 37.80224 | 48.023 Kiev | UKR | Ukraine | 30.5238 | 50.45466 Kiev | UKR | Ukraine | 30.5238 | 50.45466 Kiev | UKR | Ukraine | 30.5238 | 50.45466 Odesa | UKR | Ukraine | 30.74383 | 46.48572 Odesa | UKR | Ukraine | 30.74383 | 46.48572 Odesa | UKR | Ukraine | 30.74383 | 46.48572 Vinnitsa | UKR | Ukraine | 37.71861 | 49.84639 Kiev | N/A | Ukraine | 30.5238 | 50.45466 Odesa | N/A | Ukraine | 30.74383 | 46.48572
0
NCT00332488
[ 3 ]
43
RANDOMIZED
SINGLE_GROUP
0TREATMENT
0NONE
true
0ALL
true
The purpose of this study is to compare the amount of acetylcholine release after a single injection of clonidine in normal volunteers and individuals with neuropathic pain.
This study is part of a pain center grant that focuses on how pain, especially chronic neuropathic pain, alters the response to traditional and non-traditional analgesics (pain medications). The way that nerve fibers carry pain information to the brain is thought to change after surgery and in cases of chronic pain. For this reason, some medicines work better to relieve pain in healthy people who have a sudden painful injury when compared to people after surgery or to people with chronic pain. Currently available pain medications may not relieve all types of pain or may relieve pain only at doses that produce side effects and potential complications. The aim of this study is to understand the mechanisms by which intrathecal clonidine (or clonidine injected into cerebrospinal fluid) increases in potency and efficacy by examining the cerebrospinal fluid of healthy individuals, before and after clonidine administration, as well as looking at the spinal fluid of people with chronic neuropathic nerve pain. More specifically, in this study, researchers will compare acetylcholine release (a protein-like substance found in cerebrospinal fluid) in normal volunteers and patients with neuropathic pain after a single injection of clonidine. After baseline measurements, including blood pressure and heart rate, participants will be trained to accurately estimate pain by way of thermal heat testing. Next a small amount of spinal fluid will be withdrawn from each participant to measure the amounts of naturally-made chemicals in the participants' cerebrospinal fluid. Participants then will receive an injection of clonidine. After the injection, additional samples of spinal fluid will be taken to measure chemical changes in the fluid. Duration of the study for participants is 1 day, and includes 1 visit to the research center, lasting approximately 3 hours.
Pain
pain, chronic pain acetylcholine clonidine a2-adrenergic agonists alpha2-adrenergic agonists
null
2
arm 1: Chronic Pain Participants will be trained to accurately estimate pain by way of thermal heat testing. Next a small amount of spinal fluid will be withdrawn from each participant to measure the amounts of naturally-made chemicals in the participants' cerebrospinal fluid. Participants then will receive an injection of clonidine. After the injection, additional samples of spinal fluid will be taken to measure chemical changes in the fluid. arm 2: Healthy Participants will be trained to accurately estimate pain by way of thermal heat testing. Next a small amount of spinal fluid will be withdrawn from each participant to measure the amounts of naturally-made chemicals in the participants' cerebrospinal fluid. Participants then will receive an injection of clonidine. After the injection, additional samples of spinal fluid will be taken to measure chemical changes in the fluid.
[ 1, 1 ]
2
[ 0, 0 ]
intervention 1: Patients will receive intrathecal clonidine (or clonidine injected into cerebrospinal fluid) intervention 2: Patients will receive intrathecal clonidine (or clonidine injected into cerebrospinal fluid)
intervention 1: clonidine intervention 2: clonidine
2
Winston-Salem | North Carolina | United States | -80.24422 | 36.09986 Winston-Salem | North Carolina | United States | -80.24422 | 36.09986
0
NCT00350532
[ 3, 4 ]
163
RANDOMIZED
PARALLEL
0TREATMENT
2DOUBLE
false
0ALL
false
The purpose of this clinical research study is to learn if BMS-512148, added to insulin and one or two anti-diabetes medications (metformin and/or pioglitazone or rosiglitazone), can help reduce the blood sugar levels compared to insulin and one or two anti-diabetes medications (metformin and/or pioglitazone or rosiglitazone) alone, in subjects with type 2 diabetes. The safety of this treatment will also be studied.
null
Type 2 Diabetes
null
4
arm 1: 20 mg arm 2: 10 mg arm 3: 20 mg arm 4: None
[ 0, 0, 0, 2 ]
2
[ 0, 0 ]
intervention 1: Tablets, Oral, once daily, up to 12 weeks intervention 2: Tablets, Oral, 0 mg, once daily, up to 12 weeks
intervention 1: Dapagliflozin intervention 2: Placebo
23
Jonesboro | Arkansas | United States | -90.70428 | 35.8423 Fresno | California | United States | -119.77237 | 36.74773 Greenbrae | California | United States | -122.5247 | 37.94854 Jacksonville | Florida | United States | -81.65565 | 30.33218 Roswell | Georgia | United States | -84.36159 | 34.02316 Indianapolis | Indiana | United States | -86.15804 | 39.76838 Baltimore | Maryland | United States | -76.61219 | 39.29038 Ann Arbor | Michigan | United States | -83.74088 | 42.27756 St Louis | Missouri | United States | -90.19789 | 38.62727 Syracuse | New York | United States | -76.14742 | 43.04812 Asheville | North Carolina | United States | -82.55402 | 35.60095 Mentor | Ohio | United States | -81.33955 | 41.66616 Dallas | Texas | United States | -96.80667 | 32.78306 San Antonio | Texas | United States | -98.49363 | 29.42412 Renton | Washington | United States | -122.21707 | 47.48288 Milwaukee | Wisconsin | United States | -87.90647 | 43.0389 Winnipeg | Manitoba | Canada | -97.14704 | 49.8844 Bathurst | New Brunswick | Canada | -65.65112 | 47.61814 Gatineau | Quebec | Canada | -75.70164 | 45.47723 Laval | Quebec | Canada | -73.692 | 45.56995 Longueuil | Quebec | Canada | -73.46818 | 45.5152 Pointe-Claire | Quebec | Canada | -73.81669 | 45.44868 Sherbrooke | Quebec | Canada | -71.89908 | 45.40008
0
NCT00357370