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values | class_subclass stringclasses 511
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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
DB00001 | Lepirudin | Lepirudin is a recombinant hirudin formed by 65 amino acids that acts as a highly specific and direct thrombin inhibitor.[L41539,L41569] Natural hirudin is an endogenous anticoagulant found in _Hirudo medicinalis_ leeches.[L41539] Lepirudin is produced in yeast cells and is identical to natural hirudin except for the a... | solid | Lepirudin is indicated for anticoagulation in adult patients with acute coronary syndromes (ACS) such as unstable angina and acute myocardial infarction without ST elevation. In patients with ACS, lepirudin is intended for use with [aspirin].[L41539] Lepirudin is also indicated for anticoagulation in patients with hepa... | Lepirudin is a recombinant hirudin that acts as a highly specific thrombin inhibitor. Its activity is measured by anti-thrombin units (ATUs) that correspond to the amount of lepirudin required to neutralize a unit of the World Health Organization α-thrombin (89/588) standard. The activity of lepirudin is 16,000 ATU/mg.... | Lepirudin is a direct thrombin inhibitor used as an anticoagulant in patients for whom heparin is contraindicated.[L41539,A3] Thrombin is a serine protease that participates in the blood-clotting cascade, and it is formed by the cleavage of pro-thrombin. Active thrombin cleaves fibrinogen and generates fibrin monomers ... | Lepirudin administered as a single intravenous bolus injection of 0.4 mg/kg in 9 healthy volunteers (male and female) resulted in a C<sub>max</sub> of 2924 ng/mL, a t<sub>max</sub> of 0.17 h and an AUC<sub>0-∞</sub> of 2500 ng•h/mL.[L41539] When 0.1, 0.15 and 0.2 mg/kg of lepirudin was administered as a single intraven... | As a polypeptide, lepirudin is expected to be metabolized by the sequential cleavage of amino acids by kidney exoproteases, which have carboxypeptidase and dipeptidase-like activity.[L41539,L41544] The C-terminal cleavage of lepirudin aminoacids (aminoacids 1 to 65) produces four metabolites with anti-thrombotic activi... | The acute toxicity of intravenous lepirudin was evaluated in mice (0.1-1000 mg/kg), rats (1-1000 mg/kg), and monkeys (1-100 mg/kg), and toxicity was not detected at the doses investigated.[L41539] The acute toxicity of lepirudin administered subcutaneously was also evaluated in mice (1-1250 mg/kg) and rats (1-500 mg/kg... | Lepirudin has an initial half-life of approximately 10 minutes, and in young healthy volunteers, it has a terminal half-time of 1.3 hours.[L41539] Lepirudin has a first-order elimination kinetic; plasma concentration increases proportionally as the lepirudin intravenous dose is increased. Elimination half-life values o... | In human plasma, the protein binding of lepirudin was approximately 3%.[L41539] | Lepirudin is mostly excreted through urine (48.3%). About 35% of lepirudin is excreted unchanged, while metabolites are found in a smaller proportion (2.5% of M1, 5.4% of M2, 3.9% of M3 and 1.6% of M4).[L41544] | The volume of distribution of lepirudin at steady state was 12.2 L in healthy young subjects (n=18, 18-60 years), 18.7 L in healthy elderly subjects (n=10, 65-80 years), 18.0 L in renally impaired subjects (n=16, creatinine clearance < 80 mL/min, and 32.1 L in heparin-induced thrombocytopenia patients (n=73).[L41539] T... | The clearance of lepirudin is proportional to the glomerular filtration rate. On average, lepirudin clearance was 164 mL/min in healthy young subjects (n=18, 18-60 years) and 25% lower in women than in men. In healthy elderly subjects (n=10, 65-80 years), clearance was 139 mL/min, about 20% lower than in younger patien... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"withdrawn"
] | [
"B01AE",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "273.19",
"description": "Refludan 50 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1993-01-19",
"country": "United States",
"expires": "2010-01-19",
"number": "5180668"
}
] | [Leu1, Thr2]-63-desulfohirudin | Desulfatohirudin | Hirudin variant-1 | Lepirudin | Lepirudin recombinant | R-hirudin | 3.4.21.5 | Coagulation factor II | [
"Refludan",
"Refludan",
"Refludan",
"Refludan",
"Refludan",
"Refludan"
] | [] | [] | [
"P00734"
] | [] | [] | [] |
DB01022 | Phylloquinone | Vitamin K1, also called phylloquinone or phytonadione, is a fat soluble vitamin.[L33319,L33345] Phylloquinone is a cofactor of the enzyme γ-carboxylase, which modifies and activates precursors to coagulation factors II, VII, IX, and X.[A234264,A234195,A234259] It is indicated in the treatment of coagulation disorders d... | liquid | Oral phylloquinone is indicated to treat prothrombin deficiency caused by coumarin or indanedione derivatives; and hypoprothrombinemia secondary to antibacterial therapy, salicylates, or obstructive jaundice or biliary fistulas with concomitant bile salt administration.[L33345]
Parenteral (intravenous, intramuscular... | Phylloquinone is a vitamin K indicated in the treatment of coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by deficiency or interference in the activity of vitamin K.[L33319] It has a long duration of action as vitamin K is cycled in the body,[A234259] and a wide therapeut... | Vitamin K is a cofactor of gamma-carboxylase.[A234264,A234195] Gamma carboxylase attaches carboxylic acid functional groups to glutamate, allowing precursors of factors II, VII, IX, and X to bind calcium ions.[A234259] Binding of calcium ions converts these clotting factors to their active form, which are then secreted... | A 4 µg oral dose of phylloquinone is 13% ± 9% bioavailable, with a T<sub>max</sub> of 4.7 ± 0.8 hours.[A234264] 1.5 ± 0.8 nmol is found in the plasma compartment, and 3.6 ± 3.4 nmol is found in the second compartment.[A234264]
A 10 mg intramuscular phylloquinone dose is 89.2% ± 25.4% bioavailable.[A234344] The same ... | Phylloquinone's phytyl side chain is omega hydroxylated by CYP4F2.[A137578] The side chain is then cleaved to 5 or 7 carbons long, and then glucuronidated prior to elimination.[A234104,A234109,A234114,A234119]
Vitamin Ks in general undergo a cycle of reduction to vitamin K hydroquinone by vitamin K epoxide reductase... | High doses of vitamin K1 are not associated with toxicity.[A234259] Intravenous administration has been associated with an increased risk of toxicity.[A234284] These patients should be treated with symptomatic and supportive measures.
The intravenous LD<sub>50</sub> in mice is 1170 mg/kg and the oral LD<sub>50</sub>... | Intravenous phylloquinone has an initial half life of 22 minutes, followed by a half life of 125 minutes.[A234104] | null | Intravenous phylloquinone is 36% eliminated in the feces in 5 days and 22% recovered in urine in 3 days.[A234104,A234329] | The steady state volume of distribution of phylloquinone is 20 ± 6 L in subjects who are also taking phenprocoumon therapy.[A234374] | Intravenous phylloquinone is 90% cleared in 2 hours, and 99% cleared in 8 hours.[A234104,A234329] A 10 mg intravenous dose of phylloquinone has a mean clearance of 91 ± 24 mL/min.[A234344] | Organic compounds | Lipids and lipid-like molecules | Prenol lipids | Quinone and hydroquinone lipids | [
"approved",
"investigational"
] | [
"B02BA",
"B02B",
"B02",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "2.76",
"description": "Vitamin K1 10 mg/ml",
"unit": "ml"
},
{
"cost": "4.79",
"description": "Vitamin K1 Pediatric 2 mg/ml",
"unit": "ml"
},
{
"cost": "5.95",
"description": "Mephyton 5 mg tablet",
"unit": "tablet"
},
{
"cost": "35.0",
"description... | [] | 2-Methyl-3-(3,7,11,15-tetramethyl-2-hexadecenyl)-1,4-naphthalenedione | 2-Methyl-3-[(2E)-3,7,11,15-tetramethyl-2-hexadecenyl]naphthoquinone | 2-Methyl-3-phytyl-1,4-naphthochinon | 2-Methyl-3-phytyl-1,4-naphthoquinone | 3-Phytylmenadione | alpha-Phylloquinone | Fitomenadiona | Phyllochinon | Phyllochinonum | Phylloquino... | [
"Adeks - Dps",
"Adeks Tablets",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"AquaMEPHYTON",
"AquaMEPHYTON",
"Decara K Vegicaps",
"Infuvite Adult",
"Infuvite Adult",
"Infuvite Pediatric",
"Infu... | [
"Aqua-Mephyton",
"Konakion"
] | [
"Omega-3 Rx Complete",
"M.V.I. Pediatric",
"Pro Pcos Citrus",
"Pro Hers Vanilla",
"M.V.I. Adult",
"M.V.I. Adult",
"Pediatric Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple V... | [
"P38435",
"P02818"
] | [
"P78329",
"Q9Y5Z9",
"Q9BQB6"
] | [] | [] |
DB01373 | Calcium | Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloodstream under controlled conditions. Circulating calcium is either in t... | solid | Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. It is vital in cell signaling, muscular contractions, bone health, and signalling cascades. | Calcium (Ca2+) plays a pivotal role in the physiology and biochemistry of organisms and the cell. It plays an important role in signal transduction pathways, where it acts as a second messenger, in neurotransmitter release from neurons, contraction of all muscle cell types, and fertilization. Many enzymes require calci... | Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. More than 500 human proteins are known to bind or transport calcium. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloo... | null | null | null | null | null | The kidney excretes 250 mmol a day in urine, and resorbs 245 mmol, leading to a net loss in the urine of 5 mmol/d. | null | null | null | null | null | null | [
"nutraceutical"
] | [
"M05BB",
"M05B",
"M05",
"M",
"A11AA",
"A11A",
"A11",
"A",
"M05BB",
"M05B",
"M05",
"M",
"A11GB",
"A11G",
"A11",
"A",
"M05BB",
"M05B",
"M05",
"M",
"M05BB",
"M05B",
"M05",
"M",
"M05BB",
"M05B",
"M05",
"M"
] | [
"Humans and other mammals"
] | [] | [] | Calcio | Calcium, elemental | Elemental calcium | Kalzium | CACH2 | CACN2 | CACNL1A1 | Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle | CCHL1A1 | Voltage-gated calcium channel subunit alpha Cav1.2 | 7.2.2.10 | ATP-dependent Ca(2+) pump PMR1 | ATPase 2C1 | Ca(2+)/Mn(2+)-ATPase 2C1 | KIAA1347 | P... | [
"24 Multivitamins + Minerals",
"50 Plus Multiple Vitamins & Minerals",
"7030 Calcium Gold",
"7030 Calcium Gold",
"7030 Calcium Premium",
"7030 Calcium Premium",
"7030 Calcium Premium",
"A D Calcium Tab",
"A-D Calcium Cap",
"A.R.T.H. Away Formula",
"A/o-26 - Caplet",
"Acti-cal/mag 2:1 + Zinc an... | [] | [
"Pure Calcium calcium",
"Oyster Shell Calcium with Vitamin D",
"O-Cal Prenatal Vitamin",
"Cavan One",
"Zingiber",
"PreNatal Vitamins Plus",
"Prenatal Vitamin No 53 Iron Fum Folic Acid Docusate CA DHA",
"Vitafol Caplet",
"Ferrous Sulfate",
"PreFol-DHA",
"Focalgin B",
"Nata Komplete",
"PreNata... | [
"Q13936",
"P98194",
"P02585",
"P63316",
"Q01082",
"P04271",
"P20810",
"P49747",
"P19801",
"Q99584",
"P05187",
"P05109",
"P06702",
"P29034",
"P00450",
"P12644",
"P08493",
"Q8TAB3",
"O75340",
"P0DP23",
"P0DP24",
"P0DP25"
] | [] | [] | [] |
DB00002 | Cetuximab | Cetuximab is a recombinant chimeric human/mouse IgG1 monoclonal antibody that competitively binds to epidermal growth factor receptor (EGFR) and competitively inhibits the binding of epidermal growth factor (EGF).[A227973] EGFR is a member of the ErbB family of receptor tyrosine kinases found in both normal and tumour ... | liquid | Cetuximab indicated for the treatment of locally or regionally advanced squamous cell carcinoma of the head and neck in combination with radiation therapy. It is indicated for treating a recurrent locoregional disease or metastatic squamous cell carcinoma of the head and neck in combination with platinum-based therapy ... | Cetuximab is an anticancer agent that works by inhibiting the growth and survival of epidermal growth factor receptor (EGFR)-expressing tumour cells with high specificity and higher affinity than epidermal growth factor (EGF) and transforming growth factor-alpha (TGF-α), which are natural ligands of EGFR.[L31418] Cetux... | The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein and a type I receptor tyrosine kinase expressed on both normal and malignant cells. It has been investigated as a therapeutic target for anticancer treatment, as it is often upregulated in cancer types, including head and neck, colon, and recta... | After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> weekly dose, the steady-state levels of cetuximab was reached by the third weekly infusion with mean peak and trough concentrations across studies ranging from 168 µg/mL to 235 µg/mL and 41 µg/mL to 85 µg/mL, respectively.[L3... | Like other monoclonal antibodies, cetuximab is expected to undergo lysosomal degradation by the reticuloendothelial system and protein catabolism by a target‐mediated disposition pathway.[A40006] | The intravenous LD<sub>50</sub> is > 300 mg/kg in mice and > 200 mg/kg in rats.[L31408] There is limited information on the overdose from cetuximab.
In clinical trials, cetuximab was associated with serious and fatal infusion reactions, cardiopulmonary arrest or sudden death, and serious dermatologic toxicities. Pul... | After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> weekly dose, the mean half-life for cetuximab was approximately 112 hours, with a range of 63 to 230 hours.[L30448] | There is no information available. | There is limited information available. | The volume of the distribution is about 2-3 L/m<sup>2</sup> and is independent of dose.[L30448] | In patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck, the estimated clearance rate was 0.103 L/h.[A228003] At doses ranging from 200 to 400 mg/m<sup>2</sup>, complete saturation of systemic clearance was observed. In a population pharmacokinetic study, female patients had a 25% low... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L01FE",
"L01F",
"L01",
"L"
] | [
"Humans and other mammals"
] | [] | [
{
"approved": "1999-03-02",
"country": "Canada",
"expires": "2016-03-02",
"number": "1340417"
}
] | Cetuximab | Cétuximab | Cetuximabum | 2.7.10.1 | ERBB | ERBB1 | HER1 | Proto-oncogene c-ErbB-1 | Receptor tyrosine-protein kinase erbB-1 | CD16-I | CD16B | Fc-gamma RIII | Fc-gamma RIII-beta | Fc-gamma RIIIb | FCG3 | FCGR3 | FcR-10 | FcRIII | FcRIIIb | IGFR3 | IgG Fc receptor III-1 | C1QG | CD16-II | CD16A | CD16a anti... | [
"Erbitux",
"Erbitux",
"Erbitux",
"Erbitux",
"Erbitux"
] | [] | [] | [
"P00533",
"O75015",
"P02745",
"P02746",
"P02747",
"P08637",
"P12314",
"P12318"
] | [] | [] | [] |
DB00003 | Dornase alfa | Dornase alfa is a biosynthetic form of human deoxyribunuclease I (DNase I) enzyme. It is produced in genetically modified Chinese hamster ovary (CHO) cells using recombinant DNA technology. The 260-amino acid sequence of dornase alfa is identical to the endogenous human enzyme. Dornase alfa cleaves extracellular DNA to... | liquid | Used as adjunct therapy in the treatment of cystic fibrosis. | Cystic fibrosis (CF) is a disease characterized by the retention of viscous purulent secretions in the airways. These thick secretions contribute both to reduced pulmonary function and to frequent pulmonary infection. Purulent pulmonary secretions of individuals with cystic fibrosis contain very high concentrations of ... | Dornase alfa is a biosynthetic form of human DNase I. The enzyme is involved in endonucleolytic cleavage of extracellular DNA to 5´-phosphodinucleotide and 5´-phosphooligonucleotide end products. It has no effect on intracellular DNA. Optimal activity is dependent on the presence of divalent cations such as calcium and... | Studies in rats and monkeys after inhalation of dornase alfa shows very little systemic absorption (less than 15% for rats and less than 2% for monkeys). The results were also witnessed in patients. Dornase alfa is also associated with very low accumulation with no serum concentration greater than 10ng/mL observed no m... | While no conclusive studies have yet been published, dornase alfa is expected to be metabolized by proteases in biofluids. | Adverse reactions occur at a frequency of < 1/1000 and are usually mild and transient in nature. Reported adverse effects include chest pain (pleuritic/non-cardiac), fever, dyspepsia, voice alteration (hoarseness), pharyngitis, dyspnea, laryngitis, rhinitis, decreased lung function, rash, urticaria, and conjunctivitis.... | null | null | null | In studies in rats and monkeys, the initial volume of distribution is similar to the serum volume. Concentrations in sputum decline rapidly after inhalation. | Studies in rats indicate that, following aerosol administration, the disappearance half-life of dornase alfa from the lungs is 11 hours. In humans, sputum DNase levels declined below half of those detected immediately post-administration within 2 hours but effects on sputum rheology persisted beyond 12 hours. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"R05CB",
"R05C",
"R05",
"R"
] | [
"Humans and other mammals"
] | [
{
"cost": "3.21",
"description": "Lufyllin 200 mg tablet",
"unit": "tablet"
},
{
"cost": "3.84",
"description": "Lufyllin-gg tablet",
"unit": "tablet"
},
{
"cost": "3.99",
"description": "Lufyllin-GG 200-200 mg tablet",
"unit": "tablet"
},
{
"cost": "4.62",
"d... | [
{
"approved": "2005-02-22",
"country": "Canada",
"expires": "2015-02-28",
"number": "2184581"
},
{
"approved": "2004-10-26",
"country": "Canada",
"expires": "2013-05-28",
"number": "2137237"
}
] | Deoxyribonuclease (human clone 18-1 protein moiety) | Dornasa alfa | Dornase alfa | Dornase alfa, recombinant | Dornase alpha | Recombinant deoxyribonuclease (DNAse) | 3.1.21.1 | Deoxyribonuclease I | DNase I | DNL1 | DRNI | [
"Pulmozyme",
"Pulmozyme"
] | [
"Viscozyme"
] | [] | [
"P24855"
] | [] | [] | [] |
DB00004 | Denileukin diftitox | Denileukin diftitox is an IL2-receptor-directed cytotoxin, is a recombinant DNA-derived fusion protein composed of the amino acid sequences for diphtheria toxin fragments A and B (Met<sub>1</sub>-Thr<sub>387</sub>)-His and the sequence for human interleukin-2 (IL-2; Ala<sub>1</sub>-Thr<sub>133</sub>).[L51254] It is des... | liquid | Denileukin diftitox was previously indicated for the treatment of adult patients with persistent or recurrent cutaneous T-cell lymphoma (CTCL) whose malignant cells express the CD25 component of the IL-2 receptor.[L26381] It is also indicated for the treatment of adult patients with relapsed or refractory Stage I-III C... | Denileukin diftitox is an anticancer drug with cytocidal actions on cancer cells.[L51254] Denileukin diftitox demonstrated the ability to deplete immunosuppressive regulatory T lymphocytes (T<sub>regs</sub>) and antitumor activity through direct cytocidal action on IL-2R-expressing tumours.[L51254] | Denileukin diftitox is a fusion protein composed of truncated diphtheria toxin (DT), which is a cytocidal moiety, and the full-length sequence of interleukin-2 (IL-2), which acts as a ligand for the IL-2 receptor.[A264344] Denileukin diftitox is reported to bind to a high- or intermediate-affinity receptor.[A264344] On... | Following a single dose of denileukin diftitox 9 mcg/kg via one-hour infusion in patients with CTCL, the geometric mean (coefficient of variation [CV]%) maximum serum concentration (C<sub>max</sub>) was 94.4 ng/mL (77%) and area under the concentration over time curve (AUC<sub>0-inf</sub>) was 20700 ng x min/L (60%) on... | Denileukin diftitox is expected to be metabolized into small peptides by catabolic pathways.[L51254] | There is limited information regarding the acute toxicity (LD<sub>50</sub>) and overdose of denileukin diftitox. | The arithmetic mean (CV%) denileukin diftitox terminal half-life is 112 minutes (31%) on the first day of the first cycle.[L51254] | null | null | The geometric mean (CV%) volume of distribution of denileukin diftitox is 5.0 L (43%) on the first day of the first administration cycle.[L51254] | The geometric mean (CV%) clearance is 36.5 mL/min (73%) after the first dose of denileukin diftitox at the recommended dose level.[L51254] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L01XX",
"L01X",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "878.4",
"description": "Ontak 150 mcg/ml vial",
"unit": "ml"
}
] | [] | DAB(SUB 389)IL2 | Denileukin | Denileukin diftitox | Interleukin-2/diptheria toxin fusion protein | N-L-METHIONYL-387-L-HISTIDINE-388-L-ALANINE-1-388-TOXIN (CORYNEBACTERIUM DIPHTHERIAE STRAIN C7) (388->2') PROTEIN WITH 2-133-INTERLEUKIN 2 (HUMAN CLONE PTIL2-21A) | N-MET-187-HIS-388-ALA-1-388-TOXIN (CORYNEBACTERIUM DIPH... | [
"Ontak"
] | [] | [] | [
"P01589",
"P14784"
] | [] | [] | [] |
DB00005 | Etanercept | Dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1.[L14862,A216522] The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of ... | liquid | Etanercept is indicated for the treatment of moderately to severely active rheumatoid arthritis in adults and in chronic moderate to severe plaque psoriasis in patients 4 years of age and older.[L14862,L45523] It is also used to manage signs and symptoms of polyarticular idiopathic arthritis and Juvenile Psoriatic Arth... | Etanercept binds specifically to tumor necrosis factor (TNF) and thereby modulates biological processes that are induced or regulated by TNF.[L14862,A216522] Such processes or molecules affected include the level of adhesion molecules expressed, as well as serum levels of cytokines and matrix metalloproteinases. | There are two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75). The biological activity of TNF is dependent upon binding to either cell surface receptor (p75 or p55).[A216522] Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecul... | Population pharmacokinetic modeling in adults with RA, AS, or who were healthy showed a subcutaneous bioavailability of 56.9% with a Ka of 0.0223/h.[A215352] Another model in pediatric JIA patients showed an increased Ka of 0.05/h with a high mean interindividual variability of 215%.[A215357] Cmax after a single 25 mg ... | As etanercept is a fusion protein antibody, it is assumed to be metabolized via proteinases similarly to endogenous proteins. | null | Etanercept has a mean half-life of elimination of 102 hours in RA patients.[L14862] Population models have shown a mean half-life of 68 hours in healthy adults and 70.7-94.8 hours in pediatric JIA patients.[A215657,A215357] | No significant protein binding has been identified. | null | Population pharmacokinetic modeling predicts a total Vd of 5.49 L with a peripheral compartment of 1.24 L in adults with RA and an apparent Vd with subcutaneous administration in pediatric JIA patients of 7.88 L.[A215352,A215357] | Etanercept has a mean apparent clearance of 160 mL/h in RA patients.[L14862] Population models predict a mean apparent clearance of 132 mL/h in healthy adults and 0.0576 L/h in pediatric JIA patients.[A215657,A215357] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L04AB",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "250.37",
"description": "Enbrel 25 mg kit",
"unit": "each"
},
{
"cost": "488.74",
"description": "Enbrel 50 mg/ml sureclick syr",
"unit": "syringe"
},
{
"cost": "1016.57",
"description": "Enbrel 4 25 mg Kit (1 Box = 1 Kit = Four 25 mg Vials)",
"unit": "box"
}... | [
{
"approved": "2009-06-16",
"country": "Canada",
"expires": "2023-02-27",
"number": "2476934"
},
{
"approved": "2000-03-14",
"country": "Canada",
"expires": "2013-09-14",
"number": "2123593"
},
{
"approved": "2007-10-02",
"country": "United States",
"expires": "20... | Etanercept | etanercept-szzs | etanercept-ykro | Recombinant human TNF | rhu TNFR:Fc | rhu-TNFR:Fc | TNFR-Immunoadhesin | Cachectin | TNF-a | TNF-alpha | TNFA | TNFSF2 | Tumor necrosis factor ligand superfamily member 2 | LT-alpha | TNF-beta | TNFB | TNFSF1 | Tumor necrosis factor ligand superfamily member 1 | Fc-gamma... | [
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Brenzys",
"Brenzys",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
... | [
"Davictrel",
"Tunex"
] | [
"Enbrel",
"Enbrel"
] | [
"P01375",
"P01374",
"P12314",
"P12318",
"P31994",
"P31995",
"P08637",
"O75015",
"P02745",
"P02746",
"P02747"
] | [] | [] | [] |
DB00006 | Bivalirudin | Bivalirudin is a synthetic 20 residue peptide (thrombin inhibitor) which reversibly inhibits thrombin. Once bound to the active site, thrombin cannot activate fibrinogen into fibrin, the crucial step in the formation of thrombus. It is administered intravenously. Because it can cause blood stagnation, it is important t... | solid | For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is plan... | Bivalirudin mediates an inhibitory action on thrombin by directly and specifically binding to both the catalytic site and anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible because thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site... | Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalent... | Following intravenous administration, bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 +/- 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr intravenous infusion given over 4 hours. | 80% proteolytic cleavage | Based on a study by Gleason et al., the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h. | * Normal renal function: 25 min (in normal conditions)
* Creatinine clearance 10-29mL/min: 57min
* Dialysis-dependant patients: 3.5h | Other than thrombin and red blood cells, bivalirudin does not bind to plasma proteins. | Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage. | 0.2L/kg | * 3.4 mL/min/kg [Normal renal function]
* 3.4 mL/min/kg [mild renal function]
* 2.7 mL/min/kg [moderate renal function]
* 2.8 mL/min/kg [severe renal function]
* 1 mL/min/kg [Dialysis-dependent patients] | Organic compounds | Organic Polymers | Polypeptides | null | [
"approved",
"investigational"
] | [
"B01AE",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "780.0",
"description": "Angiomax 250 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1993-03-23",
"country": "United States",
"expires": "2010-05-23",
"number": "5196404"
},
{
"approved": "1999-12-14",
"country": "Canada",
"expires": "2010-08-17",
"number": "2065150"
},
{
"approved": "2009-10-06",
"country": "United States",
"expire... | Bivalirudin | Bivalirudina | Bivalirudinum | 3.4.21.5 | Coagulation factor II | 1.11.2.2 | MPO | [
"Angiomax",
"Angiomax",
"Angiomax",
"Angiomax",
"Angiomax RTU",
"Angiox",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivaliru... | [
"Angiox",
"Hirulog"
] | [] | [
"P00734"
] | [
"P05164"
] | [] | [] |
DB00007 | Leuprolide | Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours.[A203222] As a Gn... | solid | Leuprolide is indicated for the treatment of advanced prostate cancer [L13781, L34415] and as palliative treatment of advanced prostate cancer.[L13790]
It is also used for the treatment of pediatric patients with central precocious puberty (CPP).[L13784, L13787]
In combination with oral [norethisterone] (also k... | Leuprolide is a gonadotropin-releasing hormone (GnRH) analogue that functions as a GnRH receptor superagonist.[A203132, A203222] After an initial spike in GnRH-mediated steroidal production, including testosterone and estradiol, prolonged use results in a significant drop in circulating steroid levels, in line with tho... | Gonadotropin-releasing hormone (GnRH) is a naturally occurring decapeptide that modulates the hypothalamic-pituitary-gonadal (HPG) axis. GnRH binds to corresponding receptors (GnRHRs) on the anterior pituitary gonadotropes, which in turn release luteinizing hormone (LH) and follicle-stimulating hormone (FSH); these, in... | Leuprolide is typically administered as a single-dose long-acting formulation employing either microsphere or biodegradable solid depot technologies.[A203126] Regardless of the exact formulation and initial dose strength, the C<sub>max</sub> is typically achieved by 4-5 hours post-injection and displays large variabili... | Radiolabeling studies suggest that leuprolide is primarily metabolized to inactive penta-, tri-, and dipeptide entities, which are likely further metabolized. It is expected that various peptidases encountered throughout systemic circulation are responsible for leuprolide metabolism.[L10310, L13781, L13784, L13787, L13... | Leuprolide is considered extremely safe, with low dose-related toxicity and comparatively mild adverse effects.[A203126] Prostate cancer patients treated with leuprolide at doses as high as 20 mg/day for two years showed no additional adverse effects compared to those receiving 1 mg/day.[L13814] | Leuprolide has a terminal elimination half-life of approximately three hours.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Leuprolide displays _in vitro_ binding to human plasma proteins between 43% and 49%.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Following administration of 3.75 mg leuprolide depot suspension to three patients, less than 5% of the initial dose was recovered as unchanged or pentapeptide metabolite in the urine.[L10310, L13781, L13784, L13814] | Leuprolide has an apparent steady-state volume of distribution of 27 L following intravenous bolus administration to healthy males. The volume of distribution for indicated routes of subcutaneous or intramuscular injection has not been reported.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Leuprolide administered as a 1 mg intravenous bolus in healthy males has a mean systemic clearance between 7.6 and 8.3 L/h.[L10310, L13781, L13784, L13787, L13790, L13814, L34415] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L02AE",
"L02A",
"L02",
"L",
"L02AE",
"L02A",
"L02",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "385.33",
"description": "Leuprolide 2wk 1 mg/0.2 ml kit",
"unit": "kit"
},
{
"cost": "400.74",
"description": "Leuprolide Acetate 1 mg/0.2ml Kit 2.8ml 2-Week Kit",
"unit": "box"
},
{
"cost": "493.2",
"description": "Eligard 7.5 mg syringe",
"unit": "syringe"
... | [
{
"approved": "2000-03-14",
"country": "United States",
"expires": "2016-12-13",
"number": "6036976"
},
{
"approved": "2014-12-30",
"country": "United States",
"expires": "2031-02-05",
"number": "8921326"
},
{
"approved": "2008-09-30",
"country": "United States",
... | Leuprorelin | Leuprorelina | Leuproreline | Leuprorelinum | GnRH receptor | GnRH-R | GRHR | GNRH | GRH | LHRH | Progonadoliberin I | [
"Camcevi",
"Camcevi",
"Camcevi",
"Camcevi",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Fen... | [
"Camcevi",
"Leuplin",
"LeuProMaxx",
"Memryte",
"Prostap 3",
"Prostap SR"
] | [
"Viadur",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Lupron Depot",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Lupaneta Pack",
"Lupaneta Pack",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprol... | [
"P30968",
"P01148"
] | [] | [] | [] |
DB00008 | Peginterferon alfa-2a | Peginterferon alfa-2a is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most co... | liquid | Peginterferon alfa-2a is indicated for the treatment of HCV in combination with other antiviral drugs in patients over 5 years of age with compensated liver disease [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies.
Peginterferon ... | Peginterferon alfa-2a induces the body's innate antiviral response [FDA Label]. | Peginterferon alfa-2a is derived from recombinant human interferon's alfa-2a moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involv... | Peginterferon alfa-2a reaches peak plasma concentration 72-96 hours after subcutaneous administration [FDA Label]. Trough concentrations at week 48 are approximately 2 fold higher than week 1. The peak to trough ratio at week 48 is 2. | null | Peginterferon alfa-2a may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterf... | The mean terminal half-life of peginterferon alfa-2a is 164 in a range of 84-353 hours [FDA Label]. | null | null | null | The mean systemic clearance of peginterferon alfa-2a is 94 milliliters per hour [FDA Label]. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AB",
"L03A",
"L03",
"L",
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "642.64",
"description": "Pegasys 180 mcg/ml vial",
"unit": "ml"
},
{
"cost": "2533.2",
"description": "Pegasys 180 mcg/0.5 ml conv.pk",
"unit": "each"
},
{
"cost": "2634.53",
"description": "Pegasys (1 Kit = Four 180 mcg/ml Vials Prefilled Syringes) Box",
"unit... | [
{
"approved": "2009-06-30",
"country": "Canada",
"expires": "2017-04-23",
"number": "2203480"
},
{
"approved": "2000-10-03",
"country": "Canada",
"expires": "2016-03-26",
"number": "2172664"
}
] | PEG-IFN alfa-2A | PEG-Interferon alfa-2A | Peginterferon alfa-2a | Pegylated Interfeaon alfa-2A | Pegylated interferon alfa-2a | Pegylated interferon alpha-2a | Pegylated-interferon alfa 2a | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I in... | [
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Peg... | [] | [
"Pegasys Rbv",
"Pegasys Rbv"
] | [
"P48551",
"P17181"
] | [
"P05177"
] | [] | [] |
DB00009 | Alteplase | Alteplase is a recombinant tissue plasminogen activator (rt-PA) used as a thrombolytic agent.[L43125] It cleaves plasminogen to form plasmin, an enzyme involved in the degradation of fibrin clots. In the absence of fibrin, the alteplase-mediated conversion of plasminogen is limited, thanks to the high affinity between ... | liquid | Alteplase is indicated for the treatment of acute ischemic stroke (AIS) and for use in acute myocardial infarction (AMI) for the reduction of mortality and incidence of heart failure. Alteplase is also indicated for the lysis of acute massive pulmonary embolism, defined as acute pulmonary emboli obstructing blood flow ... | Alteplase binds to fibrin and plasminogen. Alteplase specificity for fibrin is achieved thanks to its high affinity for lysine residues. Also, it can bind plasminogen via loop structures called kringles, stabilized by three disulphide linkages similar to the ones in plasminogen. The specificity of alteplase for plasmin... | Alteplase is a recombinant tissue plasminogen activator (rt-PA) that converts plasminogen to plasmin in a fibrin-dependent process. In the absence of fibrin, alteplase converts a limited amount of plasminogen. However, in the presence of fibrin clots, alteplase binds to fibrin and cleaves the arginine-valine bond at po... | Healthy volunteers with a baseline endogenous tissue plasminogen activator (t-PA) of 3.3 ng/ml had a 290-fold increase in baseline concentrations after receiving alteplase at an infusion rate of 0.25 mg/kg for 30 min; with an infusion rate of 0.5 mg/kg, a 550-fold increase was observed.[A252270] Acute myocardial infarc... | Alteplase is mainly metabolized by the liver. The carbohydrate and polypeptide domains of alteplase interact with hepatic glycoprotein receptors, leading to receptor-mediated endocytosis.[A252270] _In vivo_ studies suggest that alteplase follows zero-order kinetics, meaning that its metabolism is saturable at higher pl... | Toxicity information regarding alteplase is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as risk of bleeding and thromboembolic events.[L43125] Symptomatic and supportive measures are recommended. The carcinogenic potential of alteplase or its effect o... | Alteplase has an initial half-life of less than 5 minutes in patients with acute myocardial infarction (AMI). The dominant initial plasma half-life of the 3-hour and the accelerated regimens for AMI are similar.[L43125] | Not available. | In healthy volunteers, more than 80% of alteplase is eliminated through urine 18 hours after administration.[A252270] | The initial volume of distribution approximates plasma volume.[L43125] The average volume of distribution of the central compartment goes from 3.9 to 4.3 L, and the volume of distribution at steady state goes from 7.2 to 12 L.[A252270] | Alteplase has a plasma clearance between 380 and 570 mL/min.[L43125] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B01AD",
"B01A",
"B01",
"B",
"S01XA",
"S01X",
"S01",
"S"
] | [
"Humans and other mammals"
] | [
{
"cost": "106.33",
"description": "Cathflo activase 2 mg vial",
"unit": "vial"
},
{
"cost": "2389.85",
"description": "Activase 50 mg vial",
"unit": "vial"
},
{
"cost": "4779.71",
"description": "Activase 100 mg vial",
"unit": "vial"
}
] | [] | Alteplasa | Alteplase | Alteplase (genetical recombination) | Alteplase, recombinant | Alteplase,recombinant | Plasminogen activator (human tissue-type protein moiety) | rt-PA | t-PA | t-plasminogen activator | Tissue plasminogen activator | Tissue plasminogen activator alteplase | Tissue plasminogen activator, recombi... | [
"Activase",
"Activase",
"Activase RT-PA",
"Activase RT-PA",
"Activase RT-PA Inj",
"Activase RT-PA Inj",
"Activase RT-PA Inj",
"Cathflo",
"Cathflo Activase",
"Lysatec RT - Pa"
] | [] | [
"Lysatec RT - Pa",
"Activase RT-PA",
"Activase RT-PA"
] | [
"P00747",
"P02671",
"P02679",
"P05121"
] | [] | [] | [] |
DB00010 | Sermorelin | Sermorelin acetate is the acetate salt of an amidated synthetic 29-amino acid peptide (GRF 1-29 NH 2 ) that corresponds to the amino-terminal segment of the naturally occurring human growth hormone-releasing hormone (GHRH or GRF) consisting of 44 amino acid residues | liquid | For the treatment of dwarfism, prevention of HIV-induced weight loss | Sermorelin is used in the treatment of children with growth hormone deficiency or growth failure. Geref increases plasma growth hormone (GH) concentration by stimulating the pituitary gland to release GH. Geref is similar to the full-length native hormone (44 residues) in its ability to stimulate GH secretion in humans... | Sermorelin binds to the growth hormone releasing hormone receptor and mimics native GRF in its ability to stimulate growth hormone secretion. | null | null | null | 11-12 min | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"withdrawn"
] | [
"V04CD",
"V04C",
"V04",
"V",
"H01AC",
"H01A",
"H01",
"H"
] | [
"Humans and other mammals"
] | [] | [] | Sermorelin | GHRH receptor | GRF receptor | GRFR | Growth hormone-releasing factor receptor | [] | [
"Geref"
] | [] | [
"Q02643"
] | [] | [] | [] |
DB00011 | Interferon alfa-n1 | Interferon alfa-n1 consists of purified, natural (n is for natural) alpha interferon subtypes, at least two of which are glycosylated. This differs from recombinant alpha interferons, which are individual non-glycosylated proteins produced from individual alpha interferon genes. | liquid | For the treatment of venereal or genital warts caused by the Human Papiloma Virus. | Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also indu... | Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers ... | null | null | null | 1.2 hours (mammalian reticulocytes, in vitro); >20 hours (yeast, in vivo); >10 hours (Escherichia coli, in vivo). | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [] | [] | Interferon alfa-n1 | Interferon alpha-n1 (INS) | WELL-FERON | WELLFERON | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | ... | [
"Wellferon Inj 10 000 000unit/ml",
"Wellferon Inj 3000000unit/ml"
] | [
"Wellferon"
] | [] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00012 | Darbepoetin alfa | Human erythropoietin with 2 aa substitutions to enhance glycosylation (5 N-linked chains), 165 residues (MW=37 kD). Produced in Chinese hamster ovary (CHO) cells by recombinant DNA technology. | liquid | For the treatment of anemia (from renal transplants or certain HIV treatment) | Darbepoetin alfa is used in the treatment of anemia. It is involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass. | Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts with
progenitor stem cells to increase red cell production. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling... | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B03XA",
"B03X",
"B03",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "156.36",
"description": "Aranesp 25 mcg/ml vial",
"unit": "ml"
},
{
"cost": "162.61",
"description": "Aranesp (Albumin Free) 25 mcg/ml vial",
"unit": "vial"
},
{
"cost": "250.2",
"description": "Aranesp 40 mcg/ml vial",
"unit": "ml"
},
{
"cost": "375.3"... | [
{
"approved": "2003-03-18",
"country": "Canada",
"expires": "2010-10-15",
"number": "2165694"
},
{
"approved": "2002-11-05",
"country": "Canada",
"expires": "2014-08-16",
"number": "2147124"
}
] | Darbepoetin | Darbepoetin alfa | Darbepoetin alfa,recombinant | Darbepoetina alfa | EPO-R | [
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Ara... | [] | [] | [
"P19235"
] | [] | [] | [] |
DB00013 | Urokinase | Urokinase is an endogenous peptide that is cleaved in the presence of plasmin between lysine 158 and isoleucine 159 to yield active urokinase.[A191943] Urokinase remains connected between these 2 chains by a sulfhydryl bond.[A191943]
Urokinase was granted FDA approval on 16 January 1978.[L12138] | liquid | In Canada, urokinase is indicated for lysis of acute massive pulmonary emboli, acute thrombi obstructing coronary arteries, occlusive thromboemboli in peripheral arteries and grafts, and restoration of patency to intravenous catheters.[L12141] | Urokinase is a serine protease that activates plasminogen to an active fibrinolytic protease.[A191928] The duration of action is short due to the short half life.[L12138] Patients should be counselled regarding the risk of bleeding, anaphylaxis, infusion reactions, and cholesterol embolization.[L12138 | Urokinase is a serine protease.[A191928] It cleaves plasminogen to form the active fibrinolytic protease, plasmin.[A191928] | Urokinase is delivered intravenously, so the bioavailability is high. | Because urokinase is a protein, it is expected to be metabolized by proteases to smaller proteins and amino acids. | Patients experiencing an overdose may present with bleeding.[L12141] Treat patients with symptomatic and supportive measures which may include application of local pressure, administration of whole blood or plasma, and administration of aminocaproic acid.[L12141] | Urokinase has a half life of 12.6±6.2 minutes.[L12138] | Data regarding the protein binding of urokinase in plasma is not readily available. | Urokinase is eliminated in the bile and urine.[L12138] | The volume of distribution of urokinase is 11.5L.[L12138] | Data regarding the clearance of urokinase is not readily available. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational",
"withdrawn"
] | [
"B01AD",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [] | [] | Kinase (enzyme-activating), uro-urokinase | TCUK | Tissue culture urokinase | Two-chain urokinase | Urochinasi | Urokinase | Urokinasum | Uroquinasa | 3.4.21.7 | MO3 | Monocyte activation antigen Mo3 | U-PAR | UPAR | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1 | Monocyte Arg-se... | [
"Kinlytic",
"Kinlytic (urokinase for Injection)",
"Kinlytic Open-cath"
] | [
"Abbokinase"
] | [] | [
"P00747",
"Q03405",
"P05121",
"P05120",
"P05154",
"P98164",
"Q9Y5Y6",
"P14543"
] | [
"P39900"
] | [] | [] |
DB00014 | Goserelin | Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medi... | solid | Goserelin is indicated for:
- Use in combination with flutamide for the management of locally confined carcinoma of the prostate
- Palliative treatment of advanced carcinoma of the prostate
- The management of endometriosis
- Use as an endometrial-thinning agent prior to endometrial ablation for dysfunctional ute... | The pharmacokinetics of goserelin have been determined in both male and female healthy volunteers and patients. In these studies, goserelin was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route. | Goserelin is a synthetic decapeptide analogue of LHRH. Goserelin acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels. | Inactive orally, rapidly absorbed following subcutaneous administration. | Hepatic | No experience of overdosage from clinical trials. | 4-5 hours | 27.3% | Clearance of goserelin following subcutaneous administration of a radiolabeled solution of goserelin was very rapid and occurred via a combination of hepatic and urinary excretion. More than 90% of a subcutaneous radiolabeled solution formulation dose of goserelin was excreted in urine. | * 44.1 ± 13.6 L [subcutaneous administration of 250 mcg] | * 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot] | Organic compounds | Organic acids and derivatives | Carboxylic acids and derivatives | Amino acids, peptides, and analogues | [
"approved"
] | [
"L02AE",
"L02A",
"L02",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "451.19",
"description": "Zoladex 3.6 mg implant syringe",
"unit": "syringe"
},
{
"cost": "1380.65",
"description": "Zoladex 10.8 mg implant syringe",
"unit": "syringe"
}
] | [
{
"approved": "2006-10-10",
"country": "United States",
"expires": "2022-04-13",
"number": "7118552"
},
{
"approved": "2007-05-22",
"country": "United States",
"expires": "2022-04-09",
"number": "7220247"
},
{
"approved": "2009-03-10",
"country": "United States",
... | Goserelin | Goserelina | LCGR | LGR2 | LH/CG-R | LHR | LHRHR | LSH-R | Luteinizing hormone receptor | GNRH | GRH | LHRH | Progonadoliberin I | GnRH receptor | GnRH-R | GRHR | [
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex LA"
] | [] | [] | [
"P22888",
"P01148",
"P30968"
] | [] | [] | [] |
DB00015 | Reteplase | Human tissue plasminogen activator, purified, glycosylated, 355 residues purified from CHO cells. Retavase is considered a "third-generation" thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids p... | liquid | For lysis of acute pulmonary emboli, intracoronary emboli, and management of myocardial infarction. | Reteplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction. | Reteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B01AD",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "2605.93",
"description": "Retavase vial half-kit",
"unit": "vial"
}
] | [
{
"approved": "2007-12-18",
"country": "Canada",
"expires": "2012-04-15",
"number": "2107476"
}
] | Human t-PA (residues 1-3 and 176-527) | Reteplasa | Reteplase | Reteplase, recombinant | Reteplase,recombinant | 3.4.21.7 | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1 | [
"Rapilysin",
"Retavase",
"Retavase",
"Retavase",
"Retavase",
"Retavase"
] | [] | [] | [
"P00747",
"P02671",
"P05121"
] | [] | [] | [] |
DB00016 | Erythropoietin | Erythropoietin (EPO) is a growth factor produced in the kidneys that stimulates the production of red blood cells. It works by promoting the division and differentiation of committed erythroid progenitors in the bone marrow [FDA Label]. Epoetin alfa (Epoge) was developed by Amgen Inc. in 1983 as the first rhEPO commerc... | liquid | Indicated in adult and paediatric patients for the:
- treatment of anemia due to Chronic Kidney Disease (CKD) in patients on dialysis and not on dialysis.
- treatment of anemia due to zidovudine in patients with HIV-infection.
- treatment of anemia due to the effects of concomitant myelosuppressive chemotherapy,... | Erythropoietin and epoetin alfa are involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass. It is reported to increase the reticulocyte count within 10 days of initiation, followed by increases in the RBC count, hemoglobin, and hematocrit, ... | Erythropoietin or exogenous epoetin alfa binds to the erythropoietin receptor (EPO-R) and activates intracellular signal transduction pathways [A33079]. The affinity (Kd) of EPO for its receptor on human cells is ∼100 to 200 pM [A33080]. Upon binding to EPO-R on the surface of erythroid progenitor cells, a conformation... | The time to reach peak concentration is slower via the subcutaneous route than the intravenous route which ranges from 20 to 25 hours, and the peak is always well below the peak achieved using the intravenous route (5–10% of those seen with IV administration).[A33080] The bioavailability of subcutaneous injectable eryt... | Binding of erythropoietin and epoetin alfa to EPO-R leads to cellular internalization, which involves the degradation of the ligand. Erythropoietin and epoetin alfa may also be degraded by the reticuloendothelial scavenging pathway or lymphatic system [A33080]. | Overdose from epoetin alfa include signs and symptoms associated with an excessive and/or rapid increase in hemoglobin concentration, including cardiovascular events. Patients with suspected or known overdose should be monitored closely for cardiovascular events and hematologic abnormalities. Polycythemia should be man... | **Healthy volunteers:** The half life is approximately 4 hours in healthy volunteers receiving an intravenous injection [F85]. A half-life of approximately 6 hours has been reported in children [F85].
**Adult and paediatric patients with CRF:** The elimination half life following intravenous administration ranges fr... | No information of serum protein binding available. | Erythropoietin and epoetin alfa are cleared via uptake and degradation via the EPO-R-expressing cells, and may also involve other cellular pathways in the interstitium, probably via cells in the reticuloendothelial scavenging pathway or lymphatic system [A33080]. Only a small amount of unchanged epoetin alfa is found i... | In healthy volunteers, the volume of distribution of intravenous epoetin alfa was generally similar to the plasma volume (range of 40–63.80 mL/kg), indicating limited extravascular distribution [A33080, A33076]. | **Healthy volunteers: ** In male volunteers receiving intravenous epoetin alfa, the total body clearance was approximately 8.12 ± 1.00 mL/h/kg [A33076].
**Cancer patients receiving cyclic chemotherapy:** The average clearance was approximately 20.2 ± 15.9 mL/h/kg after 150 Units/kg three times per week (TIW) subcut... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B03XA",
"B03X",
"B03",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "34.14",
"description": "Epogen 2000 unit/ml vial",
"unit": "vial"
},
{
"cost": "37.09",
"description": "Procrit 2000 unit/ml vial",
"unit": "vial"
},
{
"cost": "47.53",
"description": "Epogen 3000 unit/ml vial",
"unit": "vial"
},
{
"cost": "55.63",
... | [
{
"approved": "1997-05-27",
"country": "Canada",
"expires": "2014-05-27",
"number": "1339047"
}
] | 1-165-Erythropoietin (human clone λHEPOFL13 protein moiety), glycoform α | E.P.O. | EPOETIN | Epoetin alfa | Epoetin alfa rDNA | Epoetin alfa-epbx | Epoetin alfa, recombinant | Epoetin epsilon | Epoetin gamma | Epoetin gamma rDNA | Epoetin kappa | Epoetin omega | Epoetin theta | Epoetin zeta | Epoetina alfa | Epoetina ... | [
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseame... | [
"Epobel",
"Epocept",
"Epofit",
"Epogin",
"Eqralys",
"Nanokine"
] | [] | [
"P19235"
] | [] | [] | [] |
DB00017 | Salmon calcitonin | Synthetic peptide, 32 residues long formulated as a nasal spray. | liquid | Used in the treatment of symptomatic Paget's disease for patients unresponsive to alternate treatments or intolerant to such treatments. In addition, it is used in emergency situations when serum calcium levels must be decreased quickly until the underlying condition is identified. It can also be added to existing ther... | Calcitonin inhibits bone resorption by osteoclasts (bone remodeling cells) and promotes bone formation by osteoblasts. This leads to a net increase in bone mass and a reduction in plasma calcium levels. It also promotes the renal excretion of ions such as calcium, phosphate, sodium, magnesium, and potassium by decreasi... | Calcitonin binds to the calcitonin receptor (found primarily in osteoclasts) which then enhances the production of vitamin D producing enzymes (25-hydroxyvitamine D-24-hydroxylase), leading to greater calcium retention and enhanced bone density. Binding of calcitonin to its receptor also activates adenylyl cyclase and ... | Salmon calcitonin is rapidly absorbed with bioavailability of 71% following subcutaneous injection and 66% following intramuscular injection in humans. Via the nasal route, the bioavailability varies between 3 to 5% relative to IM. | Salmon calcitonin primarily undergoes degradation in the kidneys to form pharmacologically inactive metabolites. It is also metabolized in the blood and the peripheral tissue. | Salmon calcitonin was shown to inhibit lactation in animals and is not recommend in nursing mothers. While research in animals have shown a decrease in fetal weight, no studies have yet shown similar results in humans. It is recommended however to proceed carefully when administering salmon calcitonin to pregnant women... | Half-life elimination (terminal): I.M. 58 minutes; SubQ 59 to 64 minutes; Nasal: ~18 to 23 minutes | Protein binding is about 30 to 40%. | Urine. Studies with injectable calcitonin show increases in the excretion of filtered phosphate, calcium, and sodium by decreasing their tubular reabsorption in the kidney. | 0.15 to 0.3 L/kg | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"H05BA",
"H05B",
"H05",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "8.81",
"description": "Caltine 100 (100 Iu/Ml) 100 iu/ml",
"unit": "ml"
},
{
"cost": "29.94",
"description": "Calcimar 200 iu/ml",
"unit": "ml"
},
{
"cost": "30.73",
"description": "Miacalcin 200 unit/ml vial",
"unit": "ml"
},
{
"cost": "34.3",
"des... | [
{
"approved": "1998-03-31",
"country": "United States",
"expires": "2015-03-31",
"number": "5733569"
},
{
"approved": "2002-08-27",
"country": "United States",
"expires": "2021-02-02",
"number": "6440392"
},
{
"approved": "2012-08-14",
"country": "United States",
... | Calcitonin (Salmon Synthetic) | Calcitonin salmon | Calcitonin salmon recombinant | Calcitonin-salmon | Calcitonin, salmon | Calcitonina salmón sintética | Recombinant salmon calcitonin | Salmon calcitonin | CT-R | [
"Apo-calcitonin Injectable",
"Apo-calcitonin Nasal Spray",
"Calcimar",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calciton... | [
"Calcimar"
] | [] | [
"P30988"
] | [] | [] | [] |
DB00018 | Interferon alfa-n3 | Purified, natural (n is for natural) human interferon alpha proteins (consists of 3 forms or polymorphisms including 2a, 2b and 2c). 166 residues, some are glycosylated (MW range from 16 kD to 27 kD). | liquid | For the intralesional treatment of refractory or recurring external condylomata acuminata. | Interferon alfa-n3 upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interfe... | Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers ... | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [] | [
"Humans and other mammals"
] | [
{
"cost": "412.87",
"description": "Alferon n 5 million unit vial",
"unit": "ml"
}
] | [] | Interferon alfa-n3 | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interferon ... | [
"Alferon"
] | [
"Alferon",
"Alferon N"
] | [] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00019 | Pegfilgrastim | Pegfilgrastim is a PEGylated form of the recombinant human granulocyte colony-stimulating factor (G-CSF) analogue, [filgrastim].[A187601] The drug is approved for use to decrease the incidence of infection, as manifested by febrile neutropenia, in susceptible patients with with non-myeloid cancer receiving myelosuppres... | liquid | Pegfilgrastim is indicated to decrease the incidence of infection, as manifested by febrile neutropenia, in patients with non myeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a clinically significant incidence of febrile neutropenia.[L44221]
It is also indicated to increase survival... | Pegfilgrastim is a recombinant human granulocyte colony-stimulating factor (G-CSF) that promotes the production, proliferation, and maturation of neutrophils, which are white blood cells involved in both innate and adaptive immune responses.[A187631,A248855] The safety and efficacy of pegfilgrastim in reducing the risk... | Neutrophils are short-lived immune cells that are highly susceptible to cell death following myelosuppressive chemotherapy. This marked reduction in neutrophil numbers during chemotherapy increases the risk of hospitalization, infection, and infection-related mortality. It also directly impacts the clinical outcome of ... | Pegfilgrastim has a lower absolute bioavailability than filgrastim following subcutaneous administration. The absorption of pegfilgrastim is largely dependent on the lymphatic system due to the attached PEG group contributing to the large size of the drug. It is slowly absorbed following subcutaneous administration wit... | It is not know whether pegfilgrastim is metabolized into major metabolites.[L10022] Once it binds to the therapeutic target, pegfilgrastim is internalized by the neutrophil and undergoes nonspecific degradation.[A29] | The maximum safe dose of pegfilgrastim has not been established; however, the highest dose used in clinical trials was 300 mcg/kg.[A248855] Overdosage of pegfilgrastim may result in leukocytosis and bone pain. Events of edema, dyspnea, and pleural effusion have been reported in a single patient who self-administered pe... | The serum half-life of Pegfilgrastim is highly variable depending on the absolute neutrophil count, with the range of 15 to 80 hours following subcutaneous administration. The median serum half-life of 42 hours.[A187607,L9746] | The plasma protein binding of pegfilgrastim is unlikely.[L10022] | The polyethylene glycol moiety limits the renal clearance by glomerular filtration of pegfilgrastim, making neutrophil-mediated clearance as the predominant route of elimination.[A187607] This elimination pathway is initiated by the binding of pegfilgrastim to the G-CSF receptor on the neutrophil cell surface, leading ... | Pegfilgrastim appears to have a volume of distribution of approximately 170 L.[A33290] | Pegfilgrastim has a self-regulating clearance that involves neutrophil-induced clearance.[A29,A187631] The clearance is dependent on the number of neutrophils and body weight of the patient: the clearance increases with increasing number of granulocytes and lower body weights.[L9746] Pegfilgrastim is not eliminated fro... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AA",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "4026.05",
"description": "Neulasta 6 mg/0.6ml Solution 0.6ml Syringe",
"unit": "syringe"
},
{
"cost": "4102.37",
"description": "Neulasta 6 mg/0.6 ml syringe",
"unit": "syringe"
}
] | [
{
"approved": "2007-07-31",
"country": "Canada",
"expires": "2024-07-31",
"number": "1341537"
},
{
"approved": "1997-07-29",
"country": "Canada",
"expires": "2014-07-29",
"number": "1339071"
}
] | Granulocyte colony-stimulating factor pegfilgrastim | peg-filgrastim | Pegfilgrastim | pegfilgrastim-apgf | pegfilgrastim-bmez | pegfilgrastim-cbqv | pegfilgrastim-jmdb | G-CSF receptor | G-CSF-R | GCSFR | 3.4.21.37 | Bone marrow serine protease | ELA2 | Elastase-2 | HLE | Human leukocyte elastase | Medullasin | PMN el... | [
"Armlupeg",
"Cegfila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fylnetra",
"Grasustek",
"Lapelga",
"Lapelga",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neupopeg",
"Neupopeg",
"Neupopeg",
"Niopeg",
... | [] | [] | [
"Q99062"
] | [
"P08246"
] | [] | [] |
DB00020 | Sargramostim | Sargramostim is a human recombinant granulocyte macrophage colony-stimulating factor (GM-CSF) expressed in yeast. It is a glycoprotein that is 127 residues. Substitution of Leu23 leads to a difference from native protein. | liquid | For the treatment of cancer and bone marrow transplant | Sargramostim is used in the treatment of bone marrow transplant recipients or those exposed to chemotherapy an recovering from acut myelogenous leukemia, Leukine or GM-CSF is a hematopoietic growth factor which stimulates the survival, clonal expansion (proliferation) and differentiation of hematopoietic progenitor cel... | Sargramostim binds to the Granulocyte-macrophage colony stimulating factor receptor (GM-CSF-R-alpha or CSF2R) which stimulates a JAK2 STAT1/STAT3 signal transduction pathway. This leads to the production of hemopoietic cells and neutrophils | null | null | null | null | null | null | null | * 420 mL/min/m2 [Normal people with liquid LEUKINE (IV)]
* 431 mL/min/m2 [Normal people with lyophilized LEUKINE (IV)]
* 549 mL/min/m2 [Normal people with liquid LEUKINE (SC)]
* 529 mL/min/m2 [Normal people with lyophilized LEUKINE (SC)] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AA",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "204.79",
"description": "Leukine 250 mcg vial",
"unit": "vial"
},
{
"cost": "0.42",
"description": "Bio-immunex capsule",
"unit": "capsule"
}
] | [
{
"approved": "2000-12-05",
"country": "Canada",
"expires": "2017-12-05",
"number": "1341150"
}
] | Recombinant human granulocyte-macrophage colony stimulating factor | rGM-CSF | rHu GM-CSF | Sargramostim | CDw116 | CSF2R | CSF2RY | GM-CSF-R-alpha | GMCSFR-alpha | GMR-alpha | IL-3 receptor subunit alpha | IL-3R subunit alpha | IL-3R-alpha | IL-3RA | IL3R | CDw131 | GM-CSF/IL-3/IL-5 receptor common beta subunit | IL3R... | [
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine"
] | [
"Leucomax"
] | [] | [
"P15509",
"P26951",
"P32927",
"P34741",
"P13727"
] | [] | [] | [] |
DB00022 | Peginterferon alfa-2b | Peginterferon alfa-2b is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most co... | liquid | Peginterferon alfa-2b is indicated for the treatment of HCV in combination with [DB00811] and a NS3/4A protease inhibitor for genotype 1 or without a NS3/4A protease inhibitor for genotypes 2-6 [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral... | Peginterferon alfa-2b inhibits viral replication in infected cells, suppresses cell proliferation, induces apoptosis, and exerts an anti-angiogenic effect [FDA Label]. Exerts immunomodulatory effects such as enhancement of the phagocytic activity of macrophages, activation of NK cells, stimulation of cytotoxic T-lympho... | Peginterferon alfa-2b is derived from recombinant human interferon's alfa-2b moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involv... | Peginterferon alfa-2b reaches peak plasma concentration 15-44 hours after subcutaneous administration [FDA Label]. The mean absorption half-life is 4.6 hours. After multiple doses the bioavailability of Peginterferon alfa-2b increases with trough concentrations at week 48 3-fold higher than those at week 4. | null | Peginterferon alfa-2b may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterf... | The mean half-life of elimination of Peginterferon alfa-2b is 40 hours in a range of 22-60 hours [FDA Label]. | null | Renal elimination accounts for 30% of Peginterferon alfa-2b elimination [FDA Label]. | null | The estimated apparent clearance of Peginterferon alfa-2b is 22 milliters per hour per kilogram [FDA Label]. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AB",
"L03A",
"L03",
"L",
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "553.4",
"description": "Peg-Intron 50 mcg kit",
"unit": "kit"
},
{
"cost": "553.4",
"description": "Peg-Intron redipen 50 mcg",
"unit": "redipen"
},
{
"cost": "581.02",
"description": "Peg-Intron redipen 80 mcg",
"unit": "redipen"
},
{
"cost": "607.19",... | [
{
"approved": "2008-02-19",
"country": "Canada",
"expires": "2025-02-19",
"number": "1341567"
},
{
"approved": "2002-02-26",
"country": "Canada",
"expires": "2016-10-31",
"number": "2329474"
}
] | Peginterferon alfa-2b | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interfer... | [
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"PegIntron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"PegIntron",
"PegIntron",
"PegIntron",
"PegIntron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron... | [
"PEG-Intron"
] | [
"Pegetron",
"Pegetron",
"Pegetron",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron"
] | [
"P17181",
"P48551"
] | [
"P05177",
"P10635",
"P11712"
] | [] | [] |
DB00023 | Asparaginase Escherichia coli | Asparaginase derived from _Escherichia coli_ (L-asparagine amidohydrolase, EC 3.5.1.1) is an enzyme responsible for the metabolism of L-asparagine, by catalyzing L-asparagine into L-aspartic acid and ammonia. It also facilitates the production of oxaloacetate which is needed for general cellular metabolism. Asparaginas... | liquid | Indicated as a component of a multi-agent chemotherapeutic regimen for the treatment of patients with acute lymphoblastic leukemia (ALL).[L39809] | In clinical trials of patients with previously untreated, standard-risk ALL, administration of asparaginase resulted in a decrease of plasma asparagine levels from average of 41 μM to less than 3 μM [FDA Label]. The native asparaginase in whom plasma enzyme activity before treatment was greater than 0.1 International U... | Asparagine is a non-essential amino acid that maintains DNA, RNA and protein synthesis and promotes cell growth. While healthy and normal cells are capable of obtaining asparagine via dietary intake or synthesizing the asparagine from aspartate via asparagine synthetase activity, lymphoblastic leukemic cells lack the a... | In a study in patients with metastatic cancer and leukemia, daily intravenous administration of L-asparaginase derived from _E. coli_ resulted in a cumulative increase in plasma levels. Following intramuscular injection in patients with metastatic cancer and leukemia, peak plasma levels of asparaginase was achieved 14 ... | null | No studies assessing the mutagenic or carcinogenic potential of _E. coli_ L-asparagine have been conducted. In the Ames assay, no mutagenic effect was demonstrated when tested against Salmonella typhimurium strains [FDA Label]. No studies have been performed on impairment of fertility [FDA Label]. Following a single, i... | Plasma half life of L-asparagine derived from _E. coli_ following intravenous injection was 8-30 hrs [FDA Label]. Plasma half-life was 34 to 49 hours after intramuscular injection [FDA Label]. Half-life (mean ± SD) of native _E. coli_ asparaginase is approximately 1.28 ± 0.35 days [A31999]. | null | null | Apparent volume of distribution was slightly greater than the plasma volume. Asparaginase levels in cerebrospinal fluid were less than 1% of concurrent plasma levels [A31999]. | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L01XX",
"L01X",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "74.6",
"description": "Elspar 10000 unit vial",
"unit": "vial"
}
] | [] | Asparaginase | Asparaginase (E. coli) | Colaspase | Escherichia coli L-asparaginase | L-asparaginase | L-asparagine amidohydrolase | Serpin A7 | T4-binding globulin | TBG | [
"Elspar",
"Kidrolase",
"Rylaze",
"Spectrila",
"Spectrila"
] | [] | [] | [] | [] | [
"P05543"
] | [] |
DB00024 | Thyrotropin alfa | Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients who have had their thyroid gland removed because of thyroid cance... | liquid | For detection of residueal or recurrent thyroid cancer | Binding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differen... | Thyrotropin Alfa binds to the thyrotropin receptors found on any residual thyroid cells or tissues. This stimulates radioactive iodine uptake for better radiodiagnostic imaging. | Time to peak: Median: 10 hours (range: 3-24 hours)
After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L. | null | No difference in efficacy and toxicity between adult and geriatric patients. No studies in lactating women, pregnant women and pediatrics. Cautionary administration is advised. | 25 ± 10 hours | null | kidney and liver | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"vet_approved"
] | [
"H01AB",
"H01A",
"H01",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "1196.4",
"description": "Thyrogen 1.1 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1998-11-24",
"country": "United States",
"expires": "2015-11-24",
"number": "5840566"
}
] | Recombinant Human Thyroid Stimulating Hormone | Recombinant thyrotropin alfa | rhTSH | rTSH | Thyrotropin alfa | Thyrotropin alpha | LGR3 | Thyroid-stimulating hormone receptor | TSH-R | [
"Thyrogen",
"Thyrogen",
"Thyrogen",
"Thyrogen",
"Thyrogen"
] | [] | [] | [
"P16473"
] | [] | [] | [] |
DB00025 | Antihemophilic factor, human recombinant | Human recombinant antihemophilic factor (AHF) or Factor VIII, 2332 residues, glycosylated, produced by CHO cells | solid | The human recombinant antihemophilic factor is indicated for use in adults and children with hemophilia A for the control and prevention of bleeding episodes, perioperative management, and routine prophylaxis to prevent or reduce the frequency of bleeding episodes.[L41025, L36130] | Antihemophilic Factor binds factor IXa along with calcium and phospholipid, This complex converts factor X to factor Xa to facilitate clotting cascade. | Antihemophilic factor (AHF) is a protein found in normal plasma which is necessary for clot formation. The administration of AHF provides an increase in plasma levels of AHF and can temporarily correct the coagulation defect of patients with hemophilia A (classical hemophilia). | null | null | null | 8.4-19.3 hrs | null | null | null | * 4.1 mL/h•kg [Previously treated pediatric patients] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B02BD",
"B02B",
"B02",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "1.01",
"description": "Monoclate-p 1000 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"description": "Monoclate-p 1500 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"description": "Monoclate-p 250 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"descr... | [
{
"approved": "2007-09-11",
"country": "Canada",
"expires": "2013-10-01",
"number": "2124690"
},
{
"approved": "1997-09-23",
"country": "Canada",
"expires": "2014-09-23",
"number": "1339477"
}
] | Antihemophilic factor (recombinant) | Antihemophilic factor recombinant | Antihemophilic factor, human recombinant | Antihemophilic factor, recombinant | Coagulation factor VIII, recombinant | Factor VIII (rDNA) | Factor VIII (Recombinant) | Factor VIII recombin | Factor VIII, recombinant | Human Factor VIII (Recombina... | [
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Adv... | [
"Bioclate",
"Helixate",
"Hyate:C",
"Koate-HP",
"Kogenate",
"Monarc-M",
"ReFacto"
] | [] | [
"P00742",
"P00740",
"P04275",
"O14832",
"P07307",
"P11021",
"P27797",
"P27824",
"P49257",
"Q07954",
"Q8NI22"
] | [
"P00734",
"P04070"
] | [] | [] |
DB00026 | Anakinra | Anakinra is a recombinant human interleukin-1 (IL-1) receptor antagonist (IL-1Ra) composed of 153 amino acid residues. Unlike native human IL-1Ra, anakinra has an additional methionine residue at the amino terminus. This drug binds to the IL-1 receptor, competing with and inhibiting the activity of IL-1 alpha and beta.... | liquid | Anakinra is an interleukin-1 receptor antagonist indicated for the reduction in signs and symptoms and slowing the progression of structural damage in moderately to severely active rheumatoid arthritis (RA), in patients 18 years of age or older who have failed one or more disease-modifying antirheumatic drugs (DMARDs).... | Anakinra is a recombinant human interleukin-1 receptor antagonist (IL-1Ra) that blocks the biologic activity of interleukin-1 (IL-1) by competitively inhibiting its ability to bind to the IL-1 type I receptor (IL-1RI). IL-1 production is higher in inflammatory diseases such as rheumatoid arthritis, where the amount of ... | Interleukin-1 (IL-1) plays an important role in inflammation and immunological responses. Inflammatory stimuli trigger its production, and it binds to the IL-1 receptor to activate a wide variety of mechanisms. The activity of the IL-1 receptor is also regulated by a naturally occurring IL-1 receptor antagonist (IL-1Ra... | The bioavailability of anakinra is 95% in healthy subjects administered a 70 mg subcutaneous bolus injection. In patients with rheumatoid arthritis (RA) administered a subcutaneous dose of anakinra, the maximum plasma concentration was detected 3 to 7 hours later. No unexpected accumulation was observed in RA patients ... | As a protein-based therapy, anakinra is expected to be metabolized by proteases throughout the body. | In clinical trials done in patients with rheumatoid arthritis (RA) and neonatal-onset multisystem inflammatory disease (NOMID) treated with anakinra, no cases of overdose were reported.[L35415] Sepsis trials were performed using mean calculated doses up to 35 times the ones given to patients with RA over 72 hours. Anak... | In patients with rheumatoid arthritis (RA), the terminal half-life of anakinra ranged from 4 to 6 hours. In patients with neonatal-onset multisystem inflammatory disease (NOMID), the median half-life of anakinra was 5.7 h (range=3.1-28.2, n=12).[L35415] | Not Available | Anakinra is mostly excreted by the kidney; therefore, the risk of toxic reactions may increase in patients with impaired renal function.[L35415] | In adult subjects with rheumatoid arthritis (RA) treated with anakinra (n=35), the volume of distribution averaged 18.5 L.[L41628] | In patients with rheumatoid arthritis (RA), the clearance of anakinra was relatively consistent for different dose levels.[L41628] Clearance is variable and increases with increasing creatinine clearance and body weight. However, gender and age were not significant factors.[L35415] In patients with mild (creatinine cle... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L04AC",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "61.8",
"description": "Kineret 100 mg/0.67 ml syr",
"unit": "syringe"
},
{
"cost": "449.9",
"description": "Kineret 1 Box = 7 Syringes, 4.69ml Box",
"unit": "box"
}
] | [
{
"approved": "2008-04-08",
"country": "Canada",
"expires": "2013-09-17",
"number": "2141953"
},
{
"approved": "2001-11-27",
"country": "Canada",
"expires": "2018-11-27",
"number": "1341322"
}
] | Anakinra | IL-1RA | Interleukin-1 receptor antagonist anakinra | 3.2.2.6 | CD121 antigen-like family member A | IL-1R-1 | IL-1R-alpha | IL-1RT-1 | IL-1RT1 | IL1R | IL1RA | IL1RT1 | Interleukin-1 receptor alpha | Interleukin-1 receptor type I | p80 | [
"Kineret",
"Kineret",
"Kineret",
"Kineret",
"Kineret",
"Kineret",
"Kineret",
"Kineret"
] | [] | [] | [
"P14778"
] | [] | [] | [] |
DB00027 | Gramicidin D | Gramcidin D is a heterogeneous mixture of three antibiotic compounds, gramicidins A, B and C, making up 80%, 6%, and 14% respectively all of which are obtained from the soil bacterial species Bacillus brevis and called collectively gramicidin D. Gramcidins are 15 residue peptides with alternating D and L amino acids, w... | liquid | For treatment of skin lesions, surface wounds and eye infections. | Gramicidin is particularly effective against gram-positive bacteria. Because the drug is highly hemolytic, it cannot be administered internally and so is used only on the skin as a lotion or ointment. It is used primarily in the treatment of infected surface wounds, and in eye, nose, and throat infections. It is normal... | Gramicidin D binds to and inserts itself into bacterial membranes (with a strong preference to gram-positive cell membranes). This results in membrane disruption and permeabilization (it acts as a channel). This leads to (i) loss of intracellular solutes (e.g., K+ and amino acids); (ii) dissipation of the transmembrane... | null | null | null | null | null | null | null | null | Organic compounds | Organic Polymers | Polypeptides | null | [
"approved"
] | [
"R02AB",
"R02A",
"R02",
"R"
] | [
"Staphylococcus aureus",
"Streptococcus agalactiae",
"Streptococcus pneumoniae",
"Escherichia coli",
"Haemophilus influenzae",
"Klebsiella",
"Enterobacter",
"Neisseria gonorrhoeae",
"Neisseria meningitidis",
"Pseudomonas aeruginosa"
] | [
{
"cost": "23.12",
"description": "Neosporin gu irr 40 mg/ml amp",
"unit": "ml"
},
{
"cost": "240.0",
"description": "Gramicidin d powder",
"unit": "g"
},
{
"cost": "0.32",
"description": "Neosporin + pain relief cream",
"unit": "g"
}
] | [] | Bacillus brevis gramicidin D | Gramicidin | Gramicidin A | Gramicidin B | Gramicidin C | Gramicidina | Gramicidine | 2.5.1.15 | dhpS | Dihydropteroate pyrophosphorylase | ATP-binding cassette sub-family B member 1 | MDR1 | Multidrug resistance protein 1 | P-glycoprotein 1 | PGY1 | Phospholipid transporter ABCB1 | [
"Antibiotic Cream",
"Antibiotic Cream",
"Antibiotic Cream",
"Antibiotic Cream for Kids",
"Antibiotic Cream for Kids",
"Antibiotic Cream Plus Pain Relief",
"Antibiotic Cream Plus Pain Relief",
"Antibiotic Cream Plus Pain Relief for Kids",
"Antibiotic Drops",
"Antibiotic Ear Drops",
"Antibiotic Ey... | [
"Sofradex"
] | [
"Neomycin and Polymyxin B Sulfates and Gramicidin",
"Neomycin and Polymyxin B Sulfates and Gramicidin",
"Neomycin and Polymyxin B Sulfates and Gramicidin",
"Neosporin",
"Neomycin and Polymyxin B Sulfates and Gramicidin",
"Neomycin and Polymyxin B Sulfates and Gramicidin",
"Neomycin and Polymyxin B Sulfa... | [] | [] | [] | [
"P08183"
] |
DB00028 | Human immunoglobulin G | Intravenous immunoglobulin (IVIg) is a mixture of IgG1 and other antibodies derived from healthy human plasma via Cohn fractionation. The purification process includes cold alcohol fractionation, polyethylene glycol precipitation, and ion exchange chromatography. IVIg contains the same distribution of IgG antibody subc... | liquid | Human immunoglobulin G is indicated for the following conditions:
### Primary Immunodeficiency
- for the treatment of primary immunodeficiency in adult and pediatric patients[L39920, L39930, L39935, L39940, L39945, L39950, L39955, L39960, L39965, L39975, L39980, L40029, L40034, L40044]
- in combination with [hyalu... | Used as a replacement therapy in inherited humoral immunodeficiency disorders such as severe combined immunodeficiency syndrome, x-linked agammaglobulinemia, and Wiskott-Aldrich Syndrome. The immunoglobulins target, bind and kill bacterial cells as well as viral particles. IgG is the monomeric immunoglobulin of which t... | IVIg interacts with a number of different components of the immune system, including cytokines, complement, Fc receptors and several cell surface immunocompetent molecules. IVIg also impacts different effector cells of the immune system (B and T lymphocytes, dendritic cells, etc.) and regulates a wide range of genes. I... | null | null | null | >20 hours (mammalian reticulocytes, in vitro). | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [] | [
"Humans and other mammals",
"Bacteria and protozoa",
"Various viruses"
] | [
{
"cost": "4.84",
"description": "Flebogamma 5% vial",
"unit": "ml"
},
{
"cost": "4.84",
"description": "Flebogamma dif 5% vial",
"unit": "ml"
},
{
"cost": "9.34",
"description": "Immune globulin vial",
"unit": "ml"
},
{
"cost": "11.6",
"description": "Gamunex... | [] | Aerosolized pooled immune globulin | Human gammaglobulin | Human IGG | Human immunoglobulin G | Human normal immunoglobulin | Immune globulin (human) | Immune globulin human | Immunoglobulin (human) | Immunoglobulin G (human) | Immunoglobulin G, human | Intravenous immune globulin (human) | Intravenous immunoglobulin (... | [
"Alyglo",
"Asceniv",
"Bivigam",
"Bivigam",
"Bivigam",
"Bivigam",
"Bivigam",
"Carimune Nanofiltered",
"Carimune Nanofiltered",
"Carimune Nanofiltered",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cutaquig",
"Cuta... | [
"ClairYg"
] | [
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Iveegam Immuno 5000mg (iv)",
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Iypoly",
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Hyqvia",
"Hyqvia"
] | [
"P12314",
"Q92637",
"P12318",
"P31994",
"P31995",
"P08637",
"O75015",
"P01024",
"P0C0L4",
"P0C0L5",
"P01031"
] | [] | [] | [] |
DB00029 | Anistreplase | Human tissue plasminogen activator, purified, glycosylated, 527 residues purified from CHO cells. Eminase is a lyophilized (freeze-dried) formulation of anistreplase, the p-anisoyl derivative of the primary Lys-plasminogen-streptokinase activator complex (a complex of Lys-plasminogen and streptokinase). A p-anisoyl gro... | liquid | For lysis of acute pulmonary emboli, intracoronary emboli and management of myocardial infarction | Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction. | Anistreplase cleaves the Arg/Val bond in plasminogen to form plasmin. This in turn leads to the degradation of blood clots. | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B01AD",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [] | [] | Anisoylated plasminogen streptokinase activator complex | Anistreplase | APSAC | 3.4.21.7 | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1 | [
"Eminase 30 Units"
] | [
"Eminase"
] | [] | [
"P00747",
"P02671",
"P05121"
] | [] | [] | [] |
DB00030 | Insulin human | Human Insulin, also known as Regular Insulin, is a short-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Human insulin is produced by recombinant DNA technology and is identical to endogenously produced insulin. Typically prescribed for the management of diabetes mel... | liquid | Human insulin is indicated to improve glycemic control in adults and pediatric patients with diabetes mellitus. | Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes following meals. Postprandial insulin spikes are responsible for the metabolic changes that occur as the body transitions from a postabsorptive to absorptive sta... | The primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in ... | When injected subcutaneously, the glucose-lowering effect of human insulin begins approximately 30 minutes post-dose. After a single subcutaneous administration of 0.1 unit/kg of human insulin to healthy subjects, peak insulin concentrations occurred between 1.5 to 2.5 hours post-dose.
When administered in an inhal... | The metabolism and elimination of orally inhaled human insulin are comparable to regular human insulin. | null | Systemic insulin disposition (apparent terminal half-life) following oral inhalation of 4 to 48 units of human insulin was 120-206 minutes. | null | Following oral inhalation of human insulin, a mean of 39% of the inhaled dose of carrier particles was distributed to the lungs and a mean of 7% of the dose was swallowed. The swallowed fraction was not absorbed from the GI tract and was eliminated unchanged in the feces. | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"A10AC",
"A10A",
"A10",
"A",
"A10AE",
"A10A",
"A10",
"A",
"A10AB",
"A10A",
"A10",
"A",
"A10AD",
"A10A",
"A10",
"A",
"A10AF",
"A10A",
"A10",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "2.14",
"description": "Novolin Ge Nph 100 unit/ml",
"unit": "cartridge"
},
{
"cost": "2.14",
"description": "Novolin Ge Toronto 100 unit/ml",
"unit": "cartridge"
},
{
"cost": "2.29",
"description": "Humulin N 100 unit/ml",
"unit": "cartridge"
},
{
"cost... | [
{
"approved": "2002-10-08",
"country": "United States",
"expires": "2010-02-12",
"number": "RE37872"
},
{
"approved": "2007-10-30",
"country": "Canada",
"expires": "2015-02-07",
"number": "2183577"
},
{
"approved": "2007-10-09",
"country": "Canada",
"expires": "20... | High molecular weight insulin human | Human insulin | human insulin (rDNA) | Insulin (human) | Insulin human | Insulin human [rDNA origin] | Insulin Human Regular | Insulin human regular (rDNA) | Insulin human, rDNA origin | Insulin recombinant human | Insulin recombinant purified human | Insulin regular | Insulin, hum... | [
"Actraphane 30",
"Actraphane 30",
"Actraphane 30",
"Actraphane 30",
"Actraphane 30",
"Actraphane 30",
"Actraphane 30 Flexpen",
"Actraphane 30 Flexpen",
"Actraphane 30 Flexpen",
"Actraphane 30 Innolet",
"Actraphane 30 Innolet",
"Actraphane 30 Innolet",
"Actraphane 30 Penfill",
"Actraphane 3... | [] | [
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Afrezza",
"Exubera",
"Exubera",
"Novolin Ge 40/60 Penfill",
"Novolin Ge 40/60 Penfill"... | [
"P06213",
"P08069",
"P16870",
"P48745",
"P98164",
"Q16270"
] | [
"P14735",
"P16519",
"P29120",
"P05177"
] | [] | [] |
DB00031 | Tenecteplase | Tenecteplase is a tissue plasminogen activator (tPA) developed from modifications of natural human tPA complementary DNA (cDNA). It is a 527 amino acid with a substitution of threonine 103 with asparagine and substitution of asparagine 117 with glutamine within the kringle 1 domain, and a tetra-alanine substitution at ... | liquid | For treatment of myocardial infarction and lysis of intracoronary emboli | Tenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cau... | Tenecteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. | null | null | null | 1.9 hours (mammalian reticulocytes, in vitro)
>20 hours (yeast, in vivo)
>10 hours (Escherichia coli, in vivo) | null | null | null | * 99 - 119 mL/min [acute myocardial infarction patients] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B01AD",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "3238.76",
"description": "Tnkase 50 mg kit",
"unit": "kit"
}
] | [
{
"approved": "2005-06-28",
"country": "Canada",
"expires": "2013-05-28",
"number": "2129660"
},
{
"approved": "2003-06-17",
"country": "Canada",
"expires": "2020-06-17",
"number": "1341432"
}
] | Tenecteplasa | Tenecteplase | TNK-tPA | 3.4.21.7 | [
"Metalyse",
"Metalyse",
"Metalyse",
"TNKase",
"TNKase",
"TNKase",
"TNKase"
] | [] | [
"TNKase"
] | [
"P00747"
] | [] | [] | [] |
DB00032 | Menotropins | Menotropins contains follicle stimulating hormone (FSH) and luteinizing hormone (LH) purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunits, alpha = 92 residues, beta = 121 residues and FSH wi... | liquid | For the treatment of female infertility | Used to treat female infertility, Menotropins stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endoge... | Being a combination drug, Menotropins bind to the follicle stimulating hormone receptor (FSH), which results in ovulation in the absence of sufficient endogenous luteinizing hormone (LH). It also binds the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH, therefore, it induces ... | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"G03GA",
"G03G",
"G03",
"G",
"G03GA",
"G03G",
"G03",
"G"
] | [
"Humans and other mammals"
] | [
{
"cost": "93.85",
"description": "Menopur 75 unit vial",
"unit": "vial"
},
{
"cost": "93.85",
"description": "Repronex 75 unit vial",
"unit": "vial"
},
{
"cost": "488.04",
"description": "Repronex 5 75 unit Solution 1 Box Contains Five 1ml Vials",
"unit": "box"
}
] | [] | Human menopausal gonadotrophin | Menotrophin | Menotropin | Menotropina | Menotropins (FSH;LH) | Follitropin receptor | FSH-R | LGR1 | LCGR | LGR2 | LH/CG-R | LHR | LHRHR | LSH-R | Luteinizing hormone receptor | [
"Menopur",
"Repronex"
] | [] | [] | [
"P23945",
"P22888"
] | [] | [] | [] |
DB00033 | Interferon gamma-1b | Human Interferon gamma-1b (140 residues), produced from E. coli. Production of Actimmune is achieved by fermentation of a genetically engineered Escherichia coli bacterium containing the DNA which encodes for the human protein. Purification of the product is achieved by conventional column chromatography.
The sequenc... | liquid | Interferon gamma-1b is used for the treatment of Chronic granulomatous disease and Osteopetrosis. | IFN gamma stimulates expression of the immunoglobulin heavy chain C gamma 3 and C gamma 2a germline transcripts in B cells. Many components of the antigen presentation pathways are also up-regulated by interferon gamma. It is also a potent activator of macrophages, it has antiproliferative effects on transformed cells ... | Binds directly to the type II interferon gamma receptor IFNGR1, leading to a complex of IFNGR1 and IFNGR2. This activates JAK1 and JAK2 kinases which form a STAT1 docking site. This leads to STAT1 phosphorylation, nuclear translocation and initiation of gene transcription of multiple immune-related genes. | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [] | [] | [
{
"cost": "344.4",
"description": "Actimmune 2 million unit vial",
"unit": "vial"
}
] | [
{
"approved": "2005-08-30",
"country": "United States",
"expires": "2022-08-30",
"number": "6936695"
},
{
"approved": "2005-08-30",
"country": "United States",
"expires": "2022-08-30",
"number": "6936694"
}
] | IFN-gamma 1b | IFN-gamma-1b | Interferon gamma 1-b | Interferon gamma-1b | Interferon gamma-1b, recombinant | Interferon gamma-2a | CDw119 | IFN-gamma receptor 1 | IFN-gamma-R-alpha | IFN-gamma-R1 | Interferon gamma receptor alpha-chain | AF-1 | IFN-gamma receptor 2 | IFN-gamma-R-beta | IFN-gamma-R2 | IFNGT1 | Interfer... | [
"Actimmune",
"Actimmune",
"Actimmune"
] | [
"Immukin"
] | [] | [
"P15260",
"P38484"
] | [
"P05177"
] | [] | [] |
DB00034 | Interferon alfa-2a | Interferon a (human leukocyte protein moiety reduced). A type I interferon consisting of 165 amino acid residues with lysine in position 23. This protein is produced by recombinant DNA technology and resembles interferon secreted by leukocytes. It is used extensively as an antiviral or antineoplastic agent. An oral for... | liquid | For the treatment of chronic hepatitis C, hairy cell leukemia, AIDS-related Kaposi's sarcoma, and chronic myelogenous leukemia. Also for the treatment of oral warts arising from HIV infection. | Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also indu... | Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers ... | Absorption is high (greater than 80%) when administered intramuscularly or subcutaneously. | null | Interferon alfa-2 may cause serious adverse effects such as anemia; autoimmune diseases, including vasculitis, arthritis, hemolytic anemia, and erythematosus syndrome; cardiotoxicity; hepatotoxicity; hyperthyroidism or hypothyroidism; transient ischemic attacks; leukopenia; neurotoxicity; peripheral neuropathy; and thr... | The IM half-life of interferon alfa-2a is 6 hours to 8 hours; the half-life for IV infusion is 3.7 hours to 8.5 hours (mean 5.1 hours). | null | Alpha-interferons are totally filtered through the glomeruli and undergo rapid proteolytic degradation during tubular reabsorption, rendering a negligible reappearance of intact alfa interferon in the systemic circulation. | * 0.223 to 0.748 L/kg [healthy people] | * 2.14 - 3.62 mL/min/kg [healthy] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [] | [
{
"approved": "2000-10-03",
"country": "Canada",
"expires": "2016-03-26",
"number": "2172664"
}
] | Interferon alfa-2a | Interferon alfa-2a (genetical recombination) | Interferon alfa-2a (recombinant) | Interferon alfa-2a, recombinant | Interferon alfa-2a,recombinant | Interferon alpha-2a | Interferon-alfa-2a | Recombinant human interferon alfa-2a | Recombinant human interferon-alfa-2a | rIFN-alpha-2a | SH-polypeptid... | [
"Roferon A Soln Inj 6 Million",
"Roferon A Sterile Pws 18m Unit/vial",
"Roferon A Sterile Pws 3m Unit/vial",
"Roferon A Sterile Pws 9m Unit/vial",
"Roferon-A",
"Roferon-A",
"Roferon-A",
"Roferon-A Sol Inj 3million Iu/vial",
"Roferon-A Soln-liq Im Sc 4.5million I.u/ml",
"Roferon-A Soln-liq Im Sc 9m... | [
"Roferon A",
"Veldona"
] | [] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00035 | Desmopressin | Desmopressin (dDAVP), a synthetic analogue of 8-arginine vasopressin (ADH), is an antidiuretic peptide drug modified by deamination of 1-cysteine and substitution of 8-L-arginine by 8-D-arginine. ADH is an endogenous pituitary hormone that has a crucial role in the control of the water content in the body. Upon release... | solid | - Indicated for the treatment of nocturia due to nocturnal polyuria in adults who awaken at least 2 times per night to void (intranasal).
- Indicated as antidiuretic replacement therapy in the management of central cranial diabetes insipidus and for management of the temporary polyuria and polydipsia following head... | By mimicking the actions of endogenous ADH, desmopressin acts as a selective agonist of V2 receptors expressed in the renal collecting duct (CD) to increase water re-absorption and reduce urine production. Desmopressin has been shown to be more potent than ADH in increasing plasma levels of factor VIII activity in pati... | Upon binding of desmopressin to V2 receptors in the basolateral membrane of the cells of the distal tubule and collecting ducts of the nephron, adenylyl cyclase is stimulated. The resulting intracellular cascades in the collecting duct lead to increased rate of insertion of water channels, called aquaporins, into the l... | Following nasal spray administration of 0.83 mcg and 1.66 mcg, median time to peak plasma concentrations (Tmax) was 0.25 and 0.75 hour, respectively [FDA Label]. The peak plasma concentration was approximately 4.00 (± 3.85) pg/mL and 9.11 (± 6.90) pg/mL, respectively [FDA Label]. The bioavailability of 1.5 mg/mL desmop... | In vitro, in human liver microsome preparations, it has been shown that no significant amount of desmopressin is metabolised in the liver and thus human liver metabolism in vivo is not likely to occur [L1184]. | Intravenous TDLo in humans is reported to be 0.3 µg/kg/10M [MSDS]. Desmopressin is associated with hyponatremia in case of overdose, which may require temporary or permanent discontinuation of the therapy depending on severity. The effects of hyponatremia include seizure, altered mental status (confusion, drowsiness or... | Following an intranasal dose of 1.66 mcg of desmopressin, the median apparent terminal half-life was 2.8 hours [FDA Label]. Terminal half-life significantly increased from 3 hours in normal healthy patients to 9 hours in patients with severe renal impairment [FDA Label]. The oral terminal half life of desmopressin rang... | Following radioiodination (125I) in the N-terminal, the fraction of plasma protein binding of desmopressin was reported to be 17.3 ± 1.5% in a pharmacokinetic study involving healthy subjects [A31736]. | Desmopressin is mainly excreted in the urine. About 65% of the amount of desmopressin absorbed after oral administration
could be recovered in the urine within 24 hours [L1184]. | The distribution volume of orally administered desmopressin is 0.2 – 0.32 l/kg [L1184]. It is not reported to cross the blood-brain barrier. | null | null | null | null | null | [
"approved"
] | [
"H01BA",
"H01B",
"H01",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "1.48",
"description": "Apo-Desmopressin 10 mcg/dose Metered Dose Spray",
"unit": "dose"
},
{
"cost": "1.49",
"description": "Ddavp 0.1 mg Tablet",
"unit": "tablet"
},
{
"cost": "1.67",
"description": "Apo-Desmopressin 0.2 mg Tablet",
"unit": "tablet"
},
{
... | [
{
"approved": "2006-04-04",
"country": "United States",
"expires": "2023-04-30",
"number": "7022340"
},
{
"approved": "1996-03-19",
"country": "United States",
"expires": "2013-06-29",
"number": "5500413"
},
{
"approved": "2007-01-16",
"country": "Canada",
"expire... | 1-(3-mercaptopropionic acid)-8-D-arginine-vasopressin | 1-deamino-8-D-arginine vasopressin | 1-desamino-8-D-arginine vasopressin | dDAVP | Desmopresina | Desmopressin | Desmopressine | Desmopressinum | OT-R | ADHR | Antidiuretic hormone receptor | AVPR V2 | DIR | DIR3 | Renal-type arginine vasopressin receptor | V2R | ... | [
"Apo-desmopressin",
"Apo-desmopressin",
"Bipazen",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp",
"Ddavp Inj 4mcg/ml",
"Ddavp Melt",
"Ddavp Melt",
"Ddavp Melt",
"DDAVP Rhinal Tube",
"Ddavp Rhinyle",
"Ddavp Spray",
"Ddavp T... | [
"Adiuretin",
"DesmoMelt"
] | [] | [
"P30559",
"P30518",
"P37288",
"P47901"
] | [
"P35354",
"P23219"
] | [] | [] |
DB00036 | Coagulation factor VIIa Recombinant Human | Recombinant human coagulation Factor VIIa (rFVIIa), intended for promoting hemostasis by activating the extrinsic pathway of the coagulation cascade. NovoSeven is a vitamin K-dependent glycoprotein consisting of 406 amino acid residues. Cloned and expressed in hamster kidney cells, the protein is catalytically active i... | liquid | For treatment of hemorrhagic complications in hemophilia A and B. | Used in the treatment of bleeding episodes in hemophilia A or B. NovoSeven is recombinant Factor VIIa and, when complexed with tissue factor can activate coagulation Factor X to Factor Xa, as well as coagulation Factor IX to Factor IXa. Factor Xa, in complex with other factors, then converts prothrombin to thrombin, wh... | NovoSeven activates the coagulation or clotting cascade by cleaving Factor IX and Factor X, which activates them and then leads to activation of thrombin and fibrin. | null | null | null | null | null | null | * 121 ± 30 mL/kg [adults]
* 153 ± 29 mL/kg [children]
* 280 to 290 mL/kg [congenital Factor VII deficiency] | * 33 - 37 mL/h x kg [healthy]
* 1375 +/- 396 mL/hr [severe hemophilia A male children]
* 57.3 +/- 9.5 mL/hr/kg [severe hemophilia A male children]
* 2767 +/- 385 mL/hr [severe hemophilia A men]
* 37.6 +/- 13.1 mL/hr/kg [severe hemophilia A men] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B02BD",
"B02B",
"B02",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "1.64",
"description": "Novoseven 1200 mcg vial",
"unit": "vial"
},
{
"cost": "1.64",
"description": "Novoseven 2400 mcg vial",
"unit": "vial"
},
{
"cost": "1.64",
"description": "Novoseven 4800 mcg vial",
"unit": "vial"
}
] | [] | Coagulation factor VIIa | Coagulation factor VIIa (recombinant) | Coagulation factor VIIa (recombinant)-jncw | Eptacog alfa | Eptacog alfa (activated) | rFVIIa | 3.4.21.6 | Stuart factor | Stuart-Prower factor | Coagulation factor III | TF | Thromboplastin | [
"Cevenfacta",
"Cevenfacta",
"Cevenfacta",
"Niastase",
"Niastase",
"Niastase",
"Niastase RT",
"Niastase RT",
"Niastase RT",
"Niastase RT",
"Niastase RT",
"Niastase RT",
"Niastase RT",
"Niastase RT",
"Novoseven",
"Novoseven",
"Novoseven",
"Novoseven",
"Novoseven",
"Novoseven",
... | [] | [] | [
"P00742",
"P13726"
] | [] | [] | [] |
DB00038 | Oprelvekin | Oprelvekin, the active ingredient in Neumega®, is recombinant Interleukin-11 (IL-11), which is produced in Escherichia coli (E. coli) by recombinant DNA technology. With a molecular mass of approximately 19,000 daltons, the non-glycosylated protein is 177 amino acids in length in comparison to the natural IL-11, which ... | liquid | Indicated for the prevention of severe thrombocytopenia and the reduction of the need for platelet transfusions following myelosuppressive chemotherapy in adult patients with nonmyeloid malignancies who are at high risk of severe thrombocytopenia.[Label] | Oprelvekin promotes hematopoiesis by stimulating megakaryocytopoiesis and thrombopoiesis. It is used in adult patients with nonmyeloid malignancies to prevent severe thrombocytopenia and reduce the need for platelet transfusions following therapies that cause myelosuppression. Its use is prioritized in patients who are... | Oprelvekin binds to the interleukin 11 receptor which leads to a cascade of signal transduction events. Its pharmacological action mimics the biological activity of endogenous IL-11, which is a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenit... | Absolute bioavailability is over 80%. | null | null | 6.9 +/- 1.7 hrs | null | The kidney is the primary route of elimination. The amount of intact Neumega in urine was low, indicating that the molecule was metabolized before excretion. | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AC",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "352.9",
"description": "Neumega 5 mg vial",
"unit": "vial"
}
] | [] | IL-11 | Interleukin 11 | Interleukin-11 | Oprelvekin | Recombinant interleukin-11 | IL-11 receptor subunit alpha | IL-11R subunit alpha | IL-11R-alpha | IL-11RA | [
"Neumega"
] | [] | [] | [
"Q14626"
] | [] | [] | [] |
DB00039 | Palifermin | Palifermin is a recombinant human keratinocyte growth factor (KGF). It is 140 residues long, and is produced using E. coli.
Palifermin was granted FDA approval on 15 December 2004.[L17933] | liquid | For treatment of oral mucositis associated with chemotherapy and radiation therapy. | Used in the prevention or treatment of oral mucoscitis (mouth ulcers arising from chemotherapy), Kepivance binds to the human keratinocyte growth factor (KGF) receptor on buccal cell surfaces. Kepivance acts as both a cell growth and survival factor by stimulating epithelial cell proliferation, differentiation, and mig... | Palifermin has been shown to protect oral and intestinal epithelia from the effects of radiation and chemotherapy, though the exact mechanism is not well understood.[A222248] As a recombinant keratinocyte growth factor (KGF), palifermin may promote cell proliferation, reducing the severity of oral mucositis in patients... | null | null | null | Elimination half-life: 4.5 hours (range: 3.3-5.7 hours) | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"V03AF",
"V03A",
"V03",
"V"
] | [
"Humans and other mammals"
] | [
{
"cost": "1650.0",
"description": "Kepivance 6.25 mg vial",
"unit": "vial"
}
] | [] | 24-163 fibroblast growth factor 7 (human) | Palifermin | Palifermina | 2.7.10.1 | BEK | FGFR-2 | K-sam | Keratinocyte growth factor receptor | KGFR | KSAM | 2.7.10.1 | Basic fibroblast growth factor receptor 1 | bFGF-R-1 | BFGFR | CEK | FGFBR | FGFR-1 | FLG | FLT-2 | FLT2 | Fms-like tyrosine kinase 2 | HBGFR | N-sam | ... | [
"Kepivance",
"Kepivance",
"Kepivance",
"Kepivance"
] | [] | [] | [
"P21802",
"P11362",
"P98160"
] | [] | [] | [] |
DB00040 | Glucagon | Glucagon is a 29 amino acid hormone used as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and to treat severe hypoglycemia.[L7634,L7637,L7640,L7643,L8519] Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and... | liquid | Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and to treat severe hypoglycemia.[L7634,L7637,L7640,L7643,L8519] | Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and severe hypoglycemia.[A19402,L7634,L7637,L7640,L7643,L8519] Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and the release of gluco... | Glucagon binds to the glucagon receptor activating G<sub>s</sub>α and G<sub>q</sub>.[A19402] This activation activates adenylate cyclase, which increases intracellular cyclic AMP and activates protein kinase A.[A19402] Activating G<sub>q</sub> activates phospholipase C, increases production of inositol 1,4,5-triphospha... | A 1mg intravenous dose of glucagon reaches a C<sub>max</sub> of 7.9ng/mL with a T<sub>max</sub> of 20 minutes.[L7637] An intramuscular dose reaches a C<sub>max</sub> of 6.9ng/mL with a T<sub>max</sub> of 13 minutes.[L7637] A 3mg dose of glucagon nasal powder reaches a C<sub>max</sub> of 6130pg/mL with a T<sub>max</sub>... | Glucagon is a protein and so it is metabolized into smaller polypeptides and amino acids in the liver, kidney, and plasma.[L7634,L7643] | Patients experiencing an overdose may present with nausea, vomiting, inhibition of GI tract motility, increased blood pressure and heart rate, and decreased serum potassium.[L7634,L7637,L7640,L7643] Phentolamine may be given to control blood pressure.[L7634,L7637,L7640,L7643] Treatment of glucagon overdose is largely s... | The half life of glucagon is 26 minutes for an intramuscular dose.[L7634] The half life of glucagon nasal powder is approximately 35 minutes.[L7643] The half life of glucagon by a subcutaneous auto-injector or pre-filled syringe is 32 minutes.[L8519] | Glucagon has not been described in the literature as bound to a protein in serum.[A181649,A181667,L7634,L7637,L7640,L7643,L7658] | Elimination of glucagon is not fully characterized in literature, however the kidney and liver appear to contribute significantly in animal models.[A181649] The liver and kidney are responsible for approximately 30% of glucagon elimination each.[L7658] | The volume of distribution of glucagon is 0.25L/kg.[L7637] The apparent volume of distribution is 885L.[L7643] | A 1mg intravenous dose of glucagon has a clearance of 13.5mL/min/kg.[L7637] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"H04AA",
"H04A",
"H04",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "84.0",
"description": "Glucagen 1 mg vial",
"unit": "vial"
},
{
"cost": "94.98",
"description": "Glucagon 1 mg/vial",
"unit": "vial"
},
{
"cost": "119.28",
"description": "Glucagon 1 mg emergency kit",
"unit": "kit"
},
{
"cost": "120.36",
"descripti... | [
{
"approved": "2019-02-26",
"country": "United States",
"expires": "2036-02-16",
"number": "10213487"
},
{
"approved": "2005-09-06",
"country": "United States",
"expires": "2022-01-03",
"number": "6938798"
},
{
"approved": "2017-05-16",
"country": "United States",
... | Glucagon | Glucagon (recombinant dna origin) | Glucagon recombinant | Glucagon, human | Glucagon, porcine | Glucagone | Glucagonum | GL-R | GLP-2 receptor | GLP-2-R | GLP-2R | GLP-1 receptor | GLP-1-R | GLP-1R | [
"Baqsimi",
"Baqsimi",
"Baqsimi",
"Baqsimi",
"Baqsimi",
"Baqsimi",
"Glucag0n",
"GlucaGen",
"GlucaGen",
"GlucaGen",
"GlucaGen",
"GlucaGen HypoKit",
"GlucaGen HypoKit",
"Glucagon",
"Glucagon",
"Glucagon",
"Glucagon",
"Glucagon",
"Glucagon",
"Glucagon",
"Glucagon",
"Glucagon",
... | [] | [
"Glucagon",
"Glucagon",
"Glucagon",
"Glucagon"
] | [
"P47871",
"O95838",
"P43220"
] | [] | [] | [] |
DB00041 | Aldesleukin | Aldesleukin, a lymphokine, is produced by recombinant DNA technology using a genetically engineered E. coli strain containing an analog of the human interleukin-2 gene. Genetic engineering techniques were used to modify the human IL-2 gene, and the resulting expression clone encodes a modified human interleukin-2. This... | liquid | For treatment of adults with metastatic renal cell carcinoma. | Used to treat renal cell carcinoma, Aldesleukin induces the enhancement of lymphocyte mitogenesis and stimulation of long-term growth of human interleukin-2 dependent cell lines, the enhancement of lymphocyte cytotoxicity, the induction of killer cell (lymphokine-activated (LAK) and natural (NK)) activity; and the indu... | Aldesleukin binds to the IL-2 receptor which leads to heterodimerization of the cytoplasmic domains of the IL-2R beta and gamma(c) chains, activation of the tyrosine kinase Jak3, and phosphorylation of tyrosine residues on the IL-2R beta chain. These events led to the creation of an activated receptor complex, to which... | null | null | null | 13 min-85 min | null | The pharmacokinetic profile of Proleukin is characterized by high plasma concentrations following a short IV infusion, rapid distribution into the extravascular space and elimination from the body by metabolism in the kidneys with little or no bioactive protein excreted in the urine. Following the initial rapid organ d... | 0.18 l/kg | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AC",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "976.66",
"description": "Proleukin 22000000 unit Solution Vial",
"unit": "vial"
},
{
"cost": "1092.34",
"description": "Proleukin 22 million unit vial",
"unit": "each"
}
] | [] | 125-L-serine-2-133-interleukin 2 (human reduced) | Aldesleukin | Aldesleukina | ILT-101 | ILT101 | Interleukin-2 aldesleukin | Interleukin-2(2-133),125-ser | Recombinant human interleukin-2 | Recombinant interleukin-2 human | High affinity IL-2 receptor subunit beta | IL-2 receptor subunit beta | IL-2R subunit beta | I... | [
"Proleukin",
"Proleukin",
"Proleukin",
"Proleukin",
"Proleukin",
"Proleukin"
] | [] | [] | [
"P14784",
"P01589",
"P31785"
] | [
"P35354",
"P47712",
"P08684",
"P47989",
"P05181"
] | [] | [] |
DB00042 | Botulinum toxin type B | Neurotoxin produced by fermentation of clostridium botulinum type B. The protein exists in noncovalent association with hemagglutinin and nonhemagglutinin proteins as a neurotoxin complex. The neurotoxin complex is recovered from the fermentation process and purified through a series of precipitation and chromatography... | liquid | For the treatment of patients with cervical dystonia to reduce the severity of abnormal head position and neck pain associated with cervical dystonia. | Botulinum Toxin Type B inhibits acetylcholine release at the neuromuscular junction via a three stage process: 1) Heavy Chain mediated neurospecific binding of the toxin, 2) internalization of the toxin by receptor-mediated endocytosis, and 3) ATP and pH dependent translocation of the Light Chain to the neuronal cytoso... | Botulinum Toxin Type B binds to and cleaves the synaptic Vesicle Associated Membrane Protein (VAMP, also known as synaptobrevin) which is a component of the protein complex responsible for docking and fusion of the synaptic vesicle to the presynaptic membrane, a necessary step to neurotransmitter release. | Though pharmacokinetic or ADME studies were not performed, Botulinum Toxin Type B is not expected to be present in the peripheral blood at measurable levels following IM injection at the recommended doses. | null | One unit of Botulinum Toxin Type B corresponds to the calculated median lethal intraperitoneal dose (LD50) in mice. | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"M03AX",
"M03A",
"M03",
"M"
] | [
"Humans and other mammals"
] | [
{
"cost": "299.4",
"description": "Myobloc 2500 unit/0.5 ml vial",
"unit": "vial"
},
{
"cost": "1245.5",
"description": "Myobloc 10000 unit/2ml Solution 2ml Vial",
"unit": "vial"
}
] | [] | Botulin B | Botulinum antitoxin type B | Botulinum B toxin | Botulinum neurotoxin type B precursor | Botulinum toxin type B | BTX-B | RimabotulinumtoxinB | Toxina botulínica B | SYB2 | Synaptobrevin-2 | VAMP-2 | SYB1 | Synaptobrevin-1 | VAMP-1 | Synaptotagmin II | SytII | [
"Myobloc",
"Myobloc",
"Myobloc",
"Myobloc",
"Neurobloc",
"Neurobloc",
"Neurobloc",
"Neurobloc"
] | [
"Neurobloc"
] | [] | [
"P63027",
"P23763",
"Q8N9I0"
] | [] | [] | [] |
DB00043 | Omalizumab | Omalizumab is a recombinant DNA-derived humanized monoclonal antibody directed against human immunoglobulin E (IgE).[L50482] IgE promotes the release of inflammatory mediators from mast cells and basophils during allergic and inflammatory reactions. By binding to IgE and neutralizing it, omalizumab reduces free IgE lev... | liquid | Omalizumab is indicated for:
- the treatment of patients six years of age and older with moderate to severe persistent asthma who have a positive skin test or in vitro reactivity to a perennial aeroallergen and whose symptoms are inadequately controlled with inhaled corticosteroids.[L50477, L50482]
- add-on maintenan... | Omalizumab decreases free IgE levels in serum in a dose-dependent manner. Serum total IgE levels, accounting for bound and unbound IgE, increased after the first dose of omalizumab due to the formation of drug:IgE complexes, which have a slower elimination rate compared with free IgE. At 16 weeks after the first dose, ... | IgE antibodies have been implicated in several immune-mediated diseases, including allergic hypersensitivity reactions and asthma. IgE binds to the high-affinity IgE receptor Fc-epsilon-RI typically found on inflammatory cells such as eosinophils, mast cells, and basophils.[A39518, A263507] IgE binding to Fc-epsilon-RI... | After subcutaneous administration, omalizumab has an average absolute bioavailability of 62%. In adult and adolescent patients with asthma, omalizumab was absorbed slowly and the peak serum concentrations occurred after seven to eight days.[L50477]
The pharmacokinetics of omalizumab were linear at doses which were h... | Omalizumab is degraded in the reticuloendothelial system and endothelial cells.[A263507] | The intravenous LD<sub>50</sub> in monkeys is 200 mg/kg.[L50487]
Maximum tolerated dose of omalizumab has not been determined. Single intravenous doses up to 4000 mg have been administered to patients without evidence of dose-limiting toxicities. The highest cumulative dose administered to patients was 44,000 mg ove... | In asthma patients, the serum elimination half-life averaged 26 days. In CSU patients, at steady state, based on population pharmacokinetics, omalizumab serum elimination half-life averaged 24 days.[L50477] | null | Liver elimination of IgG includes degradation in the liver reticuloendothelial system (RES) and endothelial cells. Intact IgG was also shown to be excreted in bile. In studies with mice and monkeys, omalizumab:IgE complexes were eliminated by interactions with Fc-gamma receptors within the RES at rates that were gener... | In patients with asthma, the apparent volume of distribution was 78 ± 32 mL/kg following subcutaneous administration.[L50477] | In pharmacokinetic studies, the clearance of omalizumab involved IgG clearance as well as clearance by specific binding and complex formation with its target ligand, IgE. The apparent clearance averaged 2.4 ± 1.1 mL/kg/day in patients with asthma. The apparent clearance averaged 240 mL/day (corresponding to 3.0 mL/kg/d... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"R03DX",
"R03D",
"R03",
"R"
] | [
"Humans and other mammals"
] | [
{
"cost": "715.42",
"description": "Xolair 150 mg vial",
"unit": "vial"
}
] | [
{
"approved": "2005-04-12",
"country": "Canada",
"expires": "2012-08-14",
"number": "2113813"
},
{
"approved": "1998-12-15",
"country": "Canada",
"expires": "2015-12-15",
"number": "1340233"
}
] | Omalizumab | RHUMAB-E25 | Ig epsilon chain C region | Ig epsilon chain C region ND | [
"Omlyclo",
"Omlyclo",
"Omlyclo",
"Omlyclo",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
"Xolair",
... | [] | [] | [
"P01854"
] | [] | [] | [] |
DB00044 | Lutropin alfa | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein made up of monomeric units. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulatio... | liquid | For treatment of infertility in women with hypothalamic or pituitary insufficiency (hypogonadotropic hypogonadism) and profound LH deficiency (LH <1.2 international units [IU]/L) | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone (LH), which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. Together they stimulate the development of a follicle to prepare the reproductive tract for implem... | Luteinizing hormone binds to a receptor shared with the human chorionic gonadotropin hormone (hCG) on the ovarian theca (and granulosa) cells and testicular Leydig cells. This LH/CG transmembrane receptor is a member of the super-family of G protein-coupled receptors. Adenylate cyclase then activates many other pathway... | Mean absolute bioavailability is 56%, following sub-Q administration, maximum serum concentrations reached after 4–16 hours. Time to peak, serum: 9 hours | <5% of dose excreted renally as unchanged drug. | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primar... | Biphasic; terminal half-life is approximately 18 hours. | null | Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. | The steady state volume of distribution is around 10-14 L. | * 2 – 3 L/h [healthy female following subcutaneous administration] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"G03GA",
"G03G",
"G03",
"G"
] | [
"Humans and other mammals"
] | [
{
"cost": "38.88",
"description": "Luveris 75 unit vial",
"unit": "vial"
}
] | [
{
"approved": "1998-06-16",
"country": "United States",
"expires": "2015-06-16",
"number": "5767251"
}
] | Lutropin alfa | Lutropin alpha | Lutropina alfa | LCGR | LGR2 | LH/CG-R | LHR | LHRHR | LSH-R | Luteinizing hormone receptor | [
"Luveris",
"Luveris",
"Luveris",
"Luveris",
"Luveris",
"Luveris",
"Luveris",
"Luveris",
"Luveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris"
] | [] | [
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris"
] | [
"P22888"
] | [] | [] | [] |
DB00045 | Lyme disease vaccine (recombinant OspA) | Vaccine against Lyme disease that contains lipoprotein OspA, an outer surface protein of Borrelia burgdorferi sensu stricto ZS7, as expressed by Escherichia coli. Lipoprotein OspA is a single polypeptide chain of 257 amino acids with lipids covalently bonded to the N terminus. It is conjugated with alum (aluminum hydro... | liquid | For prophylactic treatment of Lyme Disease | OspA lipoprotein is a single polypeptide chain of 270 amino acids. It is a vaccination used to prevent Lyme Disease. | OspA lipoprotein, an outer surface protein of the bacteria Borrelia burgdorferi sensu stricto ZS7, is used to stimulate the production of specific antibodies against B. burgdorferi. It is used as a vaccination against Lyme Disease, a disease carried by ticks. | null | null | null | 1.2 hours (mammalian reticulocytes, in vitro). | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"withdrawn"
] | [] | [
"Humans and other mammals"
] | [] | [] | Lipoprotein OspA antigen recombinant | Lipoprotein outer surface a borrelia burgdorferi antigen | OspA lipoprotein | TIL4 | Toll/interleukin-1 receptor-like protein 4 | [] | [
"LYMErix"
] | [] | [
"O60603"
] | [] | [] | [] |
DB00046 | Insulin lispro | Insulin lispro is a rapid-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promote... | liquid | Insulin lispro is indicated to improve glycemic control in adult and pediatric patients with diabetes mellitus.[L47616] | Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes following meals. Increased insulin secretion following meals is responsible for the metabolic changes that occur as the body transitions from a postabsorptive to... | Insulin lispro binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor autophos... | Studies in healthy volunteers and patients with diabetes demonstrated that insulin lispro is absorbed more quickly than regular human insulin, specifically at the abdominal, deltoid, or femoral subcutaneous sites. In healthy volunteers given subcutaneous doses of insulin lispro ranging from 0.1 to 0.4 unit/kg, peak ser... | Human metabolism studies have not been conducted. However, animal studies indicate that the metabolism of insulin lispro is identical to that of regular human insulin.[L47616] | Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs ... | After subcutaneous administration of insulin lispro, the t<sub>1/2</sub> is shorter than that of regular human insulin (1 versus 1.5 hours, respectively).[L47616] For intravenous administration, insulin lispro demonstrated a mean t<sub>1/2</sub> of 0.85 hours (51 minutes) and 0.92 hours (55 minutes), respectively for 0... | null | null | When administered intravenously as bolus injections of 0.1 and 0.2 U/kg dose in two separate groups of healthy subjects, the mean volume of distribution of HUMALOG appeared to decrease with increase in dose (1.55 and 0.72 L/kg, respectively) in contrast to that of regular human insulin for which, the volume of distribu... | When administered intravenously, insulin lispro and regular human insulin demonstrated similar dose-dependent clearance, with a mean clearance of 21.0 mL/min/kg and 21.4 mL/min/kg, respectively (0.1 unit/kg dose), and 9.6 mL/min/kg and 9.4 mL/min/kg, respectively (0.2 unit/kg dose).[L47616] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"A10AC",
"A10A",
"A10",
"A",
"A10AB",
"A10A",
"A10",
"A",
"A10AD",
"A10A",
"A10",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "2.95",
"description": "Humalog 100 unit/ml",
"unit": "cartridge"
},
{
"cost": "9.37",
"description": "Humalog 100 unit/ml Cartridge",
"unit": "cartridge"
},
{
"cost": "11.83",
"description": "Humalog mix 50/50 kwikpen",
"unit": "ml"
},
{
"cost": "15.4",... | [
{
"approved": "1995-12-12",
"country": "United States",
"expires": "2014-06-16",
"number": "5474978"
},
{
"approved": "1996-05-07",
"country": "United States",
"expires": "2013-05-07",
"number": "5514646"
},
{
"approved": "2003-02-11",
"country": "Canada",
"expire... | Insulin lispro | Insulin lispro (genetical recombination) | Insulin lispro (rDNA origin) | Insulin lispro protamine | Insulin lispro protamine recombinant | Insulin lispro recombinant | insulin lispro-aabc | Insulin,lispro,human/rDNA | Insulin,lispro,protamine/rDNA | Insulina lispro | 2.7.10.1 | IR | 2.7.10.1 | IGF-I r... | [
"Admelog",
"Admelog",
"Admelog",
"Admelog",
"Admelog",
"Admelog",
"Admelog Solostar",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog",
"Humalog... | [] | [
"Humalog Mix 25 (cartridge)",
"Humalog Mix 25 (cartridge)",
"Humalog Mix 50 (cartridge)",
"Humalog Mix 50 (cartridge)",
"Humalog Mix 25 (kwikpen)",
"Humalog Mix 25 (kwikpen)",
"Humalog Mix 25 (pen)",
"Humalog Mix 25 (pen)",
"Humalog Mix 50 (kwikpen)",
"Humalog Mix 50 (kwikpen)"
] | [
"P06213",
"P08069"
] | [
"P05177",
"P14735"
] | [] | [] |
DB00047 | Insulin glargine | Insulin glargine is a long-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is typically prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas t... | liquid | Insulin glargine is indicated to improve glycemic control in adults and pediatric patients with type 1 diabetes mellitus and in adults with type 2 diabetes mellitus.[L12474,L43532,L43587] | Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, the pancreas produces a continuous supply of low levels of basal insulin along with spikes of insulin following meals. Increased insulin secretion following meals is responsible for the metabolic changes that occur as the ... | Insulin glargine binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor autoph... | Because of the modifications to the A and B chain, the isoelectric point shifts towards a neutral pH and insulin glargine is more stable in acidic conditions than regular insulin. As insulin glargine is less soluble at neutral pH, once injected, forms microprecipitates. Slow release of insulin glargine from microprecip... | Insulin glargine is metabolized in the liver into two active metabolites with similar activity to insulin: 21a-Gly-human insulin (M1) and 21a-Gly-des-30b- threonine insulin (M2), with M1 being the predominant metabolite. | Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs ... | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"A10AE",
"A10A",
"A10",
"A",
"A10AE",
"A10A",
"A10",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "14.35",
"description": "Lantus 100 unit/ml cartridge",
"unit": "ml"
},
{
"cost": "14.35",
"description": "Lantus solostar 100 unit/ml",
"unit": "ml"
},
{
"cost": "44.78",
"description": "Lantus for OptiClik 100 unit/ml Solution 3ml Cartridge",
"unit": "cartridg... | [
{
"approved": "2000-08-08",
"country": "United States",
"expires": "2009-11-06",
"number": "6100376"
},
{
"approved": "1997-04-01",
"country": "Canada",
"expires": "2014-04-01",
"number": "1339044"
},
{
"approved": "2015-04-21",
"country": "United States",
"expire... | Insulin glargine | Insulin glargine (rDNA origin) | Insulin glargine recombinant | insulin glargine-yfgn | Insulina glargina | 2.7.10.1 | IR | 2.7.10.1 | IGF-I receptor | Insulin-like growth factor I receptor | 1.14.14.1 | Cholesterol 25-hydroxylase | CYPIA2 | Cytochrome P(3)450 | Cytochrome P450 4 | Cytochrome P450-P3... | [
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Abasaglar",
"Basaglar",
"Basaglar",
"Basaglar",
"Basaglar",
"BASAGLAR KwikPen",
"BASAGLAR Tem... | [
"Lantus R",
"Lusduna Nexvue",
"Optisulin",
"Semglee"
] | [
"Soliqua 100/33",
"Soliqua",
"Suliqua",
"Suliqua",
"Suliqua",
"Suliqua",
"Suliqua",
"Suliqua Pen"
] | [
"P06213",
"P08069"
] | [
"P05177"
] | [] | [] |
DB00048 | Collagenase clostridium histolyticum | Collagenase clostridium histolyticum is an enzyme produced by the bacterium Clostridium histolyticum. It is beneficial in the breakdown of collagen plaques for the treatment of Dupuytren's contracture and Peyronie's disease.[L14882] The topical formulation is used for the debridement of necrotic tissue due to burns or ... | solid | Collagenase clostridium histolyticum is indicated for the treatment of adults with Dupuytren's contracture with a palpable cord. Additionally, it is used to treat men with Peyronie's disease diagnosed with a penile curvature deformity of at least a 30-degree angle at the beginning of therapy in addition to palpable pla... | Collagenase digests collagen, treating conditions such as Peyronie's disease, cellulite, chronic ulcers, burns, and contractures.[L14872,L14882,L14912] | Peyronie's disease is a fibrous lesion of the tunica albuginea in the penile tissues.[A215067] Cellulite is a multifactorial condition resulting in the accumulation of fibrotic dermal septae and the expansion of subcutaneous fat.[A215062] Dupuytren's contracture is a fibroproliferative disease that results in the fibro... | There is currently limited readily available regarding the absorption of collagenase through the skin.[L14912]
In a pharmacokinetic study, the serum concentrations of clostridium type I collagenase (AUX-I) and clostridium type II collagenase (AUX-II) were measured. Both were detected under the lower limit of quantita... | No formal systemic metabolism studies have been performed with collagenase histolyticum.[A215277] | No clinical reaction has been attributed to an overdose of collagenase in clinical trials.[L14912] If required, the collagenase enzymes can be inactivated with a povidone-iodine wash.[L14912] | null | There is no readily available information regarding the protein binding of collagenase.[L14912] | null | There is no currently available information regarding the presence of collagenase in body fluids or uptake by particular organs and passage through the blood-brain barrier.[L14912] Systemic pharmacokinetic studies evaluation volume of distribution have not been performed, however, collagenase histolyticum is likely to ... | Clearance information for collagenase is not readily available.[L14912] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"D03BA",
"D03B",
"D03",
"D",
"M09AB",
"M09A",
"M09",
"M",
"D03BA",
"D03B",
"D03",
"D"
] | [
"Humans and other mammals"
] | [
{
"cost": "4.13",
"description": "Santyl ointment",
"unit": "g"
},
{
"cost": "62.98",
"description": "Santyl 250 unit/gm Ointment 15 gm Tube",
"unit": "tube"
},
{
"cost": "2432.7",
"description": "Collagenase powder",
"unit": "g"
},
{
"cost": "3900.0",
"descri... | [] | Clostridiopeptidase A | Clostridium histolyticum enzymes | Collagenase | Collagenase clostridium histolyticum | collagenase clostridium histolyticum-aaes | Alpha-1 type I collagen | Alpha-1 type II collagen | [
"Collagen Film",
"Collagenase Santyl",
"Collagenase Santyl",
"Kimchi Vitamin chewable multivitamin",
"Qwo",
"Santyl",
"Xiaflex",
"Xiaflex",
"Xiapex"
] | [
"Cordase"
] | [
"Kimchi Vitamin chewable multivitamin",
"Collagen Film"
] | [
"P02452",
"P02458",
"P02461"
] | [] | [] | [] |
DB00049 | Rasburicase | Rasburicase is a recombinant urate-oxidase enzyme produced by a genetically modified <i>Saccharomyces cerevisiae</i> strain. The cDNA coding for rasburicase was cloned from a strain of _Aspergillus flavus_. | liquid | For treatment of hyperuricemia, reduces elevated plasma uric acid levels (from chemotherapy) | Drugs used to treat lympohoid leukemia, non-Hodgkin's lymphoma and acute myelogenous leukemia often lead to the accumulation of toxic plasma levels of purine metabolites (i.e. uric acid). The injection of rasburicase reduces levels of uric acid and mitigates the toxic effects of chemotherapy induced tumor lysis. | Rasburicase catalyzes enzymatic oxidation of uric acid into an inactive and soluble metabolite (allantoin). | null | null | null | 18 hours | null | null | * 110 to 127 mL/kg [pediatric patients]
* 75.8 to 138 mL/kg [adult patients] | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"V03AF",
"V03A",
"V03",
"V",
"M04AX",
"M04A",
"M04",
"M"
] | [
"Humans and other mammals"
] | [
{
"cost": "627.23",
"description": "Elitek 1.5 mg vial",
"unit": "vial"
},
{
"cost": "3136.18",
"description": "Elitek 7.5 mg vial",
"unit": "vial"
}
] | [
{
"approved": "2003-12-30",
"country": "Canada",
"expires": "2016-05-07",
"number": "2175971"
},
{
"approved": "2002-07-16",
"country": "Canada",
"expires": "2015-05-03",
"number": "2148537"
}
] | Rasburicasa | Rasburicase | Recombinant urate oxidase | Urate oxidase | [
"Elitek",
"Elitek",
"Fasturtec",
"Fasturtec",
"Fasturtec",
"Fasturtec"
] | [] | [] | [] | [] | [] | [] |
DB00050 | Cetrorelix | Cetrorelix is a man-made hormone that blocks the effects of Gonadotropin Releasing Hormone (GnRH). GnRH controls another hormone that is called luteinizing hormone (LH), which is the hormone that starts ovulation during the menstrual cycle. When undergoing hormone treatment sometimes premature ovulation can occur, lead... | solid | For the inhibition of premature LH surges in women undergoing controlled ovarian stimulation | Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle... | Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. | Rapidly absorbed following subcutaneous injection. The mean absolute bioavailability following subcutaneous administration to healthy female subjects is 85%. | In in vitro studies, cetrorelix was stable against phase I- and phase II-metabolism. Cetrorelix was transformed by peptidases, and the (1-4) peptide was the predominant metabolite. | null | ~62.8 hours | 86% | Following subcutaneous administration of 10 mg cetrorelix to males and females, only unchanged cetrorelix was detected in urine. | * 1.16 L/kg | * 1.28 ml/min·kg [adult healthy female with 3 mg single SC administration] | Organic compounds | Organic Polymers | Polypeptides | null | [
"approved",
"investigational"
] | [
"H01CC",
"H01C",
"H01",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "137.99",
"description": "Cetrotide 0.25 mg kit",
"unit": "kit"
},
{
"cost": "689.92",
"description": "Cetrotide 3 mg kit",
"unit": "kit"
}
] | [
{
"approved": "1993-03-30",
"country": "United States",
"expires": "2010-10-24",
"number": "5198533"
},
{
"approved": "2003-08-05",
"country": "Canada",
"expires": "2014-02-18",
"number": "2115943"
},
{
"approved": "2001-11-20",
"country": "United States",
"expire... | Cetrorelix | Cetrorelixum | GnRH receptor | GnRH-R | GRHR | LCGR | LGR2 | LH/CG-R | LHR | LHRHR | LSH-R | Luteinizing hormone receptor | [
"Cetrorelix",
"Cetrorelix",
"Cetrorelix acetate",
"Cetrorelix acetate",
"Cetrorelix Acetate",
"Cetrorelix Acetate",
"Cetrorelix Acetate",
"Cetrotide",
"Cetrotide",
"Cetrotide",
"Cetrotide",
"Cetrotide",
"Cetrotide"
] | [] | [] | [
"P30968",
"P22888"
] | [] | [] | [] |
DB00051 | Adalimumab | Adalimumab is a subcutaneously administered biological disease modifier for the treatment of rheumatoid arthritis and other chronic debilitating diseases mediated by tumor necrosis factor.[A39984,A39999] It was originally launched by Abbvie in the U.S. and approved in 2002 by the FDA.[A39983] This drug is frequently kn... | liquid | Adalimumab is indicated for the following conditions:[L49101]
- Moderately to severely active Rheumatoid Arthritis (RA) in adults, as monotherapy or in combination with [methotrexate] or other non-biologic disease-modifying anti-rheumatic drugs (DMARDs).[L42290, L42495, L42935, L44953, L45643, L45818, L49101]
- Mod... | After treatment with adalimumab, a decrease in levels of acute phase reactant proteins of inflammation (C reactive protein [CRP] and erythrocyte sedimentation rate [ESR]) and serum cytokines (IL-6) was measured compared to baseline in patients diagnosed with rheumatoid arthritis. A decrease in CRP levels was also obse... | Adalimumab binds with specificity to tumor necrosis factor-alpha (TNF-alpha) and inhibits its interaction with the p55 and p75 cell surface TNF receptors. Adalimumab also lyses surface tumor necrosis factor expressing cells in vitro when in the presence of complement.[A39984,A39999] Adalimumab does not bind or inactiva... | The maximum serum concentration (Cmax) and the time to reach the maximum concentration (Tmax) were 4.7 ± 1.6 μg/mL and 131 ± 56 hours respectively, following a single 40 mg subcutaneous administration of adalimumab to healthy adult subjects. The average absolute bioavailability of adalimumab estimated from three clinic... | null | Doses up to 10 mg/kg have been administered to patients in clinical trials without evidence of dose-limiting toxicities. In case of overdosage, it is recommended that the patient be monitored for any signs or symptoms of adverse reactions or effects and appropriate symptomatic treatment instituted immediately.[L42290] | The mean terminal half-life was approximately 2 weeks, ranging from 10 to 20 days across studies.[L35370] | null | Adalimumab is most likely removed by opsonization via the reticuloendothelial system.[A40006] | The distribution volume (Vss) ranged from 4.7 to 6.0 L following intravenous administration of doses ranging from 0.25 to 10 mg/kg in RA patients.[L35370] | The single-dose pharmacokinetics of adalimumab in RA patients were determined in several studies with intravenous doses ranging from 0.25 to 10 mg/kg. The systemic clearance of adalimumab is approximately 12 mL/hr. In long-term studies with dosing more than two years, there was no evidence of changes in clearance over ... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"experimental"
] | [
"L04AB",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "959.19",
"description": "Humira 20 mg/0.4 ml syringe",
"unit": "syringe"
},
{
"cost": "959.19",
"description": "Humira 40 mg/0.8 ml pen",
"unit": "pen"
},
{
"cost": "959.19",
"description": "Humira crohn's starter pack",
"unit": "each"
},
{
"cost": "959... | [
{
"approved": "2002-09-17",
"country": "Canada",
"expires": "2017-02-10",
"number": "2243459"
}
] | Adalimumab | Adalimumab (genetical recombination) | adalimumab-adaz | adalimumab-adbm | adalimumab-afzb | adalimumab-atto | adalimumab-bwwd | adalimumab-fkjp | Cachectin | TNF-a | TNF-alpha | TNFA | TNFSF2 | Tumor necrosis factor ligand superfamily member 2 | [
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Abrilada",
"Adalimumab",
"Adalimumab",
"Adalimumab",
"Adalimumab",
"Adalimumab",
"Adalimumab"... | [
"Amjevita",
"Cyltezo",
"Humira Pen"
] | [
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Humira",
"Cyltezo",
"Cyltezo",
"Cyltezo",
"Cyltezo",
"Hulio",
"Hulio",
"Hulio",
"Adalimumab",
"Adalimumab",
"Adalim... | [
"P01375"
] | [] | [] | [] |
DB00052 | Somatotropin | Human growth hormone (HGH), also known as somatotropin, is a peptide hormone that is synthesized and secreted by the somatotropic cells of the anterior pituitary gland.[A228183] Growth hormone plays an essential role in growth regulation during childhood as well as other basal metabolic functions, muscle and fat mass r... | liquid | Somatotropin is indicated for the treatment of pediatric patients who have growth failure due to an inadequate secretion of endogenous growth hormone, short stature associated with Turner syndrome, Prader-Willi syndrome (PWS), idiopathic short stature (ISS), short stature or growth failure in short stature homeobox-con... | Somatotropin induces growth in nearly every tissue and organ in the body.[L31508] It stimulates linear growth and cartilaginous growth of long bones. In children with short stature, growth hormone increases both the number and size of muscle cells. It also promotes the growth of internal organs, and it also increases r... | In conditions of growth failure, growth hormone deficiency, low body mass, and malnutrition, somatotropin treatment acts to mimic and restore the actions of endogenous growth hormone of stimulating linear bone growth, increasing bone mass, increasing muscle and reduced fat mass, and regulating blood glucose and lipid l... | When somatotropin was administered subcutaneously at the dose of 0.024 mg/kg or 3 IU/m<sup>2</sup>, the C<sub>max</sub> ranged from 13.8 (±5.8) to 17.1 (±10.0) ng/mL and the T<sub>max</sub> was four to five hours. Following intravenous infusion of 33 ng/kg/min of somatotropin in patients with growth hormone deficiency,... | Information is unavailable. | The oral LD<sub>50</sub> is 242 mg/kg in rats and 828 mg/kg in mice. The inhalatory LD<sub>50</sub> is 710 mg/m<sup>3</sup> and dermal LD<sub>50</sub> is 1100 mg/kg in rats. The intraperitoneal LD<sub>50</sub> in mice is 828 mg/kg.[L31528]
Hypoglycemia followed by hyperglycemia, possibly with fluid retention, can be... | When somatotropin was administered subcutaneously at the dose of 0.024 mg/kg or 3 IU/m<sup>2</sup>, the mean apparent terminal half-life was Following intravenous infusion of 33 ng/kg/min of somatotropin in patients with growth hormone deficiency, the terminal elimination half-life was approximately 21.1 (±5.1) minute... | While there is no information regarding the protein binding profile of recombinant human growth hormones, endogenous growth hormone is typically complexed with growth hormone-binding protein, which is a soluble form of growth hormone receptor, when it is incubated with plasma _in vitro_.[A228463] | Information is unavailable. | Information is unavailable. | Following intravenous infusion of 33 ng/kg/min of somatotropin in patients with growth hormone deficiency, the mean clearance rate was approximately 2.3 (±1.8) mL/min/kg or 139 (±105) mL/min.[L10971] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"H01AC",
"H01A",
"H01",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "15.05",
"description": "Genotropin miniquick 0.2 mg",
"unit": "each"
},
{
"cost": "30.09",
"description": "Genotropin miniquick 0.4 mg",
"unit": "each"
},
{
"cost": "45.14",
"description": "Genotropin miniquick 0.6 mg",
"unit": "each"
},
{
"cost": "60.1... | [
{
"approved": "1994-02-22",
"country": "United States",
"expires": "2011-10-07",
"number": "5288703"
},
{
"approved": "2009-06-23",
"country": "Canada",
"expires": "2017-04-24",
"number": "2252535"
},
{
"approved": "1994-01-25",
"country": "Canada",
"expires": "20... | Growth hormone | Growth hormone (human) | hGH | Human growth hormone | Recombinant human growth hormone | rhGH | Somatotropin (human) | Somatotropin human | Somatotropin human growth hormone | Somatropin | Somatropin (rDNA origin) | Somatropin (recombinant DNA origin) | Somatropin [rDNA origin] | Somatropin recombinant... | [
"Bio-tropin",
"Bio-tropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin",
"Genotropin"... | [
"BioTropin"
] | [
"Saizen 10iu - Kit",
"Serostim",
"Nutropin - Kit Pws(5mg) & Liq(10ml) Im Sc",
"Nutropin - Kit Pws(10mg) & Liq(10ml) Im Sc",
"Serostim",
"Bio-tropin",
"Bio-tropin",
"Omnitrope",
"Humatrope",
"Humatrope",
"Humatrope"
] | [
"P10912",
"P16471"
] | [
"P05177",
"P33261"
] | [] | [
"P08183"
] |
DB00053 | Imiglucerase | Human Beta-glucocerebrosidase or Beta-D-glucosyl-N-acylsphingosine glucohydrolase E.C. 3.2.1.45. 497 residue protein with N-linked carbohydrates, MW=59.3 kD. Alglucerase is prepared by modification of the oligosaccharide chains of human Beta-glucocerebrosidase. The modification alters the sugar residues at the non-redu... | liquid | For the treatment of Gaucher's disease (deficiency in glucocerebrosidase) | Gaucher disease is characterized by a functional deficiency in Beta-glucocerebrosidase enzymatic activity and the resultant accumulation of lipid glucocerebroside in tissue macrophages which become engorged and are termed Gaucher cells. Gaucher cells are typically found in liver, spleen and bone marrow. This can lead t... | Imiglucerase catalyzes the hydrolysis of the glycolipid, glucocerebroside, to glucose and ceramide as part of the normal degradation pathway for membrane lipids. | null | null | null | 3.6-10.4 min | null | null | * 0.09 to 0.15 L/kg | * 14.5 +/- 4.0 mL/min/kg | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"A16AB",
"A16A",
"A16",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "380.64",
"description": "Ceredase 80 unit/ml vial",
"unit": "ml"
},
{
"cost": "951.6",
"description": "Cerezyme 200 unit vial",
"unit": "vial"
},
{
"cost": "1903.2",
"description": "Cerezyme 400 unit vial",
"unit": "vial"
}
] | [
{
"approved": "1996-08-27",
"country": "United States",
"expires": "2013-08-27",
"number": "5549892"
}
] | Imiglucerasa | Imiglucerase | [
"Cerezyme",
"Cerezyme",
"Cerezyme",
"Cerezyme",
"Cerezyme",
"Cerezyme",
"Cerezyme"
] | [] | [] | [] | [] | [] | [] |
DB00054 | Abciximab | Abciximab is a Fab fragment of the chimeric human-murine monoclonal antibody 7E3. Abciximab binds to the glycoprotein (GP) IIb/IIIa receptor of human platelets and inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive molecules. It also binds to vitronectin (αv... | liquid | Abciximab is indicated as an adjunct to percutaneous coronary intervention for the prevention of cardiac ischemic complications in patients undergoing percutaneous coronary intervention and in patients with unstable angina not responding to conventional medical therapy when percutaneous coronary intervention is planned... | Abciximab inhibits platelet aggregation by preventing the binding of fibrinogen, von Willebrand factor, and other adhesive molecules to GPIIb/IIIa receptor sites on activated platelets. A single intravenous bolus dose from 0.15 mg/kg to 0.30 mg/kg produced rapid dose-dependent inhibition of platelet function. After two... | Abciximab binds to the intact platelet GPIIb/IIIa receptor, which is a member of the integrin family of adhesion receptors and the major platelet surface receptor involved in platelet aggregation. This binding is thought to involve steric hindrance and/or conformational alterations which block access of large molecules... | null | Most likely removed by opsonization via the reticuloendothelial system when bound to platelets, or by human antimurine antibody production. Excreted renally. | null | Following intravenous bolus administration, free plasma concentrations of Abciximab decrease rapidly with an initial half-life of less than 10 minutes and a second phase half-life of about 30 minutes, probably related to rapid binding to the platelet GPIIb/IIIa receptors. | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B01AC",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "155.77",
"description": "Reopro 2 mg/ml vial",
"unit": "ml"
}
] | [
{
"approved": "2002-05-07",
"country": "Canada",
"expires": "2019-05-07",
"number": "1341357"
}
] | Abciximab | Abciximab (genetical recombination) | c7E3 | GP3A | GPIIIa | Platelet membrane glycoprotein IIIa | GP2B | GPalpha IIb | GPIIb | ITGAB | Platelet membrane glycoprotein IIb | CD32 | CDw32 | Fc-gamma RII-a | Fc-gamma-RIIa | FCG2 | FCGR2A1 | FcRII-a | IGFR2 | IgG Fc receptor II-a | CD32 | CDw32 | Fc-gamma RII-b... | [
"Reopro",
"Reopro",
"Reopro"
] | [] | [] | [
"P05106",
"P08514",
"P12318",
"P31994",
"P04004"
] | [] | [] | [] |
DB00055 | Drotrecogin alfa | Drotrecogin alfa is activated human protein C that is synthesized by recombinant DNA technology. It is a glycoprotein of approximately 55 kilodalton molecular weight, consisting of a heavy chain and a light chain linked by a disulfide bond. Drotrecogin alfa was withdrawn from the market after a major study indicated th... | liquid | For reduction of mortality in patients with severe sepsis. | Drotrecogin alfa is activated human protein C that is synthesized by recombinant DNA technology. It is a glycoprotein of approximately 55 kilodalton molecular weight, consisting of a heavy chain and a light chain linked by a disulfide bond.
Drotrecogin alfa inhibits factor Va and VIIIa, thereby reducing the coagulabil... | Activated protein C combines with protein S on platelet surfaces and then degrades factor Va and factor VIIIa, thereby reducing blood coagulability. | null | null | null | 5.5 hours (mammalian reticulocytes, in vitro). | null | null | null | * 40 L/hr [severe sepsis adults]
* 30 +/- 8 L/hr [patients without sepsis undergoing hemodialysis]
* 28 +/- 9 L/hr [heathy] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational",
"withdrawn"
] | [
"B01AD",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "370.42",
"description": "Xigris 5 mg vial",
"unit": "vial"
},
{
"cost": "1481.66",
"description": "Xigris 20 mg vial",
"unit": "vial"
}
] | [
{
"approved": "2007-08-21",
"country": "Canada",
"expires": "2015-01-03",
"number": "2139468"
},
{
"approved": "2002-01-15",
"country": "Canada",
"expires": "2011-02-22",
"number": "2036894"
}
] | Activated protein C | Blood coagulation factor XIV (human) | Drotrecogin alfa (activated) | Drotrecogin alfa (activated), lyophilized | Drotrecogin alfa activated | Drotrecogin alfa, activated | Drotrecogin-alfa | Recombinant human activated protein C (rH-APC) | AHF | Antihemophilic factor | F8C | Procoagulant componen... | [
"Xigris",
"Xigris",
"Xigris",
"Xigris",
"Xigris (20mg/vial)",
"Xigris (5mg/vial)"
] | [] | [] | [
"P00451",
"P12259",
"P05121",
"P07204",
"P07225",
"P00734",
"P02776",
"P05154",
"P35237",
"Q9UNN8"
] | [] | [] | [] |
DB00056 | Gemtuzumab ozogamicin | Gemtuzumab ozogamicin is a recombinant humanized IgG4 kappa antibody which is conjugated with calicheamicin derivative, a cytotoxic antitumor antibiotic isolated from fermentation of Micromonospora echinospora ssp. calichensis. Gemtuzumab ozogamicin has approximately 50% of the antibody loaded with 4-6 moles calicheami... | liquid | Indicated for the treatment of patients with CD33 positive acute myeloid leukemia in first relapse who are 60 years of age or older and who are not considered candidates for other cytotoxic chemotherapy. Indicated for the treatment of patients aged 2 years and older with CD33-positive AML who have experienced a relapse... | Used for the treatment of acute myeloid leukemia (AML), mylotarg binds to the CD33 antigen, which is expressed on the surface of leukemic cells in more than 80% of patients with AML. The CD33 antigen is not expressed on pluripotent hematopoietic stem cells or nonhematopoietic cells. This gives mylotarg the selectivity ... | Mylotarg is directed against the CD33 antigen expressed by hematopoietic cells. Binding of the anti-CD33 antibody portion of Mylotarg with the CD33 antigen results in the formation of a complex that is internalized. Upon internalization, the calicheamicin derivative is released inside the lysosomes of the myeloid cell.... | In pediatric patients receiving a dose level of 9mg/m^2, the peak plasma concentration (Cmax) was approximately 3.47±1.04 mg/L with the AUC of 136 ±107 mg * h/L [A20377]. | Metabolic studies indicate hydrolytic release of the calicheamicin derivative from gemtuzumab ozogamicin. The drug is most likely removed by opsonization via the reticuloendothelial system. | The most frequently reported toxicities are myelosuppression and hepatic veno-occlusive disorder. | In pediatric patients receiving a dose level of 9mg/m^2, the half life was approximately 64±44 h after the first dose [A20377]. | null | null | The volume of distribution at steady state (Vss) was approximately 6.5 ± 5.5 L in pediatric patients receiving a dose level of 9mg/m^2 [A20377]. | The mean clearance rate was approximately 0.12±0.15 L/h/m^2 in pediatric patients receiving a dose level of 9mg/m^2 [A20377]. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L01FX",
"L01F",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "3104.82",
"description": "Mylotarg 5 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1998-06-30",
"country": "United States",
"expires": "2015-06-30",
"number": "5773001"
},
{
"approved": "1996-12-17",
"country": "United States",
"expires": "2013-12-17",
"number": "5585089"
}
] | Gemtuzumab ozogamicin | gp67 | Sialic acid-binding Ig-like lectin 3 | Siglec-3 | SIGLEC3 | CD16-I | CD16B | Fc-gamma RIII | Fc-gamma RIII-beta | Fc-gamma RIIIb | FCG3 | FCGR3 | FcR-10 | FcRIII | FcRIIIb | IGFR3 | IgG Fc receptor III-1 | CD16-II | CD16A | CD16a antigen | Fc-gamma RIII | Fc-gamma RIII-alpha | Fc-gamma RI... | [
"Mylotarg",
"Mylotarg",
"Mylotarg"
] | [] | [] | [
"P20138",
"O75015",
"P08637",
"P12314"
] | [] | [] | [] |
DB00057 | Indium In-111 satumomab pendetide | Tumor associated glycoprotein (TAG) 72 (B72.3) monoclonal antibody conjugated with Indium 111 for radioimaging colon tumors. Satumomab Pendetide (trade name: OncoScint®) is no longer commercially available. | liquid | For diagnosis of extrahepatic malignant cancers | Binds to the tumor associated glycoprotein 72 antigen, which is a cell surface protein generally over-expressed in colorectal cancers. The radioactive Indium 111, which is covalently attached to the antibody, allows radiodiagnostic detection of TAG-72 expressing cells and tumors. | Satumomab Pendetide is a monoclonal antibody which is attached to the chelator pentetic acid (DTPA) linked to the tripeptide glycine (G) – L-tyrosine (Y) – L-lysine (K), which chelates Indium 111. Satumomab pendetide binds selectively to cell-surface TAG-72 expressed on colorectal tumors. | null | Most likely removed by opsonization via the reticuloendothelial system or by human antimurine antibody production | null | 0.8 hours (mammalian reticulocytes, in vitro) | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"experimental",
"withdrawn"
] | [
"V09IB",
"V09I",
"V09",
"V"
] | [
"Humans and other mammals"
] | [] | [] | Indium (111In) satumomab pendetide | Indium In 111 satumomab pendetide | Indium-111 satumomab pendetide | [] | [
"OncoScint"
] | [] | [] | [] | [] | [] |
DB00058 | Alpha-1-proteinase inhibitor | Human alpha-1 proteinase inhibitor or alpha-1-antitrypsin, prepared from human plasma via Cohn alcohol fractionation followed by PEG and zinc chloride fractionation. | liquid | For chronic augmentation and maintenance therapy in individuals with alpha1-proteinase inhibitor (A1-PI) deficiency and clinical evidence of emphysema. | Prevents excessive accumulation of active neutrophil elastase and consequent proteolysis of elastin tissues in alveolar lung structures. This prevents the development of emphysema. | Alpha-1 proteinase inhibitor is a serine protease inhibitor (Serpin). Its primary mechanism is inhibiting the action of the serine protease called elastase (also plasmin and thrombin) in the lungs. The reactive center loop (RCL) of alpha-1 proteinase inhibitor extends out from the body of the protein and directs bindin... | null | null | null | null | null | null | * 5632 ± 2006 mL [ARALAST NP]
* 5618 ± 1618 mL [Aralast] | * 940 +/- 275 mL/day [Patients with congenital α1-PI deficiency with single IV infusion of 60 mg/kg] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B02AB",
"B02A",
"B02",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "0.46",
"description": "Prolastin 1000 mg vial",
"unit": "vial"
},
{
"cost": "0.46",
"description": "Prolastin 500 mg vial",
"unit": "vial"
},
{
"cost": "0.46",
"description": "Prolastin c 1000 mg vial",
"unit": "vial"
},
{
"cost": "0.5",
"descriptio... | [] | .Alpha.-1 protease inhibitor | .Alpha.1-proteinase inhibitor human | 122320-05-2 | Alfa 1-proteinase inhibitor (human) | Alfa-1-antitripsina | Alfa1 antitrypsin | Alpha 1-antitrypsin | Alpha 1-Proteinase Inhibitor | Alpha 1-proteinase inhibitor (human) | Alpha 1-proteinase inhibitor human | Alpha 1-proteinase inhibitor... | [
"Alpha1-proteinase Inhibitor (human)",
"Alpha1-proteinase Inhibitor (human)",
"Aralast NP",
"Aralast NP",
"Aralast NP",
"Aralast NP",
"Aralast NP",
"Glassia",
"Glassia",
"Prolastin Inj 25.0mg/ml",
"Prolastin-C",
"Prolastin-C",
"Prolastin-C",
"Prolastin-C",
"Prolastin-C",
"Prolastin-C L... | [
"Aralast",
"Prolastin"
] | [
"Prolastin-C"
] | [
"P08246"
] | [] | [] | [] |
DB00059 | Pegaspargase | Pegaspargase is a conjugate of monomethoxypolyethylene glycol (mPEG) and L-asparaginase (L-asparagine amidohydrolase), an asparagine-specific enzyme that converts L-asparagine into aspartic acid and ammonia.[L44667] Asparagine is an amino acid that is vital for cell survival. In humans, most normal tissues can produce ... | liquid | Pegaspargase is indicated as a component of a multi-agent chemotherapeutic regimen for the treatment of pediatric and adult patients with 1) first-line acute lymphoblastic leukemia or 2) acute lymphoblastic leukemia and hypersensitivity to asparaginase.[L44667] | Unlike normal cells, leukemia cells are dependent on an exogenous source of asparagine for survival. Pegaspargase hydrolyses asparagine into aspartic acid and ammonia, which depletes asparagine levels and leads to leukaemic cell death.[A255917] In patients given intramuscular doses of 2,500 International Units(IU)/m<su... | Pegaspargase is a pegylated L-asparaginase that catalyzes the conversion of the amino acid L-asparagine into aspartic acid and ammonia. Asparagine is an amino acid that is vital for DNA and RNA synthesis and cell division. It is not an essential amino acid in humans since most normal human tissues can produce asparagin... | In patients with acute lymphoblastic leukemia given 2,500 International Units (IU)/m<sup>2</sup> of pegaspargase, the mean asparaginase Cmax was reached at approximately 1 IU/mL (n=45-52) five days after a single intramuscular injection. Pegaspargase had a relative bioavailability of 82% after the first intramuscular d... | As a pegylated form of L-asparaginase, pegaspargase is expected to be metabolized by proteolytic enzymes throughout the body.
Since these enzymes are ubiquitously distributed, the exact role of the liver is unknown.[L44672] | Patients that received 10,000 International Units/m<sup>2</sup> of pegaspargase intravenously, had a slight increase in liver enzymes and a rash that developed 10 minutes after the start of the infusion, which was controlled with the administration of an antihistamine and by slowing down the infusion rate. There is no ... | The mean elimination half-life of pegaspargase was approximately 5.8 days after a single intramuscular dose, and 5.3 days after a single intravenous dose.[L44667] | null | Due to its high molecular weight, pegaspargase is not excreted renally.[L44672] | Based on a non-compartmental analysis, pegaspargase has a steady-state volume of distribution of approximately 1.86 L/m2 after a single intramuscular injection and 2 L after a single intravenous infusion.[L44667] | For a single intramuscular and intravenous dose, the clearance of pegaspargase is 0.17 L/m2/day and 0.2 L/day, respectively.[L44667] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L01XX",
"L01X",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "656.0",
"description": "Oncaspar 750 unit/ml vial",
"unit": "ml"
}
] | [] | Peg-asparaginase | Peg/L-asparaginase | Pegaspargasa | Pegaspargase | Serpin A7 | T4-binding globulin | TBG | [
"Lyophilized Pegaspargase",
"Lyophilized Pegaspargase",
"Oncaspar",
"Oncaspar",
"Oncaspar",
"Oncaspar",
"Oncaspar",
"Oncaspar",
"Oncaspar"
] | [
"Oncaspar"
] | [] | [] | [] | [
"P05543"
] | [] |
DB00060 | Interferon beta-1a | Human interferon beta (166 residues), glycosylated, MW=22.5kD. It is produced by mammalian cells (Chinese Hamster Ovary cells) into which the human interferon beta gene has been introduced. The amino acid sequence is identical to that of natural human interferon beta. | liquid | For treatment of relapsing/remitting multiple sclerosis, also for condyloma acuminatum | Interferon beta upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Type I int... | Interferon beta binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers a... | null | null | null | 10 hrs | null | null | null | * 33-55 L/hour [Healthy SC injection of 60 mcg] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AB",
"L03A",
"L03",
"L"
] | [] | [
{
"cost": "247.79",
"description": "Rebif 22 mcg/0.5 ml syringe",
"unit": "syringe"
},
{
"cost": "247.79",
"description": "Rebif 44 mcg/0.5 ml syringe",
"unit": "syringe"
},
{
"cost": "781.8",
"description": "Avonex admin pack 30 mcg vial",
"unit": "vial"
},
{
"co... | [
{
"approved": "2010-05-04",
"country": "Canada",
"expires": "2027-05-04",
"number": "1341604"
}
] | Interferon beta 1-a | Interferon beta 1a | Interferon beta-1a | Interferon beta-1a (recombinant human) | Interferon beta-1a (recombinant) | Interferon beta-1a,recombinant | Interferon beta, recombinant human | Interferon-beta-1a | SNG001 | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member... | [
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex",
"Avonex Pen",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"Rebif",
"... | [
"Betaferon",
"Blastoferon",
"Uribeta"
] | [
"Avonex",
"Avonex",
"Avonex",
"Rebif",
"Rebif",
"Rebif Rebidose",
"Rebif Rebidose",
"Rebif",
"Avonex",
"Rebif",
"Rebif"
] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00061 | Pegademase | Bovine adenosine deaminase derived from bovine intestine that has been extensively pegylated for extended serum half life. | liquid | For treatment of adenosine deaminase deficiency | Used to replace deficient or inactive adenosine deaminase which leads to severe combined immunodeficiency disease (SCID). The enzyme is responsible for converting adenosine to inosine. In the absence of adenosine deaminase, the purine substrates adenosine, 2'-deoxyadenosine and their metabolites are actually toxic to l... | Pegademase converts adenosine (toxic) to inosine (less toxic) by deamination. It also converts 2'-deoxyadenosine to 2'-deoxyinosine via deamination. | Time to peak for plasma adenosine deaminase is 2 to 3 days | null | null | plasma adenosine deaminase elimination half-life is 3 to >6 days | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AX",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "4375.0",
"description": "Adagen 250 unit/ml vial",
"unit": "ml"
}
] | [] | (monomethoxypolyethylene glycol succinimidyl) 11-17-adenosine deaminase | PEG-adenosine deaminase | pegADA | Pegademase | Pegademase bovine | Adapter protein GRB2 | ASH | Protein Ash | SH2/SH3 adapter GRB2 | [
"Adagen"
] | [] | [] | [
"P62993"
] | [] | [] | [] |
DB00062 | Albumin human | Human serum albumin is the primary protein present in human blood plasma. The main function of albumin is to maintain the oncotic pressure of blood [A33706]. It binds to water, cations (such as Ca2+, Na+ and K+), fatty acids, hormones, bilirubin, thyroxine (T4) and pharmaceuticals (including barbiturates). Albumin rep... | solid | Albuminex solution is indicated for adults and children for hypovolemia, ascites, hypoalbuminemia including from burns, acute nephrosis, acute respiratory distress syndrome and cardipulmonary bypass [F229]. | Serum albumin is a soluble, monomeric protein essential for maintaining and regulating the colloidal osmotic pressure of blood. It is utilized to increase the circulating plasma volume, which reduces hemoconcentration and blood viscosity. Albumin is also used as a transport protein that binds naturally occurring, thera... | The main function of albumin results from its contribution to plasma colloid oncotic pressure and transport function [F230].
Albumin stabilizes circulating blood volume and carries hormones, enzymes, medicines, and toxins. Other physiological functions include antioxidant properties, free radical scavenging, in ad... | null | null | In general, human albumin solutions are well-tolerated and no specific, clinically relevant alterations in organ function or coagulopathy have been substantiated [F229].
The most common adverse reactions are rigors, hypotension, tachycardia with increased heart rate, fever, chills, nausea, vomiting, dyspnea and/or b... | null | null | null | Albumin is distributed throughout the extracellular space and more than 60% of the body albumin pool is located in the extravascular fluid space [F230].
In healthy adults, less than 10% of infused albumin leaves the intravascular compartment during the first 2 hours following infusion of albumin. There is considerab... | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"B05AA",
"B05A",
"B05",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "1.32",
"description": "Albutein 25% vial",
"unit": "ml"
},
{
"cost": "1.97",
"description": "Albumin 25% iv solution",
"unit": "ml"
},
{
"cost": "2.22",
"description": "Buminate 25% iv solution",
"unit": "ml"
},
{
"cost": "0.3",
"description": "Albu... | [
{
"approved": "1996-09-24",
"country": "United States",
"expires": "2012-02-28",
"number": "5558094"
},
{
"approved": "2004-04-20",
"country": "United States",
"expires": "2021-04-20",
"number": "6723303"
}
] | Albumin (human) | Albumin human | Albumin, blood | Albumin, human | Albumin, human-kjda | Human albumin | Human serum albumin | Serum albumin | [
"Albuked",
"Albuked",
"Albuked",
"Albuked",
"Albuked",
"Albuked",
"Albuked",
"Albumin (Human)",
"Albumin (Human)",
"Albumin (Human)",
"Albumin (Human)",
"Albumin (Human)",
"Albumin (Human)",
"Albumin (human) 25% Solution",
"Albumin (human) 25% Solution USP",
"Albumin (human) 5% Solutio... | [] | [
"Sterile Diluent for Allergenic Extract",
"Macrotec",
"Venomil Honey Bee Venom (12mcg)",
"Venomil Wasp Venom Protein (12mcg)",
"Venomil White-faced Hornet Venom Protein (12mcg)",
"Venomil Yellow Hornet Venom Protein (12mcg)",
"Venomil Yellow Jacket Venom Protein (12mcg)",
"Albumin Human Diluent",
"B... | [] | [] | [] | [] |
DB00063 | Eptifibatide | Synthetic cyclic hexapeptide that binds to platelet receptor glycoprotein and inhibits platelet aggregation. Derived from venom of the Southeastern pygmy rattlesnake (Sistrurus miliarus barbouri), eptifibatide is a cyclic heptapeptide that belongs to the class of arginin-glycin-aspartat-mimetics. | liquid | For treatment of myocardial infarction and acute coronary syndrome. | Eptifibatide is an anti-coagulant that selectively and reversibly blocks the platelet glycoprotein IIb/IIIa receptor. | Eptifibatide inhibits platelet aggregation by reversibly binding to the platelet receptor glycoprotein (GP) IIb/IIIa of human platelets, thus preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. Inhibition of platelet aggregation occurs in a dose- and concentration-dependent manner. | null | No major metabolites have been detected in human plasma. Deamidated eptifibatide and other, more polar metabolites have been detected in urine. | Eptifibatide was not lethal to rats, rabbits, or monkeys when administered by continuous intravenous infusion for 90 minutes at a total dose of 45 mg/kg (about 2 to 5 times the recommended maximum daily human dose on a body surface area basis) | Approximately 2.5 hours | Approximately 25% | null | null | * 55 mL/kg/h [patients with coronary artery disease] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B01AC",
"B01A",
"B01",
"B"
] | [
"Humans and other mammals"
] | [
{
"cost": "3.88",
"description": "Integrilin 75 mg/100 ml vial",
"unit": "ml"
},
{
"cost": "10.74",
"description": "Integrilin 200 mg/100 ml vial",
"unit": "ml"
},
{
"cost": "12.41",
"description": "Integrilin 20 mg/10 ml vial",
"unit": "ml"
}
] | [
{
"approved": "1997-11-11",
"country": "United States",
"expires": "2014-11-11",
"number": "5686570"
},
{
"approved": "2007-04-17",
"country": "Canada",
"expires": "2013-04-27",
"number": "2133205"
},
{
"approved": "1998-09-15",
"country": "United States",
"expire... | Eptifibatida | Eptifibatide | Integrelin | Intrifiban | GP3A | GPIIIa | Platelet membrane glycoprotein IIIa | GP2B | GPalpha IIb | GPIIb | ITGAB | Platelet membrane glycoprotein IIb | BIII | Brain calcium channel III | CACH5 | CACNL1A5 | Calcium channel, L type, alpha-1 polypeptide isoform 5 | Voltage-gated calcium cha... | [
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibatide",
"Eptifibat... | [] | [] | [
"P05106",
"P08514",
"A0A024R8I1",
"Q00975"
] | [] | [] | [] |
DB00065 | Infliximab | Infliximab is a tumor necrosis factor (TNF-alpha or TNF-α) blocker and a chimeric monoclonal IgG1 antibody composed of human constant (75%) and murine variable (25%) regions [A31469]. Infliximab is produced by a recombinant cell line cultured by continuous perfusion. Tumor necrosis factor-alpha (TNF-α) is a key proinfl... | liquid | Infliximab is indicated for the following conditions:
- moderately to severely active ulcerative colitis following treatment with an infliximab product administered intravenously [L51793]
- moderately to severely active Crohn’s disease following treatment with an infliximab product administered intravenously [L51... | Infliximab disrupts the activation of pro-inflammaory cascade signalling. Infliximab has shown to reduce infiltration of inflammatory cells into sites of inflammation. It also attenautes the expression of molecules mediating cellular adhesion {including E-selectin, intercellular adhesion molecule-1 (ICAM-1) and vascula... | Infliximab is a IgG1κ monoclonal antibody that binds to soluble and transmembrane forms of TNF-α with high affinity to disrupt the pro-inflammatory cascade signalling. Binding of the antibody to TNF-α prevents TNF-α from interacting with its receptors. Infliximab does not neutralize TNF-β (lymphotoxin-α), a related cyt... | Following a single intravenous infusion, infliximab absorption displays a linear relationship between the dose administered and the maximum serum concentration [FDA Label].
In patients with Crohn's disease, the maximum plasma concentration (Cmax) of infliximab following single doses of 5 mg/kg and 10 mg/kg was 75 µ... | null | null | The median terminal half-life of infliximab is 7.7 to 9.5 days. The data is based on a pharmacokinetic study in patients with Crohn's disease, plaque psoriasis and rheumatoid arthritis receiving a single dose of infliximab [FDA Label]. | null | Therapeutic monoclonal antibodies including infliximab are predicted to be nonspecifically metabolized to peptides and amino acids that can be re-used in the body for de novo synthesis of proteins or arc excreted by the kidney [A19126]. The reticuloendothelial system (RES) are phagocytic cells of the immune system such... | Based on a pharmacokinetic study of adult patients, the distribution at steady state was independent of dose and indicated that infliximab was distributed primarily within the vascular compartment [FDA Label].
In patients with Crohn's disease, the apparent volume of distribution at steady state (Vss) of infliximab ... | In patients with Crohn's disease, the total body clearance (CL) of infliximab following single doses of 5 mg/kg and 10 mg/kg was 18.4 mL/h and 14.3 mL/h, respectively. In a maintenance therapy study, multiple infusions of infliximab (at week 0, 2 and 6) at the same dose of 5 mg/kg and 10 mg/kg resulted in CL of 15.2 mL... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L04AB",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "789.44",
"description": "Remicade 100 mg vial",
"unit": "vial"
},
{
"cost": "821.02",
"description": "Remicade 100 mg Solution Vial",
"unit": "vial"
}
] | [
{
"approved": "2001-02-06",
"country": "Canada",
"expires": "2012-03-18",
"number": "2106299"
}
] | IMMUNOGLOBULIN G (HUMAN-MOUSE MONOCLONAL CA2 HEAVY CHAIN ANTI-HUMAN TUMOR NECROSIS FACTOR), DISULFIDE WITH HUMAN-MOUSE MONOCLONAL CA2 LIGHT CHAIN, DIMER | Infliximab | Infliximab (genetical recombination) | Infliximab-abda | Infliximab-axxq | Infliximab-dyyb | Infliximab-qbtx | Cachectin | TNF-a | TNF-alpha | TNFA | TN... | [
"Avsola",
"Avsola",
"Flixabi",
"Flixabi",
"Flixabi",
"Flixabi",
"Flixabi",
"Inflectra",
"Inflectra",
"Inflectra",
"Inflectra",
"Inflectra",
"Inflectra",
"Inflectra",
"Infliximab",
"Ixifi",
"Omvyence",
"Remicade",
"Remicade",
"Remicade",
"Remicade",
"Remicade",
"Remicade",... | [
"Avsola"
] | [] | [
"P01375"
] | [] | [] | [] |
DB00066 | Follitropin | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 an... | liquid | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follic... | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt si... | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in h... | null | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with a... | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | null | Via liver and kidneys. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU]
* 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"G03GA",
"G03G",
"G03",
"G",
"G03GA",
"G03G",
"G03",
"G",
"G03GA",
"G03G",
"G03",
"G"
] | [
"Humans and other mammals"
] | [
{
"cost": "109.51",
"description": "Follistim aq 75 unit vial",
"unit": "vial"
},
{
"cost": "117.47",
"description": "Gonal-f rff 75 unit vial",
"unit": "vial"
},
{
"cost": "219.02",
"description": "Follistim aq 150 unit vial",
"unit": "vial"
},
{
"cost": "438.05"... | [
{
"approved": "1993-12-14",
"country": "United States",
"expires": "2011-03-20",
"number": "5270057"
},
{
"approved": "2003-10-21",
"country": "Canada",
"expires": "2011-03-08",
"number": "2037884"
},
{
"approved": "2009-07-21",
"country": "United States",
"expire... | Folitropina alfa | Folitropina beta | Folitropina delta | Follicle stimulating hormone | Follitrophin alfa | Follitrophin alpha | Follitrophin beta | Follitropin alfa | Follitropin alfa/beta | Follitropin alpha | Follitropin beta | Follitropin delta | Follitropin gamma | Follotropin recombinant | FSH | FSH alpha | FSH-... | [
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola",
"Bemfola Needles",
"Bravelle",
"Fertavid",
"Fertavid",
"Fertavid",
"Fertavid",
"Fertavid",
"Fertavid",
"Fertavid",
"... | [
"Cinnal-F"
] | [
"Follistim",
"Repronex",
"Menopur",
"Humegon Inj 75 I.U.",
"Pergonal 75 I.U.",
"Puregon 50 I.U.",
"Puregon 100 I.U.",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris",
"Pergoveris"
] | [
"P23945"
] | [] | [] | [] |
DB00067 | Vasopressin | Vasopressin (arginine-vasopressin or antidiuretic hormone) is a nonapeptide primarily produced in the hypothalamus that exhibits diverse physiological functions related to diuresis, hemodynamic modulation, and behaviour.[A110, A111, A112, A113, A228008] Vasopressin is very similar to oxytocin, differing in the third an... | solid | Vasopressin is indicated to increase blood pressure in adults in vasodilatory shock refractory to the application of fluids and catecholamines.[L31413] | Vasopressin is a nonapeptide antidiuretic hormone involved in modulating various physiological processes, including autonomic signalling, stress response, behaviour, and memory; the most well-known modulation is of blood pressure.[A110, A111, A112, A113, L31413] Vasopressin acts both within the brain and in the periphe... | Vasopressin, Cyclo (1-6) L-Cysteinyl-L-Tyrosyl-L-PhenylalanylL-Glutaminyl-L-Asparaginyl-L-Cysteinyl-L-Prolyl-L-Arginyl-L-Glycinamide, is a cyclic nonapeptide hormone primarily produced by the supraoptic and periventricular nuclei of the hypothalamus.[A228008, L31413] Vasopressin release is mediated by sensory pathways,... | null | Animal studies suggest that vasopressin is metabolized by serine proteases, carboxypeptidases, and disulphide oxidoreductases, primarily in the liver and kidneys. These cleavage events occur at sites important for vasopressin's activity, and hence the metabolites are expected to be inactive.[L31413] | Vasopressin overdose is expected to present with consequences related to excessive vasoconstriction of peripheral, mesenteric, coronary vascular beds, hyponatremia, and possibly with ventricular tachyarrhythmias, rhabdomyolysis, and gastrointestinal symptoms. As vasopressin is rapidly metabolized and cleared, symptoms ... | Vasopressin administered at 0.01-0.1 U/min has an apparent t<sub>1/2</sub> of ≤10 minutes,[L31413] although half-lives of up to 44 minutes have been reported in the literature. | null | Vasopressin is primarily eliminated in the urine, where only 6% of the dose is excreted unchanged.[L31413] | null | Vasopressin has a clearance of 9-25 mL/min/kg in patients with vasodilatory shock receiving 0.01-0.1 U/min of vasopressin.[L31413] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [] | [
"Humans and other mammals"
] | [
{
"cost": "1.86",
"description": "Vasopressin 20 unit/ml vial",
"unit": "ml"
},
{
"cost": "2.88",
"description": "Vasopressin 10 unit/0.5 ml vial",
"unit": "vial"
},
{
"cost": "7.68",
"description": "Pitressin 20 unit/ml vial",
"unit": "ml"
}
] | [
{
"approved": "2017-06-27",
"country": "United States",
"expires": "2035-01-30",
"number": "9687526"
},
{
"approved": "2016-06-28",
"country": "United States",
"expires": "2035-01-30",
"number": "9375478"
},
{
"approved": "2017-08-29",
"country": "United States",
... | Vasopressin, unspecified | Vasopressina | ADHR | Antidiuretic hormone receptor | AVPR V2 | DIR | DIR3 | Renal-type arginine vasopressin receptor | V2R | Antidiuretic hormone receptor 1a | AVPR V1a | AVPR1 | V1aR | Vascular/hepatic-type arginine vasopressin receptor | Antidiuretic hormone receptor 1b | AVPR V1b | AVPR V... | [
"Pitressin",
"Pitressin",
"Pitressin",
"Pitressin Inj 10 Unit/0.5ml",
"Pressyn Ar",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"Vasopressin",
"... | [] | [] | [
"P30518",
"P37288",
"P47901",
"P30559"
] | [] | [] | [
"Q92887"
] |
DB00068 | Interferon beta-1b | Human interferon beta (165 residues), cysteine 17 is substituted with serine. Produced in E. coli, no carbohydrates, MW=18.5kD | liquid | Interferon beta-1b is a drug used for the treatment of relapsing/remitting multiple sclerosis. It has been shown to slow the advance of the disease as well as to decrease the frequency of attacks. | Interferon beta upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Type I int... | Interferon beta binds to type I interferon receptors (IFNAR1 and IFNAR2c) which activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of tra... | null | null | null | null | null | null | * 0.25 to 2,88 L/kg | * 9.4 – 28.9 mL/min•kg-1 [patients with diseases other than MS receiving single intravenous doses up to 2.0 mg] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "196.76",
"description": "Extavia 0.3 mg kit",
"unit": "kit"
},
{
"cost": "227.69",
"description": "Betaseron 0.3 mg kit",
"unit": "kit"
},
{
"cost": "3315.06",
"description": "Betaseron 14 0.3 mg Solution 1 Box Contains Fourteen .3 mg Vials.",
"unit": "box"
}... | [
{
"approved": "1999-12-28",
"country": "Canada",
"expires": "2016-12-28",
"number": "1340861"
},
{
"approved": "1998-03-10",
"country": "Canada",
"expires": "2015-03-10",
"number": "1339707"
}
] | Interferon beta 1b (recombinant) | Interferon beta-1b | Interferon beta-1b,recombinant | Interferon-beta-1b | Recombinant interferon beta-1b | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha bindi... | [
"Betaferon",
"Betaferon",
"Betaferon",
"Betaferon",
"Betaferon",
"Betaferon",
"Betaferon",
"Betaferon",
"Betaferon",
"Betaferon",
"Betaseron",
"Betaseron",
"Betaseron",
"Extavia",
"Extavia",
"Extavia",
"Extavia",
"Extavia",
"Extavia",
"Extavia",
"Extavia",
"Extavia"
] | [] | [] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00069 | Interferon alfacon-1 | Interferon alfacon-1 is a recombinant non-naturally occurring type-I interferon. The 166-amino acid sequence of Interferon alfacon-1 was derived by scanning the sequences of several natural interferon alpha subtypes and assigning the most frequently observed amino acid in each corresponding position. Four additional am... | liquid | For the treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma | Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also indu... | Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers ... | Subcutaneous bioavailability averages 99% in golden Syrian hamsters and 83% to 104% in rhesus monkeys. | null | Reproductive toxicity studies in pregnant rhesus monkeys and golden Syrian hamsters demonstrated an increase in fetal loss in hamsters treated with Interferon alfacon-1 at doses of > 150 mcg/kg/day, and in rhesus monkeys at doses of 3 and 10 mcg/kg/day. The Interferon alfacon-1 toxicity profile described is consistent ... | The terminal half-life following subcutaneous dosing was 1.3 hours in golden Syrian hamsters and 3.4 hours in rhesus monkeys. | null | Due predominantly to catabolism and excretion by the kidneys. | null | Clearance, averaging 1.99 mL/minute/kg in golden Syrian hamsters and 0.71 to 0.92 mL/minute/kg in rhesus monkeys | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "129.08",
"description": "Infergen 9 mcg/0.3 ml vial",
"unit": "vial"
},
{
"cost": "134.24",
"description": "Infergen 15 mcg/0.5ml Injectable 0.5ml Vial",
"unit": "vial"
}
] | [] | IFN Alfacon-1 | IFN-Con1 | Interferon alfacon-1 | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding... | [
"Infergen",
"Infergen",
"Infergen",
"Infergen"
] | [
"Advaferon"
] | [] | [
"P17181",
"P48551"
] | [
"P05177"
] | [] | [] |
DB00070 | Hyaluronidase (ovine) | Highly purified sheep hyaluronidase for administration by injection into the vitreous of the eye. | liquid | For increase of absorption and distribution of other injected drugs and for rehydration. | Hyaluronidase hydrolyzes hyaluronic acid and increase diffusion of injected drugs, thus facilitating their absorption. Hyaluronidase is used for enhancing absorption and distribution of other injected drugs. | Hyaluronidase is a spreading or diffusing substance. It increase the permeability of connective tissue through the hydrolysis of hyaluronic acid. Hyaluronidase hydrolyzes hyaluronic acid by splitting the glucosaminidic bond between C1 of the glucosamine moiety and C4 of glucuronic acid. This temporarily decreases the v... | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [] | [
"Humans and other mammals"
] | [
{
"cost": "108.0",
"description": "Hylenex 150 unit/ml vial",
"unit": "ml"
},
{
"cost": "900.0",
"description": "Hyaluronidase powder",
"unit": "g"
},
{
"cost": "967.2",
"description": "Vitrase 6200 unit vial",
"unit": "vial"
},
{
"cost": "19200.0",
"descripti... | [] | Hyaluronidase (glycoprotein, sheep testis isoenzyme) | Hyaluronidase (ovine) | Hyaluronidase (sheep testis isoenzyme) | Hyaluronidase, ovine | Ovine hyaluronidase | TGFB | [
"Vitrase",
"Vitrase",
"Vitrase"
] | [
"Diffusin",
"Enzodase",
"Hyazyme",
"Wydase"
] | [] | [
"P01137"
] | [] | [
"P02768"
] | [] |
DB00071 | Insulin pork | Insulin isolated from pig pancreas. Composed of alpha and beta chains, processed from pro-insulin. Forms a hexameric structure. | liquid | For the treatment of type I and II diabetes mellitus. | Insulin is used in the treatment of type I and type II diabetes. The primary activity of insulin is the regulation of glucose metabolism. In muscle and other tissues (except the brain), insulin causes rapid transport of glucose and amino acids intracellularly. It also promotes anabolism, and inhibits protein catabolism... | Insulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to auto... | null | Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process. | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"A10AC",
"A10A",
"A10",
"A",
"A10AB",
"A10A",
"A10",
"A",
"A10AE",
"A10A",
"A10",
"A",
"A10AD",
"A10A",
"A10",
"A"
] | [
"Humans and other mammals"
] | [] | [] | Insulin (pork) | Insulin porcine | Insulin purified porcine | Insulin purified pork | Insulin, porcine | Insulin, regular, pork | Porcine insulin | 2.7.10.1 | IR | 2.7.10.1 | IGF-I receptor | Insulin-like growth factor I receptor | 1.14.14.1 | Cholesterol 25-hydroxylase | CYPIA2 | Cytochrome P(3)450 | Cytochrome P450 4... | [
"Hypurin Nph Insulin Isophane Pork",
"Hypurin Regular Insulin Pork",
"Regular Purified Pork Insulin Inj"
] | [] | [] | [
"P06213",
"P08069"
] | [
"P05177",
"P14735"
] | [] | [] |
DB00072 | Trastuzumab | Produced in CHO cell cultures, trastuzumab is a recombinant IgG1 kappa, humanized monoclonal antibody [A40276] that selectively binds with high affinity in a cell-based assay (Kd = 5 nM) to the extracellular domain of the human epidermal growth factor receptor protein (HER2).[L14015] It is used as a treatment of human ... | solid | For the adjuvant treatment of HER2-overexpressing breast cancer, trastuzumab is indicated in several clinical settings: as part of a treatment regimen consisting of doxorubicin, cyclophosphamide, and either paclitaxel or docetaxel; as part of a treatment regimen with docetaxel and carboplatin; or as monotherapy followi... | Trastuzumab exerts an antitumour activity and is used in the treatment of HER2-positive breast cancer. HER2 protein overexpression is observed in 20%-30% of primary breast cancers [A40277] thus HER2 presents as a useful therapeutic target for the treatment of breast cancers. Trastuzumab has been shown, in both _in vitr... | Trastuzumab is a recombinant humanized IgG1 monoclonal antibody against the HER-2 receptor, a member of the epidermal growth factor receptors which is a photo-oncogene. Over-expressed in breast tumour cells, HER-2 overamplifies the signal provided by other receptors of the HER family by forming heterodimers [A121]. The... | Peak and trough plasma concentrations at steady state (between weeks 16 and 32) were approximately 123 and 79 mcg/mL, respectively. At the highest weekly dose studied (500 mg), mean peak serum concentration was 377 mcg/mL.[L14015] | After it binds to HER2, trastuzumab is metabolized intracellularly into smaller peptides and amino acids.[A40276] | There is no experience with overdosage of trastuzumab in clinical trials - single doses >8 mg/kg have not been tested in humans.[L14015] Trastuzumab can contribute to the development of ventricular dysfunction and congestive heart failure, particularly when used in combination (or temporally adjacent) to other cardioto... | The terminal half-life is approximately 28 days,[A40276] but may decrease with lower doses - at the 10mg and 500mg doses, half-lives averaged approximately 1.7 and 12 days, respectively.[L6214] | null | Following metabolism, the complex elimination of trastuzumab in humans is mediated by epithelial cells in a dose-dependent (nonlinear) fashion.[A40276] The renal excretion of trastuzumab is very low.[A40276] | null | The predicted steady-state clearance of trastuzumab is 0.173 - 0.337 L/day, dependent primarily on the dosing regimen.[L14015] The clearance rate for subcutaneously administered trastuzumab, formulated with hyaluronidase for improved subcutaneous absorption, is 0.11 L/day.[L14132] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L01FD",
"L01F",
"L01",
"L",
"L01FY",
"L01F",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "3443.46",
"description": "Herceptin 440 mg vial",
"unit": "vial"
},
{
"cost": "3581.2",
"description": "Herceptin 440 mg Solution Vial",
"unit": "vial"
}
] | [
{
"approved": "2005-03-22",
"country": "Canada",
"expires": "2012-06-15",
"number": "2103059"
}
] | RHUMAB HER2 | Trastuzumab | trastuzumab-anns | trastuzumab-dkst | trastuzumab-dttb | trastuzumab-pkrb | trastuzumab-qyyp | 2.7.10.1 | HER2 | Metastatic lymph node gene 19 protein | MLN 19 | MLN19 | NEU | NGL | p185erbB2 | Proto-oncogene c-ErbB-2 | Proto-oncogene Neu | Tyrosine kinase-type cell surface receptor HER2 | [
"Adheroza",
"Adheroza",
"Herceptin",
"Herceptin",
"Herceptin",
"Herceptin",
"Herceptin",
"Herceptin",
"Herceptin",
"Herceptin Hylecta",
"Herceptin Sc",
"Herwenda",
"Herzuma",
"Herzuma",
"Herzuma",
"Herzuma",
"Herzuma",
"Herzuma",
"Kanjinti",
"Kanjinti",
"Kanjinti",
"Kanjint... | [
"Herclon"
] | [
"Herceptin Hylecta",
"Perjeta-herceptin",
"Ogivri",
"Phesgo",
"Phesgo",
"Phesgo",
"Phesgo",
"Phesgo",
"Phesgo"
] | [
"P04626"
] | [] | [] | [] |
DB00073 | Rituximab | Rituximab is a genetically engineered chimeric murine/human monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B lymphocytes. The antibody is an IgG1 kappa immunoglobulin containing murine light and heavy-chain variable region sequences and human constant region sequences... | liquid | Rituximab is indicated for the treatment of adult patients with relapsed or refractory, low-grade or follicular, CD20-positive, B-cell non-Hodgkin’s Lymphoma (NHL) as a single agent. Also, it is indicated for the treatment of adult patients with previously untreated follicular, CD20-positive, B-cell NHL in combination ... | Rituximab is a chimeric murine/human monoclonal antibody that binds to the CD20 antigen. CD20 is predominantly expressed on the surface of pre-B and mature B-lymphocytes, allowing rituximab to target and promote lysis in this specific type of cells.[A40017,A248980,L26641]. In Non-Hodgkin's Lymphoma patients, rituximab ... | Rituximab is a monoclonal antibody that targets CD20, an antigen expressed on the surface of pre-B and mature B-lymphocytes [A124,A125,A126,L26641]. About 85% of non-Hodgkin’s lymphoma (NHL) cases are B-cell lymphomas, characterized by the high expression of CD19, CD20 and CD22 cell surface antigens.[A248980] CD20 is i... | Rituximab follows a linear pharmacokinetic model.[A40006] In patients with non-Hodgkin’s lymphoma (NHL) administered 4 doses of 375 mg/m<sup>2</sup> of rituximab (IV) weekly, detectable levels were observed 3-6 months after treatment completion. The pharmacokinetic profile of rituximab administered in combination with ... | As a monoclonal antibody, rituximab is expected to be metabolized by proteases throughout the body. | Toxicity information regarding rituximab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as fatal infusion-related reactions and severe mucocutaneous reactions. Symptomatic and supportive measures are recommended. No long-term animal studies have been ... | In patients with non-Hodgkin's lymphoma (NHL) treated with rituximab once a week or once every three weeks (n=298), the median terminal elimination half-life was 22 days (range of 6.1-52 days).[L26641] In patients with chronic lymphocytic leukemia (CLL) treated with rituximab (n=21), the estimated median terminal half-... | Not available. | Monoclonal antibodies (mAb) such as rituximab trigger the formation of antidrug antibodies (ADAs) that form ADA-mAb immune complexes. The endogenous elimination of these immune complexes is mediated by the reticuloendothelial system, most likely via fragment crystallizable-gamma (Fcγ)-mediated endocytosis[A40006]. | Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the volume of distribution of rituximab is 3.1 L.[L26641] In pediatric patients (6-17 years old) with granulomatosis with polyangiitis (GPA) or microscopic polyangiitis (MPA) given four doses of 375 mg/m<sup>2</sup> of ritux... | In patients with non-Hodgkin’s lymphoma (NHL), those with higher CD19-positive cell counts or larger measurable tumor lesions at pretreatment had higher rituximab clearance [L26641]. Based on a pharmacokinetic analysis that included 2005 patients with rheumatoid arthritis (RA), the clearance of rituximab is 0.335 L/day... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L01FA",
"L01F",
"L01",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "68.09",
"description": "Rituxan 10 mg/ml vial",
"unit": "ml"
},
{
"cost": "708.17",
"description": "Rituxan 10 mg/ml Concentrate 10ml Vial",
"unit": "vial"
}
] | [
{
"approved": "2008-07-15",
"country": "Canada",
"expires": "2013-11-12",
"number": "2149329"
},
{
"approved": "1995-08-29",
"country": "Canada",
"expires": "2012-08-29",
"number": "1336826"
},
{
"approved": "1998-04-07",
"country": "United States",
"expires": "20... | Rituximab | rituximab-abbs | rituximab-arrx | rituximab-pvvr | B-lymphocyte surface antigen B1 | Bp35 | CD20 | Leukocyte surface antigen Leu-16 | Membrane-spanning 4-domains subfamily A member 1 | [
"Blitzima",
"Blitzima",
"Mabthera",
"Mabthera",
"Mabthera",
"Mabthera",
"Riabni",
"Riabni",
"Riabni",
"Ritemvia",
"Ritemvia",
"Rituxan",
"Rituxan",
"Rituxan",
"Rituxan Hycela",
"Rituxan Hycela",
"Rituxan Sc",
"Rituxan Sc",
"Rituzena",
"Rituzena",
"Rixathon",
"Rixathon",
"... | [
"MabThera",
"Riabni"
] | [
"Rituxan Hycela",
"Rituxan Hycela"
] | [
"P11836"
] | [] | [] | [] |
DB00074 | Basiliximab | A recombinant chimeric (murine/human) monoclonal antibody (IgG1k) that functions as an immunosuppressive agent, specifically binding to and blocking the interleukin-2 receptor a-chain (IL-2R alpha, also known as CD25 antigen) on the surface of activated T-lymphocytes. It is a 144 kDa glycoprotein obtained from fermenta... | liquid | For prophylactic treatment of kidney transplant rejection | Basiliximab functions as an IL-2 receptor antagonist. Specifically it inhibits IL-2-mediated activation of lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection. | Basiliximab binds with high-affinity to the alpha-subunit (CD25) of the high-affinity IL-2 receptor. This inhibits IL-2 binding, which inhibits T-cell activation and prevents the body from mounting an immune response against the foreign kidney. | null | Most likely removed by opsonization via the reticuloendothelial system when bound to lymphocytes, or by human antimurine antibody production | null | 7.2 +/- 3.2 days (adults) | null | null | * 7.8 ± 5.1 L [Pediatric]
* 4.8 ± 2.1 L [Adult] | * 41 +/- 19 mL/h [Adult patients undergoing first kidney transplantation]
* 17 +/- 6 mL/h [pediatric patients undergoing renal transplantation]
* 31 +/- 19 mL/h [adolescent patients undergoing renal transplantation] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L04AC",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "1883.11",
"description": "Simulect 10 mg vial",
"unit": "vial"
},
{
"cost": "2471.6",
"description": "Simulect 20 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1999-03-09",
"country": "Canada",
"expires": "2011-03-11",
"number": "2038279"
}
] | Basiliximab | IL-2 receptor subunit alpha | IL-2-RA | IL-2R subunit alpha | IL2-RA | p55 | TAC antigen | High affinity IL-2 receptor subunit beta | IL-2 receptor subunit beta | IL-2R subunit beta | IL-2RB | IL15RB | Interleukin-15 receptor subunit beta | p70-75 | p75 | [
"Simulect",
"Simulect",
"Simulect",
"Simulect",
"Simulect",
"Simulect",
"Simulect"
] | [] | [] | [
"P01589",
"P14784"
] | [] | [] | [] |
DB00075 | Muromonab | Murine monoclonal antibody specific to CD3 T-cell lymphocyte antigens. More specifically it is a purified murine (mouse) monoclonal antibody, directed against the CD3 (T3) receptor on the surface of human T-cells (T-lymphocytes) cultured using the murine ascites method. Muromonab is 93% monomeric immune globulin G type... | liquid | For treatment of organ transplant recipients, prevention of organ rejection | Used in organ transplant prophylaxis, Muromonab or OKT-3 binds specifically to the CD-3 complex, which is involved in antigen recognition and cell stimulation, on the surface of T lymphocytes. Immediately after administration CD-3-positive T lymphocytes are abruptly removed from circulation. It has been effective in re... | Muromonab binds to the T-cell surface glycoprotein CD3 epsilon chain. It appears to kill CD-3 positive cells by inducing Fc mediated apoptosis, antibody mediated cytotoxicity and complement-dependent cytotoxicity. | null | Most likely removed by opsonization via the reticuloendothelial system when bound to T lymphocytes, or by human antimurine antibody production | null | 0.8 hours (mammalian reticulocytes, in vitro) | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L04AG",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "261.75",
"description": "Orthoclone okt-3 5 mg/5 ml",
"unit": "ml"
}
] | [] | Anti-CD3 | Muromonab-CD3 | T-cell receptor T3 delta chain | T3D | T-cell surface antigen T3/Leu-4 epsilon chain | T3E | T-cell receptor T3 gamma chain | T3G | CD3Z | T-cell receptor T3 zeta chain | T3Z | TCRZ | CD16-I | CD16B | Fc-gamma RIII | Fc-gamma RIII-beta | Fc-gamma RIIIb | FCG3 | FCGR3 | FcR-10 | FcRIII | FcRII... | [
"Okt3",
"Orthoclone Okt 3 Sterile Solution IV 1mg/ml"
] | [
"Orthoclone OKT3"
] | [] | [
"P04234",
"P07766",
"P09693",
"P20963",
"O75015"
] | [] | [] | [] |
DB00076 | Digoxin Immune Fab (Ovine) | Digoxin Immune Fab is a sheep antibody (26-10) FAB fragment from sheep immunized with the digoxin derivative Digoxindicarboxymethylamine. It is used as an antidote for overdose of digoxin. | liquid | For treatment of digitoxin overdose or digitalis glycoside toxicity. | DigiFab binds molecules of digoxin, making them unavailable for binding at their site of action on cells in the body. The Fab fragment-digoxin complex accumulates in the blood, from which it is excreted by the kidney. The net effect is to shift the equilibrium away from binding of digoxin to its receptors in the body, ... | Binds excess digoxin or digitoxin molecules circulating in the blood. | null | null | null | 15-20 hrs | null | Cumulative urinary excretion of digoxin was comparable for both products and exceeded 40% of the administered dose by 24 hours. | * 0.3 L/kg [DigiFab]
* 0.4 L/kg [Digibind] | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"V03AB",
"V03A",
"V03",
"V"
] | [
"Humans and other mammals"
] | [
{
"cost": "615.6",
"description": "Digifab 40 mg vial",
"unit": "vial"
},
{
"cost": "727.91",
"description": "Digibind 38 mg vial",
"unit": "vial"
}
] | [] | Digitalis antitoxin | Digoxin Immune Fab, Ovine | Digoxin-specific Antibody Fragments | Ovine digoxin immune fab | [
"Digibind",
"Digibind",
"DigiFab",
"DigiFab",
"DigiFab"
] | [] | [] | [] | [] | [] | [] |
DB00078 | Ibritumomab tiuxetan | Indium or yttrium conjugated murine IgG1 kappa monoclonal antibody directed against the CD20 antigen, which is found on the surface of normal and malignant B lymphocytes. Ibritumomab is produced in Chinese hamster ovary cells and is composed of two murine gamma 1 heavy chains of 445 amino acids each and two kappa light... | liquid | For treatment of non-Hodgkin's lymphoma | Ibritumomab is a murine monoclonal antibody against CD20 that has been radiolabeled with yttrium-90. | The Fab segment of the antibody targets the CD20 epitope on B-cells, allowing the radioactive yttrium to destroy the cell via production of beta particles. | null | Most likely removed by opsonization via the reticuloendothelial system when bound to B cells, or by human antimurine antibody production | null | 0.8 hours (mammalian reticulocytes, in vitro) | null | null | Binding observed on lymphoid cells of the bone marrow, lymph node, thymus, red and white pulp of the spleen, lymphoid follicles of the tonsil, and lymphoid nodules of other organs (e.g., large and small intestines) | Approximately 7.2% of injected dose of yttrium Y 90 ibritumomab tiuxetan is excreted in urine within 7 days. | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"V10XX",
"V10X",
"V10",
"V"
] | [
"Humans and other mammals"
] | [
{
"cost": "4200.0",
"description": "Zevalin in-111 kit",
"unit": "kit"
},
{
"cost": "37800.0",
"description": "Zevalin y-90 kit",
"unit": "kit"
}
] | [
{
"approved": "2008-07-15",
"country": "Canada",
"expires": "2013-11-12",
"number": "2149329"
}
] | Ibritumomab | Ibritumomab tiuxetan | mAb Murine (IGG1) Anti P19437 (CD20_MOUSE) | B-lymphocyte surface antigen B1 | Bp35 | CD20 | Leukocyte surface antigen Leu-16 | Membrane-spanning 4-domains subfamily A member 1 | [
"Zevalin",
"Zevalin",
"Zevalin",
"Zevalin"
] | [] | [] | [
"P11836"
] | [] | [] | [] |
DB00080 | Daptomycin | Daptomycin is a cyclic lipopeptide antibacterial agent with a broad spectrum of activity against Gram-positive bacteria, including methicillin-susceptible and -resistant _Staphylococcus aureus_ (MSSA/MRSA) and vancomycin-resistant Enterococci (VRE).[A231379, A231384, L32534] Chemically, daptomycin comprises 13 amino ac... | solid | Daptomycin is indicated for the treatment of complicated skin and skin structure infections (cSSSI) in patients one year of age and older. It is also indicated for the treatment of _Staphylococcus aureus_ bloodstream infections (bacteremia) in patients one year of age and older, including in adult patients with right-s... | Daptomycin is a cyclic lipopeptide antibacterial agent produced as a fermentation product by the soil microbe _Streptomyces roseosporus_. The daptomycin core consists of 13 amino acids, including three D-amino acids, ornithine, 3-methyl-glutamic acid, and kynurenine, with the C-terminal 10 amino acids forming an ester-... | The mechanism of action of daptomycin remains poorly understood. Studies have suggested a direct inhibition of cell membrane/cell wall constituent biosynthesis, including peptidoglycan, uridine diphosphate-N-acid, acetyl-L-alanine, and lipoteichoic acid (LTA). However, no convincing evidence has been presented for any ... | Daptomycin administered as a 30 minute IV infusion to healthy volunteers in doses of 4, 6, 8, 10, and 12 mg/kg once daily resulted in a C<sub>max</sub> between 57.8 ± 3.0 and 183.7 ± 25.0 μg/mL and an AUC<sub>0-24</sub> of between 494 ± 75 and 1277 ± 253 μg\*h/mL.[A231449, L32534] Daptomycin pharmacokinetics are gener... | Radiolabeled daptomycin administered to five healthy adults revealed the presence of inactive metabolites in the urine. A separate study using 6 mg/kg daptomycin in healthy adults revealed small amounts of three oxidative and one unidentified metabolite(s) in urine but not in plasma.[L32534] The site of metabolism is u... | Toxicity information regarding daptomycin is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as myopathy, rhabdomyolysis, muscular/neurological system symptoms, eosinophilic pneumonia, tubulointerstitial nephritis, vomiting/diarrhea, abdominal pain, heada... | Daptomycin has a relatively long half-life, with ranges of 7.5-9 hours depending on dosing schemes and dose strength.[A231449, L32534] The half-life lengthens in patients with increasing renal impairment, being 27.83 ± 14.85 hours in patients with creatinine clearance <30 mL/min, 30.51 ± 6.51 hours in hemodialysis pati... | Daptomycin reversibly binds plasma proteins between 90-94% and independently of concentration.[A231449, L32534, A231574, A231579] Although daptomycin is mainly bound to serum albumin (HSA; 85-96%), it also binds appreciably to α-1-acid-glycoprotein (AGP; 25-51%).[A231574, A231579, A231584] Surface plasmon resonance (SP... | Daptomycin is excreted primarily by the kidneys, approximately 78% of an administered dose recovered in urine and only 5.7% recovered in feces.[A231449, L32534] Approximately 52% of the dose, recovered in urine, retains microbiological activity.[L32534] | Daptomycin has a very small volume of distribution, averaging ~0.1 L/kg in healthy adult subjects independent of dose.[A231449, L32534] The volume of distribution tends to increase with decreasing renal function, being estimated at ~0.2 L/kg in patients with severe renal impairment.[L32534] | Daptomycin administered as a 30 minute IV infusion to healthy volunteers in doses of 4, 6, 8, 10, and 12 mg/kg once daily resulted in total plasma clearance values between 7.2 ± 1.1 and 9.6 ± 1.3 mL/h/kg, with no clear dose association.[A231449, L32534] As daptomycin is primarily renally excreted, patients with mild, m... | null | null | null | null | [
"approved",
"investigational"
] | [
"J01XX",
"J01X",
"J01",
"J"
] | [
"Gram-positive Bacteria"
] | [
{
"cost": "272.7",
"description": "Cubicin 500 mg vial",
"unit": "vial"
}
] | [
{
"approved": "2006-07-04",
"country": "Canada",
"expires": "2019-09-24",
"number": "2344318"
},
{
"approved": "2002-10-22",
"country": "United States",
"expires": "2019-09-24",
"number": "6468967"
},
{
"approved": "2005-02-08",
"country": "United States",
"expire... | Daptomicina | Daptomycin | Daptomycine | Daptomycinum | 2.5.1.15 | dhpS | Dihydropteroate pyrophosphorylase | AGP 1 | AGP1 | OMD 1 | Orosomucoid-1 | AAT | Alpha-1 protease inhibitor | Alpha-1-antiproteinase | PI | Serpin A1 | LDL receptor | ABP | SBP | Sex steroid-binding protein | SHBG | TeBG | Testis-specific androge... | [
"Cubicin",
"Cubicin",
"Cubicin",
"Cubicin",
"Cubicin",
"Cubicin",
"Cubicin",
"Cubicin RF",
"Cubicin RF",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"Daptomycin",
"... | [
"Cidecin",
"Cubicin"
] | [] | [] | [] | [
"P02768",
"P02763",
"P01009",
"P01130",
"P04278",
"P02790"
] | [
"P08183"
] |
DB00081 | Tositumomab | Murine IgG2a lambda monoclonal antibody against CD20 antigen (2 heavy chains of 451 residues, 2 lambda chains of 220 residues). It is produced in an antibiotic-free culture of mammalian cells. It can be covalently linked to Iodine 131 (a radioactive isotope of iodine). | liquid | For treatment of non-Hodgkin's lymphoma (CD20 positive, follicular) | Tositumomab binds to the CD20 antigen, which is predominantly expressed on mature B cells and on >90% of B-cell non-Hodgkin's lympohomas. The antibody leads to selective killing of B-cells. | Binds to the CD20 antigen which is found on mature B lymphocytes. The antibody binding appears to induce apoptosis, complement-dependent cytotoxicity and cell death through ionizing radiation. | null | Most likely removed by opsonization via the reticuloendothelial system when bound to B lymphocytes, or by human antimurine antibody production | null | 0.8 hours (mammalian reticulocytes, in vitro) | null | Elimination of Iodine-131 occurs by decay and excretion in the urine. | null | * 68.2 mg/hr [patients with NHL] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"V10XA",
"V10X",
"V10",
"V"
] | [
"Humans and other mammals"
] | [
{
"cost": "100.43",
"description": "Bexxar 14 mg/ml dosimetric",
"unit": "ml"
},
{
"cost": "180.77",
"description": "Bexxar 131 iodine dosimetric",
"unit": "ml"
}
] | [] | Tositumomab | B-lymphocyte surface antigen B1 | Bp35 | CD20 | Leukocyte surface antigen Leu-16 | Membrane-spanning 4-domains subfamily A member 1 | CD32 | CDw32 | Fc-gamma RII-b | Fc-gamma-RIIb | FCG2 | FcRII-b | IGFR2 | IgG Fc receptor II-b | [
"Bexxar",
"Bexxar",
"Bexxar Dosimetric",
"Bexxar Therapeutic",
"Bexxar Therapy"
] | [] | [
"Bexxar",
"Bexxar"
] | [
"P11836",
"P31994"
] | [] | [] | [] |
DB00082 | Pegvisomant | Pegvisomant is a highly selective growth hormone (GH) receptor antagonist. It is used to treat acromegaly. Unlike dopamine or somatostatin analogs (which inhibit growth hormone secretion), this drug actually blocks the hepatic (GH-mediated) production of insulin like growth factor (IGF-1), which is the main mediator o... | liquid | Pegvisomant is a growth hormone receptor antagonist used for the treatment of acromegaly. | Somavert is used for the treatment of acromegaly, which arises from excessive IGF-1 levels. Somavert selectively binds to growth hormone (GH) receptors on cell surfaces, where it blocks the binding of endogenous GH, and thus interferes with GH signal transduction. Inhibition of GH action results in decreased serum conc... | Somavert selectively binds to growth hormone (GH) receptors on cell surfaces, where it blocks the binding of endogenous GH. This leads to the normalization of serum IGF-1 levels. | null | null | null | ~6 days | null | null | * 7 L | * 36 - 28 mL/h [SC doses ranging from 10 to 20 mg/day] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"H01AX",
"H01A",
"H01",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "104.18",
"description": "Somavert 10 mg vial",
"unit": "vial"
},
{
"cost": "156.29",
"description": "Somavert 15 mg vial",
"unit": "vial"
},
{
"cost": "208.38",
"description": "Somavert 20 mg vial",
"unit": "vial"
}
] | [
{
"approved": "1994-09-27",
"country": "United States",
"expires": "2011-09-27",
"number": "5350836"
},
{
"approved": "2009-05-26",
"country": "Canada",
"expires": "2016-09-20",
"number": "2230492"
},
{
"approved": "2003-04-01",
"country": "Canada",
"expires": "20... | Pegvisomant | GH receptor | Somatotropin receptor | 1.14.15.15 | 5-beta-cholestane-3-alpha,7-alpha,12-alpha-triol 26-hydroxylase | CYP27 | Cytochrome P-450C27/25 | Cytochrome P450 27 | Sterol 27-hydroxylase | Vitamin D(3) 25-hydroxylase | 6.3.1.2 | GLNS | Glutamate--ammonia ligase | GS | Palmitoyltransferase GLUL | 1,4... | [
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somavert",
"Somaver... | [] | [] | [
"P10912"
] | [
"Q02318",
"P15104",
"P08684",
"P06276",
"Q02928"
] | [] | [] |
DB00083 | Botulinum toxin type A | In 2002, botulinum toxin A, also known as onabotulinumtoxinA or Botox, was the first type A botulism toxin to be introduced into the market for cosmetic use.[A231824] With a wide variety of applications and favourable safety profile, Botulinum toxin A injection is a minimally invasive and promising treatment for cosmet... | solid | Botulinum toxin A is indicated for a variety of conditions, depending on the preparations. Cosmetically, it is used for the treatment of facial fine lines and wrinkles, specifically for upper facial rhytides, including forehead, lateral canthus, and glabellar lines.[L32559]
In addition to the above indications, botu... | Botulinum toxin A inhibits the release of acetylcholine, relieving muscle contraction and spasm associated with many conditions, such as incontinence and dystonia. Cosmetically, botulinum toxin A paralyses muscles in the face to temporarily treat wrinkles.[A231844,L32559] The maximum effects of muscle paralysis occur f... | Botulinum toxin is a 150-kDa molecular weight protein consisting of a light chain (50 kDa) and heavy chain (100 kDa) linked by a single disulfide bond. The crystal structure reveals 3 lobes - the light chain, the amino-terminal portion of the heavy chain, and the carboxyl-terminal portion of the heavy chain.[A231854]
... | The chemical complexity of botulinum toxin type A combined with its extreme potency limits the opportunity to study its pharmacokinetic profile in humans.[L32494] For this reason, human pharmacokinetic studies have not been performed. Animal studies using radio labeled botulinum toxin suggest it is absorbed systemicall... | Metabolism information for botulinum A toxin is not readily available in the literature.[A231854,L32494] | The intraperitoneal LD50 of botulinum toxin A in mice is 160 ng/kg.[L32654] An overdose of botulinum toxin A is expected to produce neuromuscular weakness, manifested by a variety of symptoms that may not appear immediately after injection. Dysphagia, dysphonia, weakness, dyspnea or respiratory distress may indicate d... | There is no readily available data about the pharmacokinetics of botulinum toxin in humans.[L32494] The elimination half-life for non-metabolized botulinum toxin in blood and serum ranged from 230 to 260 min in a pharmacokinetic study of rats and mice.[A231854] | A pharmacokinetic study in mice and rats revealed significant binding to albumin after subcutaneous injection or intranasal administration.[A231854] | Elimination information for botulinum A toxin is not readily available in the literature.[A231854,L32494] | There are extremely limited data about the pharmacokinetics of botulinum toxin in humans.[L32494] An animal study demonstrated that botulinum toxin accumulates in the liver and spleen in rats and mice when injected subcutaneously or administered intranasally.[A231854] | Clearance information for botulinum A toxin is not readily available in the literature.[A231854,L32494] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"M03AX",
"M03A",
"M03",
"M"
] | [
"Humans and other mammals"
] | [
{
"cost": "3.74",
"description": "Botox (100 - 200 unit/Vial)",
"unit": "vial"
},
{
"cost": "346.8",
"description": "Botox cosmetic 50 unit vial",
"unit": "vial"
},
{
"cost": "630.0",
"description": "Botox 100 unit vial",
"unit": "vial"
},
{
"cost": "630.0",
"... | [
{
"approved": "2005-11-15",
"country": "Canada",
"expires": "2019-08-20",
"number": "2280565"
},
{
"approved": "2001-05-15",
"country": "Canada",
"expires": "2014-06-07",
"number": "2310845"
}
] | AbobotulinumtoxinA | Botulinum A neurotoxin | Botulinum antitoxin type A | Botulinum toxin A | Botulinum toxin type A | BTX-A | EvabotulinumtoxinA | IncobotulinumtoxinA | OnabotulinumtoxinA | Prabotulinumtoxin A | Toxina botulínica A | Toxine botulinique A | SNAP | SNAP-25 | SUP | Super protein | Synaptosomal-associate... | [
"Botox",
"Botox",
"Botox",
"BOTOX Cosmetic",
"BOTOX Cosmetic",
"Dysport",
"Dysport Aesthetic",
"Dysport Therapeutic",
"Dysport Therapeutic",
"Nuceiva",
"Nuceiva",
"Nuceiva",
"Nuceiva",
"Nuceiva",
"Xeomin",
"Xeomin",
"Xeomin Cosmetic"
] | [] | [] | [
"P60880",
"P62745"
] | [] | [
"P02768"
] | [] |
DB00085 | Pancrelipase | Pancrelipase, in general, is composed of a mixture of pancreatic enzymes which include amylases, lipases, and proteases. These enzymes are extracted from porcine pancreatic glands.[L2509] The pancrelipase mixture was developed by Ortho-McNeil-Janssen Pharmaceuticals, Inc and FDA approved on April 12, 2010.[L2510] For f... | solid | The use of pancrelipase amylase is part of the pancreatic enzyme replacement therapy. This therapy is indicated for the treatment of pancreatic insufficiency attributed to cystic fibrosis, chronic pancreatitis or any other medically defined pancreatic disease that might require it.[A32721, A32736] Pancreatic diseases a... | The major maldigestion/malabsorption problems arise from incomplete fat digestion. In clinical trials, the administration of pancrelipase as a mixture of amylase, lipase, and protease demonstrated a significant improvement in the coefficient of fat absorption and nitrogen absorption. These effects are accompanied by in... | Pancrelipase is used to replace the deficiency of pancreatic enzymes. As abovementioned, pancrelipase is formed by a mixture of lipase, protease, and amylase which are able to break down fat, protein, and starches, respectively, in the small intestine.[T180] For a more specific description of each mechanism of action, ... | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount.[L2521] | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the metabolism is not relevant.[L2521] | The studies of the toxicology of pancrelipase are not needed as this drug has been used clinically for a long time.[L1770] Clinical overdose studies proved no effect on lungs, pancreas, liver and kidneys but it can produce symptoms such as diarrhea or stomach upset. Carcinogenicity studies have not shown any increased ... | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the elimination half-life is not relevant.[L2521] | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the protein binding is not relevant.[L2521] | Pancrelipase is entirely eliminated in the feces.[L2521] | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the volume of distribution is not relevant.[L2521] | Pancrelipase acts locally in the GI tract and it is not absorbed in any significant amount thus, the clearance rate is not relevant.[L2521] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"A09AA",
"A09A",
"A09",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "1.03",
"description": "Pancrelipase MST-16 48-16-48mu Enteric Coated Capsule",
"unit": "capsule"
},
{
"cost": "1.38",
"description": "Pancrelipase 10000 30-10-30mu Enteric Coated Capsule",
"unit": "capsule"
},
{
"cost": "1.49",
"description": "Pancrease MT 10 30-10... | [
{
"approved": "2015-12-01",
"country": "United States",
"expires": "2030-02-07",
"number": "9198871"
},
{
"approved": "2013-10-22",
"country": "United States",
"expires": "2028-02-20",
"number": "8562979"
},
{
"approved": "2013-10-22",
"country": "United States",
... | Pancrealipase | Pancreatic extract pancrelipase | Pancreatic protease | Pancreatin | Pancreatinum | Pancrelipase | Pancrelipase (amylase;lipase;protease) | [
"Alka-pan Tablets",
"Bio-zyme Tab 50mg",
"Duchol Ect",
"Dygest",
"Enzyme Tablets",
"Festal Plus",
"Festal Plus",
"Medichol",
"Neo Life Enzyme Tab",
"Pancreatin and Enzyme Formula - Tablet",
"Pancreatin Tab 400mg",
"Pancreatine Enzymes",
"Pancrelipase HP",
"Pancrex Granules",
"Pancrex V C... | [
"Cotazym",
"Ku-Zyme",
"Pancrease",
"Ultrase",
"Ultresa (delayed-release enteric coated capsules)",
"Viokace (tablets)",
"Zymase"
] | [
"Festal Plus",
"Stozyme",
"Pro Gest Tab",
"Medichol",
"Duchol Ect",
"Neo Life Enzyme Tab",
"Pancreatin and Enzyme Formula - Tablet",
"Enzyme Tablets",
"Pancreatine Enzymes",
"Dygest",
"Zypanax",
"Alka-pan Tablets",
"Festal Plus"
] | [] | [] | [] | [] |
DB00086 | Streptokinase | Streptokinase, is a sterile, purified preparation of a bacterial protein elaborated by group C (beta) -hemolytic streptococci. | liquid | For the treatment of acute evolving transmural myocardial infarction, pulmonary embolism, deep vein thrombosis, arterial thrombosis or emolism and occlusion of arteriovenous cannulae | Streptokinase creates an active complex which promotes the cleavage of the Arg/Val bond in plasminogen to form the proteolytic enzyme plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardia... | Plasminogen is an inactive molecule that becomes activated to plasmin when the Arg/Val bond is cleaved. Plasmin breaks down fibrin clots created by the blood clotting cascade. Streptokinase forms a highly specific 1:1 enzymatic complex with plasminogen which converts inactive plasminogen molecules into active plasmin. ... | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"B01AD",
"B01A",
"B01",
"B",
"B06AA",
"B06A",
"B06",
"B"
] | [
"Humans and other mammals"
] | [] | [] | Estreptoquinasa | Streptochinasi | Streptococcal fibrinolysin | Streptokinase | Streptokinasum | 3.4.21.7 | CF2R | Coagulation factor II receptor | PAR-1 | PAR1 | Thrombin receptor | TR | CPLA2 | Phospholipase A2 group IVA | PLA2G4 | [
"Kabikinase - Pws 1500000units/vial",
"Kabikinase - Pws 250000 Unit/vial",
"Kabikinase - Pws 750000units/vial",
"Streptase",
"Streptase",
"Streptase",
"Streptase Inj 1500000 Unit/vial",
"Streptase Inj 250000unit/vial",
"Streptase Inj 750000unit/vial"
] | [] | [] | [
"P00747",
"P25116"
] | [
"P47712"
] | [] | [] |
DB00087 | Alemtuzumab | Alemtuzumab is a humanized monoclonal antibody specific to lymphocyte antigens. It is a recombinant DNA-derived humanized monoclonal antibody (Campath-1H) that is directed against the 21-28 kD cell surface glycoprotein, CD52. The Campath-1H antibody is an IgG1 kappa with the human variable framework and constant region... | liquid | LEMTRADA is indicated for the treatment of relapsing forms of multiple sclerosis (MS), including relapsing-remitting disease and active secondary progressive disease, in adults. Because of its safety profile, the use of LEMTRADA should generally be reserved for patients who have had an inadequate response to two or mor... | Alemtuzumab depletes circulating T and B lymphocytes after each treatment course. In clinical trials, the lowest cell counts occurred 1 month after a course of treatment at the time of the first post-treatment blood count. Lymphocyte counts then increased over time: B cell counts usually recovered within 6 months; T ce... | The precise mechanism by which alemtuzumab exerts its therapeutic effects in multiple sclerosis is unknown but is presumed to involve binding to CD52, a cell surface antigen present on T and B lymphocytes, and on natural killer cells, monocytes, and macrophages. Following cell surface binding to T and B lymphocytes, al... | Serum concentrations increased with each consecutive dose within a treatment course, with the highest observed concentrations occurring following the last infusion of a treatment course. The mean maximum concentration was 3014 ng/mL on Day 5 of the first treatment course, and 2276 ng/mL on Day 3 of the second treatment... | null | LEMTRADA induces persistent thyroid disorders [see Warnings and Precautions (5.8)]. Untreated hypothyroidism in pregnant women increases the risk of miscarriage and may have effects on the fetus including mental retardation and dwarfism. In mothers with Graves’ disease, maternal thyroid stimulating hormone receptor ant... | The elimination half-life was approximately 2 weeks and was comparable between courses. The serum concentrations were generally undetectable (<60 ng/mL) within approximately 30 days following each treatment course.[L43397] | null | Alemtuzumab is a large-molecule monoclonal antibody and as such, it is cleared primarily through target-mediated clearance and
through simple non-target specific IgG clearance mechanisms. Alemtuzumab is not excreted renally or eliminated via cytochrome P450 (CYP450) isoenzymes.[L43418] Alemtuzumab is most likely remov... | Alemtuzumab is largely confined to the blood and interstitial space with a central volume of distribution of 14.1 L.[L43397] | Clearance of alemtuzumab ranged from 0.012 – 0.096 l/h depending on the study, dose group, and anti-alemtuzumab antibody status. The inter-subject variability for clearance was large (58 %). Higher clearance values were observed in cycle 1 compared to cycle 2, with the decrease in clearance from cycle 1 to cycle 2 bein... | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"L04AG",
"L04A",
"L04",
"L"
] | [] | [
{
"cost": "2042.18",
"description": "Campath 30 mg/ml vial",
"unit": "ml"
},
{
"cost": "6179.24",
"description": "Campath 30 mg/ml Solution (1 Box Contains Three 1ml Vials)",
"unit": "box"
}
] | [
{
"approved": "1997-08-05",
"country": "Canada",
"expires": "2014-08-05",
"number": "1339198"
}
] | Alemtuzumab | Cambridge pathology 1 antigen | CDW52 | Epididymal secretory protein E5 | HE5 | Human epididymis-specific protein 5 | CD16-I | CD16B | Fc-gamma RIII | Fc-gamma RIII-beta | Fc-gamma RIIIb | FCG3 | FCGR3 | FcR-10 | FcRIII | FcRIIIb | IGFR3 | IgG Fc receptor III-1 | CD16-II | CD16A | CD16a antigen | Fc-gamma... | [
"Campath",
"Campath",
"Lemtrada",
"Lemtrada",
"Lemtrada",
"Mabcampath",
"Mabcampath"
] | [] | [] | [
"P31358",
"O75015",
"P08637",
"P12314",
"P12318",
"P31994",
"P31995"
] | [] | [] | [] |
DB00088 | Alglucerase | Human Beta-glucocerebrosidase or Beta-D-glucosyl-N-acylsphingosine glucohydrolase E.C. 3.2.1.45. 497 residue protein with N-linked carbohydrates, MW=59.3 kD. Alglucerase is prepared by modification of the oligosaccharide chains of human Beta-glucocerebrosidase. The modification alters the sugar residues at the non-redu... | liquid | Alglucerase is indicated for use as a long-term enzyme replacement therapy in patients with Type I Gaucher disease who exhibit signs and symptoms that are severe enough to result in moderate-to-severe anemia, thrombocytopenia, bone disease, or significant hepato- or splenomegaly.[L44266] | Gaucher disease is characterized by a functional deficiency in Beta-glucocerebrosidase enzymatic activity and the resultant accumulation of lipid glucocerebroside in tissue macrophages which become engorged and are termed Gaucher cells. Gaucher cells are typically found in liver, spleen and bone marrow. This can lead t... | Alglucerase catalyzes the hydrolysis of the glycolipid, glucocerebroside, to glucose and ceramide as part of the normal degradation pathway for membrane lipids. | null | null | null | 3.6-10.4 min | null | null | * 49.4 to 282.1 mL/kg | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational",
"withdrawn"
] | [
"A16AB",
"A16A",
"A16",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "380.64",
"description": "Ceredase 80 unit/ml vial",
"unit": "ml"
}
] | [] | Alglucerase | [
"Ceredase"
] | [] | [] | [] | [] | [] | [] |
DB00089 | Capromab pendetide | Capromab is a Murine IgG1 monoclonal 7E11-C5.3 antibody that recognizes prostate specific membrane antigen (PSMA – also known as glutamate carboxypeptidase 2) from prostate cancer cells and normal prostate tissue. When linked to pendetide, capromab is used as a chelating agent for the radionuclide [Indium In-111] durin... | liquid | For diagnosis of prostate cancer and detection of intra-pelvic metastases. | Binds to the prostate-specific membrane antigen, which is a cell surface protein generally overexpressed in prostate tissues and prostate cancers. The radioactive Indium 111, which is covalently attached to the antibody, allows radiodiagnostic detection of PSMA expressing cells and tumors. | Binds selectively to cell-surface prostate-specific membrane antigen (PSMA) expressed on prostate tissues and tumors. | null | Most likely removed by opsonization via the reticuloendothelial system or by human antimurine antibody production | null | null | null | Approximately 10% of the administered radioisotope dose is excreted in the urine during the 72 hours following intravenous infusion. | * 4 ± 2.1 L | * 42 +/- 22 mL/hr | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"V09IB",
"V09I",
"V09",
"V"
] | [
"Humans and other mammals"
] | [
{
"cost": "1584.0",
"description": "Prostascint kit",
"unit": "kit"
}
] | [] | (111In)-Capromab pendetide | Capromab pendetide | Indium (111In) capromab pendetide | Indium 111 Capromab Pendetide | Indium In 111 capromab pendetide | 3.4.17.21 | Cell growth-inhibiting gene 27 protein | FGCP | Folate hydrolase 1 | FOLH | Folylpoly-gamma-glutamate carboxypeptidase | GCPII | Glutamate carboxypeptidase... | [
"ProstaScint Kit for the Preparation of Indium In 111 Capromab Pendetide"
] | [
"ProstaScint"
] | [] | [
"Q04609"
] | [] | [] | [] |
DB00090 | Laronidase | Human recombinant alpha-L-iduronidase, 628 residues (mature form), produced by recombinant DNAtechnology in a Chinese hamster ovary cell line. Laronidase is a glycoprotein with a molecular weight of approximately 83 kD. The predicted amino acid sequence of the recombinant form, as well as the nucleotide sequence that e... | liquid | For the treatment of mucopolysaccharidosis | Laronidase is used to treat mucopolysaccharide storage disorders (specifically mucopolysaccharidosis 1 or Hurlers syndrome) caused by deficiencies of alpha-L-iduronidase. Reduced or absent a-L-iduronidase activity results in the accumulation of the GAG substrates, dermatan sulfate and heparan sulfate, throughout the bo... | Laronidase catalyses the hydrolysis of terminal alpha-L-iduronic acid residues of dermatan sulfate and heparin sulfate. | null | null | null | 1.5-3.6 hrs | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"A16AB",
"A16A",
"A16",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "168.0",
"description": "Aldurazyme 2.9 mg/5 ml vial",
"unit": "ml"
}
] | [] | alpha-L-Idosiduronase | Human Recombinant alpha-L-iduronidase | Laronidasa | Laronidase | Laronidase (genetical recombination) | [
"Aldurazyme",
"Aldurazyme",
"Aldurazyme",
"Aldurazyme",
"Aldurazyme"
] | [] | [] | [] | [] | [] | [] |
DB00091 | Cyclosporine | Cyclosporine is a calcineurin inhibitor known for its immunomodulatory properties that prevent organ transplant rejection and treat various inflammatory and autoimmune conditions. It is isolated from the fungus _Beauveria nivea_.[A174049] Initially manufactured by Sandoz and approved for use by the FDA in 1983, cyclosp... | solid | Cyclosporine is approved for a variety of conditions. Firstly, it is approved for the prophylaxis of organ rejection in allogeneic kidney, liver, and heart transplants. It is also used to prevent bone marrow transplant rejection. For the above indications, cyclosporine can be used in conjunction with azathioprine and c... | Cyclosporine exerts potent immunosuppressive actions on T cells, thereby prolonging survival following organ and bone marrow transplants.[L3734] This drug prevents and controls serious immune-mediated reactions including allograft rejection, graft versus host disease, and inflammatory autoimmune disease.[L3734]
Som... | Cyclosporine is a calcineurin inhibitor that inhibits T cell activation.[A174049,A174088,A189411] Its binding to the receptor cyclophilin-1 inside cells produces a complex known as cyclosporine-cyclophilin. This complex subsequently inhibits calcineurin, which in turn stops the dephosphorylation as well as the activati... | The absorption of cyclosporine occurs mainly in the intestine.[A174049,A189405] Absorption of cyclosporine is highly variable with a peak bioavailability of 30% sometimes occurring 1-8 hours after administration with a second peak observed in certain patients.[A174088,L11097] The absorption of cyclosporine from the GI ... | Cyclosporine is metabolized in the intestine and the liver by CYP450 enzymes, predominantly CYP3A4 with contributions from CYP3A5.[A174049,A189402] The involvement of CYP3A7 is not clearly established.[A189402] Cyclosporine undergoes several metabolic pathways and about 25 different metabolites have been identified. On... | The oral LD50 in rats is 1480 mg/kg and the TDLO in humans is 12 mg/kg.[L11085]
**Overdose information**
In cases of overdose with oral cyclosporine, forced emesis and gastric lavage are recommended 2 hours after ingestion. There are little data available in the literature regarding overdoses with cyclosporine, ... | The half-life of cyclosporine is biphasic and very variable on different conditions but it is reported in general to last 19 hours.[A174088] Prescribing information also states a terminal half-life of approximately 19 hours, but with a range between 10 to 27 hours.[L3002] | About 50% of the administered dose is taken up by erythrocytes while about 34% is bound to lipoproteins.[A174088] Prescribing information for Sandimmune states that 90% is mainly bound to lipoproteins.[L3002] | After sulfate conjugation, cyclosporine remains in the bile where it is broken down to the original compound and then re-absorbed into the circulation. Cyclosporine excretion is primarily biliary with only 3-6%[A189402,L3002] of the dose (including the parent drug and metabolites) excreted in the urine while 90% of th... | The distribution of cyclosporine in the blood consists of 33%-47% in plasma, 4%-9% in the lymphocytes, 5%-12% in the granulocytes, and 41%-58% in the erythrocytes.[L3002] The reported volume of distribution of cyclosporine ranges from 4-8 L/kg. It concentrates mainly in leucocyte-rich tissues as well as tissues that ... | Cyclosporin shows a linear clearance profile that ranges from 0.38 to 3 Lxh/kg[A174088], however, there is substantial inter- patient variability.[A189402] A 250 mg dose of cyclosporine in the oral soft gelatin capsule of a lipid micro-emulsion formulation shows an approximate clearance of 22.5 L/h.[A189453] | Organic compounds | Organic acids and derivatives | Peptidomimetics | Peptoid-peptide hybrids | [
"approved",
"investigational",
"vet_approved"
] | [
"L04AD",
"L04A",
"L04",
"L",
"S01XA",
"S01X",
"S01",
"S"
] | [
"Humans and other mammals"
] | [
{
"cost": "1.32",
"description": "Gengraf 25 mg capsule",
"unit": "capsule"
},
{
"cost": "1.38",
"description": "Cyclosporine 25 mg softgel",
"unit": "softgel capsule"
},
{
"cost": "1.53",
"description": "Neoral 25 mg gelatin capsule",
"unit": "capsule"
},
{
"cost... | [
{
"approved": "1999-11-16",
"country": "United States",
"expires": "2014-09-26",
"number": "5985321"
},
{
"approved": "1989-06-13",
"country": "United States",
"expires": "2009-08-02",
"number": "4839342"
},
{
"approved": "2003-04-15",
"country": "Canada",
"expire... | Ciclosporin | Ciclosporina | Ciclosporine | Ciclosporinum | CsA | CyA | Cyclosporin | Cyclosporin A | Cyclosporine | Calcium signal-modulating cyclophilin ligand | CAML | GET2 | 3.1.3.16 | Calcineurin A alpha | Calmodulin-dependent calcineurin A subunit alpha isoform | CALNA | CAM-PRP catalytic subunit | CNA | CNA alph... | [
"Apo-cyclosporine Oral Solution",
"Aqua-stasis",
"Cequa",
"Cequa",
"Cequa",
"Cyclo-derm",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
"Cyclosporine",
... | [
"Sangcya",
"Verkazia"
] | [] | [
"P49069",
"Q08209",
"Q96LZ3",
"P62937",
"P30405"
] | [
"P33261",
"P10635",
"P20815",
"P08684"
] | [] | [
"P08183",
"O95342",
"Q12908",
"Q14973",
"Q4U2R8",
"Q5T3U5",
"Q92887",
"Q9UNQ0",
"Q9Y6L6",
"Q9NPD5"
] |
DB00092 | Alefacept | Immunosuppressive dimeric fusion protein that consists of the extracellular CD2-binding portion of the human leukocyte function antigen-3 (LFA-3) linked to the Fc (hinge, CH2 and CH3 domains) portion of human IgG1. Produced by CHO cells, mW is 91.4 kD. | liquid | As an immunosuppressive drug, Alefacept can be used for treatment of moderate to severe chronic plaque psoriasis | Interferes with lymphocyte activation by specifically binding to the lymphocyte antigen, CD2, and inhibiting LFA-3/CD2 interaction. Activation of T lymphocytes involving the interaction between LFA-3 on antigen-presenting cells and CD2 on T lymphocytes plays a role in the pathophysiology of chronic plaque psoriasis. Al... | Inhibits T-lymphocyte activation and production by binding to the CD2 lymphocyte antigen. | Bioavailability after IM administration is 63%. | null | While it has been found to cross the placenta in monkeys, it is not yet known if it also diffuses into breast milk. | ~270 hours | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational",
"withdrawn"
] | [
"L04AA",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "1190.4",
"description": "Amevive 15 mg vial",
"unit": "vial"
}
] | [] | Alefacept | Erythrocyte receptor | LFA-2 | LFA-3 receptor | Rosette receptor | SRBC | T-cell surface antigen T11/Leu-5 | CD16-II | CD16A | CD16a antigen | Fc-gamma RIII | Fc-gamma RIII-alpha | Fc-gamma RIIIa | FCG3 | FcgammaRIIIA | FCGR3 | FcR-10 | FcRIII | FcRIIIa | IGFR3 | IgG Fc receptor III-2 | IgG Fc receptor III-... | [
"Amevive",
"Amevive"
] | [] | [] | [
"P06729",
"P08637",
"O75015"
] | [] | [] | [] |
DB00093 | Felypressin | A synthetic nonapeptide comprising cysteinyl, phenylalanyl, phenylalanyl, glutaminyl, asparaginyl, cysteinyl, prolyl, lysyl, and glycinamide residues in sequence, with a disulfide bridge joining the two cysteine residues. Its antidiuretic effects are less than those of vasopressin. It is a non-catecholamine vasoconstri... | solid | For use as an alternative to adrenaline as a localising agent, provided that local ischaemia is not essential. | Felypressin is a synthetic analog of lypressin or vasopressin with a greater vasoconstrictor activity than antidiuretic action. It is used primarily as a hemostatic. | Felypressin binds to the vasopressin receptor V1a. This causes contraction of the smooth muscle in the vascular bed, especially capillaries, small arterioles and venules. | null | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"experimental"
] | [] | [
"Humans and other mammals"
] | [] | [] | 2-(L-phenylalanine)-8-L-lysinevasopressin | Felipresina | Felypressin | Felypressine | Felypressinum | PLV-2 | Antidiuretic hormone receptor 1a | AVPR V1a | AVPR1 | V1aR | Vascular/hepatic-type arginine vasopressin receptor | [] | [
"Colupressine",
"Octapressin"
] | [] | [
"P37288"
] | [] | [] | [] |
DB00094 | Urofollitropin | Urofollitropin is a urinary-derived follicle-stimulating hormone (FSH) that is extracted and purified from human urine samples. It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit ... | liquid | For treatment of female infertility | Used for the treatment of female infertility, urofollitropin or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of urofollitropin is the primary hormone responsible for follicular recruitment and development. | FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related surviva... | 74% | null | null | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | null | Via liver and kidneys | Time to peak in plasma:
IM: 17 hours (single dose), 11 hours (multiple doses)
SubQ: 21 hours (single dose), 10 hours (multiple doses) | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"vet_approved"
] | [
"G03GA",
"G03G",
"G03",
"G"
] | [
"Humans and other mammals"
] | [
{
"cost": "93.85",
"description": "Bravelle 75 unit vial",
"unit": "vial"
},
{
"cost": "103.85",
"description": "Fertinex 75 unit Solution",
"unit": "vial"
}
] | [
{
"approved": "1998-06-16",
"country": "United States",
"expires": "2015-06-16",
"number": "5767067"
}
] | Follitropin human | Urofollitrophin | Urofollitropin | Follitropin receptor | FSH-R | LGR1 | [
"Bravelle",
"Fertinorm Hp 150 - Pws Diluent Im Sc",
"Fertinorm Hp 75 - Pws Diluent Im Sc",
"Metrodin 75 I.U."
] | [
"Fertinex",
"Metrodin"
] | [
"Fertinorm Hp 75 - Pws Diluent Im Sc",
"Fertinorm Hp 150 - Pws Diluent Im Sc"
] | [
"P23945"
] | [] | [] | [] |
DB00095 | Efalizumab | Humanized IgG1 kappa isotype monoclonal antibody that binds to human CD11a. Efalizumab has a molecular weight of approximately 150 kilodaltons and is produced in a Chinese hamster ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin. The FDA approved efalizumab in 2003. It wa... | liquid | For the treatment of adult patients with moderate to severe chronic plaque psoriasis, who are candidates for phototherapy or systemic therapy. | Lymphocyte activation and trafficking to skin play a role in the pathophysiology of chronic plaque psoriasis. In psoriatic skin, ICAM-1 cell surface expression is upregulated on endothelium and keratinocytes. Raptiva inhibits the binding of LFA-1 to the intercellular adhesion molecule-1 (ICAM-1), thereby inhibiting the... | Efalizumab binds to CD11a, a subunit of leukocyte function antigen-1 (LFA-1), which is expressed on all leukocytes. As a result efalizumab decreases cell surface expression of CD11a. | Average efalizumab bioavailability following subcutaneous administration was estimated at 30 to 50%. | null | null | 5 days | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational",
"withdrawn"
] | [
"L04AG",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [] | [] | anti-CD11a | antiCD11 alpha | Efalizumab | CD11 antigen-like family member C | CD11C | Leu M5 | Leukocyte adhesion glycoprotein p150,95 alpha chain | Leukocyte adhesion receptor p150,95 | CD11 antigen-like family member A | CD11A | Leukocyte adhesion glycoprotein LFA-1 alpha chain | Leukocyte function-associated molecu... | [
"Raptiva",
"Raptiva",
"Raptiva",
"Raptiva"
] | [
"Xanelim"
] | [] | [
"P20702",
"P20701"
] | [] | [] | [] |
DB00097 | Choriogonadotropin alfa | Recombinant human chorionic gonadotropin with 2 subunits, alpha = 92 residues, beta = 145 residues, each with N-and O-linked carbohydrate moieties linked to ASN-52 and ASN-78 (on alpha subunit) and ASN-13, ASN-30, SER-121, SER-127, SER-132 and SER-138 (on beta subunit). The primary structure of the alpha-chain of r-hCG... | solid | For the treatment of female infertility | Choriogonadotropin alfa is used to treat female infertility, Choriogonadotropin alfa stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Ovidrel is an analogue of Luteinizing Hormone (LH) and binds to the LH/hCG receptor of the granulosa a... | Choriogonadotropin alfa binds to the Follicle stimulating hormone receptor which results in ovulation in the absence of sufficient endogenous Luteinizing hormone. | The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%. | null | null | The mean terminal half-life is about 29 ± 6 hours (initial half-life is 4.5 ± 0.5 hours). | null | One-tenth of the dose is excreted in the urine. | * 5.9 ± 1.0 L | * 0.29 +/- 0.04 L/h [healthy down-regulated females] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"G03GA",
"G03G",
"G03",
"G"
] | [
"Humans and other mammals"
] | [
{
"cost": "57.23",
"description": "Pregnyl 10000 unit vial",
"unit": "vial"
},
{
"cost": "60.7",
"description": "Pregnyl 10000 unit Solution",
"unit": "vial"
},
{
"cost": "93.22",
"description": "Ovidrel 250 mcg/0.5ml Injectable 0.5ml Syringe",
"unit": "syringe"
},
{
... | [
{
"approved": "1998-06-16",
"country": "United States",
"expires": "2015-06-16",
"number": "5767251"
},
{
"approved": "2004-03-16",
"country": "United States",
"expires": "2021-03-16",
"number": "6706681"
}
] | Choriogonadotropin alfa | Choriogonadotropin alpha | Chorionic gonadotropin (recombinant) | Follitropin receptor | FSH-R | LGR1 | LCGR | LGR2 | LH/CG-R | LHR | LHRHR | LSH-R | Luteinizing hormone receptor | [
"Chorionic Gonadotropin",
"Chorionic Gonadotropin",
"Chorionic Gonadotropin",
"Ovidrel",
"Ovidrel",
"Ovidrel",
"Ovitrelle",
"Ovitrelle",
"Pregnyl",
"Pregnyl",
"Pregnyl",
"Pregnyl",
"Pregnyl"
] | [
"Profasi"
] | [] | [
"P23945",
"P22888"
] | [] | [] | [] |
DB00098 | Antithymocyte immunoglobulin (rabbit) | Rabbit anti-thymocyte globulin. Thymoglobulin is a polyclonal antibody that suppresses certain types of immune cells responsible for acute organ rejection in transplant patients. Thymoglobulin is a mixture of antibodies intended to bind to various cell surface antigens. The most common mode of action of Thymoglobulin i... | liquid | For prevention of renal transplant rejection | Antithymocyte Globulin (ATG) is a concentrated anti-human T-lymphocyte immunoglobulin preparation derived from rabbits after immunization with a T-lympoblast cell line. ATG is an immunosuppressive product for the prevention and treatment of acute rejection following organ transplantation. ATG reduces the host immune re... | Binds to multiple, T-cell specific antigens leading to T-lymphocyte cell death via complement mediated cytotoxicity or apoptosis. | T-cell depletion usually observed within 1 day after initiating therapy. Average 21.5 and 87 mcg/mL 4–8 hours post-infusion after first and last IV doses, respectively, when given for 7–11 days. | Most likely removed by opsonization via the reticuloendothelial system when bound to T lymphocytes, or by human antimurine antibody production. | Not known whether ATG (rabbit) distributes into human milk; however, other immunoglobulins are distributed into human milk. | 2-3 days, may increase after multiple doses administration | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L04AA",
"L04A",
"L04",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "636.48",
"description": "Thymoglobulin 25 mg vial",
"unit": "vial"
}
] | [] | Anti-human thymocyte immunoglobulin, rabbit | Anti-T-lymphocyte immune globulin, rabbit | Anti-thymocyte globulin (rabbit) | Anti-thymocyte globulin rabbit | Antithymocyte immunoglobulin | Lapine T-lymphocyte immune globulin | Rabbit anti-human thymocyte globulin | Rabbit anti-human thymocyte globulin (rATG) | Rabbit a... | [
"Thymoglobulin",
"Thymoglobulin"
] | [
"ATG-Fresenius",
"ATG-Fresenius S"
] | [] | [
"Q95460",
"P20701",
"P42081",
"P31994",
"P01730",
"P05556",
"P06756",
"P05106",
"P06126"
] | [] | [] | [] |
DB00099 | Filgrastim | Filgrastim is a short-acting recombinant, non-pegylated human granulocyte colony-stimulating factor (G-CSF) analog produced by recombinant DNA technology. It has an amino acid sequence identical to endogenous G-CSF, but it is non-glycosylated unlike the endogenous G-CSF and has an N-terminal methionine added in the seq... | liquid | Filgrastim is indicated to decrease the incidence of infection‚ as manifested by febrile neutropenia‚ in patients with nonmyeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a significant incidence of severe neutropenia with fever.[L40714]
Filgrastim is indicated for reducing the time t... | Filgrastim is used to reduce the incidence, severity and duration of neutropenia and febrile neutropenia in patients undergoing cytotoxic chemotherapy. In clinical trials in patients, filgrastim reduced the duration of febrile neutropenia, antibiotic use, and hospitalization after induction chemotherapy for acute myelo... | Neutrophils are critical granulocytes involved in the acute inflammatory response and host defences against bacterial infections.[A245873] They also contribute to long-term adaptive immunity by promoting immediate host immune response and attracting other cells, such as macrophages and dendritic cells. As neutrophils p... | Filgrastim exhibits nonlinear pharmacokinetics. Subcutaneous administration of 3.45 mcg/kg and 11.5 mcg/kg of filgrastim resulted in maximum serum concentrations of 4 and 49 ng/mL‚ respectively‚ within 2 to 8 hours.
Continuous 24-hour intravenous infusions of 20 mcg/kg over an 11 to 20-day period produced steady-st... | Like other G-CSF compounds, filgrastim is cleared from plasma via neutrophil-mediated clearance involving internalization via G-CSF receptors and degradation within the neutrophil. Filgrastim is also subject to extracellular proteolytic degradation by neutrophil elastase: this enzyme rapidly cleaves filgrastim and rend... | The oral LD<sub>50</sub> in mouse and rat was >3 mg/kg. The intravenous LD<sub>50</sub> in rat was also >3 mg/kg.[L40734]
There is limited information regarding filgrastim overdose. The maximum tolerated dose of filgrastim has not been determined. In clinical trials of patients with cancer receiving myelosuppressive... | After intravenous administration, the elimination half-life of filgrastim was approximately 3.5 hours in both normal subjects and patients with cancer. Single parenteral doses or daily intravenous doses‚ over a 14-day period‚ resulted in comparable half-lives. The half-lives were similar for intravenous administration ... | There is limited information available. | There is limited information available; however, filgrastim is subject to renal elimination.[A245878] | After intravenous administration, the volume of distribution averaged 150 mL/kg.[L40714] There is no evidence of drug accumulation.[L40719] | Clearance rates of filgrastim were approximately 0.5 to 0.7 mL/minute/kg after intravenous administration.[L40714] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AA",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "286.04",
"description": "Neupogen 300 mcg/ml vial",
"unit": "vial"
},
{
"cost": "437.94",
"description": "Neupogen 480 mcg/1.6 ml vial",
"unit": "ml"
},
{
"cost": "3138.1",
"description": "Neupogen 300 mcg/0.5ml Solution 1 Box Contains Ten 0.5ml Syringes",
"uni... | [
{
"approved": "2007-07-31",
"country": "Canada",
"expires": "2024-07-31",
"number": "1341537"
},
{
"approved": "1997-07-29",
"country": "Canada",
"expires": "2014-07-29",
"number": "1339071"
}
] | Filgrastim | Filgrastim-aafi | Filgrastim-sndz | G-CSF | Granulocyte Colony Stimulating Factor | Tbo-filgrastim | G-CSF receptor | G-CSF-R | GCSFR | 3.4.21.37 | Bone marrow serine protease | ELA2 | Elastase-2 | HLE | Human leukocyte elastase | Medullasin | PMN elastase | [
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Accofil",
"Acc... | [
"Biocilin",
"Biofigran",
"Biofilgran",
"Endufil",
"Filatil",
"Filgen",
"Gran",
"Granulokine",
"Grimatin",
"Inmunef",
"Jiexin",
"Leucogen",
"Leucostim",
"Macroleuco",
"Neukine",
"Neutromax",
"Neutroval",
"Recombicyte",
"SciLocyte",
"Tevagastrim",
"White-C",
"Zarzio"
] | [] | [
"Q99062"
] | [
"P08246"
] | [] | [] |
DB00100 | Coagulation Factor IX (Recombinant) | Recombinant Coagulation Factor IX is a purified Factor IX glycoprotein produced by recombinant DNA technology. It has a primary amino acid sequence that is identical to the Ala148 allelic form of human factor IX, and has structural and functional characteristics similar to those of endogenous factor IX. It is not deriv... | liquid | For treatment of hemophilia (Christmas disease). | Binds vitamin K and factor VIIIa. Cleaves the Arg-Ile bond in factor X to form active factor Xa. Plays a key role in blood coagulation and clotting. Injections of factor IX are used to treat hemophilia B, which is sometimes called Christmas disease. AlphaNine is injected to increase plasma levels of Factor IX and can t... | Coagulation Factor IX is an important protein in the process of hemostasis and normal blood clotting as it plays a key role within the coagulation cascade. It is located within the blood plasma as a zymogen, an antecedent to enzymatic function, in its inactivated state. Factor IX is dependent on the presence of Vitamin... | null | null | null | 18.8 ± 5.4 hours | null | null | null | 8.62 ± 1.7 | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [] | [
"Humans and other mammals"
] | [
{
"cost": "1.0",
"description": "Benefix 1000 unit vial",
"unit": "vial"
},
{
"cost": "1.0",
"description": "Benefix 250 unit vial",
"unit": "vial"
},
{
"cost": "1.0",
"description": "Benefix 500 unit vial",
"unit": "vial"
},
{
"cost": "1.12",
"description": "... | [] | Coagulation factor IX (recombinant) | Coagulation factor IX recombinant human | Coagulation factor IX, recombinant | Factor IX (Recombinant) | nonacog alfa | nonacog gamma | Recombinant factor IX | 3.4.21.6 | Stuart factor | Stuart-Prower factor | 3.4.21.27 | FXI | Plasma thromboplastin antecedent | PTA | 3.4.21.21 | P... | [
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"Benefix",
"Benefix",
"Benefix",
"Benefix",
"Benefix",
"Benefix",
"Benefix - (250iu)",
"Benefix - (500iu)",... | [] | [
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"BeneFIX",
"Benefix - (250iu)",
"Benefix - (500iu)",
"Benefix -(1000iu)"
] | [
"P00742",
"P03951",
"P08709",
"P00451",
"P00734",
"Q07954",
"P38435"
] | [] | [] | [] |
DB00102 | Becaplermin | Becaplermin is produced by recombinant DNA technology by insertion of the gene for the B chain of platelet derived growth factor (PDGF) into the yeast, Saccharomyces cerevisiae. Becaplermin has a molecular weight of approximately 25 KD and is a homodimer composed of two identical polypeptide chains that are bound toget... | liquid | For topical treatment of skin ulcers (from diabetes) | Used for the topical treatment of skin ulcers, Regranex has a biological activity similar to that of endogenous platelet-derived growth factor, which includes promoting the chemotactic recruitment and proliferation of cells involved in wound repair and enhancing the formation of granulation tissue. | Binds to the beta platelet-derived growth factor (PDGF) receptor, a tyrosine kinase receptor. PDGF is known to exist as a dimer, and activates its signaling pathway by a ligand induced receptor dimerization and autophosphorylation. PDGF receptors also contain many auto-phosphorylation sites, which serve to mediate bind... | very little systemic absorption. 15% of patients experienced complete healing within 8 weeks, while for 25% of patients, it was at 10 weeks. | null | null | null | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"D03AX",
"D03A",
"D03",
"D",
"A01AD",
"A01A",
"A01",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "46.4",
"description": "Regranex 0.01% gel",
"unit": "g"
},
{
"cost": "723.82",
"description": "Regranex 0.01% Gel 15 gm Tube",
"unit": "tube"
}
] | [
{
"approved": "1999-12-07",
"country": "Canada",
"expires": "2015-12-15",
"number": "1340846"
}
] | Becaplermin | PDGF-2 | PDGF-BB | PDGFB | Platelet-derived growth factor BB, recombinant | Platelet-derived growth factor beta polypeptide | Recombinant platelet-derived growth factor BB | rhPDGF-BB | rPDGF-BB | SH-POLYPEPTIDE-59 | 2.7.10.1 | Beta platelet-derived growth factor receptor | Beta-type platelet-derived grow... | [
"Regranex",
"Regranex",
"Regranex",
"Regranex",
"Regranex (becaplermin) 0.01%"
] | [] | [] | [
"P09619",
"P16234",
"P01023"
] | [] | [] | [] |
DB00103 | Agalsidase beta | Agalsidase beta is a recombinant human α-galactosidase A similar to [agalsidase alfa]. While patients generally do not experience a clinically significant difference in outcomes between the two drugs, some patients may experience greater benefit with agalsidase beta.[A220228,A220233] Use of agalsidase beta has decrease... | liquid | Agalsidase beta is indicated in the treatment of Fabry disease.[L16383] | Agalsidase beta is a recombinant human α-galactosidase A used as enzyme replacement therapy in the treatment of Fabry disease.[L16398] It has a long duration of action and a wide therapeutic index.[L16383] Patients should be counselled regarding the risk of infusion related reactions and hypersensitivity.[L16383] | α-galactosidase A is uptaken by cells via the mannose 6 phosphate receptor.[A220323] Agalsidase beta hydrolyzes globotriaosylceramide and other glycosphingolipids that would normally be hydrolyzed by endogenous α-galactosidase A.[L16383] Preventing the accumulation of glycosphingolipids prevents or reduces the severity... | A 1 mg/kg dose of agalsidase beta with a mean infusion length of 115 minutes reaches a C<sub>max</sub> 5.0 ± 1.1 µg/mL with an AUC of 496 ± 137 µg\*min/mL.[L16383] | Data regarding the metabolism of agalsidase beta is not readily available.[L16383] However, protein drugs are expected to be degraded by proteases and other catalytic enzymes to smaller peptides and amino acids.[A182009] | Data regarding overdoses of agalsidase beta are not readily available.[L16383] Patients experiencing an overdose of agalsidase beta may experience an increased incidence and severity of adverse effects.[L16383] Overdose can be managed through the use of symptomatic and supportive measures. | agalsidase beta has a half like of 67 ± 12 min for a 1 mg/kg dose with a mean infusion length of 115 minutes.[L16383] | Data regarding the protein binding of agalsidase beta is not readily available.[L16383] | After nonspecific proteolysis, the amino acids from protein drugs are reused for protein synthesis or further broken down and eliminated by the kidneys.[A182009] | A 1 mg/kg dose of agalsidase beta with a mean infusion length of 115 minutes has a V<sub>SS</sub> of 112 ± 13 mL/kg.[L16383] | A 1 mg/kg dose of agalsidase beta with a mean infusion length of 115 minutes has a clearance of 2.1 ± 0.7 mL/min/kg.[L16383] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"A16AB",
"A16A",
"A16",
"A"
] | [
"Humans and other mammals"
] | [
{
"cost": "771.6",
"description": "Fabrazyme 5 mg vial",
"unit": "vial"
},
{
"cost": "5403.6",
"description": "Fabrazyme 35 mg vial",
"unit": "vial"
}
] | [
{
"approved": "2007-06-26",
"country": "Canada",
"expires": "2017-09-12",
"number": "2265464"
}
] | Agalsidasa beta | Agalsidase beta | Agalsidase beta (genetical recombination) | 46 kDa mannose 6-phosphate receptor | CD Man-6-P receptor | CD-MPR | MPR 46 | MPR46 | MPRD | [
"Fabrazyme",
"Fabrazyme",
"Fabrazyme",
"Fabrazyme",
"Fabrazyme",
"Fabrazyme",
"Fabrazyme",
"Fabrazyme",
"Fabrazyme",
"Fabrazyme"
] | [] | [] | [] | [] | [] | [
"P20645"
] |
DB00104 | Octreotide | Acromegaly is a disorder caused by excess growth hormone (GH), increasing the growth of body tissues and causing metabolic dysfunction.[L14501] In most cases, it results from an anterior pituitary growth hormone-releasing tumor. Typically, the feet, hands, and face grow abnormally large; organomegaly and insulin resist... | solid | Octreotide by injection is used for the treatment of acromegaly and the reduction of flushing and diarrhea symptoms related to carcinoid tumors and/or vasoactive intestinal peptide (VIPoma) tumors.[L14513] The delayed-release oral formulation is used for the long-term treatment of acromegaly in patients who tolerate an... | Octreotide mimics the naturally occurring hormone known as somatostatin. Like somatostatin, it demonstrates activity against growth hormone and glucagon, treating the disordered tissue growth and insulin regulation in patients with acromegaly.[L14501,L14513] In addition, octreotide relieves the flushing and diarrhea as... | Octreotide binds to somatostatin receptors coupled to phospholipase C through G proteins and leads to smooth muscle contraction in the blood vessels.[L14519] Downstream effects that stimulate phospholipase C, the production of 1, 4,5-inositol triphosphate, and action on the L-type calcium channels lead to the inhibitio... | After a subcutaneous dose, octreotide is absorbed completely upon administration.[A214721,L14513] After the administration of an oral delayed-release capsule, peak concentrations were found to be 33% lower than after subcutaneous administration.[L14528] The Cmax was attained at 1.67–2.5 hours after oral administration ... | Octreotide has been reported to be heavily metabolized in the liver.[A214721] | There is limited information regarding cases of octreotide overdose aside from case reports of an overdose with injectable octreotide. The dose ranged from 2.4 mg/day to 6 mg/day administered by continuous infusion or subcutaneous administration of 1.5 mg three times daily. Effects of an overdose with octreotide may in... | After a subcutaneous dose, the plasma half-life is estimated to be 0.2 hours. The average elimination half-lives for subcutaneous and oral administration ranged from 2.3 - 2.7 hours and did not differ significantly.[L14528] One pharmacokinetic study revealed a plasma half-life ranging from 72-113 minutes.[A214721] | Approximately 65% of the dose is bound in the plasma to lipoproteins and albumin.[L14513,L14528] | About 32% of an oral octreotide dose is excreted into the urine [L14528] and 30-40% is excreted by the liver into the feces.[A214721]. About 11% of the unchanged parent drug is found in the urine, and 2% of the unchanged parent drug can be recovered in the feces.[A214721] | In a pharmacokinetic study, the volume of distribution was 13.6 L in healthy volunteers.[L14528] One pharmacokinetic study revealed a volume of distribution ranging from 18.1-30.4L after intravenous administration in healthy volunteers.[A214721] | The total body clearance of octreotide is 7-10 L/h.[L14528] One pharmacokinetic study revealed a total body clearance of 11.4 L/h.[A214721] | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved",
"investigational"
] | [
"H01CB",
"H01C",
"H01",
"H"
] | [
"Humans and other mammals"
] | [
{
"cost": "3.6",
"description": "Octreotide acet 50 mcg/ml vial",
"unit": "ml"
},
{
"cost": "11.92",
"description": "Sandostatin 0.05 mg/ml ampul",
"unit": "ml"
},
{
"cost": "14.4",
"description": "Octreotide acet 200 mcg/ml vial",
"unit": "ml"
},
{
"cost": "15.36... | [
{
"approved": "1996-07-23",
"country": "United States",
"expires": "2013-07-23",
"number": "5538739"
},
{
"approved": "1994-04-12",
"country": "Canada",
"expires": "2011-04-12",
"number": "1328402"
},
{
"approved": "1999-07-13",
"country": "United States",
"expire... | Octreotida | Octreotide | Octreotidum | Octrotide | SRIF-1 | SS-2-R | SS2-R | SS2R | SST2 | 1.11.2.2 | MPO | 1,4-cineole 2-exo-monooxygenase | 1,8-cineole 2-exo-monooxygenase | 1.14.14.1 | Albendazole monooxygenase (sulfoxide-forming) | Albendazole sulfoxidase | Cholesterol 25-hydroxylase | CYP3A3 | CYPIIIA3 | CYPIIIA4... | [
"BYNFEZIA Pen",
"Mycapssa",
"Mycapssa",
"Mycapssa",
"Ocphyl",
"Ocphyl",
"Ocphyl",
"Octreotide",
"Octreotide",
"Octreotide",
"Octreotide",
"Octreotide",
"Octreotide acetate",
"Octreotide acetate",
"Octreotide acetate",
"Octreotide acetate",
"Octreotide acetate",
"Octreotide acetate"... | [
"Sandostatin LAR"
] | [] | [
"P30874"
] | [
"P05164",
"P08684"
] | [
"P02768"
] | [
"P08183",
"Q92887"
] |
DB00105 | Interferon alfa-2b | Interferon alpha 2b (human leukocyte clone hif-sn 206 protein moiety reduced). A type I interferon consisting of 165 amino acid residues with arginine in position 23. This protein is produced by recombinant DNA technology and resembles interferon secreted by leukocytes. It is used extensively as an antiviral or antineo... | liquid | For the treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma. | Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also indu... | Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which upon dimerization activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers an... | Absorption is high (greater than 80%) when administered intramuscularly or subcutaneously. | null | There is limited experience with overdosage. Postmarketing surveillance includes reports of patients receiving a single dose as great as 10 times the recommended dose. In general, the primary effects of an overdose are consistent with the effects seen with therapeutic doses of interferon alfa-2b. Hepatic enzyme abnorma... | The elimination half-life following both intramuscular and subcutaneous injections was approximately 2 to 3 hours. The elimination half-life was approximately 2 hours following intravenous injection. | null | null | null | null | Organic Compounds | Organic Acids | Carboxylic Acids and Derivatives | Amino Acids, Peptides, and Analogues | [
"approved"
] | [
"L03AB",
"L03A",
"L03",
"L"
] | [
"Humans and other mammals"
] | [
{
"cost": "394.21",
"description": "Intron a 3 million unit/ml pen",
"unit": "pen"
},
{
"cost": "657.06",
"description": "Intron a 5 million unit/ml pen",
"unit": "pen"
},
{
"cost": "683.34",
"description": "Intron-A 5000000 unit/0.2ml Kit Box",
"unit": "box"
},
{
... | [
{
"approved": "2008-02-19",
"country": "Canada",
"expires": "2025-02-19",
"number": "1341567"
},
{
"approved": "1999-06-15",
"country": "Canada",
"expires": "2015-10-10",
"number": "2201749"
}
] | Interferon alfa-2b | Interferon alfa-2b (recombinant) | Interferon alfa-2b, recombinant | Interferon alpha-2B | Interferon α-2b | Intron (Interferon α2b) | Intron A | Intron A (Interferon α2b) | r-INF-alpha | rIFN-alpha-2b | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon ... | [
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A",
"Intron A - Kit (pws+diluent) 3000000iu/vial",
"Intron A - Kit... | [
"Locteron"
] | [
"Intron A",
"Intron A - Kit (pws+diluent) 3000000iu/vial",
"Intron A - Kit (pws+diluent) 5000000iu/vial",
"Rebetron Ready To Use Solution (albumin(human)free) (6000000 Iu/ml and 200mg Capsules)",
"Rebetron Solution (albumin (human) Free) (18 Miu Multi-dose Pen / 200mg Capsules)",
"Intron A"
] | [
"P48551",
"P01563",
"P17181"
] | [
"P05177"
] | [] | [] |
DB00106 | Abarelix | Synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market. | solid | For palliative treatment of advanced prostate cancer. | Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis. | Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. | Following IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection. | <i>In vitro</i> hepatocyte (rat, monkey, human) studies and <i>in vivo</i> studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either <i>in vitro</i> or <i>in vivo</i>. There is n... | The maximum tolerated dose of abarelix has not been determined. The maximum dose used in clinical studies was 150 mg. There have been no reports of accidental overdose with abarelix. | 13.2 ± 3.2 days | 96-99% | null | null | null | Organic compounds | Organic acids and derivatives | Carboxylic acids and derivatives | Amino acids, peptides, and analogues | [
"approved",
"investigational",
"withdrawn"
] | [
"L02BX",
"L02B",
"L02",
"L"
] | [
"Humans and other mammals"
] | [] | [
{
"approved": "2002-07-23",
"country": "United States",
"expires": "2015-06-07",
"number": "6423686"
},
{
"approved": "2001-01-30",
"country": "United States",
"expires": "2016-12-11",
"number": "6180608"
},
{
"approved": "1999-10-19",
"country": "United States",
... | Abarelix | GnRH receptor | GnRH-R | GRHR | [] | [
"Plenaxis"
] | [] | [
"P30968"
] | [] | [] | [] |
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