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PMC11181725 | core_pubmed_pmc | Safety and Pharmacokinetics of Intravesical Chitosan/Interleukin-12 Immunotherapy in Murine Bladders | Safety and Pharmacokinetics of Intravesical Chitosan/Interleukin-12 Immunotherapy in Murine Bladders Abstract Abstract BACKGROUND: Intravesical administration of interleukin 12 (IL-12) co-formulated with the biopolymer, chitosan (CS/IL-12), has demonstrated remarkable antitumor activity against preclinical models of bl... |
PMC12263804 | core_pubmed_pmc | Rifampicin Exposure in Tuberculosis Patients with Comorbidities in Sub-Saharan Africa: Prioritising Populations for Treatment—A Systematic Review and Meta-analysis | Rifampicin Exposure in Tuberculosis Patients with Comorbidities in Sub-Saharan Africa: Prioritising Populations for Treatment—A Systematic Review and Meta-analysis Abstract Abstract Background and Objectives Emerging evidence suggests that comorbidities like human immunodeficiency virus (HIV) infection, diabetes mellit... |
PMC5794840 | core_pubmed_pmc | Effects of Metformin and Furosemide on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Implications for Their Use as Probe Drugs in a Transporter Cocktail | Effects of Metformin and Furosemide on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Implications for Their Use as Probe Drugs in a Transporter Cocktail Abstract Abstract Background In a recently described probe drug cocktail for clinically relevant drug transporters containing digoxin, furosemide, metformin and... |
PMC7919190 | core_pubmed_pmc | Population Pharmacokinetics of Phosphocreatine and Its Metabolite Creatine in Children With Myocarditis | Population Pharmacokinetics of Phosphocreatine and Its Metabolite Creatine in Children With Myocarditis Abstract Objective: This study aimed to develop a parent-metabolite joint population pharmacokinetic model to characterize the pharmacokinetic (PK) profile for phosphocreatine (PCr) and its metabolite creatine (Cr) i... |
PMC11641171 | core_pubmed_pmc | In Silico Hydrolysis of Lupin ( Lupinus angustifolius L.) Conglutins with Plant Proteases Releases Antihypertensive and Antidiabetic Peptides That Are Bioavailable, Non-Toxic, and Gastrointestinal Digestion Stable | In Silico Hydrolysis of Lupin ( Lupinus angustifolius L.) Conglutins with Plant Proteases Releases Antihypertensive and Antidiabetic Peptides That Are Bioavailable, Non-Toxic, and Gastrointestinal Digestion Stable Abstract Abstract Lupin ( Lupinus angustifolius L.) proteins are potential sources of bioactive peptides (... |
PMC12163317 | core_pubmed_pmc | The food effect on the pharmacokinetics of TQB3616 capsule in Chinse healthy subjects: a randomized, open-label, single-center, two-period, two-sequence crossover phase I clinical trial | The food effect on the pharmacokinetics of TQB3616 capsule in Chinse healthy subjects: a randomized, open-label, single-center, two-period, two-sequence crossover phase I clinical trial Abstract Purpose The purpose of this study was to evaluate the food effect on the pharmacokinetics of TQB3616 capsule in Chinse health... |
PMC6105922 | core_pubmed_pmc | Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study | Verinurad combined with febuxostat in Japanese adults with gout or asymptomatic hyperuricaemia: a phase 2a, open-label study Abstract Abstract Objectives Verinurad (RDEA3170) is a high-affinity inhibitor of the URAT1 transporter in clinical development for treating gout and asymptomatic hyperuricaemia. The aim of this ... |
PMC6968529 | core_pubmed_pmc | Effects of Fuzheng Huayu recipe on entecavir pharmacokinetics in normal and dimethylnitrosamine-induced hepatic fibrosis rats | Effects of Fuzheng Huayu recipe on entecavir pharmacokinetics in normal and dimethylnitrosamine-induced hepatic fibrosis rats Abstract Abstract Context Fuzheng Huayu recipe (FZHY) combined with entecavir (ETV) is used to treat the cirrhosis caused by chronic hepatitis B (CHB) infection. Objective To investigate the eff... |
PMC9854584 | core_pubmed_pmc | Synergistic Activity of Pep16, a Promising New Antibacterial Pseudopeptide against Multidrug-Resistant Organisms, in Combination with Colistin against Multidrug-Resistant Escherichia coli , In Vitro and in a Murine Peritonitis Model | Synergistic Activity of Pep16, a Promising New Antibacterial Pseudopeptide against Multidrug-Resistant Organisms, in Combination with Colistin against Multidrug-Resistant Escherichia coli , In Vitro and in a Murine Peritonitis Model Abstract Abstract Colistin is a drug of last resort to treat extreme drug-resistant Ent... |
PMC3689905 | core_pubmed_pmc | Bioequivalence of Eslicarbazepine Acetate from Two Different Sources of its Active Product Ingredient in Healthy Subjects | Bioequivalence of Eslicarbazepine Acetate from Two Different Sources of its Active Product Ingredient in Healthy Subjects Abstract Purpose To compare the bioavailability (BA) and pharmacokinetic (PK) properties and to demonstrate the bioequivalence (BE) between two active product ingredient (API) sources of eslicarbaze... |
PMC12946599 | core_pubmed_pmc | A Phase 1, Randomized, Placebo‐Controlled, Multiple‐Dose, Double‐Blind Study to Evaluate and Compare the Pharmacokinetics and Safety of Rimegepant in Healthy Adult Japanese and Caucasian Individuals | A Phase 1, Randomized, Placebo‐Controlled, Multiple‐Dose, Double‐Blind Study to Evaluate and Compare the Pharmacokinetics and Safety of Rimegepant in Healthy Adult Japanese and Caucasian Individuals Abstract Abstract This Phase 1, randomized, placebo‐controlled, double‐blind study assessed the pharmacokinetic profile o... |
PMC9710098 | core_pubmed_pmc | The PBPK LeiCNS-PK3.0 framework predicts Nirmatrelvir (but not Remdesivir or Molnupiravir) to achieve effective concentrations against SARS-CoV-2 in human brain cells | The PBPK LeiCNS-PK3.0 framework predicts Nirmatrelvir (but not Remdesivir or Molnupiravir) to achieve effective concentrations against SARS-CoV-2 in human brain cells Abstract SARS-CoV-2 was shown to infect and persist in the human brain cells for up to 230 days, highlighting the need to treat the brain viral load. The... |
PMC9540501 | core_pubmed_pmc | Population Pharmacokinetic Models for Direct Oral Anticoagulants: A Systematic Review and Clinical Appraisal Using Exposure Simulation | Population Pharmacokinetic Models for Direct Oral Anticoagulants: A Systematic Review and Clinical Appraisal Using Exposure Simulation Abstract Available data have shown an association between direct oral anticoagulant (DOAC) plasma concentration and clinical, particularly bleeding, events. Factors that may influence D... |
PMC10564307 | core_pubmed_pmc | First-in-Human, Phase I Dose-Escalation and Dose-Expansion Study of Trophoblast Cell-Surface Antigen 2–Directed Antibody-Drug Conjugate Datopotamab Deruxtecan in Non–Small-Cell Lung Cancer: TROPION-PanTumor01 | First-in-Human, Phase I Dose-Escalation and Dose-Expansion Study of Trophoblast Cell-Surface Antigen 2–Directed Antibody-Drug Conjugate Datopotamab Deruxtecan in Non–Small-Cell Lung Cancer: TROPION-PanTumor01 Abstract Abstract PURPOSE This first-in-human, dose-escalation and dose-expansion study evaluated the safety, t... |
PMC8606554 | core_pubmed_pmc | Quantitative Analysis of the Efficacy of PARP Inhibitors as Maintenance Therapy in Recurrent Ovarian Cancer | Quantitative Analysis of the Efficacy of PARP Inhibitors as Maintenance Therapy in Recurrent Ovarian Cancer Abstract Objective: This study aimed to establish a pharmacodynamic model and to screen reasonable covariates to quantitatively describe the efficacy of poly (ADP-ribose) polymerase inhibitors (PARPis) as mainten... |
PMC4898026 | core_pubmed_pmc | Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections | Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections Abstract We have a limited arsenal with which to treat invasive fungal infections caused by Aspergillus and Mucorales. The morbidity and mortality for both pathogens remains high. A triazole antifungal, isavuconazole, was recently gran... |
PMC8953076 | core_pubmed_pmc | Prodrug Therapies for Infectious and Neurodegenerative Diseases | Prodrug Therapies for Infectious and Neurodegenerative Diseases Abstract Prodrugs are bioreversible drug derivatives which are metabolized into a pharmacologically active drug following chemical or enzymatic modification. This approach is designed to overcome several obstacles that are faced by the parent drug in physi... |
PMC8019741 | core_pubmed_pmc | Efficacy Prediction of Four Pharmaceutical Formulations for Intramammary Administration Containing Aloe vera (L.) Burm. f. Combined With Ceftiofur or Cloxacillin in Lactating Cows as an Alternative Therapy to Treat Mastitis Caused by Staphylococcus aureus | Efficacy Prediction of Four Pharmaceutical Formulations for Intramammary Administration Containing Aloe vera (L.) Burm. f. Combined With Ceftiofur or Cloxacillin in Lactating Cows as an Alternative Therapy to Treat Mastitis Caused by Staphylococcus aureus Abstract Synergy or additive effect between Aloe vera (L.) Burm.... |
PMC3734837 | core_pubmed_pmc | A combination of cilostazol and Ginkgo biloba extract protects against cisplatin-induced Cochleo-vestibular dysfunction by inhibiting the mitochondrial apoptotic and ERK pathways | A combination of cilostazol and Ginkgo biloba extract protects against cisplatin-induced Cochleo-vestibular dysfunction by inhibiting the mitochondrial apoptotic and ERK pathways Abstract Cisplatin ( cis -diammine-dichloroplatinum; CDDP) is an anticancer drug that induces significant hearing loss and balance dysfunctio... |
PMC4716580 | core_pubmed_pmc | Agent‐Based Modeling in Systems Pharmacology | Agent‐Based Modeling in Systems Pharmacology Abstract Modeling and simulation (M&S) techniques provide a platform for knowledge integration and hypothesis testing to gain insights into biological systems that would not be possible a priori . Agent‐based modeling (ABM) is an M&S technique that focuses on describing indi... |
PMC11315871 | core_pubmed_pmc | Evaluation of Ornidazole Tablets Bioequivalence in Chinese Healthy Participants Under Fasted and Fed Conditions Using Pharmacokinetic Parameters | Evaluation of Ornidazole Tablets Bioequivalence in Chinese Healthy Participants Under Fasted and Fed Conditions Using Pharmacokinetic Parameters Abstract Background and Objective Ornidazole, the third generation of nitroimidazole derivatives after metronidazole and tinidazole, it exerts both bactericidal and antiprotoz... |
PMC8074352 | core_pubmed_pmc | Clinical Impact of Revised Ciprofloxacin Breakpoint in Patients with Urinary Tract Infections by Enterobacteriaceae | Clinical Impact of Revised Ciprofloxacin Breakpoint in Patients with Urinary Tract Infections by Enterobacteriaceae Abstract Abstract In 2018, the Clinical and Laboratory Standards Institute (CLSI) revised ciprofloxacin (CIP)-susceptible breakpoint for Enterobacteriaceae from ≤1 μg/mL to ≤0.25 μg/mL, based on pharmacok... |
PMC3231982 | core_pubmed_pmc | Immunogenicity of panitumumab in combination chemotherapy clinical trials | Immunogenicity of panitumumab in combination chemotherapy clinical trials Abstract Abstract Background Panitumumab is a fully human antibody against the epidermal growth factor receptor that is indicated for the treatment of metastatic colorectal cancer (mCRC) after disease progression on standard chemotherapy. The pur... |
PMC6759287 | core_pubmed_pmc | Effect Of Chinese Herb Danzhi Xiaoyao Pills On Pharmacokinetics Of Venlafaxine In Beagles | Effect Of Chinese Herb Danzhi Xiaoyao Pills On Pharmacokinetics Of Venlafaxine In Beagles Abstract Abstract Objective To investigate the effects of Chinese herb Danzhi Xiaoyao pills on the pharmacokinetics of venlafaxine and its metabolites O-desmethylvenlafaxine (ODV) and N-desmethylvenlafaxine (NDV) in beagles by usi... |
PMC6757420 | core_pubmed_pmc | Identifying the active components of Baihe–Zhimu decoction that ameliorate depressive disease by an effective integrated strategy: a systemic pharmacokinetics study combined with classical depression model tests | Identifying the active components of Baihe–Zhimu decoction that ameliorate depressive disease by an effective integrated strategy: a systemic pharmacokinetics study combined with classical depression model tests Abstract Abstract Background Modern pharmacological studies have demonstrated that Baihe–Zhimu decoction (BZ... |
PMC7038301 | core_pubmed_pmc | A Subcutaneous Implant of Tenofovir Alafenamide Fumarate Causes Local Inflammation and Tissue Necrosis in Rabbits and Macaques | A Subcutaneous Implant of Tenofovir Alafenamide Fumarate Causes Local Inflammation and Tissue Necrosis in Rabbits and Macaques Abstract We describe the in vitro and in vivo evaluation of a subcutaneous reservoir implant delivering tenofovir alafenamide hemifumarate (TAF) for the prevention of HIV infection. These long-... |
PMC10657194 | core_pubmed_pmc | An Integrative Approach to Study the Inhibition of Providencia vermicola FabD Using C2-Quaternary Indolinones | An Integrative Approach to Study the Inhibition of Providencia vermicola FabD Using C2-Quaternary Indolinones Abstract Background The present study investigates the potential bioactivity of twelve experimentally designed C-2 quaternary indolinones against Providencia spp., a bacterial group of the Enterobacteriaceae fa... |
PMC6685729 | core_pubmed_pmc | User-Centered Development of an Online Platform for Drug Dosing Recommendations in Pediatrics | User-Centered Development of an Online Platform for Drug Dosing Recommendations in Pediatrics Abstract Abstract Background Drug therapy in pediatric patients is a complex process. Children are subject to continuous growth and variation in drug-metabolizing enzyme activity, requiring continuous adaption of dosages. In G... |
PMC11389886 | core_pubmed_pmc | Developing Parametric and Nonparametric Models for Model-Informed Precision Dosing: A Quality Improvement Effort in Vancomycin for Patients With Obesity | Developing Parametric and Nonparametric Models for Model-Informed Precision Dosing: A Quality Improvement Effort in Vancomycin for Patients With Obesity Abstract Supplemental Digital Content is Available in the Text. Background: Both parametric and nonparametric methods have been proposed to support model-informed prec... |
PMC4079632 | core_pubmed_pmc | Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection | Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection Abstract Abstract According to the World Health Organization, approximately 150 million people worldwide are chronic carriers of hepatitis C virus (HCV). HCV infection can evolve into cirrhosis of the liver and its complications, which are ult... |
PMC8839099 | core_pubmed_pmc | Enhancing Ocular Bioavailability of Ciprofloxacin Using Colloidal Lipid-Based Carrier for the Management of Post-Surgical Infection | Enhancing Ocular Bioavailability of Ciprofloxacin Using Colloidal Lipid-Based Carrier for the Management of Post-Surgical Infection Abstract Conjunctivitis and endogenous bacterial endophthalmitis mostly occurred after ophthalmic surgery. Therefore, the present study aimed to maximize the ocular delivery of ciprofloxac... |
PMC8892746 | core_pubmed_pmc | Exposure–response analyses of cabozantinib in patients with metastatic renal cell cancer | Exposure–response analyses of cabozantinib in patients with metastatic renal cell cancer Abstract Abstract Aim In the registration trial, cabozantinib exposure ≥ 750 ng/mL correlated to improved tumor size reduction, response rate and progression free survival (PFS) in patients with metastatic renal cell cancer (mRCC).... |
PMC11047404 | core_pubmed_pmc | Comparative Efficacy of Continuous Ceftazidime Infusion vs. Intermittent Bolus against In Vitro Ceftazidime-Susceptible and -Resistant Pseudomonas aeruginosa Biofilm | Comparative Efficacy of Continuous Ceftazidime Infusion vs. Intermittent Bolus against In Vitro Ceftazidime-Susceptible and -Resistant Pseudomonas aeruginosa Biofilm Abstract Background : As the anti-biofilm pharmacokinetic/pharmacodynamic (PK/PD) properties of antibiotics are not well-defined, we have evaluated the PK... |
PMC5034805 | core_pubmed_pmc | Evaluation of CYP3A‐mediated drug–drug interactions with romidepsin in patients with advanced cancer | Evaluation of CYP3A‐mediated drug–drug interactions with romidepsin in patients with advanced cancer Abstract Abstract Two multicenter, single‐arm, single‐infusion, open‐label studies were conducted to evaluate the effect of ketoconazole (a strong CYP3A inhibitor) or rifampin (a strong CYP3A inducer) daily for 5 days o... |
PMC9585207 | core_pubmed_pmc | SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™ | SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™ Abstract The study is based on using SeDeM expert system in developing controlled-release tramad... |
PMC10925492 | core_pubmed_pmc | Effects of Aripiprazole on Olanzapine Population Pharmacokinetics and Initial Dosage Optimization in Schizophrenia Patients | Effects of Aripiprazole on Olanzapine Population Pharmacokinetics and Initial Dosage Optimization in Schizophrenia Patients Abstract Objective Olanzapine has already been used to treat schizophrenia patients; however, the initial dosage recommendation when multiple drugs are used in combination, remains unclear. The pu... |
PMC9609097 | core_pubmed_pmc | Pharmacometric Modeling of the Impact of Azelastine Nasal Spray on SARS-CoV-2 Viral Load and Related Symptoms in COVID-19 Patients | Pharmacometric Modeling of the Impact of Azelastine Nasal Spray on SARS-CoV-2 Viral Load and Related Symptoms in COVID-19 Patients Abstract Abstract The histamine-1 receptor antagonist azelastine was recently found to impact SARS-CoV-2 viral kinetics in a Phase 2 clinical trial (CARVIN). Thus, we investigated the relat... |
PMC10725261 | core_pubmed_pmc | Tutorial on model selection and validation of model input into precision dosing software for model‐informed precision dosing | Tutorial on model selection and validation of model input into precision dosing software for model‐informed precision dosing Abstract Abstract There has been rising interest in using model‐informed precision dosing to provide personalized medicine to patients at the bedside. This methodology utilizes population pharmac... |
PMC5701813 | core_pubmed_pmc | PK-PD Analysis of Marbofloxacin against Streptococcus suis in Pigs | PK-PD Analysis of Marbofloxacin against Streptococcus suis in Pigs Abstract Marbofloxacin is a fluoroquinolone antibiotic and highly effective treatment for respiratory diseases. Here we aimed to evaluate the ex vivo activity of marbofloxacin against Streptococcus suis in pig serum, as well as the optimal dosages schem... |
PMC8248190 | core_pubmed_pmc | Pharmacokinetics of meropenem in children with sepsis undergoing extracorporeal life support: A prospective observational study | Pharmacokinetics of meropenem in children with sepsis undergoing extracorporeal life support: A prospective observational study Abstract Summary What is known and Objective Meropenem, a broad‐spectrum carbapenem, is frequently used to treat severe bacterial infections in critically ill children. Recommendations for mer... |
PMC11615922 | core_pubmed_pmc | Quantitative pharmacodynamics functional evaluation of Chinese medicine Qizhu formula in mice with dynamic near-infrared photoacoustic imaging | Quantitative pharmacodynamics functional evaluation of Chinese medicine Qizhu formula in mice with dynamic near-infrared photoacoustic imaging Abstract Background & Aims Effective anti-fibrotic drugs and new non-invasive evaluation methods for liver fibrosis (LF) are urgently needed. Our study aimed to evaluate the his... |
PMC4128785 | core_pubmed_pmc | 44 Sc: An Attractive Isotope for Peptide-Based PET Imaging | 44 Sc: An Attractive Isotope for Peptide-Based PET Imaging Abstract The overexpression of integrin α v β 3 has been linked to tumor aggressiveness and metastasis in several cancer types. Because of its high affinity, peptides containing the arginine–glycine–aspartic acid (RGD) motif have been proven valuable vectors fo... |
PMC12506027 | core_pubmed_pmc | AntiviralDB: an expert-curated database of antiviral agents against human infectious diseases | AntiviralDB: an expert-curated database of antiviral agents against human infectious diseases Abstract ABSTRACT Viral infectious diseases have caused millions of deaths worldwide. Antiviral agents are critical for controlling these infections; however, an open-access database dedicated specifically to antiviral agents ... |
PMC8016788 | core_pubmed_pmc | Evaluation of the Pharmacokinetics and Exposure–Response Relationship of Dapagliflozin in Patients without Diabetes and with Chronic Kidney Disease | Evaluation of the Pharmacokinetics and Exposure–Response Relationship of Dapagliflozin in Patients without Diabetes and with Chronic Kidney Disease Abstract Abstract Background and Objective Dapagliflozin, a sodium-glucose co-transporter inhibitor, was originally developed as an oral glucose-lowering drug for the treat... |
PMC12947315 | core_pubmed_pmc | Evaluation of Drug–Drug Interaction Potential Between the Oral Antibiotic Zoliflodacin and the CYP3A4 Inhibitor Itraconazole: A Phase 1 Study in Healthy Participants | Evaluation of Drug–Drug Interaction Potential Between the Oral Antibiotic Zoliflodacin and the CYP3A4 Inhibitor Itraconazole: A Phase 1 Study in Healthy Participants Abstract ABSTRACT Zoliflodacin is a first‐in‐class oral spiropyrimidinetrione antibiotic being developed for patients with uncomplicated gonorrhea, includ... |
PMC4955259 | core_pubmed_pmc | Abediterol, a novel long-acting β 2 -agonist: bronchodilation, safety, tolerability and pharmacokinetic results from a single-dose, dose-ranging, active-comparator study in patients with COPD | Abediterol, a novel long-acting β 2 -agonist: bronchodilation, safety, tolerability and pharmacokinetic results from a single-dose, dose-ranging, active-comparator study in patients with COPD Abstract Background Abediterol is a novel, once-daily long-acting β 2 -agonist in development for the treatment of chronic obstr... |
PMC12947316 | core_pubmed_pmc | Population PK – PD Modeling of Danicopan Add‐On Therapy in Participants With Paroxysmal Nocturnal Hemoglobinuria Treated With Ravulizumab or Eculizumab | Population PK – PD Modeling of Danicopan Add‐On Therapy in Participants With Paroxysmal Nocturnal Hemoglobinuria Treated With Ravulizumab or Eculizumab Abstract ABSTRACT Danicopan is a first‐in‐class orally administered complement factor D inhibitor, approved as an add‐on therapy to ravulizumab or eculizumab for the tr... |
PMC11023281 | core_pubmed_pmc | Pharmacokinetic profile of oral and subcutaneous administration of paracetamol in the koala ( Phascolarctos cinereus ) and prediction of its analgesic efficacy | Pharmacokinetic profile of oral and subcutaneous administration of paracetamol in the koala ( Phascolarctos cinereus ) and prediction of its analgesic efficacy Abstract Abstract The pharmacokinetic profile of paracetamol in koalas is described when administered orally at 15 mg/kg; followed by the same dose, administere... |
PMC8708464 | core_pubmed_pmc | Development of a Model-Informed Dosing Tool to Optimise Initial Antibiotic Dosing—A Translational Example for Intensive Care Units | Development of a Model-Informed Dosing Tool to Optimise Initial Antibiotic Dosing—A Translational Example for Intensive Care Units Abstract The prevalence and mortality rates of severe infections are high in intensive care units (ICUs). At the same time, the high pharmacokinetic variability observed in ICU patients inc... |
PMC4790317 | core_pubmed_pmc | Utilizing Monte Carlo Simulations to Optimize Institutional Empiric Antipseudomonal Therapy | Utilizing Monte Carlo Simulations to Optimize Institutional Empiric Antipseudomonal Therapy Abstract Abstract Pseudomonas aeruginosa is a common pathogen implicated in nosocomial infections with increasing resistance to a limited arsenal of antibiotics. Monte Carlo simulation provides antimicrobial stewardship teams wi... |
PMC4515243 | core_pubmed_pmc | Phase 1 pharmacokinetic study of the oral pan-AKT inhibitor MK-2206 in Japanese patients with advanced solid tumors | Phase 1 pharmacokinetic study of the oral pan-AKT inhibitor MK-2206 in Japanese patients with advanced solid tumors Abstract Abstract Purpose MK-2206 is an oral, highly selective inhibitor of AKT. The safety, tolerability, pharmacokinetics (PK), and anti-tumor activity of MK-2206 was evaluated in Japanese patients with... |
PMC5412584 | core_pubmed_pmc | Exposure-Response Relationships during Free-Access Intravenous Alcohol Self-Administration in Nondependent Drinkers: Influence of Alcohol Expectancies and Impulsivity | Exposure-Response Relationships during Free-Access Intravenous Alcohol Self-Administration in Nondependent Drinkers: Influence of Alcohol Expectancies and Impulsivity Abstract Abstract Background: Self-administration is a hallmark of all addictive drugs, including alcohol. Human laboratory models of alcohol self-admini... |
PMC3439798 | core_pubmed_pmc | Pharmacokinetics of drospirenone and ethinylestradiol in Caucasian and Japanese women | Pharmacokinetics of drospirenone and ethinylestradiol in Caucasian and Japanese women Abstract Objective To investigate the pharmacokinetics of drospirenone (DRSP) and ethinylestradiol (EE) in Caucasian and Japanese women. Method Three open-label, non-randomised studies were performed to assess the pharmacokinetics fol... |
PMC4762905 | core_pubmed_pmc | Polymorphisms in the ABCB1 gene and effect on outcome and toxicity in childhood acute lymphoblastic leukemia | Polymorphisms in the ABCB1 gene and effect on outcome and toxicity in childhood acute lymphoblastic leukemia Abstract Abstract The membrane transporter P-glycoprotein, encoded by the ABCB1 gene, influences the pharmacokinetics of anti-cancer drugs. We hypothesized that variants of ABCB1 affect outcome and toxicity in c... |
PMC12299168 | core_pubmed_pmc | Preparation and Evaluation of Long-Acting Injectable Levocetirizine Prodrug Formulation | Preparation and Evaluation of Long-Acting Injectable Levocetirizine Prodrug Formulation Abstract Background/Objectives : Levocetirizine (LCZ) is a second-generation antihistamine with minimal central nervous system effects. However, its short half-life necessitates daily dosing, potentially reducing adherence in pediat... |
PMC5387714 | core_pubmed_pmc | Glycoengineering of pertuzumab and its impact on the pharmacokinetic/pharmacodynamic properties | Glycoengineering of pertuzumab and its impact on the pharmacokinetic/pharmacodynamic properties Abstract Abstract Pertuzumab is an antihuman HER2 antibody developed for HER2 positive breast cancer. Glycosylation profiles are always the important issue for antibody based therapy. Previous findings have suggested the imp... |
PMC5009327 | core_pubmed_pmc | Noninvasive mapping of the redox status of dimethylnitrosamine-induced hepatic fibrosis using in vivo dynamic nuclear polarization-magnetic resonance imaging | Noninvasive mapping of the redox status of dimethylnitrosamine-induced hepatic fibrosis using in vivo dynamic nuclear polarization-magnetic resonance imaging Abstract Abstract Hepatic fibrosis is a chronic disorder caused by viral infection and/or metabolic, genetic and cholestatic disorders. A noninvasive procedure th... |
PMC12185614 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Modelling and Monte Carlo Simulations to Predict Cytomegalovirus Viral Load in Pediatric Transplant Recipients Treated with (val)Ganciclovir | Pharmacokinetic/Pharmacodynamic Modelling and Monte Carlo Simulations to Predict Cytomegalovirus Viral Load in Pediatric Transplant Recipients Treated with (val)Ganciclovir Abstract Abstract Background and Objectives Cytomegalovirus (CMV) infection poses significant challenges in pediatric transplant recipients. Gancic... |
PMC8604827 | core_pubmed_pmc | Development of PBPK model for intra-articular injection in human: methotrexate solution and rheumatoid arthritis case study | Development of PBPK model for intra-articular injection in human: methotrexate solution and rheumatoid arthritis case study Abstract Abstract A physiologically based model describing the dissolution, diffusion, and transfer of drug from the intra-articular (IA) space to the plasma, was developed for GastroPlus® v9.8. T... |
PMC6610295 | core_pubmed_pmc | First evaluation of tapentadol oral solution for the treatment of moderate to severe acute pain in children aged 6 to <18 | First evaluation of tapentadol oral solution for the treatment of moderate to severe acute pain in children aged 6 to <18 Abstract Abstract Background This is the first clinical trial in the global pediatric clinical development program for the use of the analgesic tapentadol in children and adolescents. Patients and m... |
PMC9146797 | core_pubmed_pmc | [ 99m Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging | [ 99m Tc]Tc-Labeled Plectin-Targeting Peptide as a Novel SPECT Probe for Tumor Imaging Abstract Abstract Certain receptors are often overexpressed during tumor occurrence and development and closely correlate with carcinogenesis. Owing to its overexpression on the cell membrane and cytoplasm of various tumors, plectin,... |
PMC7857992 | core_pubmed_pmc | Combined docking methods and molecular dynamics to identify effective antiviral 2, 5-diaminobenzophenonederivatives against SARS-CoV-2 | Combined docking methods and molecular dynamics to identify effective antiviral 2, 5-diaminobenzophenonederivatives against SARS-CoV-2 Abstract Abstract The aim of this work is to contribute to the research in finding lead compounds for clinical use, to identify new drugs that target the SARS-CoV-2 virus main protease ... |
PMC9791580 | core_pubmed_pmc | Editorial: Model-informed drug development and evidence-based translational pharmacology | Editorial: Model-informed drug development and evidence-based translational pharmacology Modeling 2 Application of model-informed drug development (MIDD) There is a long-standing history of applying MIDD to inform regulatory decisions at the FDA ( Madabushi et al., 2022 ). In the early 90s, the utilities of MIDD were l... |
PMC11247122 | core_pubmed_pmc | Population pharmacokinetics of imetelstat, a first‐in‐class oligonucleotide telomerase inhibitor | Population pharmacokinetics of imetelstat, a first‐in‐class oligonucleotide telomerase inhibitor Abstract Abstract Imetelstat is a novel, first‐in‐class, oligonucleotide telomerase inhibitor in development for the treatment of hematologic malignancies including lower‐risk myelodysplastic syndromes and myelofibrosis. A ... |
PMC8416343 | core_pubmed_pmc | A Facile Procedure for One-Pot Stable Conjugation of Two Proglucagon Cysteine-Containing Peptide Analogs | A Facile Procedure for One-Pot Stable Conjugation of Two Proglucagon Cysteine-Containing Peptide Analogs Abstract Abstract Optimization of peptides for therapeutic purposes often includes chemical conjugation or modification with substituents that serve to broaden pharmacology or improve pharmacokinetics. We report a c... |
PMC9353711 | core_pubmed_pmc | A Novel Berberine–Glycyrrhizic Acid Complex Formulation Enhanced the Prevention Effect to Doxorubicin-Induced Cardiotoxicity by Pharmacokinetic Modulation of Berberine in Rats | A Novel Berberine–Glycyrrhizic Acid Complex Formulation Enhanced the Prevention Effect to Doxorubicin-Induced Cardiotoxicity by Pharmacokinetic Modulation of Berberine in Rats Abstract Developing a new drug delivery system is one of the useful approaches to overcome the limited use of berberine (BBR) to enhance its abs... |
PMC11074474 | core_pubmed_pmc | Nivolumab plus ONC201 plus in microsatellite stable (MSS) metastatic colorectal cancer (mCRC) patients: a Brown University Oncology Research Group phase Ib/II study (BrUOG379) | Nivolumab plus ONC201 plus in microsatellite stable (MSS) metastatic colorectal cancer (mCRC) patients: a Brown University Oncology Research Group phase Ib/II study (BrUOG379) Abstract Abstract Background Immune checkpoint inhibitors alone, or in combination with chemotherapy failed to provide meaningful clinical activ... |
PMC5011461 | core_pubmed_pmc | Pharmacokinetics of oseltamivir in infants under the age of 1 year | Pharmacokinetics of oseltamivir in infants under the age of 1 year Abstract Background Oseltamivir is the only antiviral treatment recommended for influenza in young children over the age of 1 year. There is scant data on oseltamivir pharmacokinetics (PK) in infants <1 year. We set out to perform PK measurements in inf... |
PMC7285563 | core_pubmed_pmc | Epinephrine delivery via EpiPen ® Auto-Injector or manual syringe across participants with a wide range of skin-to-muscle distances | Epinephrine delivery via EpiPen ® Auto-Injector or manual syringe across participants with a wide range of skin-to-muscle distances Abstract Abstract Background Intramuscular (IM) injection of epinephrine (adrenaline) at the mid-anterolateral (AL) thigh is the international standard therapy for acute anaphylaxis. Conce... |
PMC6084602 | core_pubmed_pmc | Evaluation of the Relative Intranasal Abuse Potential of a Hydrocodone Extended-Release Tablet Formulated with Abuse-Deterrence Technology in Nondependent, Recreational Opioid Users | Evaluation of the Relative Intranasal Abuse Potential of a Hydrocodone Extended-Release Tablet Formulated with Abuse-Deterrence Technology in Nondependent, Recreational Opioid Users Abstract Abstract Objective To assess the intranasal abuse potential of hydrocodone extended-release (ER) tablets developed with CIMA Abus... |
PMC9938066 | core_pubmed_pmc | A proof of concept reinforcement learning based tool for non parametric population pharmacokinetics workflow optimization | A proof of concept reinforcement learning based tool for non parametric population pharmacokinetics workflow optimization Abstract Abstract The building of population pharmacokinetic models can be described as an iterative process in which given a model and a dataset, the pharmacometrician introduces some changes to th... |
PMC12818054 | core_pubmed_pmc | Understanding Pharmacokinetic-Drug Interactions With Drugs Approved by the US Food and Drug Administration in 2024 to Better Manage the Risk of Drug Interactions With Concomitant Medications: A Review of Clinical Data From New Drug Applications | Understanding Pharmacokinetic-Drug Interactions With Drugs Approved by the US Food and Drug Administration in 2024 to Better Manage the Risk of Drug Interactions With Concomitant Medications: A Review of Clinical Data From New Drug Applications Abstract Abstract Objective This analysis aimed to provide a mechanistic un... |
PMC6358270 | core_pubmed_pmc | Quantitative Systems Toxicology Analysis of In Vitro Mechanistic Assays Reveals Importance of Bile Acid Accumulation and Mitochondrial Dysfunction in TAK-875-Induced Liver Injury | Quantitative Systems Toxicology Analysis of In Vitro Mechanistic Assays Reveals Importance of Bile Acid Accumulation and Mitochondrial Dysfunction in TAK-875-Induced Liver Injury Abstract Abstract TAK-875 (fasiglifam), a GPR40 agonist in development for the treatment of type 2 diabetes (T2D), was voluntarily terminated... |
PMC7183353 | core_pubmed_pmc | Effect of diabetes mellitus on TB drug concentrations in Tanzanian patients | Effect of diabetes mellitus on TB drug concentrations in Tanzanian patients Abstract Abstract Background Diabetes mellitus (DM) is associated with poor TB treatment outcome. Previous studies examining the effect of DM on TB drug concentrations yielded conflicting results. No studies have been conducted to date in an Af... |
PMC4235188 | core_pubmed_pmc | Effects of Danshen Ethanol Extract on the Pharmacokinetics of Fexofenadine in Healthy Volunteers | Effects of Danshen Ethanol Extract on the Pharmacokinetics of Fexofenadine in Healthy Volunteers Abstract Abstract This study investigated the effect of multidose administration of danshen ethanol extract on fexofenadine pharmacokinetics in healthy volunteers. A sequential, open-label, two-period pharmacokinetic intera... |
PMC3119073 | core_pubmed_pmc | Pharmacological Blockade of Serotonin 5-HT 7 Receptor Reverses Working Memory Deficits in Rats by Normalizing Cortical Glutamate Neurotransmission | Pharmacological Blockade of Serotonin 5-HT 7 Receptor Reverses Working Memory Deficits in Rats by Normalizing Cortical Glutamate Neurotransmission Abstract Abstract The role of 5-HT 7 receptor has been demonstrated in various animal models of mood disorders; however its function in cognition remains largely speculative... |
PMC8520749 | core_pubmed_pmc | Multistate model for pharmacometric analyses of overall survival in HER2‐negative breast cancer patients treated with docetaxel | Multistate model for pharmacometric analyses of overall survival in HER2‐negative breast cancer patients treated with docetaxel Abstract Abstract The aim of this study was to develop a multistate model for overall survival (OS) analysis, based on parametric hazard functions and combined with an investigation of predict... |
PMC6585851 | core_pubmed_pmc | Bioequivalence of Olanzapine Given in Combination With Samidorphan as a Bilayer Tablet (ALKS 3831) Compared With Olanzapine‐Alone Tablets: Results From a Randomized, Crossover Relative Bioavailability Study | Bioequivalence of Olanzapine Given in Combination With Samidorphan as a Bilayer Tablet (ALKS 3831) Compared With Olanzapine‐Alone Tablets: Results From a Randomized, Crossover Relative Bioavailability Study Abstract Abstract The objective of this study was to evaluate the relative bioavailability of olanzapine in 3 ola... |
PMC7032967 | core_pubmed_pmc | A review of three years' experience of the first pharmacometrics company in Korea | A review of three years' experience of the first pharmacometrics company in Korea Abstract As the pharmaceutical industry in Korea is reaching the golden era of drug discovery due to increased investments in research and development and government funds, the need for a more efficient tool for the quantitative analysis ... |
PMC7601252 | core_pubmed_pmc | Progress in Clinical Trials of Photodynamic Therapy for Solid Tumors and the Role of Nanomedicine | Progress in Clinical Trials of Photodynamic Therapy for Solid Tumors and the Role of Nanomedicine Abstract Simple Summary Photodynamic therapy (PDT) has been undertaken with growing focus in recent studies to identify successful anticancer therapies. The field of PDT has evolved rapidly and is continuously being evalua... |
PMC7505726 | core_pubmed_pmc | A Meta-Analysis on the Performance of Cystatin C- versus Creatinine-based eGFR Equations in Predicting Vancomycin Clearance | A Meta-Analysis on the Performance of Cystatin C- versus Creatinine-based eGFR Equations in Predicting Vancomycin Clearance Abstract Background The objective of this study was to compare the performance of cystatin C- and creatinine-based estimated glomerular filtration rate (eGFR) equations in predicting the clearance... |
PMC12655566 | core_pubmed_pmc | Biodistribution and Toxicological Impact Assessment of Cerium Dioxide Nanoparticles in Murine Models: A Systematic Review of In Vivo and Ex Vivo Studies | Biodistribution and Toxicological Impact Assessment of Cerium Dioxide Nanoparticles in Murine Models: A Systematic Review of In Vivo and Ex Vivo Studies Abstract Background/Objectives: This review summarizes and analyzes current data on the toxicological effects of cerium dioxide nanoparticles (nanoceria) on various an... |
PMC11357403 | core_pubmed_pmc | pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy | pH-Sensitive In Situ Gel of Mirtazapine Invasomes for Rectal Drug Delivery: Protruded Bioavailability and Anti-Depressant Efficacy Abstract The present research emphasizes fabrication alongside the assessment of an innovative nano-vesicular membranous system known as invasomes (NVMs) laden with Mirtazapine for rectal a... |
PMC10714982 | core_pubmed_pmc | Population Pharmacokinetics of Isavuconazole in Adult: A Systematic Review | Population Pharmacokinetics of Isavuconazole in Adult: A Systematic Review Abstract Abstract Isavuconazole (ISA) is a second generation broad-spectrum triazole antifungal drug derived from voriconazole structure, and its oral capsules is currently the only oral preparation approved for invasive mucormycosis. In recent ... |
PMC11578135 | core_pubmed_pmc | Physiologically based pharmacokinetic modeling of drug–drug interactions between ritonavir‐boosted atazanavir and rifampicin in pregnancy | Physiologically based pharmacokinetic modeling of drug–drug interactions between ritonavir‐boosted atazanavir and rifampicin in pregnancy Abstract Abstract Ritonavir‐boosted atazanavir (ATV/r) and rifampicin are mainstays of second‐line antiretroviral and multiple anti‐TB regimens, respectively. Rifampicin induces CYP3... |
PMC7318213 | core_pubmed_pmc | Long‐term safety and efficacy of rIX‐FP prophylaxis with extended dosing intervals up to 21 days in adults/adolescents with hemophilia B | Long‐term safety and efficacy of rIX‐FP prophylaxis with extended dosing intervals up to 21 days in adults/adolescents with hemophilia B Abstract Abstract Background An international, multicenter extension study evaluated recombinant fusion protein linking recombinant coagulation factor IX (FIX) with recombinant human ... |
PMC3033031 | core_pubmed_pmc | Pharmacokinetic profile of an intradeltoid diclofenac injection in obese Indian volunteers | Pharmacokinetic profile of an intradeltoid diclofenac injection in obese Indian volunteers Abstract Background A new propylene glycol-free and reduced-volume formulation of diclofenac sodium 75 mg/mL designed for intradeltoid administration has been found to be bioequivalent to a reference formulation of diclofenac sod... |
PMC10865485 | core_pubmed_pmc | Phase 1 study of latozinemab in progranulin‐associated frontotemporal dementia | Phase 1 study of latozinemab in progranulin‐associated frontotemporal dementia Abstract Abstract INTRODUCTION Heterozygous mutations in the GRN gene lead to reduced progranulin (PGRN) levels in plasma and cerebrospinal fluid (CSF) and are causative of frontotemporal dementia (FTD) with > 90% penetrance. Latozinemab is ... |
PMC10788539 | core_pubmed_pmc | Repurposing celecoxib for colorectal cancer targeting via pH-triggered ultra-elastic nanovesicles: Pronounced efficacy through up-regulation of Wnt/β-catenin pathway in DMH-induced tumorigenesis | Repurposing celecoxib for colorectal cancer targeting via pH-triggered ultra-elastic nanovesicles: Pronounced efficacy through up-regulation of Wnt/β-catenin pathway in DMH-induced tumorigenesis Abstract Abstract Celecoxib (CLX), a selective inhibitor for cyclooxygenase 2 (COX-2), has manifested potential activity agai... |
PMC5264215 | core_pubmed_pmc | Canakinumab treatment for patients with active recurrent or chronic TNF receptor-associated periodic syndrome (TRAPS): an open-label, phase II study | Canakinumab treatment for patients with active recurrent or chronic TNF receptor-associated periodic syndrome (TRAPS): an open-label, phase II study Abstract Abstract Objective To evaluate the efficacy of canakinumab, a high-affinity human monoclonal anti-interleukin-1β antibody, in inducing complete or almost complete... |
PMC8521408 | core_pubmed_pmc | Impact of a vancomycin loading dose on the achievement of target vancomycin exposure in the first 24 h and on the accompanying risk of nephrotoxicity in critically ill patients | Impact of a vancomycin loading dose on the achievement of target vancomycin exposure in the first 24 h and on the accompanying risk of nephrotoxicity in critically ill patients Abstract Abstract Background The advocated pharmacokinetic/pharmacodynamic (PK/PD) target for vancomycin, AUC/MIC ≥ 400 mg·h/L, may not be reac... |
PMC5901008 | core_pubmed_pmc | Impact of the Norepinephrine Prodrug Droxidopa on the QTc Interval in Healthy Individuals | Impact of the Norepinephrine Prodrug Droxidopa on the QTc Interval in Healthy Individuals Abstract Abstract A double‐blind, 4‐period crossover study ( NCT01327066 ) was conducted to assess the effect of the novel norepinephrine prodrug droxidopa on the QT interval in in healthy subjects. Subjects were randomized to rec... |
PMC11179707 | core_pubmed_pmc | Joint modeling of tumor dynamics and progression‐free survival in advanced breast cancer: Leveraging data from amcenestrant early phase I–II trials | Joint modeling of tumor dynamics and progression‐free survival in advanced breast cancer: Leveraging data from amcenestrant early phase I–II trials Abstract Abstract A joint modeling framework was developed using data from 75 patients of early amcenestrant phase I–II AMEERA‐1‐2 dose escalation and expansion cohorts. A ... |
PMC8245906 | core_pubmed_pmc | Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment | Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An in vitro and in vivo DMPK assessment Abstract Abstract Remdesivir (RDV) is the only US Food and Drug Administration (FDA)-approved drug for treating COVID-19. However, RDV can only be given by intravenous route, and there is a pressing medic... |
PMC4947994 | core_pubmed_pmc | Inhibition of Poly(ADP-Ribose) Polymerase by Nucleic Acid Metabolite 7-Methylguanine | Inhibition of Poly(ADP-Ribose) Polymerase by Nucleic Acid Metabolite 7-Methylguanine Abstract The ability of 7-methylguanine, a nucleic acid metabolite, to inhibit poly(ADP-ribose)polymerase-1 (PARP-1) and poly(ADP-ribose)polymerase-2 (PARP-2) has been identified in silico and studied experimentally. The amino group at... |
PMC4572077 | core_pubmed_pmc | Clinical and In Vitro Studies on Impact of High-Dose Etoposide Pharmacokinetics Prior Allogeneic Hematopoietic Stem Cell Transplantation for Childhood Acute Lymphoblastic Leukemia on the Risk of Post-Transplant Leukemia Relapse | Clinical and In Vitro Studies on Impact of High-Dose Etoposide Pharmacokinetics Prior Allogeneic Hematopoietic Stem Cell Transplantation for Childhood Acute Lymphoblastic Leukemia on the Risk of Post-Transplant Leukemia Relapse Abstract The impact of etoposide (VP-16) plasma concentrations on the day of allogeneic hema... |
PMC5762195 | core_pubmed_pmc | Liquid chromatography–tandem mass spectrometry method for the estimation of adefovir in human plasma: Application to a pharmacokinetic study | Liquid chromatography–tandem mass spectrometry method for the estimation of adefovir in human plasma: Application to a pharmacokinetic study Abstract An analytical method based on solid phase extraction was developed and validated for analysis of adefovir in human plasma. Adefovir-d 4 was used as an internal standard a... |
PMC10666625 | core_pubmed_pmc | Exploring the benefits of in-diet versus repeated oral dosing of saracatinib (AZD0530) in chronic studies: insights into pharmacokinetics and animal welfare | Exploring the benefits of in-diet versus repeated oral dosing of saracatinib (AZD0530) in chronic studies: insights into pharmacokinetics and animal welfare Abstract Abstract Saracatinib/AZD0530 (SAR), a Src tyrosine kinase inhibitor, mitigates seizure-induced brain pathology in epilepsy models upon repeated oral dosin... |
PMC10328216 | core_pubmed_pmc | A State-of-the-Science Review of Interactions of Per- and Polyfluoroalkyl Substances (PFAS) with Renal Transporters in Health and Disease: Implications for Population Variability in PFAS Toxicokinetics | A State-of-the-Science Review of Interactions of Per- and Polyfluoroalkyl Substances (PFAS) with Renal Transporters in Health and Disease: Implications for Population Variability in PFAS Toxicokinetics Abstract Background: Per- and polyfluoroalkyl substances (PFAS) are ubiquitous in the environment and have been shown ... |
PMC7763054 | core_pubmed_pmc | Disposition of Cannabidiol Metabolites in Serum and Urine from Healthy Individuals Treated with Pharmaceutical Preparations of Medical Cannabis | Disposition of Cannabidiol Metabolites in Serum and Urine from Healthy Individuals Treated with Pharmaceutical Preparations of Medical Cannabis Abstract The use of cannabis flowering tops with standardized amounts of active phytocannabinoids was recently authorized in several countries to treat several painful patholog... |
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