The selection of a biologically active molecule as a successful inhaled therapeutic agent depends on its pharmacokinetic and safety properties...
Modeling Drug Disposition of Timolol in Ocular Tissues of Rabbit following Topical Eye Drops
Recently, we reported the successful application of a novel mathematical model describing drug disposition in eye compartments to simulate disposition of clonidine after topical (eye drop) administration.
Modeling Fluconazole – a Case with Concentration-Dependent Liver:Plasma Partition Coefficient
Fluconazole is an antifungal agent widely used in the clinical setting for the treatment of candidiasis and meningitis. It undergoes minimal metabolism and is excreted renally.
PBPK Modeling of Fluoxetine and its Metabolite Norfluoxetine: Prediction of the Extent of Their Involvement in Drug Interactions
The aim of our study was to simulate the human pharmacokinetics of fluoxetine and its major metabolite, norfluoxetine, and predict the magnitude of their drug-drug interactions (DDIs) using physiologically…
A Pharmacokinetic Simulation-Based Comparison Of Varying Adherence Rates For Paliperidone ER And Risperidone In Patients With Schizophrenia
Medication adherence is important to successful management of • patients with schizophrenia and related psychotic disorders; patient nonadherence is documented in numerous studies (e.g., 30%-35%…
Simulation of Cilostazol Absorption and Pharmacokinetics
Cilostazol absorption and pharmacokinetics were simulated using GastroPlus™. The program’s Advanced Compartmental and Transit (ACAT) model described the absorption of the drug, while pharmacokinetics was…
Physiologically Based Model for Ketoconazole Disposition and Prediction of its Drug-Drug Interactions
Ketoconazole is a potent inhibitor of the major drug-metabolizing enzyme, CYP3A4 and, as the result of that, is involved in many drug-drug interactions. Pharmacokinetic (PK) information available for…
Forensic Pharmacometrics: Part 1 – Data Assembly
Pharmacometric modeling and simulation (M&S) is moving from merely describing pharmacokinetic (PK) and pharmacodynamic (PD) phenomena to informing critical drug development and regulatory decision-making…
Population PK/PD Modeling of Efficacy and Safety of CB1R Inverse Agonist Taranabant in Obese Patients
Taranabant is a cannabinoid-1 receptor (CB1R) inverse agonist, that was being developed by Merck and Co., Inc. as a potential treatment of obesity.
Simulation of Food Effect on Cilostazol Exposure in Human
For certain drugs, the time of administration respective to meal times can have a significant impact on exposure. The effect of food is usually attributed to increased solubility/dissolution rate and/or…
Improving the Efficiency and Ensuring the Quality of Data Assembly for Pharmacometric Analysis
Better tools and processes can improve the efficiency of data assembly and the quality of analysis-ready datasets for pharmacometric analyses.
Modeling and Simulation Approach to Pediatric Drug Development
Describe a process for determining pediatric drug doses using pharmacokinetic/pharmacodynamic (PK/PD) modeling and simulation.
Prediction of Dose-Dependent Intestinal and Liver First Pass Extraction for CYP3A4 Substrates
Cilostazol and midazolam absorption and pharmacokinetics were simulated using GastroPlus™. The program’s Advanced Compartmental and Transit model described the absorption and intestinal metabolism of both…
Physiologically-Based Model for Fluvoxamine Disposition and Prediction of Drug-Drug Interactions
Fluvoxamine absorption and pharmacokinetics were simulated using GastroPlus™. The program’s Advanced Compartmental and Transit model described the absorption; pharmacokinetics was simulated with a…
Prediction of drug -drug interactions for fluconazole using PBPK – a case with concentration-dependent liver:plasma partition coefficient
Fluconazole is an antifungal agent widely used in the clinical setting for the treatment of candidiasis and meningitis. It undergoes minimal metabolism and is excreted renally(1). Fluconazole is a moderate…
Modeling Drug Disposition in Ocular Tissues following Topical Eye Drops and Intravitreal Injection
The purpose of this study was to model the ocular absorption, distribution and clearance of clonidine and voriconazole from topical and intravitreal applications, respectively. Clonidine is a potent…
Development of a Steady-State Exposure-Response Model for Exenatide Once Weekly
Exenatide is dosed as a subcutaneous (SC) injection of 5 and 10 μg twice daily (BID) before main meals and is indicated for the treatment of type 2 diabetes mellitus in patients failing to achieve adequate…
Omeprazole: Physiologically Based Pharmacokinetic (PBPK) Modeling and Prediction of Drug-Drug Interactions (DDI)
To optimize a PBPK model of omeprazole for prediction of DDIs with respect to polymorphic expression of CYP enzymes. Omeprazole absorption and pharmacokinetics were simulated using GastroPlus™.
Azole Antifungals: Physiologically-Based Pharmacokinetic (PBPK) Modeling and Prediction of Drug-Drug Interactions (DDIs)
Develop PBPK models for azole antifungals for prediction of DDIs. The absorption and pharmacokinetics of azole antifungals were simulated using GastroPlus™. The program's Advanced Compartmental and…
Azole Antifungals: Physiologically-Based Pharmacokinetic (PBPK) Modeling and Prediction of Drug-drug Interactions (DDIs)
Download the poster presented at the Rosenon conference in 2009 on the development of PBPK models for common azole antifungals and DDI predictions