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Physiologically-based PharmacoKinetic (PBPK) Modeling Tools: How to Fit with Our Needs? Blog Post

In 2005, a survey compared a number of commercial PBPK software available at the time, mainly focusing on ‘ready to use’ modelling tools. Since then, these tools and software have…

Using Simcyp to Project Human Oral Pharmacokinetic Variability in Early Drug Research to Mitigate Mechanism-based Adverse Events Blog Post

Positive allosteric modulators (‘potentiators’) of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) have been shown to display a mechanism-based exposure-response continuum in preclinical species with procognitive electrophysiological and behavioral effects (‘efficacy’) at…

Evaluation of Methods for Achieving Stable INR in Healthy Subjects During a Multiple-dose Warfarin Study Blog Post

No consistent method is available for finding stable warfarin maintenance doses and fast stabilization of international normalized ratio (INR) values among healthy subjects in experimental warfarin interaction studies. Using data…

Mechanism-based Population Modeling of the Effects of Vildagliptin on GLP-1, Glucose, and Insulin in Patients with Type 2 Diabetes Blog Post

The aim of this study was to build a mechanism-based population pharmacodynamic model to describe and predict the time course of active GLP-1, glucose and insulin in type 2 diabetic…

Interactions Between Buprenorphine and the Protease Inhibitors Darunavir-ritonavir and Fosamprenavir-ritonavir Blog Post

This study examined drug interactions between buprenorphine, a partial opioid agonist used for opioid dependence treatment and pain management, and the protease inhibitors (PIs) darunavir-ritonavir and fosamprenavir-ritonavir. The pharmacokinetics of…

Effect of Ketoconazole on the Pharmacokinetics of Axitinib in Healthy Volunteers Blog Post

Axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, is metabolized primarily by cytochrome P450 (CYP) 3A with minor contributions from…

Phase 1 Safety, Pharmacokinetic and Pharmacodynamic Trial of BMS-599626 (AC480), an Oral Pan-HER Receptor Tyrosine Kinase Inhibitor, in Patients with Advanced Solid Tumors Blog Post

We studied the safety, tolerability, and recommended dose of BMS-599626, an orally bioavailable inhibitor of the human epidermal growth factor receptor (HER) family of receptor tyrosine kinases. Patients with advanced…

Brain Uptake of the Drug of Abuse Gamma-hydroxybutyric Acid in Rats Blog Post

γ-Hydroxybutyric acid (GHB) is an endogenous compound and a substrate for the ubiquitous monocarboxylate transporter (MCT) family. GHB is also a drug of abuse due to its sedative/hypnotic and euphoric…

Preliminary Comparison of Sertraline Levels in Postbariatric Surgery Patients Versus Matched Non-surgical Cohort Blog Post

Roux-en-Y gastric bypass (RYGB) is the most frequent bariatric procedure performed in the United States, with thousands performed. Because of the changes to the gastrointestinal tract, the potential exists for…

Effects of Omeprazole and Genetic Polymorphism of CYP2C19 on the Clopidogrel Active Metabolite Blog Post

Clopidogrel is an antiplatelet agent widely used in cardiovascular diseases and an inactive prodrug that needs to be converted to an active metabolite in two sequential metabolic steps. Several CYP450…

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