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Assessment of Inter-individual Variability in Predicted Phenytoin Clearance Blog Post

The objective of this study was to assess the inter-individual variability in phenytoin (PHT) clearance predicted from in vitro kinetic data. The Simcyp Population-based ADME Simulator was used to predict…

Pre-clinical Assessment of the Absorption, Distribution, Metabolism, and Excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an Orally Bioavailable Systemic Hedgehog Signaling Pathway Inhibitor Blog Post

GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide) is a potent, selective Hedgehog (Hh) signalling pathway inhibitor being developed for the treatment of various cancers. The in vivo clearance of GDC-0449 was estimated to be 23.0,…

Prediction of Phase 1 Single-dose Pharmacokinetics Using Recombinant Cytochromes P450 and Physiologically-based Modeling Blog Post

1. Ten compounds from the Merck Research Laboratories pipeline were selected to evaluate the utility of using intrinsic clearance derived from recombinantly expressed cytochromes P450 (CYP) and physiologically based pharmacokinetic modelling to predict Phase I pharmacokinetics using simCYP®. The compounds selected were…

In Vitro Inhibition of Multiple Cytochrome P450 Isoforms by Xanthone Derivatives from Mangosteen Extract Blog Post

Mangosteen is a xanthone-containing fruit found in Southeast Asia for which health claims include maintaining healthy immune and gastrointestinal systems to slowing the progression of tumor growth and neurodegenerative diseases. Previous studies…

Excluding Venous Thromboembolism Using Point of Care D-dimer Tests in Outpatients: A Diagnostic Meta-analysis Blog Post

This article is a review the evidence on the diagnostic accuracy of the currently available point of care D-dimer tests for excluding venous thromboembolism. We conducted a systematic review of…

Comparison of Different Algorithms for Predicting Clinical Drug-drug Interactions, Based on the Use of CYP3A4 In Vitro Data: Predictions of Compounds as Precipitants of Interaction Blog Post

Cytochrome P450 3A4 (CYP3A4) is the most important enzyme in drug metabolism and because it is the most frequent target for pharmacokineticdrug-drug interactions (DDIs) it is highly desirable to be able to…

Pharmacokinetic Analysis of Capsaicin After Topical Administration of a High-concentration Capsaicin Patch to Patients With Peripheral Neuropathic Pain Blog Post

Capsaicin, a pungent compound in chili peppers, is a highly selective agonist for the transient receptor potential vanilloid 1 receptor expressed in nociceptive sensory nerves. A high-concentration (640 μg/cm2) capsaicin…

The Conduct of In Vitro Studies to Address Time-dependent Inhibition of Drug-metabolizing Enzymes: A Perspective of the Pharmaceutical Research and Manufacturers of America (PhRMA) Blog Post

Time-dependent inhibition (TDI) of cytochrome P450 (P450) enzymes caused by new molecular entities (NMEs) is of concern because such compounds can be responsible for clinically relevant drug-drug interactions (DDI). Although…

In Vitro and In Vivo Induction of Cytochrome p450: A Survey of the Current Practices and Recommendations: A Pharmaceutical Research and Manufacturers of America Perspective Blog Post

Cytochrome P450 (P450) induction is one of the factors that can affect the pharmacokinetics of a drug molecule upon multiple dosing, and it can result in pharmacokinetic drug-drug interactions with coadministered drugs causing potential…

Assessing the Efficiency of Mixed Effects Modeling in Quantifying Metabolism-based Drug-drug Interactions: Using In Vitro Data as an Aid to Assess Study Power Blog Post

The clinical assessment of metabolic drug-drug interactions (mDDI) may involve population-based pharmacokinetic (POPPK) assessment as part of Phase 3 clinical trials. The elements of such POPPK study design have not…

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