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A Poor Metabolizer of Both CYP2C19 and CYP2D6 Identified by Mechanistic Pharmacokinetic Simulation in a Fatal Drug Poisoning Case Involving Venlafaxine Blog Post

We present a fatal drug poisoning case involving venlafaxine (VEN). The deceased took his medication regularly (including 150 mg VEN twice daily), and nothing in the case or autopsy findings…

Plasma Topiramate Concentrations from Doses Associated with Neuroprotection Against White Matter Injury and Stroke in Two Strains of Rat Pups Blog Post

Cerebral white matter (WM) injury and stroke are common neuropathological injuries in newborns with congenital heart defects (CHDs) requiring surgery. Previous investigations in Long Evans rat pups subjected to hypoxia-ischemia…

Race and Drug Formulation Influence on Mycophenolic Acid Pharmacokinetics in Stable Renal Transplant Recipients Blog Post

Limited mycophenolic acid (MPA) data are available comparing racial influence on mycophenolate mofetil (MMF) and enteric-coated mycophenolate sodium (EC-MPS) pharmacokinetics. Intrapatient MPA pharmacokinetics of MMF versus EC-MPS were compared in…

Pharmacokinetic and Pharmacodynamic Modeling to Determine the Human Dose of ST-246(R) to Protect Against Smallpox Blog Post

Although smallpox has been eradicated, the United States government considers it a “material threat” and has funded the discovery and development of potential therapeutic compounds. As reported here, the human…

Application of Knockout Mouse Models to Investigate the Influence of FcγR on the Pharmacokinetics and Anti-platelet Effects of MWReg30, a Monoclonal Anti-GPIIb Antibody Blog Post

This work evaluates the influence of FcγR on the pharmacokinetics and pharmacodynamics of a rat anti-integrin-αIIb IgG1 monoclonal antibody, MWReg30, in mice. The pharmacokinetics and pharmacodynamics of MWReg30 were investigated…

Nonlinear PK: What Does That Mean? Blog Post

You may come across a phrase like the following and wonder what it means: “… this drug exhibits nonlinear pharmacokinetics …”. An example of a drug that has nonlinear pharmacokinetics...

Why Cmax is a Continuous Variable and Tmax is a Categorical Variable Blog Post

The maximum observed concentration (Cmax) and the time of Cmax (tmax) are both obtained directly from the concentration-time data. In this post, I will review how to determine both of...

What is Quantification Anyway? Blog Post

Bioanalytical analysis is a fundamental tool for the pharmacokineticist. The results of a bioanalysis are the source data for all pharmacokinetic work. Thus a clear understanding of the methodologies and…

Inhibitory Effect of Ketoconazole on the Pharmacokinetics of a Multireceptor Tyrosine Kinase Inhibitor BMS-690514 in Healthy Participants: Assessing the Mechanism of the Interaction with Physiologically-based Pharmacokinetic Simulations Blog Post

BMS-690514, a selective inhibitor of the ErbB and vascular endothelial growth factor receptors, has shown antitumor activity in early clinical development. The compound is metabolized by multiple enzymes, with CYP3A4…

Bioavailability of Intranasal vs. Rectal Diazepam Blog Post

There remains an unmet medical need in the out-of-hospital management of seizure emergencies because older children and adults often refuse treatment with rectal gel due to social objections. We have previously…

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