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Application of CYP3A4 In Vitro Data to Predict Clinical Drug-drug Interactions: Predictions of Compounds as Objects of Interaction Blog Post

Numerous retrospective analyses have shown the utility of in vitro systems for predicting potential drug-drug interactions (DDIs). Prediction of DDIs from in vitro data is commonly obtained using estimates of enzyme KI, inhibitor and substrate concentrations and absorption…

CYP2D6 is Primarily Responsible for the Metabolism of Clomiphene Blog Post

Clomiphene is a first line treatment for anovulation, a common cause of infertility. Response to clomiphene is variable and unpredictable. Tamoxifen is structurally related to clomiphene, and also shows considerable…

The Effects of CYP3A4 Inhibition on Erlotinib Pharmacokinetics: Computer-based Simulation (Simcyp) Predicts In Vivo Metabolic Inhibition Blog Post

BACKGROUND: Erlotinib is an orally active antitumor agent. Analyses in vitro using human liver microsomes and recombinant enzymes showed thaterlotinib was metabolized primarily by CYP3A4, with a secondary contribution from CYP1A2. METHODS: A computer-based simulation model, SimCYP®,…

Comparison of Different Approaches to Predict Metabolic Drug-drug Interactions Blog Post

Three approaches were compared to predict the actual magnitude of drug interaction (the mean fold-change in the area under the curve (AUC)) of reversible or irreversible (mechanism-based) cytochrome P450 (CYP) inhibitors. These were: (1)…

Disparity in Holoprotein/Apoprotein Ratios of Different Standards Used for Immunoquantification of Hepatic Cytochrome P450 Enzymes Blog Post

An analysis of reported hepatic abundances of CYP3A4 and 3A5 indicated that values determined by immunoquantification using commercially available, unpurified recombinant enzymes as standards are significantly lower than those determined…

Inactivation of CYP2D6 by Methylenedioxymethamphetamine in Different Recombinant Expression Systems Blog Post

Recombinantly expressed CYP450 systems (rCYPs) are often used to screen for irreversible/quasi-irreversible enzyme inhibitors during drug development. The concentration- and time-dependent inactivation of CYP2D6 by methylenedioxymethamphetamine (MDMA) was compared in…

The Use of Mechanistic DM-PK-PD Modeling to Assess the Power of Pharmacogenetic Studies—CYP2C9 and Warfarin as an Example Blog Post

The aim of this study was to assess the power of in vivo studies needed to discern the effect of genotype on pharmacokinetics (PK) and pharmacodynamics (PD) using CYP2C9 and…

Kinetics of the Time-dependent Inactivation of CYP2D6 in Cryopreserved Human Hepatocytes by Methylenedioxymethamphetamine (MDMA) Blog Post

Methylenedioxymethamphetamine (MDMA) was investigated in cryopreserved human hepatocytes as a time-dependent inactivator (TDI) of CYP2D6 using dextromethorphan (DEX) as a probe substrate. Inhibition kinetic parameters kinact, the maximal rate of…

The Problems in Scaling Adult Drug Doses to Children Blog Post

Many drugs are unlicensed in children and consequently their doses have been scaled down from those used in adults. The objective of this study was to compare the performance of…

Predictive Population Pharmacokinetic/Pharmacodynamic Model for a Novel COX-2 Inhibitor Blog Post

The objectives of these analyses were to (1) develop a population pharmacokinetic/pharmacodynamic model for a novel COX-2 inhibitor (CS-706) using data from primarily Caucasian subjects, (2) predict responses in subpopulations…

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