CYP3A4 drug interactions: correlation of 10 in vitro probe substrates

• Published in: British journal of clinical pharmacology Vol. 48; no. 5; pp. 716 - 727
• Main Authors: KENWORTHY, K. E, BLOOMER, J. C, CLARKE, S. E, HOUSTON, J. B
• Format: Journal Article Conference Proceeding
• Language: English
• Published: Oxford, UK Blackwell Science Ltd 01.11.1999; Blackwell Science; Blackwell Science Inc
• Subjects: allostery; Biological and medical sciences; CYP3A4; Cytochrome P-450 CYP1A1 - metabolism; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System - metabolism; cytochrome P450 inhibition; Enzyme Inhibitors - pharmacology; General pharmacology; Humans; in vitro probes; Kinetics; Medical sciences; Mixed Function Oxygenases - antagonists & inhibitors; Mixed Function Oxygenases - metabolism; Original; Pharmaceutical Preparations - metabolism; Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions; Pharmacology. Drug treatments; Recombinant Proteins - antagonists & inhibitors; Recombinant Proteins - metabolism; Substrate; Drug combination; Enzymatic activity; Isozyme; Cytochrome P450; Enzyme inhibitor; Drug interaction; Inhibition; Measurement method; Metabolism; Pharmacokinetics; In vitro

Aims Many substrates of cytochrome P450 (CYP) 3A4 are used for in vitro investigations of drug metabolism and potential drug–drug interactions. The aim of the present study was to determine the relationship between 10 commonly used CYP3A4 probes using modifiers with a range of inhibitory potency. Me...