CYP3A5 Contributes Significantly to CYP3A-mediated Drug Oxidations in Liver Microsomes from Japanese Subjects

• Published in: DRUG METABOLISM AND PHARMACOKINETICS Vol. 19; no. 2; pp. 120 - 129
• Main Authors: Yamaori, Satoshi, Yamazaki, Hiroshi, Iwano, Shunsuke, Kiyotani, Kazuma, Matsumura, Keiko, Honda, Goro, Nakagawa, Kazuko, Ishizaki, Takashi, Kamataki, Tetsuya
• Format: Journal Article
• Language: English; Japanese
• Published: England Elsevier Ltd 2004; Japanese Society for the Study of Xenobiotics
• Subjects: Calcium Channel Blockers - metabolism; CYP3A5; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System - genetics; Cytochrome P-450 Enzyme System - metabolism; Dealkylation; diltiazem; Diltiazem - metabolism; DNA - genetics; DNA Primers; Escherichia coli - metabolism; GABA Modulators - metabolism; Genotype; Humans; Hydroxylation; In Vitro Techniques; Japan; Kinetics; liver; Microsomes, Liver - enzymology; midazolam; Midazolam - metabolism; NADPH-Ferrihemoprotein Reductase - genetics; NADPH-Ferrihemoprotein Reductase - metabolism; Oxidation-Reduction; Pharmaceutical Preparations - metabolism; polymorphism; Reverse Transcriptase Polymerase Chain Reaction; testosterone; Testosterone - metabolism; diltiazem; polymorphism; testosterone; liver; midazolam; CYP3A5

The purpose of this study was to evaluate a contribution of polymorphic cytochrome P450 (CYP) 3A5 to the oxidation of diltiazem, midazolam and testosterone by liver microsomes from Japanese subjects. Twenty-seven liver samples were classified into three groups according to the CYP3A5 genotypes; CYP3...