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Article

Effect of CYP3A5 expression on the inhibition of CYP3A-catalyzed drug metabolism: impact on modeling CYP3A-mediated drug-drug interactions.

Drug metabolism and disposition: the biological fate of chemicals - 1 Aug 2013

Shirasaka Yoshiyuki, Chang Shu-Ying, Grubb Mary F, Peng Chi-Chi, Thummel Kenneth E, Isoherranen Nina, Rodrigues A David

Abstract excerpt

The purpose of this study was to determine the impact of CYP3A5 expression on inhibitory potency (Ki or IC50 values) of CYP3A inhibitors, using recombinant CYP3A4 and CYP3A5 (rCYP3A4 and rCYP3A5) and CYP3A5 genotyped human liver microsomes (HLMs). IC50 ratios between rCYP3A4 and rCYP3A5 (rCYP3A5/rCYP3A4) of ketoconazole (KTZ) and itraconazole (ITZ) were 8.5 and 8.8 for midazolam (MDZ), 4.7 and 9.1 for...

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PMID: 23723360
DOI: 10.1124/dmd.112.049940
PMCID: PMC3716306

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