CYP2C8 and CYP3A4 are the principal enzymes involved in the human <i>in vitro</i> biotransformation of the insulin secretagogue repaglinide

Abstract

The results confirm an important role for both CYP3A4 and CYP2C8 in the human in vitro biotransformation of repaglinide. This dual CYP biotransformation may have consequences for the clinical pharmacokinetics and drug-drug interactions involving repaglinide if one CYP pathway has sufficient capacity to compensate if the other is inhibited.