Repaglinide metabolism by human hepatocytes reveals CYP2C8 dominance and misassignment of CYP3A4 by liver subcellular fractions and recombinant enzymes.
Repaglinide is an antidiabetic agent and Food and Drug Administration-endorsed clinical CYP2C8 probe with a well characterized human disposition profile in which a dicarboxylic acid, M2, is the main metabolite accounting for 66% of the administered dose. The remainder is distributed among M1 (4%), unchanged repaglinide...