Integrated in vitro analysis for the in vivo prediction of cytochrome P450-mediated drug-drug interactions.

Unbound IC50 (IC50,u) values of 15 drugs were determined in eight recombinantly expressed human cytochromes P450 (P450s) and human hepatocytes, and the data were used to simulate clinical area under the plasma concentration-time curve changes (δAUC) on coadministration with prototypic CYP2D6 substrates. Significant differences in IC50,u values between enzyme sources were observed for quinidine (0.02 µM […]

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