Prediction of Cytochrome P 450 3 a Inhibition by Verapamil Enantiomers and Their Metabolites

@inproceedings{Wang2004PredictionOC,
  title={Prediction of Cytochrome P 450 3 a Inhibition by Verapamil Enantiomers and Their Metabolites},
  author={Yinghong Wang and David R. Jones and Stephen D. Hall},
  year={2004}
}
Verapamil inhibition of CYP3A activity results in many drug-drug interactions with CYP3A substrates, but the mechanism of inhibition is unclear. The present study showed that verapamil enantiomers and their major metabolites [norverapamil and N-desalkylverapamil (D617)] inhibited CYP3A in a timeand concentrationdependent manner by using pooled human liver microsomes and the cDNA-expressed CYP3A4 ( b5). The values of the inactivation kinetic parameters kinact and KI obtained with the cDNA… CONTINUE READING