Prediction of human drug-drug interactions from time-dependent inactivation of CYP3A4 in primary hepatocytes using a population-based simulator.

@article{Xu2009PredictionOH,
  title={Prediction of human drug-drug interactions from time-dependent inactivation of CYP3A4 in primary hepatocytes using a population-based simulator.},
  author={Lilly Xu and Yuping Chen and Yvonne Pan and Gary L. Skiles and Magang Shou},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2009},
  volume={37 12},
  pages={2330-9}
}
Time-dependent inactivation (TDI) of human cytochromes P450 3A4 (CYP3A4) is a major cause of clinical drug-drug interactions (DDIs). Human liver microsomes (HLM) are commonly used as an enzyme source for evaluating the inhibition of CYP3A4 by new chemical entities. The inhibition data can then be extrapolated to assess the risk of human DDIs. Using this approach, under- and overpredictions of in vivo DDIs have been observed. In the present study, human hepatocytes were used as an alternative to… CONTINUE READING

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