Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant.

@article{Sanchez2004CytochromeP3,
  title={Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant.},
  author={Rosa I Sanchez and R. W. Y. Wang and Deborah J Newton and Ray Bakhtiar and Ping Lu and S. L. Chiu and David C. Evans and S W Huskey},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2004},
  volume={32 11},
  pages={1287-92}
}
The contribution of human cytochrome P450 (P450) isoforms to the metabolism of aprepitant in humans was investigated using recombinant P450s and inhibition studies. In addition, aprepitant was evaluated as an inhibitor of human P450s. Metabolism of aprepitant by microsomes prepared from baculovirus-expressed human P450s was observed only when CYP1A2, CYP2C19, or CYP3A4 was present in the expression system. Incubation with CYP1A2 and CYP2C19 yielded only products of O-dealkylation, whereas… CONTINUE READING

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