The metabolic disposition of aprepitant, a substance P receptor antagonist, in rats and dogs.

@article{Huskey2004TheMD,
  title={The metabolic disposition of aprepitant, a substance P receptor antagonist, in rats and dogs.},
  author={Su-Er W. Huskey and Brian J. Dean and George A. Doss and Zhen Wang and Cornelis Eca Hop and R. Ghadiri Anari and Paul E. Finke and Albert Jean Robichaud and Min Zhang and Bonnie I. Wang and John R Strauss and Paul K. Cunningham and William P. Feeney and Ronald B. Franklin and Thomas A Baillie and Shuet-Hing Lee Chiu},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2004},
  volume={32 2},
  pages={
          246-58
        }
}
The absorption, metabolism, and excretion of [14C]aprepitant, a potent and selective human substance P receptor antagonist for the treatment of chemotherapy-induced nausea and vomiting, was evaluated in rats and dogs. Aprepitant was metabolized extensively and no parent drug was detected in the urine of either species. The elimination of drug-related radioactivity, after i.v. or p.o. administration of [14C]aprepitant, was mainly via biliary excretion in rats and by way of both biliary and… CONTINUE READING

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

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