Metabolism of amprenavir in liver microsomes: role of CYP3A4 inhibition for drug interactions.

@article{Decker1998MetabolismOA,
  title={Metabolism of amprenavir in liver microsomes: role of CYP3A4 inhibition for drug interactions.},
  author={Caroline J Decker and Leena Laitinen and G W Bridson and Scott A. Raybuck and Roger D. Tung and Pravin R Chaturvedi},
  journal={Journal of pharmaceutical sciences},
  year={1998},
  volume={87 7},
  pages={803-7}
}
Amprenavir (141W94, VX-478, KVX-478) is metabolized primarily by CYP3A4 (cytochrome P450 3A4) in recombinant systems and human liver microsomes (HLM). The effects of ketoconazole, terfenadine, astemizole, rifampicin, methadone, and rifabutin upon amprenavir metabolism were examined in vitro using HLM. Ketoconazole, terfenadine, and astemizole were observed to inhibit amprenavir depletion, consistent with their known specificity for CYP3A4. The HIV protease inhibitors, indinavir, saquinavir… CONTINUE READING