In vitro analysis and quantitative prediction of efavirenz inhibition of eight cytochrome P450 (CYP) enzymes: major effects on CYPs 2B6, 2C8, 2C9 and 2C19.

@article{Xu2013InVA,
  title={In vitro analysis and quantitative prediction of efavirenz inhibition of eight cytochrome P450 (CYP) enzymes: major effects on CYPs 2B6, 2C8, 2C9 and 2C19.},
  author={Cong Xu and Zeruesenay Desta},
  journal={Drug metabolism and pharmacokinetics},
  year={2013},
  volume={28 4},
  pages={362-71}
}
In order to quantitatively predict drug interactions associated with efavirenz-based anti-HIV therapy, we evaluated reversible and time-dependent inhibitions of efavirenz on eight cytochrome P450 (CYP) enzymes in vitro. The present study showed that efavirenz was a potent competitive inhibitor of CYP2B6 (average K(i) = 1.68 µM in HLMs and K(i) = 1.38 µM in expressed CYP2B6) and CYP2C8 (K(i) = 4.78 µM in pooled HLMs and K(i) = 4.80 µM in HLMs with CYP2C8*3/*3 genotype). Efavirenz was a moderate… CONTINUE READING

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