In vitro assessment of drug-drug interaction potential of boceprevir associated with drug metabolizing enzymes and transporters.

@article{Chu2013InVA,
  title={In vitro assessment of drug-drug interaction potential of boceprevir associated with drug metabolizing enzymes and transporters.},
  author={Xiao-yan Chu and Xiaoxin Cai and Donghui Cui and Cuyue Tang and Anima Ghosal and Grace Chan and Mitchell D. Green and Yuhsin Kuo and Yuexia Liang and Cheri M Maciolek and Jairam R. Palamanda and Raymond Evers and Thomayant Prueksaritanont},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2013},
  volume={41 3},
  pages={
          668-81
        }
}
The inhibitory effect of boceprevir (BOC), an inhibitor of hepatitis C virus nonstructural protein 3 protease was evaluated in vitro against a panel of drug-metabolizing enzymes and transporters. BOC, a known substrate for cytochrome P450 (P450) CYP3A and aldo-ketoreductases, was a reversible time-dependent inhibitor (k(inact) = 0.12 minute(-1), K(I) = 6.1 µM) of CYP3A4/5 but not an inhibitor of other major P450s, nor of UDP-glucuronosyltransferases 1A1 and 2B7. BOC showed weak to no inhibition… CONTINUE READING

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