System-dependent outcomes during the evaluation of drug candidates as inhibitors of cytochrome P450 (CYP) and uridine diphosphate glucuronosyltransferase (UGT) enzymes: human hepatocytes versus liver microsomes versus recombinant enzymes.

@article{Parkinson2010SystemdependentOD,
  title={System-dependent outcomes during the evaluation of drug candidates as inhibitors of cytochrome P450 (CYP) and uridine diphosphate glucuronosyltransferase (UGT) enzymes: human hepatocytes versus liver microsomes versus recombinant enzymes.},
  author={Andrew Parkinson and Faraz Kazmi and David B. Buckley and Phyllis Yerino and Brian W Ogilvie and Brandy L. Paris},
  journal={Drug metabolism and pharmacokinetics},
  year={2010},
  volume={25 1},
  pages={16-27}
}
The ability of a drug to cause clinically significant drug-drug interactions due to direct or metabolism-dependent inhibition of cytochrome P450 (CYP) can generally be predicted from in vitro studies with human liver microsomes (HLM) or recombinant CYP enzymes, as recommended by the FDA and other regulatory agencies. This review highlights some examples of system-dependent inhibition of CYP and uridine diphosphate glucuronosyltransferase (UGT) enzymes. In the case of CYP enzymes, examples are… CONTINUE READING
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The proton pump inhibitors (PPIs) omeprazole and rabeprazole, but not lansoprazole, are in vitro time-dependent inhibitors of CYP2C19

  • B. L. Paris, P. Yerino, B. W. Ogilvie, A. Parkinson
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