Glucuronidation of DRF-6574, hydroxy metabolite of DRF-4367 (a novel COX-2 inhibitor) by pooled human liver, intestinal microsomes and recombinant human UDP-glucuronosyltransferases (UGT): Role of UGT1A1,1A3 and 1A8

@article{Muzeeb2010GlucuronidationOD,
  title={Glucuronidation of DRF-6574, hydroxy metabolite of DRF-4367 (a novel COX-2 inhibitor) by pooled human liver, intestinal microsomes and recombinant human UDP-glucuronosyltransferases (UGT): Role of UGT1A1,1A3 and 1A8},
  author={S. Muzeeb and S. J. S. Basha and D. Shashikumar and R. Mullangi and N. Srinivas},
  journal={European Journal of Drug Metabolism and Pharmacokinetics},
  year={2010},
  volume={31},
  pages={299-309}
}
  • S. Muzeeb, S. J. S. Basha, +2 authors N. Srinivas
  • Published 2010
  • Biology, Medicine
  • European Journal of Drug Metabolism and Pharmacokinetics
    • SummaryDRF-4367 is a novel COX-2 inhibitor, which showed good efficacy in several animal models of inflammation. In a comparative in vitro metabolism in various liver microsomes, DRF-4367 forms a hydroxy metabolite (DRF-6574) mediated by CYP2D6 and 2C19 isoenzymes. DRF-6574 readily undergoes Phase-II metabolism and forms glucuronide and sulfate conjugates both in vitro and in vivo. The objective of the present study was two folds: to study the glucuronidation of DRF-6574 in human liver and… CONTINUE READING
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