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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    References

    SHOWING 1-10 OF 73 REFERENCES
    Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of posaconazole (Noxafil).
    • 146
    • PDF
    Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7.
    • Z. Cheng, G. Rios, +5 authors T. Tephly
    • Chemistry, Medicine
    • Toxicological sciences : an official journal of the Society of Toxicology
    • 1998
    • 95
    • PDF
    UDP-glucuronosyltransferases and clinical drug-drug interactions.
    • 484
    Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
    • 1,374