Metabolism of MK-0524, a Prostaglandin D2 Receptor 1 Antagonist, in Microsomes and Hepatocytes from Preclinical Species and Humans

@article{Dean2007MetabolismOM,
  title={Metabolism of MK-0524, a Prostaglandin D2 Receptor 1 Antagonist, in Microsomes and Hepatocytes from Preclinical Species and Humans},
  author={B. Dean and S. Chang and M. Elipe and Y. Xia and M. Braun and Eric D. Soli and Yuming Zhao and R. Franklin and B. Karanam},
  journal={Drug Metabolism and Disposition},
  year={2007},
  volume={35},
  pages={283 - 292}
}
  • B. Dean, S. Chang, +6 authors B. Karanam
  • Published 2007
  • Medicine, Chemistry
  • Drug Metabolism and Disposition
  • (3R)-4-(4-Chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl acetic acid (MK-0524) is a potent orally active human prostaglandin D2 receptor 1 antagonist that is currently under development for the prevention of niacin-induced flushing. The major in vitro and in vivo metabolite of MK-0524 is the acyl glucuronic acid conjugate of the parent compound, M2. To compare metabolism of MK-0524 across preclinical species and humans, studies were undertaken to determine… CONTINUE READING
    Influence of Laropiprant, a Selective Prostaglandin D2 Receptor 1 Antagonist, on the Pharmacokinetics and Pharmacodynamics of Warfarin
    • 6
    • Highly Influenced
    • Open Access

    References

    Publications referenced by this paper.
    SHOWING 1-10 OF 25 REFERENCES
    Human UGT2B7 catalyzes morphine glucuronidation.
    • 379
    In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites.
    • 11
    Specificity of human UDP-glucuronosyltransferases and xenobiotic glucuronidation.
    • 219
    • Highly Influential
    Bilirubin UDP-glucuronosyltransferase 1 is the only relevant bilirubin glucuronidating isoform in man.
    • 362
    • Highly Influential