Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).

Journal Article

Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx) were prepared by synthetic or biosynthetic methods. Metabolites include products of oxidation, glucuronidation, reduction and hydrolytic ring opening. Based on an in vitro whole blood assay, none of the known human metabolites of rofecoxib inhibits COX-1 nor contributes significantly to the inhibition of COX-2.

Full Text

Duke Authors

Cited Authors

  • Nicoll-Griffith, DA; Yergey, JA; Trimble, LA; Silva, JM; Li, C; Chauret, N; Gauthier, JY; Grimm, E; Léger, S; Roy, P; Thérien, M; Wang, Z; Prasit, P; Zamboni, R; Young, RN; Brideau, C; Chan, CC; Mancini, J; Riendeau, D

Published Date

  • December 2000

Published In

Volume / Issue

  • 10 / 23

Start / End Page

  • 2683 - 2686

PubMed ID

  • 11128651

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(00)00538-2

Language

  • eng