Bioorganic and Medicinal Chemistry Letters p. 1059 - 1062 (2001)
Update date:2022-09-26
Topics:
Chauret, Nathalie
Yergey, James A
Brideau, Christine
Friesen, Richard W
Mancini, Joseph
Riendeau, Denis
Silva, Jose
Styhler, Angela
Trimble, Laird A
Nicoll-Griffith, Deborah A
Characterization of the metabolites of the COX-2 inhibitor etoricoxib (MK-0663 and L-791, 456) produced in vitro indicate formation of an N-oxide pyridine and hydroxymethyl pyridine that can further be glucuronidated or oxidized to an acid. Significant turnover is observed in human hepatocytes. Several CYPs are involved in the oxidative biotranformations and, from in vitro studies, etoricoxib is not a potent CYP3A4 inducer or inhibitor. Based on an in vitro whole blood assay, none of the metabolites of etoricoxib inhibits COX-1 or contributes significantly to the inhibition of COX-2.
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