Investigation on the hydroxylation metabolism of imrecoxib in vivtro by using recombinant human CYPs

AimTo identify the drug-metabolizing enzymes involved in the hydroxylation of the new anti-inflammatory and anodyne imrecoxib. MethodsImrecoxib was incubated with heterologous expression human cytochrome P450 (rCYPs) in vivtro, and metabolites and remained parent drug were detected with liquid chromatography-multistage mass spectrometry. The contribution of 4 CYPs in the hydroxylation metabolism of imrecoxib was evaluated by total normalized rate (TNR) method. Results Imrecoxib is metabolized by CYP2C9, CYP2D6 and CYP3A4, with the rate of 62.5%, 21.1% and 16.4%, respectively. ConclusionCYP2C9 is the major enzyme involved in imrecoxib hydroxylation metabolism.