Article
In-vitro metabolism of celecoxib, a cyclooxygenase-2 inhibitor, by allelic variant forms of human liver microsomal cytochrome P450 2C9: correlation with CYP2C9 genotype and in-vivo pharmacokinetics.
Pharmacogenetics - 1 Apr 2001
Tang C, Shou M, Rushmore T H, Mei Q, Sandhu P, Woolf E J, Rose M J, Gelmann A, Greenberg H E, De Lepeleire I, Van Hecken A, De Schepper P J, Ebel D L, Schwartz J I, Rodrigues A D
Abstract excerpt
In-vitro studies were conducted to assess the impact of CYP2C9 genotype on the metabolism (methyl hydroxylation) and pharmacokinetics of celecoxib, a novel cyclooxygenase-2 inhibitor and CYP2C9 substrate. When compared to cDNA-expressed wild-type CYP2C9 (CYP2C9*1), the Vmax/Km ratio for celecoxib methyl hydroxylation was reduced by 34% and 90% in the presence of recombinant CYP2C9*2 and CYP2C9*3, respectively....
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