Article
Metabolic profile, enzyme kinetics, and reaction phenotyping of β-lapachone metabolism in human liver and intestine in vitro.
Molecular pharmaceutics - 3 Dec 2012
Cheng Xuefang, Liu Fang, Yan Tingting, Zhou Xueyan, Wu Liang, Liao Ke, Wang Guangji, Hao Haiping
Abstract excerpt
β-Lapachone (β-Lap) is an NAD(P)H: quinone oxidoreductase 1 (NQO1) target antitumor drug candidate in phase II clinical trials. The present study aimed to uncover the metabolic profile, enzyme kinetics, and enzyme isoforms for the metabolism of β-Lap in human liver and intestine in vitro. NQO1-mediated quinone reduction and subsequent glucuronidation is the predominant metabolic pathway for β-Lap in humans; a...
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