Université Paris Diderot, Sorbonne Paris Cité, Paris, France.
Division of Clinical Pharmacokinetics and Pharmacometrics, Institut de Recherches Internationales Servier, Suresnes, France.
Antimicrob Agents Chemother. 2017 Nov 22;61(12). doi: 10.1128/AAC.00733-17. Print 2017 Dec.
Nevirapine is metabolized by several hepatic cytochrome P450 (CYP) isoforms to generate four primary hydroxylated metabolites: 2-hydroxynevirapine, 3-hydroxynevirapine, 8-hydroxynevirapine, and 12-hydroxynevirapine. The present study characterized associations between genetic polymorphisms and metabolite ratios in HIV-infected Cambodians. We demonstrate associations between polymorphisms and metabolite ratios for both 3-hydroxynevirapine and 8-hydroxynevirapine, suggesting involvement of CYP2B6 in generating these metabolites.
奈韦拉平通过多种肝细胞色素 P450(CYP)同工酶代谢生成四种主要的羟化代谢产物:2-羟基奈韦拉平、3-羟基奈韦拉平、8-羟基奈韦拉平、和 12-羟基奈韦拉平。本研究描述了柬埔寨 HIV 感染者中遗传多态性与代谢产物比值之间的相关性。我们证明了 3-羟基奈韦拉平和 8-羟基奈韦拉平的代谢产物比值与遗传多态性之间存在相关性,表明 CYP2B6 参与了这些代谢产物的生成。