Stereospecific Metabolism of Itraconazole by CYP3A4: Dioxolane Ring Scission of Azole Antifungals
نویسندگان
چکیده
منابع مشابه
Stereospecific metabolism of itraconazole by CYP3A4: dioxolane ring scission of azole antifungals.
Itraconazole (ITZ) is a mixture of four cis-stereoisomers that inhibit CYP3A4 potently and coordinate CYP3A4 heme via the triazole nitrogen. However, (2R,4S,2'R)-ITZ and (2R,4S,2'S)-ITZ also undergo stereoselective sequential metabolism by CYP3A4 at a site distant from the triazole ring to 3'-OH-ITZ, keto-ITZ, and N-desalkyl-ITZ. This stereoselective metabolism demonstrates specific interaction...
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ژورنال
عنوان ژورنال: Drug Metabolism and Disposition
سال: 2011
ISSN: 0090-9556,1521-009X
DOI: 10.1124/dmd.111.042739