In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function by di Iulio Julia, Fayet Aurélie, Arab-Alameddine Mona, Rotger Margalida, Lubomirov Rubin, Cavassini Matthias, Furrer Hansjakob, Günthard Huldrych F, Colombo Sara, Csajka Chantal, Eap Chin B, Decosterd Laurent A, Telenti Amalio, Swiss HIV Cohort Study in Pharmacogenetics and genomics (2009). PubMed

Abstract

The antiretroviral drug efavirenz (EFV) is extensively metabolized into three primary metabolites: 8-hydroxy-EFV, 7-hydroxy-EFV and N-glucuronide-EFV. There is a wide interindividual variability in EFV plasma exposure, explained to a great extent by cytochrome P450 2B6 (CYP2B6), the main isoenzyme responsible for EFV metabolism and involved in the major metabolic pathway (8-hydroxylation) and to a lesser extent in 7-hydroxylation. When CYP2B6 function is impaired, the relevance of CYP2A6, the main isoenzyme responsible for 7-hydroxylation may increase. We hypothesize that genetic variability in this gene may contribute to the particularly high, unexplained variability in EFV exposure in individuals with limited CYP2B6 function.

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