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2019•Clinical Pharmacology & TherapeuticsOpen access

Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2B6 and Efavirenz‐Containing Antiretroviral Therapy

Zeruesenay Desta, Roseann S. Gammal, Li Gong, Michelle Whirl‐Carrillo, Aditya H. Gaur, Chonlaphat Sukasem, Jennifer Hockings, Alan L. Myers, Marelize Swart, Rachel F. Tyndale, Collen Masimirembwa, Otito F. Iwuchukwu, Sanika Chirwa, Jeffrey L. Lennox, Andrea Gaedigk, Teri E. Klein, David W. Haas

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Abstract

The HIV type-1 nonnucleoside reverse transcriptase inhibitor, efavirenz, is widely used to treat HIV type-1 infection. Efavirenz is predominantly metabolized into inactive metabolites by cytochrome P450 (CYP)2B6, and patients with certain CYP2B6 genetic variants may be at increased risk for adverse effects, particularly central nervous system toxicity and treatment discontinuation. We summarize the evidence from the literature and provide therapeutic recommendations for efavirenz prescribing based on CYP2B6 genotypes.

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What this paper is about

The HIV type-1 nonnucleoside reverse transcriptase inhibitor, efavirenz, is widely used to treat HIV type-1 infection. Efavirenz is predominantly metabolized into inactive metabolites by cytochrome P450 (CYP)2B6, and patients with certain CYP2B6 genetic variants may be at increased risk for adverse effects, particularly central nervous system toxicity and treatment discontinuation. We summarize the evidence from the literature and provide therapeutic recommendations for efavirenz prescribing based on CYP2B6 genotypes.

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Available abstract

The HIV type-1 nonnucleoside reverse transcriptase inhibitor, efavirenz, is widely used to treat HIV type-1 infection. Efavirenz is predominantly metabolized into inactive metabolites by cytochrome P450 (CYP)2B6, and patients with certain CYP2B6 genetic variants may be at increased risk for adverse effects, particularly central nervous system toxicity and treatment discontinuation. We summarize the evidence from the literature and provide therapeutic recommendations for efavirenz prescribing based on CYP2B6 genotypes.

Key concepts: Efavirenz, CYP2B6, Discontinuation, Medicine, Reverse-transcriptase inhibitor, Pharmacogenetics, Adverse effect, Guideline

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