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Efavirenz (Sustiva)

Raw research findings for this medication. Mostly single studies, not curated or confirmed robust.

About Efavirenz

What it is

Efavirenz is an HIV medicine of the NNRTI group (non-nucleoside reverse transcriptase inhibitors): it blocks reverse transcriptase, the enzyme HIV needs to copy itself into a cell's DNA. It is taken together with other HIV medicines. It is sold as Sustiva, among other names, and is part of several combination tablets.

How genes come into it

Efavirenz is broken down mainly by the liver enzyme CYP2B6. The common variant CYP2B6*6 (which carries rs3745274) makes the enzyme work more slowly; people with two slow copies, up to about 1 in 5 in some African populations, have much higher blood levels, with more side effects such as dizziness, vivid dreams and trouble sleeping. CPIC and DPWG have published guidelines on CYP2B6 and efavirenz. Studies have also looked at CYP2A6, the transporter ABCB1 and other genes, with weaker evidence.

Published guidelines

Clinical guidelines that name a gene for Efavirenz. They sort people into groups by the gene copies they carry.

CPIC guideline: CYP2B6. Ultrarapid Metabolizer · Rapid Metabolizer · Normal Metabolizer · Intermediate Metabolizer · Poor Metabolizer · Indeterminate. Strong. 2019.

DPWG guideline: CYP2B6. Ultrarapid Metabolizer · Rapid Metabolizer · Normal Metabolizer · Intermediate Metabolizer · Poor Metabolizer · Indeterminate.

US FDA: CYP2B6. Poor Metabolizer. Data that Indicate a Potential Impact on Safety or Response.

What research found

Every published finding on gene variants and Efavirenz. Upload your DNA file to see which of these rows apply to you.

Rated evidence (33 rated variants)

PharmGKB weighs all studies of a variant and rates how strong the evidence is, from 1A (strongest) to 4.

CYP2B6 rs3745274: Level 1A · replicated. Metabolism/PK: HIV infectious disease. 78.

CYP2B6 CYP2B6*1, CYP2B6*4, CYP2B6*6, CYP2B6*9, CYP2B6*18, CYP2B6*28: Level 1A · replicated. Metabolism/PK: HIV infectious disease. 44.

CYP2B6 rs3745274: Level 1A · replicated. Toxicity: HIV infectious disease. 29.

CYP2B6 CYP2B6*1, CYP2B6*2, CYP2B6*6, CYP2B6*18, CYP2B6*38: Level 1A · replicated. Toxicity: HIV infectious disease. 12.

Metabolism (249 findings)

Studies of how quickly the body processes this medication.

ABCB1 rs1045642: Genotype AG is associated with increased concentrations of efavirenz in people with HIV Infections as compared to genotype GG.

ABCB1 rs1045642: Genotype GG is associated with increased concentrations of efavirenz in people with HIV Infections as compared to genotypes AA + AG.

ABCB1 rs1045642: Genotype AA is associated with decreased concentrations of efavirenz in people with HIV Infections as compared to genotypes AG + GG.

ABCB1 rs2032582: Genotype AA is associated with decreased concentrations of efavirenz in people with HIV Infections as compared to genotypes AC + CC.

Response (24 findings)

Studies of how well it worked in people carrying a variant.

CYP2B6 rs2279343: Genotypes AG + GG is associated with increased clinical benefit to efavirenz, lamivudine and tenofovir in people with HIV Infections as compared to genotype AA.

CYP2B6 rs3745274: Genotypes GT + TT are associated with decreased resistance to efavirenz in people with HIV Infections as compared to genotype GG.

CYP2B6 rs3745274: Allele T is associated with increased response to efavirenz or non-nucleoside reverse transcriptase inhibitors in women with HIV Infections as compared to genotype GG.

CYP2B6 rs3745274: Genotype TT is associated with increased response to efavirenz in people with HIV Infections and Tuberculosis as compared to genotypes GG + GT.

Dosing (5 findings)

Studies of how much of the drug people needed or tolerated.

CYP2B6 CYP2B6*1, CYP2B6*6, CYP2B6*26: CYP2B6 *1/*26 + *6/*6 + *6/*26 is associated with decreased dose of efavirenz in people with HIV.

CYP2B6 rs3745274: Genotype GG is associated with increased dose of efavirenz in people with HIV Infections as compared to genotypes GT + TT.

CYP2B6 rs3745274: Genotype TT is associated with decreased dose of efavirenz in people with HIV Infections.

CYP2B6 rs2279343: Genotype GG is associated with decreased dose of efavirenz in men with HIV Infections.

Study findings and evidence levels: PharmGKB (CC BY-SA 4.0). Guidelines: CPIC and DPWG, as bundled in PharmCAT. Most studies were done mainly in people of European ancestry.

Related Drugs

More drugs from the same category

Intelence (NNRTIs)

NNRTIs (class) (NNRTIs)

Viramune (NNRTIs)

Not a prescribing recommendation. This page is educational information about pharmacogenomic research and clinical guidelines - it is not medical or dosing advice, and not a prediction of how any medication will work for you. Never start, stop, or change a medication or dose based on it; talk to your doctor or pharmacist, who can order clinical-grade testing if appropriate.

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Content updated September 2026.

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