Last reviewed 2026-04-22 · How we verify

Etravirine (ETR)

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to HIV-1 reverse transcriptase and blocks its ability to convert viral RNA into DNA.

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to HIV-1 reverse transcriptase and blocks its ability to convert viral RNA into DNA. Used for HIV-1 infection in treatment-experienced patients with NNRTI resistance, HIV-1 infection in antiretroviral-experienced adults.

At a glance

Mechanism of action

Etravirine inhibits HIV-1 reverse transcriptase through a non-competitive binding mechanism, preventing the enzyme from synthesizing viral DNA from the viral RNA genome. This blocks HIV replication and reduces viral load in infected individuals. It is particularly effective against certain drug-resistant HIV strains due to its unique binding interactions with the reverse transcriptase enzyme.

Approved indications

• HIV-1 infection in treatment-experienced patients with NNRTI resistance
• HIV-1 infection in antiretroviral-experienced adults

Common side effects

• Rash
• Nausea
• Diarrhea
• Headache
• Vomiting
• Abdominal pain

Key clinical trials

• TMC125-TiDP35-C239 - Continued Access to Etravirine (ETR) in Treatment Experienced HIV-1 Infected Participants (PHASE3)
• Pharmacokinetic Study of Antiretroviral Drugs and Related Drugs During and After Pregnancy
• Drug-drug Interaction (DDI) Study of GSK3640254 With Darunavir/Ritonavir (DRV/RTV) and Etravirine (ETR) (PHASE1)
• Switch Strategy From Etravirine (ETR) to Doravirine (DOR) in Virologically-Suppressed HIV-1 Infected Adults With ETR-Resistance (PHASE4)
• Evaluating the Safety and Tolerability of Etravirine in HIV-1 Infected Infants and Children (PHASE1, PHASE2)
• Capacity of the Dual Combination Raltegravir/Etravirine to Maintain Virological Success in HIV-1 Infected Patients of at Least 45 Years of Age- ANRS 163 ETRAL (PHASE2)
• Study to Evaluate Switching to Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (E/C/F/TAF) Fixed Dose Combination (FDC) in Virologically-Suppressed HIV-1 Infected Adults Harboring the Archived Isolated NRTI Resistance Mutation M184V/M184I (PHASE3)
• Switching From a Tenofovir Disoproxil Fumarate (TDF) Containing Regimen to Elvitegravir/Cobicistat/Emtricitabine/ Tenofovir Alafenamide (E/C/F/TAF) Fixed-Dose Combination (FDC) in Virologically-Suppressed, HIV-1 Infected Adults Aged ≥ 60 Years (PHASE3)

Primary sources

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