[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Non-nucleoside reverse transcriptase inhibitors (NNRTIs)](https://durgical.com/en/pharmacology/classes/non-nucleoside-reverse-transcriptase-inhibitors/) › Etravirine

# Etravirine

## NNRTIs?

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

A second-generation NNRTI that stays active against many HIV strains resistant to efavirenz or nevirapine. Rash is its key side effect.

Updated Nov 1, 2026

## Quick facts

**Group**
[Non-nucleoside reverse transcriptase inhibitors (NNRTIs)](https://durgical.com/en/pharmacology/classes/non-nucleoside-reverse-transcriptase-inhibitors/)

**Target**
HIV-1 reverse transcriptase (NNRTI pocket)

**Used for**
HIV-1 infection

**Key effects**
Rash · Diarrhoea and nausea · Body fat changes

**Monitor**
Skin during the first weeks · Liver tests

**ATC**
J05AG04

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**HIV-1 reverse transcriptase (NNRTI pocket)**Etravirine

ⓘ The figure shows etravirine (TMC125) in the NNRTI-binding pocket of HIV-1 reverse transcriptase.

**Target in 3D:** HIV-1 reverse transcriptase (NNRTI pocket). PDB structure 3MEC (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/3MEC) · Drag to rotate · pinch to zoom

Etravirine is a diarylpyrimidine that binds the non-nucleoside pocket of HIV-1 reverse transcriptase, close to the active site, and locks the enzyme in an inactive shape. Its flexible structure lets it adapt to the pocket when common NNRTI mutations are present, so many strains resistant to first-generation NNRTIs remain sensitive.

- Etravirine binds the NNRTI pocket of reverse transcriptase
- The enzyme is locked in an inactive shape
- Viral RNA is not copied into DNA
- Flexibility lets it fit mutated pockets

## Indications

- HIV-1 infection in treatment-experienced patients with NNRTI-resistant virus, with other active antiretrovirals [HIV infection and AIDS →](https://durgical.com/en/conditions/hiv-infection-and-aids/)

## Adverse effects

### Common

- Rash, usually in the first weeks
- Diarrhoea and nausea
- Tingling or numbness in hands or feet
- Body fat changes

### Serious (rare, important)

- Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
- Hypersensitivity with organ involvement, including the liver
- Immune reconstitution syndrome

## Contraindications

- Severe hypersensitivity or skin reaction to etravirine
- Other NNRTIs
- Some boosted protease inhibitors (tipranavir, fosamprenavir or atazanavir with ritonavir)

## Key interactions

**Other NNRTIs**
Not combined

**Tipranavir, fosamprenavir or atazanavir with ritonavir**
Unpredictable levels; not combined

**Maraviroc**
Etravirine lowers maraviroc; the regimen is adjusted

**CYP2C9 and CYP2C19 substrates; CYP3A4 substrates**
Levels of the first may rise and of the second may fall; each combination is checked

## What is monitored

- Skin during the first weeks
- Liver tests
- HIV viral load and resistance testing

## Administration and safety

- Oral, twice a day, after a meal
- Tablets can be dispersed in water if they cannot be swallowed; the mixture is drunk at once

## Pregnancy and breastfeeding

Human data are limited; the HIV team weighs benefit and risk.

## Nursing care

- Teach to stop and seek care for a rash with fever, blisters, mouth sores or eye swelling
- Check every new medicine for interactions
- Teach to report jaundice or dark urine
- Reinforce taking it after food

## Pharmacokinetics

**Absorption**
Oral; taken after a meal because food increases absorption

**Metabolism**
Liver CYP3A4, CYP2C9 and CYP2C19; induces CYP3A4 and glucuronidation and inhibits CYP2C9 and CYP2C19

## Memory aid

ETRA = «extra» flexible NNRTI: it bends to fit the pocket that beat efavirenz.

## Test yourself

Think of the answer, then tap the question to see it.

## Why is etravirine active against many efavirenz-resistant strains?

Its flexible structure adapts to the mutated NNRTI pocket.

## What is the most important adverse effect of etravirine?

Rash, which can rarely be severe (Stevens-Johnson syndrome or toxic epidermal necrolysis).

## Should etravirine be taken fasting or after a meal?

After a meal, because food increases absorption.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/etravirine/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 3

- [Efavirenz](https://durgical.com/en/pharmacology/efavirenz/)
- [Rilpivirine](https://durgical.com/en/pharmacology/rilpivirine/)
- [Doravirine](https://durgical.com/en/pharmacology/doravirine/)

## Related conditions 1

- [HIV infection and AIDS](https://durgical.com/en/conditions/hiv-infection-and-aids/)

[← Back to the class: Non-nucleoside reverse transcriptase inhibitors (NNRTIs)](https://durgical.com/en/pharmacology/classes/non-nucleoside-reverse-transcriptase-inhibitors/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Etravirine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a608016.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [HIV-1 Reverse Transcriptase in Complex with TMC125](https://www.rcsb.org/structure/3MEC) (RCSB Protein Data Bank, 2010); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=J05AG04) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/etravirine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/etravirine/