NNRTI (2nd generation) Pregnancy: eMC §4.6: placental transfer has been seen in pregnant rats but it is not known whether placental transfer of etravirine occurs in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development, and on the basis of animal data the malformative risk is unlikely in humans. The clinical data do not raise a safety concern but are very limited. Etravirine is excreted in human milk; because of the potential for adverse events in nursing infants, women should be instructed not to breastfeed while receiving etravirine, and it is recommended that women living with HIV do not breastfeed in order to avoid transmission of HIV.

Etravirine

Brand names: Intelence

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with other antiretrovirals for treatment-experienced adults with HIV-1, including some NNRTI-resistant strains.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 200 mg (one 200 mg tablet or two 100 mg tablets) twice daily

Route: Oral - taken following a meal; swallow the tablet(s) whole with a liquid such as water. Patients unable to swallow the tablet(s) whole may disperse them in a glass of water

Frequency: Twice daily

eMC §4.2 (Intelence 100 mg tablets). Therapy should be initiated by a physician experienced in the management of HIV infection, and etravirine must ALWAYS be given in combination with other antiretroviral medicinal products. MISSED DOSE: if within 6 hours of the usual time, take following a meal as soon as possible and then take the next dose at the regularly scheduled time; if more than 6 hours late, skip the missed dose and simply resume the usual schedule. VOMITING: if within 4 hours of taking the medicine, take another dose following a meal as soon as possible; if more than 4 hours after, no replacement dose is needed until the next scheduled time. ELDERLY: limited information in patients over 65 years - use with caution. HEPATIC IMPAIRMENT: no dose adjustment is suggested in mild or moderate impairment (Child-Pugh Class A or B), although it should be used with caution in moderate impairment; pharmacokinetics have not been studied in severe impairment (Child-Pugh Class C) and etravirine is not recommended in these patients. PAEDIATRIC (2 years to less than 18 years and weighing at least 10 kg) - dosing is by WEIGHT BAND, not per kg: 10 to less than 20 kg = 100 mg twice daily; 20 to less than 25 kg = 125 mg twice daily; 25 to less than 30 kg = 150 mg twice daily; 30 kg or more = 200 mg twice daily. Doses are taken orally following a meal and (per US §2.3) should not exceed the recommended adult dose. Etravirine should NOT be used in children less than 2 years of age - available data for children between 1 and 2 years suggest the benefits do not outweigh the risks, and no data are available below 1 year. Verify all paediatric dosing against a children's formulary. US labelling additionally states the recommended dosage during pregnancy is the same 200 mg twice daily following a meal.

Dose adjustments

Renal

eMC §4.2: no dose adjustment is required in patients with renal impairment.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients (eMC §4.3)
Co-administration with elbasvir/grazoprevir (eMC §4.3). Note the US labelling §4 states 'None'

Side effects

Rash - very common and the most frequent reaction; usually mild to moderate, occurring in the second week of therapy and infrequent after week 4, mostly self-limiting and generally resolving within 1 to 2 weeks on continued therapy; incidence is higher in females and rash was the most common reason for discontinuation
Diarrhoea and nausea - very common; also vomiting, abdominal pain, abdominal distension, flatulence, gastritis, constipation, dry mouth, stomatitis and gastro-oesophageal reflux disease (common)
Headache - very common; peripheral neuropathy, paraesthesia, hypoaesthesia, amnesia and somnolence (common)
Severe cutaneous and hypersensitivity reactions - Stevens-Johnson syndrome and erythema multiforme were rarely reported (less than 0.1%) in clinical trials, and toxic epidermal necrolysis and DRESS (Drug Rash with Eosinophilia and Systemic Symptoms), sometimes fatal, have been reported. DRESS onset is usually around 3 to 6 weeks. Discontinue immediately if a severe cutaneous or hypersensitivity reaction develops; delay in stopping after the onset of severe rash may result in a life-threatening reaction, and patients who stop for hypersensitivity must not restart
Common: thrombocytopenia, anaemia, decreased neutrophils, drug hypersensitivity, diabetes mellitus, hyperglycaemia, hypercholesterolaemia, hypertriglyceridaemia, hyperlipidaemia, dyslipidaemia, anorexia, anxiety, insomnia, blurred vision, myocardial infarction, hypertension, exertional dyspnoea, raised ALT and AST, night sweats, dry skin, prurigo, renal failure and increased blood creatinine

Interactions

Elbasvir/grazoprevir - co-administration is contraindicated (eMC §4.3)
Etravirine is a substrate of CYP3A, CYP2C9 and CYP2C19, so co-administration with inducers or inhibitors of these enzymes may alter the therapeutic effect or adverse reaction profile of etravirine (US §7.1)
Etravirine is an inducer of CYP3A and an inhibitor of CYP2C9, CYP2C19 and P-glycoprotein, so co-administration of substrates of CYP3A, CYP2C9 or CYP2C19, or drugs transported by P-gp, may alter the therapeutic effect or adverse reaction profile of the co-administered drug (US §7.2)
Raltegravir and maraviroc - no data other than drug-drug interaction data are available when etravirine is combined with these agents (eMC §4.4)
The eMC §4.5 interaction section was not captured in this bundle, and the US Table 4 of significant interactions was truncated - clinician to review both in full

Clinical monograph

How it works

It binds directly and non-competitively to HIV-1 reverse transcriptase, inducing a conformational change that inhibits the enzyme and viral replication.

Prescribing in practice

Serious skin reactions, including Stevens-Johnson syndrome and hypersensitivity with systemic features, can occur, so it must be stopped if a severe rash or systemic hypersensitivity develops.
It is metabolised by and affects cytochrome P450 enzymes, leading to numerous drug interactions that require review.
Absorption is improved when taken after food, and it is used only as part of an optimised combination regimen.

Monitoring

Monitor HIV viral load and CD4 count, for rash or hypersensitivity, and review for drug interactions.

Counselling the patient

Take after a meal to ensure the medicine is absorbed properly.
Report any rash, especially with fever, blistering or mouth sores, without delay.
Tell your team about all other medicines you take.

Evidence & guidelines

Etravirine's efficacy in treatment-experienced patients was established in the DUET trials.

Reference: BHIVA guidelines; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Pathways