Etravirine
INTELENCE
What it isSecond-generation non-nucleoside reverse transcriptase inhibitor; treatment-experienced HIV.
Why this oneIt retains activity against virus resistant to efavirenz and nevirapine.
What limits itRash, occasionally severe. Take after a meal; it both induces and inhibits CYP enzymes.
FDA-approved for
- treatment-experienced HIV-1 infection (2008)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection (treatment-experienced) | adult | 200 mg BID after a meal | 200 mg BID | 200 mg BID |
| HIV-1 infection | pregnant | 200 mg BID after a meal | 200 mg BID | 200 mg BID |
| HIV-1 infection | pediatric 2 to <18 yr, >=10 kg | weight-based BID after a meal | 100/125/150/200 mg BID by weight band | 200 mg BID |
Renal No adjustment needed
Hepatic No adjustment for mild-moderate (Child-Pugh A/B); not studied in severe (C)
Instructions
- Take following a meal
- Swallow tablet(s) whole with liquid
- If unable to swallow, disperse tablet(s) in water
Cautions
- Severe/potentially fatal skin & hypersensitivity reactions (SJS, TEN, erythema multiforme, DRESS) — discontinue immediately for severe rash or rash with systemic/hepatic involvement
- Immune reconstitution syndrome
- Fat redistribution
Adverse reactions
- Rash
- Peripheral neuropathy (adults)
- Diarrhea (pediatric)
Pregnancy Limited registry data insufficient to assess risk; no adverse developmental effects in animals at ~MRHD.
Lactation Breastfeeding not recommended (potential HIV-1 transmission).
NO BOXED WARNINGS
Principal riskRash, occasionally severe
Cost, est. cash$10–$500/month
Generic entry2021
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Mechanism of action: Etravirine ballicule
