Rilpivirine
EDURANT
What it isNon-nucleoside reverse transcriptase inhibitor; HIV.
Why this oneA small tablet with good tolerability, and it is the oral partner in the long-acting injectable regimen.
What limits itIt fails above a viral load of 100,000 or with low CD4. It needs food and acid, so PPIs are contraindicated.
FDA-approved for
- HIV-1 infection (2011)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection, treatment-naive (with other antiretrovirals) | adult | 25 mg QD with a meal | 25 mg QD with a meal | 25 mg QD (50 mg QD only during rifabutin coadministration) |
| HIV-1 infection, treatment-naive (with other antiretrovirals) | peds ≥2 y, 14 to <20 kg | 12.5 mg QD with a meal (Edurant PED oral suspension) | 12.5 mg QD | 12.5 mg QD |
| HIV-1 infection, treatment-naive (with other antiretrovirals) | peds ≥2 y, 20 to <25 kg | 15 mg QD with a meal (Edurant PED oral suspension) | 15 mg QD | 15 mg QD |
| HIV-1 infection, treatment-naive (with other antiretrovirals) | peds ≥25 kg | 25 mg QD with a meal (25 mg tablet) | 25 mg QD | 25 mg QD |
| Oral lead-in / bridging for Cabenuva (with cabotegravir 30 mg) | adult & adolescent ≥12 y, ≥35 kg | 25 mg QD with a meal x ~1 month (≥28 days) lead-in | 25 mg QD with a meal | 25 mg QD |
Renal Mild-moderate: no adjustment; severe/ESRD: use with caution and increased adverse-effect monitoring (concentrations may rise); unlikely removed by dialysis
Hepatic Mild-moderate (Child-Pugh A/B): no adjustment; severe (C): not studied
Always take with a meal; use in combination with other antiretrovirals
Instructions
- Take QD with a meal
- Edurant PED: disperse tablets in 5 mL drinking water, swirl 1-2 min, take entire suspension immediately with a meal; do not crush, chew, or swallow whole
- Edurant 25 mg tablets and Edurant PED 2.5 mg tablets for suspension are NOT substitutable mg-per-mg (different bioavailability)
- Rifabutin coadministration: take two 25 mg tablets (50 mg) QD with a meal for the duration
- Pregnancy (stable regimen, virologically suppressed): continue 25 mg QD with a meal; monitor viral load closely
Contraindications
- CYP3A inducers that markedly lower rilpivirine levels (loss of virologic response/resistance): carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, systemic dexamethasone (>single dose), St. John's wort
- Proton pump inhibitors (e.g., esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole) — gastric pH increase lowers rilpivirine levels; loss of virologic response/resistance
Cautions
- Severe skin and hypersensitivity reactions incl. DRESS — discontinue immediately; monitor incl. hepatic labs
- Hepatotoxicity — monitor LFTs before/during treatment with hepatitis B/C or elevated baseline transaminases; consider in all patients
- Severe depressive disorders (incl. suicidal ideation/attempt) — immediate medical evaluation for severe symptoms
- Immune reconstitution syndrome
Adverse reactions
- Depressive disorders
- Headache
- Insomnia
- Rash
Pregnancy APR data show no difference in overall birth-defect risk vs background; rilpivirine exposures lower during pregnancy — monitor viral load closely
Lactation Present in human milk; risks include HIV transmission, viral resistance, and infant adverse reactions
NO BOXED WARNINGS
Principal riskIt fails at high viral load; PPIs are contraindicated
Cost, est. cash$300–$2,000/month
Generic entry2026
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: Rilpivirine ballicule
