Rilpivirine
EDURANT
Pronunciation: ril-pi-VIR-een (EE-dur-ant)
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.
Rilpivirine prescription history
Animated chart of estimated U.S. prescriptions per year, HIV antiretrovirals (1987–2026). Rilpivirine enters in 2011 (estimated).
FDA-approved for
- HIV-1 infection (2011)
Principal riskIt fails at high viral load; PPIs are contraindicated
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| 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
Available strengths
- tab 2.5, 25 mg
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
Cost
| Strength | #/mo | generic $/mo | brand $/mo | CostPlus | |
|---|---|---|---|---|---|
| 2.5 mg | tab | 30 qd | — | not offered | |
| 25 mg | tab | 30 qd | — | $1,441.23 | not offered |
Available combined with: cabotegravir / rilpivirine
Generic entry2026
Open Rilpivirine in the interactive console ↗
Self-check
- Rilpivirine: Above what viral load can it fail?
100,000. - Rilpivirine: Why are PPIs contraindicated?
It needs gastric acid.