Cabotegravir
APRETUDE
What it isLong-acting HIV integrase inhibitor; alone for PrEP and with rilpivirine for HIV treatment.
Why this oneInjection-based prevention or treatment removes daily-pill adherence while drug is on schedule.
What limits itMissed injections leave a long low-level tail that can select resistance. Rifampin is contraindicated; injection reactions are common.
FDA-approved for
- HIV-1 treatment and pre-exposure prophylaxis (2021)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 treatment — oral lead-in / bridging (with rilpivirine) | Adults & adolescents ≥12y, ≥35 kg | 30 mg QD | 30 mg QD | 30 mg QD |
| HIV-1 pre-exposure prophylaxis — oral lead-in | Adults & adolescents ≥35 kg | 30 mg QD | 30 mg QD | 30 mg QD |
Renal No adjustment for mild–severe impairment (CrCl ≥15); ESRD (CrCl <15): unknown
Hepatic No adjustment for mild–moderate (Child-Pugh A/B); severe (C): unknown
Oral therapy limited to ~1–2 months to bridge or replace missed injections; longer durations require an alternative oral regimen
Instructions
- Take with a meal at approximately the same time each day
- For HIV-1 treatment, use in combination with rilpivirine (EDURANT) 25 mg QD
- Oral lead-in ~1 month (≥28 days) to assess cabotegravir tolerability before long-acting injectable
- For PrEP, screen for HIV-1 before and during use; use only in confirmed HIV-1-negative individuals
Contraindications
- Coadministration with UGT1A1 inducers: carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine (loss of virologic response/efficacy)
- Unknown or positive HIV-1 status (when used for HIV-1 PrEP)
Cautions
- Serious/severe hypersensitivity reactions including Stevens-Johnson syndrome (SJS)/TEN — discontinue immediately
- Hepatotoxicity — monitor liver chemistries
- Depressive disorders (including suicidal ideation) — evaluate promptly
- For PrEP, part of a comprehensive HIV-1 prevention strategy; not always effective
- Drug-interaction risk of reduced efficacy/resistance
Adverse reactions
- Treatment (with rilpivirine): fatigue, headache, diarrhea, nausea, dizziness, abnormal dreams, anxiety, insomnia, abdominal discomfort/distension, asthenia
- PrEP: headache, diarrhea, nausea, dizziness, upper respiratory tract infection, somnolence, fatigue, abnormal dreams, abdominal pain
Pregnancy Insufficient human data; discuss benefit-risk. Antiretroviral Pregnancy Registry available (1-800-258-4263)
Lactation No human data; breastfeeding not recommended in HIV-1 (US) due to transmission risk
NO BOXED WARNINGS
No boxed warning for CABENUVA, the long-acting treatment regimen, but APRETUDE, the pre-exposure prophylaxis product carries a boxed warning for drug-resistant HIV-1 if started during undiagnosed infection.
Principal riskA long tail allowing resistance if doses are missed
Cost, est. cash$300–$2,000/month
Generic entry2031 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Mechanism of action: Cabotegravir ballicule
