Cabotegravir
APRETUDE
Pronunciation: ka-boe-TEG-ra-veer (AP-re-tood)
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 pre-exposure prophylaxis (PrEP) | Adults | Optional oral lead-in 30 mg PO QD × 28 days, then 600 mg (3 mL) gluteal IM | 600 mg IM 1 month apart × 2 (months 1 and 2), then 600 mg IM every 2 months | 600 mg IM every 2 months |
| HIV-1 pre-exposure prophylaxis (PrEP) | Adolescents ≥35 kg | Optional oral lead-in 30 mg PO QD × 28 days, then 600 mg (3 mL) gluteal IM | 600 mg IM 1 month apart × 2 (months 1 and 2), then 600 mg IM every 2 months | 600 mg IM every 2 months; not recommended <35 kg |
Renal No adjustment for CrCl ≥15 mL/min; ESRD not on dialysis: effect unknown
Hepatic No adjustment for Child-Pugh A/B; Child-Pugh C: effect unknown
Missed injections: 2nd injection missed ≤2 months → give ASAP; >2 months → restart with 2 initiation injections 1 month apart. Later injection missed ≤3 months → give ASAP; >3 months → restart. Planned miss >7 days: oral cabotegravir 30 mg QD for up to 2 months, starting ~2 months after last injection.
Instructions
- Gluteal IM only, by a healthcare provider (ventrogluteal preferred; dorsogluteal acceptable); no dilution or reconstitution
- Give first injection on last day of oral lead-in or within 3 days; injections may be given up to 7 days before/after scheduled date
- Bring refrigerated vial to room temperature; shake vigorously until uniform
- Inject as soon as drawn up; discard if in syringe >2 hours
- Longer needle may be needed if BMI >30 kg/m2
Available strengths
- inj 600 mg/3 mL
- tab 30 mg
Contraindications
- Unknown or positive HIV-1 status
- Coadministration with UGT1A1 inducers: carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine
Cautions
- Comprehensive management to reduce HIV-1 acquisition risk
- Risk of resistance if HIV-1 acquired before, during, or after use
- Long-acting residual concentrations (up to 12 months or longer)
- Hypersensitivity reactions incl. SJS/TEN
- Hepatotoxicity
- Depressive disorders
- Reduced cabotegravir concentrations due to drug interactions
Adverse reactions
- Injection site reactions
- Diarrhea
- Headache
- Pyrexia
- Fatigue
- Sleep disorders
- Nausea
- Dizziness
- Flatulence
- Abdominal pain
- Vomiting
- Myalgia
Pregnancy Insufficient human data to assess risk; use only if benefit justifies fetal risk; Antiretroviral Pregnancy Registry available.
Lactation No human milk data (present in animal milk); residual exposure may persist ≥12 months after last injection — breastfeed only if benefit justifies infant risk.
Cost
| Strength | #/mo | generic $/unit | CostPlus | |
|---|---|---|---|---|
| 600 mg/3 mL | inj | per unit | not offered |
Available combined with: cabotegravir / rilpivirine
Generic entry2031 est.
⚠ BOXED WARNING
- Risk of drug resistance when used for PrEP in undiagnosed HIV-1 infection
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
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.