Cabotegravir

Cabotegravir is an HIV-1 antiretroviral drug [see Microbiology ( 12.4 )] in a long-acting formulation.

• APRETUDE is indicated for pre‑exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in adults and adolescents weighing at least 35 kg who are at risk for HIV-1 acquisition. Individuals must have a negative HIV-1 test prior to initiating APRETUDE (with or without an oral lead-in with oral cabotegravir) for HIV-1 PrEP [see Dosage and Administration ( 2.2 , 2.4 ), Contraindications ( 4 ), Warnings and Precautions ( 5.1 )] .ICD-10: B20

• APRETUDE is contraindicated in individuals: • with unknown or positive HIV-1 status [see Warnings and Precautions ( 5.1 , 5.2 )] . • with previous hypersensitivity reaction to cabotegravir [see Warnings and Precautions ( 5.4 )] .contraindicated

• HIV-1 Screening: Screen all individuals for HIV-1 infection immediately prior to initiating APRETUDE for HIV-1 PrEP and prior to each injection while taking APRETUDE. ( 2.2 ) • Prior to initiating APRETUDE, an oral lead-in dosing may be used for approximately 1 month with the recommended dosage to assess the tolerability of APRETUDE. ( 2.4 ) • For gluteal intramuscular injection only. ( 2.5 , 2.7 ) • Recommended Dosing Schedule: Initiate APRETUDE with a single 600-mg (3-mL) injection given 1 month apart for 2 consecutive months on the last day of an oral lead-in if used or within 3 days and continue with the injections every 2 months thereafter. ( 2.5 ) 2.1 Dosage and Administration Overview • APRETUDE contains cabotegravir extended-release injectable suspension in a single-dose vial [see Dosage Forms and Strengths ( 3 )] . • APRETUDE must be administered by a healthcare provider by gluteal intramuscular injection [see Dosage and Administration ( 2.7 )] . • APRETUDE may be initiated with oral cabotegravir prior to the intramuscular injections or the patient may proceed directly to injection of APRETUDE without an oral lead-in [see Dosage and Administration ( 2.4 )] . 2.2 HIV-1 Screening for Individuals Receiving APRETUDE for HIV-1 Pre-Exposure Prophylaxis Individuals must be tested for HIV-1 infection prior to initiating APRETUDE or oral cabotegravir, and with each subsequent injection of APRETUDE, using a test approved or cleared by the FDA for the diagnosis of acute or primary HIV-1 infection.

• Comprehensive management to reduce the risk of HIV-1 acquisition. ( 5.1 ) • Potential risk of developing resistance to APRETUDE if an individual acquires HIV-1 either before or while taking APRETUDE or following discontinuation of APRETUDE. Reassess risk of HIV-1 acquisition and test before each injection to confirm HIV-1 negative status. ( 5.2 ) • Residual concentrations of cabotegravir may remain in the systemic circulation of individuals up to 12 months or longer. ( 5.3 ) • Serious or severe hypersensitivity reactions have been reported with cabotegravir and include Stevens-Johnson syndrome (SJS)/toxic epidermal necrolysis (TEN). Discontinue APRETUDE immediately if signs or symptoms of hypersensitivity reactions develop. ( 5.4 ) • Hepatotoxicity has been reported in individuals receiving cabotegravir. Clinical and laboratory monitoring should be considered. Discontinue APRETUDE if hepatotoxicity is suspected. ( 5.5 ) • Depressive disorders have been reported with APRETUDE. Prompt evaluation is recommended for depressive symptoms. ( 5.6 ) 5.1 Comprehensive Management to Reduce the Risk of HIV-1 Infection Use APRETUDE for HIV-1 PrEP to reduce the risk of HIV-1 infection as part of a comprehensive prevention strategy including adherence to the administration schedule and safer sex practices, including condoms, to reduce the risk of sexually transmitted infections (STIs). APRETUDE is not always effective in preventing HIV-1 acquisition [see Clinical Studies ( 14.1 )] .

The following adverse reactions are described below and in other sections of the labeling: • Hypersensitivity reactions [see Warnings and Precautions ( 5.4 )] • Hepatotoxicity [see Warnings and Precautions ( 5.5 )] • Depressive disorders [see Warnings and Precautions ( 5.6 )] The most common adverse reactions (all grades) observed in at least 1% of participants receiving APRETUDE were injection site reactions, diarrhea, headache, pyrexia, fatigue, sleep disorders, nausea, dizziness, flatulence, abdominal pain, vomiting, myalgia, rash, decreased appetite, somnolence, back pain, and upper respiratory tract infection. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact ViiV Healthcare at 1-877-844-8872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect rates observed in practice. Clinical Trials Experience in Adults The safety assessment of APRETUDE is based on the analysis of data from 2 international, multicenter, double-blind trials, HPTN 083 and HPTN 084 [see Clinical Studies ( 14.1 )] . Adverse reactions were reported while on blinded study product following exposure to APRETUDE extended-release injectable suspension and oral cabotegravir tablets as oral lead-in.

• Lactation: Assess the benefit-risk of using APRETUDE to the infant while breastfeeding due to the potential for adverse reactions and residual concentrations in the systemic circulation for up to 12 months or longer after discontinuation. ( 8.2 ) • Pediatrics: Not recommended in individuals weighing <35 kg. ( 8.4 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to APRETUDE during pregnancy. Healthcare providers are encouraged to register individuals by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary There are insufficient human data on the use of APRETUDE during pregnancy to adequately assess a drug-associated risk of birth defects and miscarriage. Discuss the benefit-risk of using APRETUDE with individuals of childbearing potential or during pregnancy. Cabotegravir use in pregnant individuals has not been evaluated. APRETUDE should be used during pregnancy only if the expected benefit justifies the potential risk to the fetus. The APR has been established to monitor for birth defects following prenatal exposure to antiretrovirals. The rate of miscarriage is not reported in the APR. The background rate for major birth defects in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) is 2.7%.

Metabolism

Absorption, Distribution, and Elimination The pharmacokinetic properties of cabotegravir are provided in Table 9 . The multiple-dose pharmacokinetic parameters are provided in Table 10 .

There is no known specific treatment for overdose with APRETUDE. If overdose occurs, monitor the individual and apply standard supportive treatment as required as well as observation of the clinical status of the individual. As APRETUDE is highly bound to plasma proteins, it is unlikely that it will be significantly removed by dialysis. Consider the prolonged exposure to APRETUDE following an injection when assessing treatment needs and recovery [see Warnings and Precautions ( 5.5 )] .

• Jan 21, 2021NDANDA212887Viiv Hlthcare
• Jan 21, 2021NDANDA212888Viiv Hlthcare
• Dec 20, 2021NDANDA215499Viiv Hlthcare

1. 1Product Dose Omission Issue1,78912%
2. 2Injection Site Pain1,56411%
3. 3Off Label Use1,47010%
4. 4Viral Load Increased9346.4%
5. 5Pain6974.8%
6. 6Virologic Failure6314.3%
7. 7Product Use In Unapproved Therapeutic Environment6054.2%
8. 8Pathogen Resistance5403.7%
9. 9Pyrexia4022.8%
10. 10Product Complaint4002.7%
11. 11Inappropriate Schedule Of Product Administration3952.7%
12. 12Product Storage Error3672.5%
13. 13Injection Site Nodule3562.4%
14. 14Blood Hiv Rna Increased3442.4%
15. 15Fatigue3432.4%

The 10 most recently updated of 132 ClinicalTrials.gov registrations naming Cabotegravir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Long-Acting Cabotegravir and Rilpivirine in People Living With HIV-1 Subtype A6: A Real-World Retrospective Study
  Recruiting · Observational · 250 enrolled · Pomeranian Medical University Szczecin
  NCT07370649updated 2026-06-11
• Cabotegravir & Rilpivirine Antiretroviral Therapy in Pregnancy
  Not yet recruiting · Observational · 40 enrolled · International Maternal Pediatric Adolescent AIDS Clinical Trials Group
  NCT07637942updated 2026-06-10
• Post-Injectable Cabotegravir Antiretroviral Salvage Strategy Options Trial
  Recruiting · Phase 4 · Interventional · 100 enrolled · University of Witwatersrand, South Africa
  NCT06485154updated 2026-06-09
• NOTRE: Optimizing Long-Acting Pre-Exposure Prophylaxis and Medications for Opioid Use Disorder Interventions in Carceral Settings
  Not yet recruiting · Phase 4 · Interventional · 450 enrolled · Duke University
  NCT06854029updated 2026-06-04
• PrEP-LANA (Pre-exposure Prophylaxis- Long-acting Novel Antiviral Agent)
  Not yet recruiting · Observational · 220 enrolled · Queen Mary University of London
  NCT07620730updated 2026-06-02
• Implementation Study of Lenacapavir Pre-exposure Prophylaxis for HIV Prevention
  Recruiting · Observational · 3,000 enrolled · Gilead Sciences
  NCT07473778updated 2026-05-29
• Study to Evaluate Pharmacokinetic (PK), Safety and Tolerability of Cabotegravir (CAB) 400 Milligrams Per Milliliter (mg/mL) Formulation in Healthy Adult Participants
  Completed · Phase 1 · Interventional · 138 enrolled · ViiV Healthcare
  NCT04484337updated 2026-05-29
• The TAIL-PrEP Study
  Recruiting · Interventional · 30 enrolled · Columbia University
  NCT06868641updated 2026-05-28
• A Study to Evaluate the Effectiveness of Long-acting (LA) Cabotegravir (CAB) + Rilpivirine (RPV) LA When Given to Participants With Detectable HIV-1
  Recruiting · Phase 3 · Interventional · 332 enrolled · ViiV Healthcare
  NCT06694805updated 2026-05-27
• A Study to Evaluate the Efficacy, Safety, Participant Choice and Preference of an Oral Once-daily Regimen or a Long-acting Injectable Regimen Every Two Months for Treatment of Human Immunodeficiency Virus (HIV-1) in Adults Who Have Not Previously Taken Antiretroviral Therapy
  Completed · Phase 3 · Interventional · 171 enrolled · ViiV Healthcare
  NCT05917509updated 2026-05-27

Frequently asked questions

How does Cabotegravir work?

Cabotegravir is an HIV-1 antiretroviral drug [see Microbiology ( 12.4 )] in a long-acting formulation.

What is Cabotegravir used for?

According to FDA labeling, Cabotegravir carries indications including: APRETUDE is indicated for pre‑exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in adults and adolescents weighing at least 35 kg who are at risk for HIV-1 acquisition. Individuals must have a negative HIV-1 test prior to initiating APRETUDE (with or without an oral lead-in with oral cabotegravir) for HIV-1 PrEP [see Dosage and Administration ( 2.2 , 2.4 ), Contraindications ( 4 ), Warnings and Precautions ( 5.1 )] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Cabotegravir?

Cabotegravir is classified as Integrase inhibitors, Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor, HIV Integrase Inhibitors, Organic Anion Transporter 1 Inhibitors, Organic Anion Transporter 3 Inhibitors, Immunologic Activity Alteration.

What are the brand names for Cabotegravir?

Cabotegravir is marketed under brand names including Apretude, Vocabria.

What are the contraindications for Cabotegravir?

Cabotegravir labeling lists contraindications including: APRETUDE is contraindicated in individuals: • with unknown or positive HIV-1 status [see Warnings and Precautions ( 5.1 , 5.2 )] . • with previous hypersensitivity reaction to cabotegravir [see Warnings and Precautions ( 5.4 )] .. Always consult the full prescribing information and a clinician.