Last reviewed 2026-04-22 · How we verify

Cabotegravir (CAB) tablet

Cabotegravir is an integrase strand transfer inhibitor (INSTI) that blocks HIV integrase, preventing the virus from inserting its genetic material into human host cell DNA.

Cabotegravir is an integrase strand transfer inhibitor (INSTI) that blocks HIV integrase, preventing the virus from inserting its genetic material into human host cell DNA. Used for HIV-1 infection treatment (in combination antiretroviral therapy), HIV-1 pre-exposure prophylaxis (PrEP).

At a glance

Mechanism of action

Cabotegravir binds to the active site of HIV integrase and inhibits the strand transfer step of viral integration. By blocking this critical step in the HIV replication cycle, the drug prevents establishment of persistent infection. It is designed for long-acting formulation, allowing extended dosing intervals compared to daily oral antiretrovirals.

Approved indications

• HIV-1 infection treatment (in combination antiretroviral therapy)
• HIV-1 pre-exposure prophylaxis (PrEP)

Common side effects

• Injection site reactions (pain, induration, erythema)
• Headache
• Fatigue
• Nausea
• Diarrhea
• Hypersensitivity reactions

Key clinical trials

• Study to Evaluate the Efficacy, Safety, and Tolerability of Long-acting Intramuscular Cabotegravir and Rilpivirine for Maintenance of Virologic Suppression Following Switch From an Integrase Inhibitor in HIV-1 Infected Therapy Naive Participants (PHASE3)
• Injectable Cabotegravir Compared to TDF/FTC For PrEP in HIV-Uninfected Men and Transgender Women Who Have Sex With Men (PHASE2, PHASE3)
• Implementation Study of Lenacapavir Pre-exposure Prophylaxis for HIV Prevention
• 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 (PHASE3)
• A Study Evaluating Implementation Strategies for the Delivery of APRETUDE for Black cis-and Transgender Women in United States EHE Territories (PHASE4)
• ALIGN: A Non-randomised Study Delivering Injectable Lenacapavir for HIV Prevention Within a Pre-exposure Prophylaxis (PrEP) Choice Context in Cape Town, South Africa.
• More Options for Children and Adolescents (MOCHA): Oral and Long-Acting Injectable Cabotegravir and Rilpivirine in HIV-Infected Children and Adolescents (PHASE1, PHASE2)
• Study Evaluating the Efficacy, Safety, and Tolerability of Switching to Long-acting Cabotegravir Plus Long-acting Rilpivirine From Current Antiretroviral Regimen in Virologically Suppressed HIV-1-infected Adults (PHASE3)

Primary sources

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