Cabotegravir Extended-Release Injectable Suspension: A Review in HIV-1 Pre-Exposure Prophylaxis


Blair HA. Cabotegravir Extended-Release Injectable Suspension: A Review in HIV-1 Pre-Exposure Prophylaxis. Drugs. 2022 Oct 18. doi: 10.1007/s40265-022-01791-3. Epub ahead of print. PMID: 36255686.

Cabotegravir extended-release (ER) injectable suspension (Apretude™) is the first long-acting injectable option to be approved for HIV-1 pre-exposure prophylaxis (PrEP). As an HIV-1 integrase strand transfer inhibitor, cabotegravir ER injectable suspension prevents DNA integration and inhibits HIV-1 replication. Its slow absorption and long elimination half-life permit infrequent dosing (1 month apart for two consecutive months, and every 2 months thereafter). Cabotegravir ER injectable suspension is indicated in the USA for PrEP to reduce the risk of sexually acquired HIV-1 infection in at-risk adults and adolescents weighing ≥ 35 kg who have a negative HIV-1 test prior to initiation. In clinical trials, cabotegravir ER injectable suspension had superior efficacy to oral daily emtricitabine/tenofovir disoproxil fumarate (DF) in preventing acquisition of HIV-1 in at-risk transgender women (TGW), cisgender men who have sex with men (MSM), and cisgender women. The drug was generally well tolerated, although further long-term data are needed to fully determine its safety. With its convenient, less-frequent dosing schedule and its long-acting formulation enabling intramuscular administration, cabotegravir ER injectable suspension represents a novel and efficacious alternative to daily oral PrEP.

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