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

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. Despite major advances in the prevention of HIV-1 transmission, there remain barriers to the widespread effective use of pre-exposure prophylaxis (PrEP). Approved daily oral PrEP requires people who do not have HIV-1 to take a pill every day to protect them from acquiring the infection. The availability of long-acting injectable PrEP that does not require daily dosing has the potential to improve uptake and adherence, particularly in high-risk individuals. Cabotegravir extended-release (ER) injectable suspension is the first long-acting injectable option to be approved for PrEP, and is given as an intramuscular injection as few as six times per year. Cabotegravir ER injectable suspension is more effective than daily oral emtricitabine/tenofovir disoproxil fumarate for preventing HIV-1 infection in adults who are at risk of sexually acquiring HIV-1. Cabotegravir ER injectable suspension is generally well tolerated and offers a convenient alternative to daily oral PrEP.