Cabotegravir: The first long-acting injectable for HIV pre-exposure prophylaxis

Abstract Purpose The purpose of this article is to review the pharmacology, efficacy, and safety of the integrase inhibitor cabotegravir for HIV pre-exposure prophylaxis, including data from clinical trials. Summary A narrative review was performed by searching PubMed/MEDLINE databases to identify relevant articles published between March 2014 and December 2021 using the keyword terms cabotegravir and Apretude and the search strings “long-acting injectable AND human immunodeficiency virus” and “pre-exposure prophylaxis AND human immunodeficiency virus.” All relevant English-language articles evaluating the pharmacology, efficacy, or safety of cabotegravir in humans for HIV pre-exposure prophylaxis were included. Additional data were obtained from prescribing information, references of identified articles, and abstracts from scientific meetings. Cabotegravir has been approved by the Food and Drug Administration and is considered both safe and effective for HIV pre-exposure prophylaxis. It is the first long-acting injectable medication approved for this indication. Phase 3 clinical trials have demonstrated the noninferiority of cabotegravir to currently recommended oral once-daily dosing regimens. Injection-site reactions were common in clinical trials of cabotegravir and occurred in up to 81% of trial participants. Costs associated with the long-acting injectable formulation must also be considered. Conclusion Cabotegravir is a novel bimonthly, injectable option for pre-exposure HIV prophylaxis for high-risk adolescents and adults weighing at least 35 kg.