Bictegravir/Lenacapavir: A 2-Drug Regimen for the Treatment of HIV-1 Infection

Objective: To evaluate the efficacy and safety of bictegravir/lenacapavir for the treatment of HIV-1 infection. Data Sources: A literature search was conducted in PubMed and Google Scholar (January 2016-August 2026) using the search terms bictegravir and lenacapavir . Other data sources included abstracts presented at recent conferences and the prescribing information. Study Selection and Data Extraction: All English-language studies assessing the efficacy and safety of bictegravir/lenacapavir for the treatment of HIV-1 infection were considered for inclusion. Data Synthesis: Bictegravir is an established second-generation integrase strand transfer inhibitor (INSTI), whereas lenacapavir is a novel capsid inhibitor. Both antiretrovirals are highly active against HIV-1. Bictegravir/lenacapavir 75 mg/50 mg was shown to be safe and effective in two phase 3 clinical trials after switching from complex antiretroviral therapy (ART) or bictegravir/emtricitabine/tenofovir alafenamide. The Food and Drug Administration approved this combination for the treatment of HIV-1 infection in adults who are virologically suppressed on stable ART with no resistance to the individual components. It is available as a single-tablet regimen (STR) taken orally once daily. Relevance to Patient Care and Clinical Practice in Comparison With Existing Drugs: Bictegravir/lenacapvir is the first INSTI-capsid inhibitor 2-drug STR indicated for the treatment of HIV-1 infection. The combination could be useful for patients who want to simplify their regimen and/or those who cannot use a nucleos(t)ide or a non-nucleoside reverse transcriptase inhibitor. It is not active against hepatitis B virus coinfection. Conclusions: Bictegravir/lenacapvir is safe and efficacious as a 2-drug regimen for the treatment of adults with HIV-1 infection.