Single-Tablet HIV Regimen Combining Bictegravir and Lenacapavir Meets Phase 3 Trial Endpoints

A once-daily single-tablet regimen combining the antiretrovirals bictegravir and lenacapavir met its primary endpoint in the Phase 3 ARTISTRY-2 trial, demonstrating non-inferiority to BIKTARVY (bictegravir/emtricitabine/tenofovir alafenamide) in adults with HIV who are virologically suppressed. The investigational fixed-dose combination of bictegravir 75 mg and lenacapavir 50 mg was generally well tolerated, with no significant or new safety concerns identified during the trial.

The double-blind trial evaluated treatment responses of adults with HIV who switched from BIKTARVY to the bictegravir/lenacapavir combination. The primary efficacy endpoint was the percentage of participants with HIV-1 RNA levels ≥50 copies/mL at Week 48, defined by the FDA snapshot algorithm. Participants on BIKTARVY were randomized 2:1 to switch onto bictegravir 75 mg/lenacapavir 50 mg or continue their BIKTARVY regimen.

A separate phase 3 clinical trial published in The Lancet included over 550 people living with HIV from 15 countries with a median age of 60. The trial showed that the new treatment was just as effective at maintaining viral suppression as multi-drug regimens. Most participants were taking between two and eleven tablets daily, and around 40% were on antiretrovirals more than once a day. The results were presented at the 2026 Conference on Retroviruses and Opportunistic Infections (CROI) in Denver, USA.

The international clinical trial demonstrated that the once-daily single-tablet combination enables the safe simplification of treatment for people living with HIV who, despite maintaining viral suppression, rely on complex multi-tablet regimens due to previous resistance or other clinical constraints. In the ageing population with a long treatment history, switching to this new tablet maintained virological control with efficacy comparable to that of complex regimens, without the emergence of new resistance and with a similar safety profile.

In addition to preserving HIV control, the new regimen was associated with greater patient satisfaction and improvements in metabolic parameters—key considerations for individuals with multiple comorbidities and polypharmacy. These findings open, for the first time, the door to treatment simplification in patients previously considered difficult to simplify, a group for whom options were extremely limited. However, the data are limited to one year of follow-up and were obtained in a carefully selected population not co-infected with hepatitis B virus.

The investigational regimen combines bictegravir, a global guidelines-recommended integrase strand transfer inhibitor with a high barrier to resistance, and lenacapavir, a first-in-class capsid inhibitor with no overlapping resistance to other existing drug classes. Integrase strand transfer inhibitors are a class of antiretroviral agents that target the viral integrase. Bictegravir is used only in combination with other antiretroviral agents in the treatment of HIV.

The results of ARTISTRY-2 will be combined with the findings from the Phase 3 ARTISTRY-1 trial to form the basis of regulatory submissions. Top-line results from the ARTISTRY-1 trial announced in November 2025 showed that the investigational combination of bictegravir and lenacapavir was well tolerated and statistically non-inferior to multi-tablet antiretroviral regimens. The company plans to file the Phase 3 results from the ARTISTRY trials with regulatory authorities and submit the detailed findings for presentation at a future scientific congress.

Bictegravir and lenacapavir in combination are investigational and not approved anywhere globally. The safety and efficacy of this combination use has not been established by the U.S. FDA. There is currently no cure for HIV or AIDS.