Gilead’s Single-Tablet Bictegravi/Lenacapavir Regimen Shows Positive Phase III ARTISTRY-1 Results in Virologically Suppressed Adults with HIV

Gilead has shared positive results from the Phase III ARTISTRY-1 trial (NCT05502341) evaluating an investigational single-tablet regimen of bictegravir 75 mg/lenacapavir 50 mg (BIC/LEN) in adults with HIV who are virologically suppressed, and switched from a multi-tablet regimen.¹

Single-tablet regimen demonstrates non-inferiority

The BIC/LEN single-tablet regimen met the primary success criterion, demonstrating non-inferiority to baseline multi-tablet antiretroviral therapy regimens.

In a press release, Chloe Orkin, MBE, clinical professor of infection and inequities at Queen Mary University of London, said: “Developing new effective, convenient regimens for those left behind by advances in medical research is necessary to close the unmet HIV treatment gap. These ARTISTRY-1 trial results demonstrate that a combination regimen of bictegravir and lenacapavir maintains viral suppression in people living with HIV who would otherwise have to take a complex multi-tablet regimen. The findings are significant for those people, many of whom have lived with HIV for decades and who have medical comorbidities of aging and thus take many other medications as well.”

ARTISTRY-1 trial design

ARTISTRY-1 is a randomized, open-label, multicenter, active-controlled Phase II/III study.

• In the Phase III portion, participants were randomized 2:1 to switch to bictegravir 75 mg/lenacapavir 50 mg or continue their existing multi-drug regimen.
• The primary endpoint assessed the proportion of patients with HIV-1 RNA ≥50 copies/mL at week 48 using the FDA snapshot algorithm.
• Key secondary endpoints at week 48 included rates of virologic suppression (<50 copies/mL), changes in CD4 cell counts, and incidence of treatment-emergent adverse events.

Jared Baeten, MD, PhD, senior vice president, clinical development, virology therapeutic area head, Gilead Sciences, added: “People living with HIV who are on complex antiretroviral treatment regimens may experience pill burden, adherence challenges and difficulties with the long-term management of HIV. Gilead developed the first single-tablet complete regimen for the treatment of HIV in 2006. Today, innovative single-tablet regimens are still needed to help suit people’s needs, modernizing treatment while helping to sustain viral suppression. By reducing the multi-tablet burden, we hope to improve health outcomes while expanding options.”

Additional research in ARTISTRY-2 trial

In addition to ARTISTRY-1, Gilead is evaluating this investigational combination in the Phase III ARTISTRY-2 trial (NCT06333808).

ARTISTRY-2 is a double-blind, multicenter, randomized, active-controlled study assessing the safety and efficacy of switching from Biktarvy (bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg tablets, to a fixed-dose combination of bictegravir 75 mg/lenacapavir 50 mg in virologically suppressed participants with HIV-1. Gilead is expecting a topline data readout for the primary endpoints of this trial before the end of the year.

Earlier Phase II data of lenacapavir algonside Merck’s islatravir

In October 2024, Phase II trial (NCT05052996) results showed the novel combination of islatravir (Merck) and lenacapavir (Gilead) maintained high rates of viral suppression in virologically suppressed adults with HIV after 48 weeks of treatment.²

Results showed:

• At 48 weeks, 94.2% of participants on islatravir + lenacapavir maintained viral suppression, with no participants reaching HIV-1 RNA ≥50 copies/mL.
• Comparable viral suppression was observed in participants continuing Biktarvy (92.3%), also with no cases ≥50 copies/mL.
• Treatment-related adverse events (TRAEs) occurred in 19.2% of the islatravir + lenacapavir group versus 5.8% in the Biktarvy group.
• Most common TRAEs were dry mouth (3.8%) and nausea (3.8%).
• No grade 3 or 4 TRAEs related to study drugs were reported in either cohort.

In a company statement from the time, Baeten said: “The future of HIV treatment is person-centered, with long-acting options tailored to help meet the needs and preferences of people affected by HIV. There is no ‘one size fits all’ approach. The complexities of HIV care require putting people first in the development of biomedical innovations as we keep striving to offer options for all those living with HIV.”

References

1. Gilead’s Investigational Single-Tablet Regimen of Bictegravir and Lenacapavir for HIV-1 Treatment Meets Primary Endpoint in Phase 3 ARTISTRY-1 Trial. News release. Gilead. November 13, 2025. Accessed November 13, 2025. https://www.gilead.com/news/news-details/2025/gileads-investigational-single-tablet-regimen-of-bictegravir-and-lenacapavir-for-hiv-1-treatment-meets-primary-endpoint-in-phase-3-artistry-1-trial

2. Gilead and Merck Announce Phase 2 Data Showing a Treatment Switch to an Investigational Oral Once-Weekly Combination Regimen of Islatravir and Lenacapavir Maintained Viral Suppression in Adults at Week 48. News release. Gilead. October 19, 2024. Accessed November 13, 2025. https://www.gilead.com/news/news-details/2024/gilead-and-merck-announce-phase-2-data-showing-a-treatment-switch-to-an-investigational-oral-once-weekly-combination-regimen-of-islatravir-and-lenacapavir-maintained-viral-suppression-in-adu