Gilead Submits Regulatory Filings for Investigational Once-Daily Single-Tablet BIC/LEN Regimen Based on Positive Phase 3 ARTISTRY Data in HIV

—A novel investigational drug combination pairs bictegravir, an integrase strand transfer inhibitor recommended by global guidelines and featuring a high barrier to resistance, with lenacapavir, a first-in-class capsid inhibitor.

— Phase III ARTISTRY-1 and ARTISTRY-2 study results will provide the basis for regulatory submission

Recently, Gilead Sciences presented new data from the Phase III ARTISTRY-1 and ARTISTRY-2 studies at the Conference on Retroviruses and Opportunistic Infections 2026 (CROI 2026). The studies demonstrated that switching to the investigational single-tablet regimen of bictegravir 75 mg/lenacapavir 50 mg (BIC/LEN) effectively maintained virologic suppression in people with HIV who were already virally suppressed. This population included individuals previously treated with complex multi-tablet regimens or single-tablet regimens recommended by global guidelines. The novel combination of bictegravir and lenacapavir was generally well tolerated, with no significant or new safety concerns identified.

“Dr. Jared Baeten, Senior Vice President of Clinical Development and Head of Virology at Gilead Sciences, stated, ‘The ARTISTRY study is the latest evidence of Gilead’s commitment to advancing HIV treatment through continuous scientific innovation. This once-daily, single-tablet regimen combines bictegravir with lenacapavir, a first-in-class capsid inhibitor. This novel therapeutic combination is designed to help individuals seeking new treatment options maintain virologic suppression. We look forward to collaborating with regulatory authorities to bring this drug combination to people living with HIV.’”

Study results indicate that BIC/LEN is poised to offer more treatment options for adults with HIV who have achieved virologic suppression, demonstrating efficacy comparable to Biktarvy^®(Bictegravir 50 mg/Emtricitabine 200 mg/Tenofovir Alafenamide Fumarate 25 mg, B/F/TAF) is comparable to other complex multi-tablet regimens.

New data from the ARTISTRY-1 (NCT05502341) and ARTISTRY-2 (NCT06333808) studies, evaluating the safety and efficacy of a once-daily bictegravir/lenacapavir (BIC/LEN) single-tablet regimen, were presented in the Late-Breaking Research session at the 33rd Conference on Retroviruses and Opportunistic Infections (CROI) held in Denver, Colorado, USA. These findings build upon the positive top-line results announced in November and December 2025.

Research results presented at CROI 2026 demonstrate that the single-tablet regimen of BIC/LEN offers an important new option for optimizing treatment in people with HIV who have achieved virologic suppression on previously complex, multi-tablet regimens.

Results at Week 48 demonstrated that BIC/LEN was non-inferior to complex multi-tablet regimens in maintaining virologic suppression: 0.8% of participants in the BIC/LEN group had HIV-1 RNA ≥50 copies/mL, compared with 1.1% of those who continued on complex multi-tablet regimens. CD4 cell counts remained stable in both groups, and no treatment-emergent resistance was observed. Furthermore, participants who switched from complex multi-tablet regimens to BIC/LEN showed improvements in fasting lipid parameters compared with baseline, with a median decrease in total cholesterol of 15.1 mg/dL, whereas those who continued on complex multi-tablet regimens experienced an increase of 2.8 mg/dL. Patient-reported treatment satisfaction (HIVSTQ score) increased by an average of 7 points, while no significant change was observed in the control group.

Professor Chloe Orkin of Queen Mary University of London stated, “Prior viral resistance, intolerance, contraindications, or drug interactions may prevent many people living with HIV from benefiting from the single-tablet regimens recommended by guidelines. In the ARTISTRY-1 study, participants were taking 2 to 11 pills daily at baseline, with approximately 40% requiring multiple daily doses. Identifying single-tablet regimens that are both effective and convenient is key to optimizing treatment and enabling more individuals to benefit from the latest scientific advances, such as the combination of bictegravir and lenacapavir.”

BIC/LEN was generally well tolerated. Drug-related adverse events were reported by 14.3% of subjects who switched to BIC/LEN, compared with 1.6% of those who continued on complex multi-tablet regimens. The incidence of serious drug-related adverse events was similar between the two groups (0.3% in the BIC/LEN group vs. 0% in the complex multi-tablet regimen group). Discontinuations due to adverse events were infrequent (1.6% and 0.5%, respectively).

On February 25, 2026, The Lancet published the primary outcome results of the ARTISTRY-1 study, titledSwitch to single-tablet bictegravir/lenacapavir from a complex HIV regimen: results from ARTISTRY-1, a randomised, open-label phase 3 clinical trial. Switch to single-tablet bictegravir/lenacapavir from a complex HIV regimen: results from ARTISTRY-1, a randomised, open-label phase 3 clinical trial。

The ARTISTRY-2 study results presented at CROI 2026 further confirm that the efficacy of BIC/LEN is comparable to Biktarvy, a single-tablet regimen recommended by global guidelines, highlighting its potential to expand current HIV treatment options.

By Week 48, BIC/LEN demonstrated non-inferior efficacy to Biktarvy as the standard regimen in maintaining virologic suppression. In the BIC/LEN group, 1.3% of participants had HIV-1 RNA ≥50 copies/mL, compared with 1.0% among those who continued on Biktarvy. CD4 cell counts remained stable in both groups, and two participants in each group met the criteria for resistance analysis.

Resistance analysis showed that, through Week 48, three of the four subjects did not develop treatment-emergent resistance (including one subject receiving BIC/LEN and two subjects receiving Biktarvy). One subject in the BIC/LEN group had a single integrase substitution detected at Week 36 but did not exhibit phenotypic resistance. No capsid mutations were detected. The study demonstrated that switching to BIC/LEN had no significant effect on body weight, with body mass index remaining stable in both groups over the 48-week treatment period.

BIC/LEN was generally well tolerated, with incidence rates of drug-related adverse events comparable to those in the Biktarvy group (10.4% vs. 12.0%). No serious drug-related adverse events were reported, and discontinuation rates due to adverse events were low, at 1.6% in both groups.

Dr. Eric Meissner of the Medical University of South Carolina stated, “The results from the ARTISTRY-2 study support the potential of bictegravir/lenacapavir (BIC/LEN) to expand the options for single-tablet regimens in HIV treatment. Given its efficacy is comparable to guideline-recommended regimens, we look forward to providing another meaningful treatment option for adults with HIV who have achieved virologic suppression.”

The combination regimen of bictegravir and lenacapavir is currently still in the research phase, has not been approved in any region worldwide, and its safety and efficacy have not yet been established.

There is currently no cure for HIV or AIDS.

ARTISTRY-1 (NCT05502341) is a multicenter, Phase II/III clinical study comparing an investigational once-daily regimen of bictegravir (an integrase strand transfer inhibitor recommended by global guidelines) in combination with the first-in-class capsid inhibitor lenacapavir against the current treatment regimens in people living with HIV who have achieved virologic suppression on prior complex treatment regimens. In the Phase III portion of the study, participants were randomized in a 2:1 ratio to receive a fixed-dose combination of bictegravir 75 mg/lenacapavir 50 mg or to continue their stable baseline complex treatment regimen. The primary endpoint was the proportion of participants with HIV-1 RNA ≥50 copies/mL at Week 48, assessed using the snapshot algorithm as defined by the U.S. FDA. Key secondary endpoints included the proportion of participants achieving virologic suppression (HIV viral load <50 copies/mL) at Week 48, the change from baseline in CD4 cell count, and the proportion of participants experiencing treatment-emergent adverse events.

ARTISTRY-2 (NCT06333808) is a multicenter, double-blind, randomized Phase III clinical study comparing the safety and efficacy of an investigational once-daily combination of bictegravir and lenacapavir with Biktarvy in people living with HIV who have achieved virologic suppression with prior Biktarvy treatment. Participants currently receiving Biktarvy were randomized in a 2:1 ratio to switch to bictegravir 75 mg/lenacapavir 50 mg or to continue Biktarvy. The primary endpoint was the proportion of participants with HIV-1 RNA ≥50 copies/mL at Week 48, as determined by the FDA-defined snapshot algorithm. Key secondary endpoints included the proportion of participants achieving virologic suppression, changes from baseline in CD4 cell counts, and the incidence of treatment-emergent adverse events.