Gilead’s Single-Tablet Regimen of Bictegravir and Lenacapavir Maintained Virological Suppression in People With HIV Who Switched Antiretroviral Therapy

FOSTER CITY, Calif.--(BUSINESS WIRE)-- Gilead Sciences, Inc. (Nasdaq: GILD) today announced the presentation of new Phase 3 ARTISTRY-1 and ARTISTRY-2 trial data at CROI 2026 showing a treatment switch to an investigational, single-tablet combination regimen of bictegravir 75 mg/lenacapavir 50 mg (BIC/LEN) was effective in people living with HIV with virological suppression, including those switching from complex multi-tablet regimens or a global guideline-recommended single-tablet regimen. The novel combination of BIC/LEN was generally well tolerated, with no significant or new safety concerns identified.

“The ARTISTRY trials represent the latest example of Gilead’s commitment to advancing HIV treatment through continuous scientific innovation,” said Jared Baeten, M.D., Ph.D., Senior Vice President, Clinical Development, Virology Therapeutic Area Head, Gilead Sciences. “This once-daily single-tablet regimen combines the durability of bictegravir with lenacapavir, a first‑in‑class capsid inhibitor. The novel treatment combination is designed to sustain virologic suppression for those seeking new options. We look forward to working with regulatory authorities to potentially bring this combination forward to people with HIV.”

The results demonstrate the potential of BIC/LEN to broaden HIV treatment options for adults with virological suppression, offering comparable efficacy to BIKTARVY^® (bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg tablets, B/F/TAF), as well as to treatment with complex multi-tablet regimens.

The new data, from the ARTISTRY-1 (NCT05502341) and ARTISTRY-2 (NCT06333808) trials, assessed the safety and efficacy of the once-daily single tablet regimen of BIC/LEN and were presented during late-breaker sessions at the 33rd Conference on Retroviruses and Opportunistic Infections in Denver, Colorado. The findings build on the positive topline results announced in November and December 2025.

Late-breaking results from ARTISTRY-1

Results presented at CROI 2026 demonstrate that a single-tablet regimen combining BIC/LEN could offer an important new option with optimized dosing for people living with HIV with virologic suppression on a complex multi-tablet regimen. Week 48 results showed that the single-tablet regimen of BIC/LEN was noninferior to complex multi-tablet regimens in maintaining virologic suppression, with 0.8% of participants receiving BIC/LEN having HIV-1 RNA ≥ 50 copies/mL (as determined by the US FDA-defined snapshot algorithm) compared to 1.1% who remained on their complex antiretroviral regimen. CD4 cell count remained stable in both treatment groups, and no participant had emergent resistance. At Week 48, the switch to BIC/LEN from complex multi-tablet regimens was also associated with an improvement from baseline in fasting lipid parameters, with a median change in total cholesterol, -15 mg/dL, versus +2 mg/dL. Additionally, patient-reported treatment satisfaction on the HIVTSQs score increased by a mean of 7 points from baseline, with those treated with complex multi-tablet regimens reporting no change.

“Pre-existing viral resistance, intolerance, contraindications, or drug-drug interactions, may prevent many people living with HIV from benefiting from guideline-recommended single-tablet antiretroviral regimens. Complex treatment regimens can pose a significant burden on people’s lives as can be seen in the ARTISTRY-1 trial where participants were taking between 2 and 11 pills per day at baseline, with ~40% taking antiretroviral therapy more than once a day,” said Chloe Orkin, MBE, Clinical Professor of Infection and Inequities at Queen Mary University of London. “Finding new effective and convenient dosing with single-tablet regimens is key to optimizing treatment, ensuring that more people can benefit from recent advances in medical research like bictegravir and lenacapavir.”

BIC/LEN was generally well tolerated, with drug-related adverse events reported in 14.3% of participants who switched to BIC/LEN and 1.6% of participants who remained on complex multi-tablet regimens. A similar incidence of serious drug-related adverse events was reported in both treatment groups (0.3% BIC/LEN; 0% complex multi-tablet regimen), with discontinuations due to adverse events rare (1.6% and 0.5%, respectively).

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

Late-breaking results from ARTISTRY-2

Results from the ARTISTRY-2 trial presented at CROI 2026 further demonstrate the potential of BIC/LEN to broaden current HIV treatment options, offering comparable efficacy to BIKTARVY, a global guideline-recommended single-tablet treatment regimen. Through Week 48, BIC/LEN was non-inferior to standard of care treatment with BIKTARVY in maintaining virologic suppression, with 1.3% of participants receiving BIC/LEN having HIV-1 RNA ≥ 50 copies/mL (as determined by the US FDA-defined snapshot algorithm) compared to 1.0% who remained on BIKTARVY. CD4 cell count remained stable, and two participants in each treatment group met the criteria for resistance analysis.

Resistance analysis showed no treatment‑emergent resistance through Week 48 in three of the four participants (one BIC/LEN‑treated and both BIKTARVY‑treated participants). An isolated integrase substitution without phenotypic resistance was detected in one participant in the BIC/LEN treatment group at Week 36. No capsid mutations were detected. Switching to BIC/LEN was shown to have no significant impact on weight, with body-mass index remaining stable in both groups through 48 weeks of treatment.

BIC/LEN was generally well tolerated with similar rates of drug-related adverse events reported in the BIC/LEN and BIKTARVY treatment groups (10.4% and 12.0%, respectively). No serious drug-related adverse events were reported, and discontinuations due to adverse events were low (1.6%) in both treatment groups.

“The findings from ARTISTRY-2 support the potential of the bictegravir/lenacapavir regimen to expand the range of single-tablet antiretroviral treatments available to people living with HIV,” said Eric Meissner, MD, PhD, Associate Professor, Director of HIV and Hepatitis Patient Care and Research, Medical University of South Carolina. “With efficacy shown to be comparable to a guideline-recommended therapy, we look forward to the prospect of having another meaningful treatment option for adults with HIV who are virologically suppressed.”

Bictegravir and lenacapavir in combination are investigational and not approved anywhere globally. The safety and efficacy of this combination use has not been established.

There is currently no cure for HIV or AIDS.

About ARTISTRY-1

ARTISTRY-1 (NCT05502341) is a multicenter Phase 2/3 clinical trial comparing the investigational once-daily combination of bictegravir, a global guideline-recommended integrase strand transfer inhibitor, and lenacapavir, a first-in-class capsid inhibitor, versus current therapy in people with HIV who are virologically suppressed on complex regimens. In Phase 3, participants were randomized 2:1 to receive a fixed-dose combination of bictegravir 75 mg/lenacapavir 50 mg or continue their stable baseline complex regimen. The primary endpoint was the proportion of patients with HIV-1 RNA ≥50 copies/mL at Week 48 as determined by the US FDA-defined snapshot algorithm. Key secondary endpoints at week 48 included the proportion of participants with virologic suppression (HIV viral load <50 copies/mL per US FDA snapshot), change in baseline in CD4 cell count and the proportion of participants with treatment-emergent adverse events (TEAEs).

About ARTISTRY-2

ARTISTRY-2 (NCT06333808) is a multicenter, double-blind, randomized Phase 3 clinical trial comparing the safety and efficacy of an investigational once-daily combination of bictegravir and lenacapavir versus BIKTARVY in people with HIV who are virologically suppressed. Participants on BIKTARVY were randomized 2:1 to switch onto bictegravir 75 mg/lenacapavir 50 mg or continue their BIKTARVY regimen. The primary endpoint was the proportion of patients with HIV-1 RNA ≥50 copies/mL at Week 48 as determined by the US FDA-defined snapshot algorithm. Key secondary endpoints at Week 48 included the proportion of participants with virologic suppression (HIV viral load <50 copies/mL per US FDA snapshot), change from baseline in CD4 cell count and the proportion of participants with TEAEs.

About Bictegravir

Bictegravir is a global guideline-recommended integrase strand transfer inhibitor (INSTI) with a high barrier to resistance. INSTIs 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.

About Lenacapavir

Lenacapavir is approved in multiple countries as pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV in adults and adolescents who are at risk of HIV acquisition. Lenacapavir is also approved in multiple countries for the treatment of multi-drug-resistant HIV in adults, in combination with other antiretrovirals.

The multi-stage mechanism of action of lenacapavir is distinguishable from other currently approved classes of antiretroviral agents. While most antiretrovirals act on just one stage of viral replication, lenacapavir is designed to inhibit HIV at multiple stages of its lifecycle and has no known cross resistance exhibited in vitro to other existing drug classes.

Lenacapavir is being evaluated as a long-acting option in multiple ongoing and planned early and late-stage clinical studies in Gilead’s HIV prevention and treatment research program. Lenacapavir is being developed as a foundation for potential future HIV therapies with the goal of offering both long-acting oral and injectable options with several dosing frequencies, in combination or as a mono agent, that help address individual needs and preferences of people and communities affected by HIV. Lenacapavir was chosen as one of TIME’s Best Inventions, recognized on Fortune’s Change the World list, named the 2024 Breakthrough of the Year by the journal Science, and selected as the 2025 Prix Galien USA Award for Best Pharmaceutical Product.

About Gilead HIV

For more than 35 years, Gilead has been a leading innovator in the field of HIV, driving advances in treatment, prevention and cure research. Gilead researchers have developed 13 HIV medications, including the first single-tablet regimen to treat HIV, the first antiretroviral for pre-exposure prophylaxis (PrEP) to help reduce new HIV infections, and the first long-acting injectable HIV treatment medication administered twice-yearly. Our advances in medical research have helped to transform HIV into a treatable, preventable, chronic condition for millions of people.

Gilead is committed to continued scientific innovation to provide solutions for the evolving needs of people affected by HIV around the world. Through partnerships, collaborations and charitable giving, the company also aims to improve education, expand access and address barriers to care, with the goal of ending the HIV epidemic worldwide. Gilead has been repeatedly recognized as one of the top two leading philanthropic funders of HIV-related programs in a report released by Funders Concerned About AIDS.

Discover more about Gilead’s unique collaborations worldwide and the work to help end the HIV epidemic.

About Gilead Sciences

Gilead Sciences, Inc. is a biopharmaceutical company that has pursued and achieved breakthroughs in medicine for more than three decades, with the goal of creating a healthier world for all people. The company is committed to advancing innovative medicines to prevent and treat life-threatening diseases, including HIV, viral hepatitis, COVID-19, cancer and inflammation. In 2025, Gilead announced a planned $32 billion investment to further strengthen its U.S. footprint to power the next era of discovery, job creation and public health preparedness – while continuing to invest globally to ensure patients everywhere benefit from its scientific innovation. Gilead operates in more than 35 countries worldwide, with headquarters in Foster City, Calif.

Forward-Looking Statements

This press release includes forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 that are subject to risks, uncertainties and other factors, including Gilead’s ability to initiate, progress or complete clinical trials or studies within currently anticipated timelines or at all, and the possibility of unfavorable results from ongoing and additional clinical trials or studies, including those involving bictegravir and lenacapavir (such as ARTISTRY-1 and ARTISTRY-2); uncertainties relating to regulatory applications and related filing and approval timelines, including potential applications for programs and/or indications currently under evaluation, such as the combination of bictegravir and lenacapavir for HIV-1 infection, and the risk that any regulatory approvals, if granted, may be subject to significant limitations on use or subject to withdrawal or other adverse actions by the applicable regulatory authority; the possibility that Gilead may make a strategic decision to discontinue development of these programs and, as a result, these programs may never be successfully commercialized for the indications currently under evaluation; and any assumptions underlying any of the foregoing. These and other risks, uncertainties and factors are described in detail in Gilead’s Annual Report on Form 10-K for the year ended December 31, 2025, as filed with the U.S. Securities and Exchange Commission. These risks, uncertainties and other factors could cause actual results to differ materially from those referred to in the forward-looking statements. All statements other than statements of historical fact are statements that could be deemed forward-looking statements. The reader is cautioned that any such forward-looking statements are not guarantees of future performance and involve risks and uncertainties and is cautioned not to place undue reliance on these forward-looking statements. All forward-looking statements are based on information currently available to Gilead, and Gilead assumes no obligation and disclaims any intent to update any such forward-looking statements.

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