Results Show Single-Tablet Regimen of Bictegravir/Lenacapavir Maintains Virological Suppression of HIV

Gilead Sciences announced promising results from its phase 3 ARTISTRY trials, demonstrating that an investigational once-daily single-tablet regimen combining the integrase strand transfer inhibitor bictegravir 75 mg with the first-in-class capsid inhibitor lenacapavir 50 mg successfully maintained virological suppression in patients living with HIV.¹

These findings, presented at the 2026 Conference on Retroviruses and Opportunistic Infections, provide critical evidence for pharmacists and clinicians looking to simplify complex antiretroviral therapy without sacrificing efficacy or safety. The single-tablet combination proved effective for individuals switching from both multi-tablet regimens and standard-of-care single-tablet treatments such as bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy).¹

In the phase 3 ARTISTRY-1 (NCT05502341) trial, which specifically targeted patients on complex multi-tablet regimens, the bictegravir/lenacapavir (BIC/LEN) fixed-dose combination demonstrated statistical noninferiority in maintaining virologic suppression at 48 weeks.¹

Only 0.8% of participants on the new single-tablet regimen had HIV-1 RNA levels 50 copies/mL or more, compared to 1.1% of those who remained on their complex baseline regimens. Beyond viral control, the switch was associated with notable improvements in metabolic health and patient-reported outcomes, including a median decrease in total cholesterol of 15 mg/dL and a significant increase in treatment satisfaction scores. Many complex regimens include boosted protease inhibitors, which are often associated with metabolic complications and a higher potential for drug-drug interactions that pharmacists should be aware of.^1,2

The phase 3 ARTISTRY-2 (NCT06333808) trial further validated the regimen by comparing it to Biktarvy in virologically suppressed adults. The BIC/LEN combination again met its primary end point for noninferiority, with 1.3% of participants having viral loads 50 copies/mL or more versus 1.0% in the Biktarvy group.¹

Importantly for long-term management, the switch to BIC/LEN had no significant impact on body weight or body mass index over 48 weeks. The safety profile remained robust across both trials, with drug-related adverse events occurring in roughly 10% to 14% of participants, most of which were mild, and discontinuations due to adverse events remaining rare at only 1.6%.¹

From a pharmacological perspective, the combination pairs 2 agents with distinct, potent mechanisms. Bictegravir is a standard-of-care integrase inhibitor known for its high barrier to resistance. Lenacapavir is a novel capsid inhibitor that inhibits HIV at multiple stages of its lifecycle and currently has no known cross-resistance to other existing drug classes.^2,3

Earlier phase 2 data from ARTISTRY-1 highlighted that this combination is particularly useful for treatment-experienced individuals who may have been relegated to complex regimens due to a history of resistance, intolerance, or contraindications to current single-tablet regimen. In that phase, participants had a median HIV treatment duration of 27 years and were taking a median of 3 pills per day before switching to the simplified once-daily option.^1,4

The investigational regimen also showed high levels of treatment adherence, which is a vital factor in long-term HIV management often facilitated by pharmacy-led counseling. Phase 2 data showed median adherence rates exceeding 99% based on pill counts.⁴

Furthermore, the combination appears suitable for a wide range of patients, including an aging population. The studies included individuals with a median age of 60 years and those with estimated glomerular filtration rates as low as 15 to 30 mL/min, suggesting potential utility in patients with chronic kidney disease.⁴

Although the combination is currently investigational and not yet approved by the FDA, Gilead plans to use these phase 3 results as the basis for upcoming regulatory submissions to expand treatment options for suppressed adults.¹

READ MORE: HIV Resource Center

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REFERENCES

1. Gilead’s single-tablet regimen of bictegravir and lenacapavir maintained virological suppression in people with HIV who switched antiretroviral therapy. News release. Gilead. February 25, 2026. Accessed February 26, 2026. https://www.gilead.com/news/news-details/2026/gileads-single-tablet-regimen-of-bictegravir-and-lenacapavir-maintained-virological-suppression-in-people-with-hiv-who-switched-antiretroviral-therapy

2. Study to compare bictegravir/​lenacapavir versus current therapy in people with HIV-1 who are successfully treated with a complicated regimen (ARTISTRY-1). ClinicalTrials.gov identification: NCT05502341. Updated October 14, 2025. https://clinicaltrials.gov/study/NCT05502341

3. Study to compare bictegravir/​lenacapavir versus current therapy in people with HIV-1 who are successfully treated with biktarvy (ARTISTRY-2). ClinicalTrials.gov identification: NCT06333808. Updated November 5, 2025. https://clinicaltrials.gov/study/NCT06333808

4. Mounzer K, Slim J, Ramgopal M, Hedgcock M, Bloch M, Santana J, Mendes I, Guo Y, Arora P, Montezuma-Rusca JM, Sklar P, Baeten JM, Segal-Maurer S. Efficacy and Safety of Switching to Daily Bictegravir Plus Lenacapavir From a Complex HIV Treatment Regimen: A Randomized, Open-Label, Multicenter Phase 2 Study (ARTISTRY-1). Clin Infect Dis. 2025 Apr 30;80(4):881-888. doi: 10.1093/cid/ciae522. PMID: 39589133; PMCID: PMC12043062.