Single-Tablet Bictegravir/Lenacapavir Effective After Treatment Switch

Patients with HIV may be able to switch from a multi-tablet regimen to a single-tablet regimen, as a single-tablet regimen of bictegravir 75 mg/lenacapavir 50 mg (BIC/LEN) was found to be equally effective when patients switched from multi-tablet regimens to treat their HIV diagnosis. These results come from the ARTISTRY-1 clinical trial, a phase 3 study.¹

Results from the ARTISTRY-1 trial had previously been published earlier in the year, with ARTISTRY-1 showing BIC/LEN was able to keep all but 1 of 103 participants virally suppressed compared with all 25 patients who remained virally suppressed on complex antiretroviral therapy (ART) regimens through 24 weeks.² These new results update the previous study to evaluate the efficacy through 48 weeks.

Patients on complex regimens are often not able to benefit from single-tablet regimens due to drug-drug interactions, pre-existing resistance, and tolerability, which can leave them with a higher burden of pills to take. Those who participated in ARTISTRY-1 were taking between 2 and 11 pills per day to continue to be virally suppressed. The single-tablet regimen of BIC/LEN aims to address these patients by offering a combination therapy in a single tablet.

“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,” said Jared Baeten, MD, PhD, senior vice president of clinical development at Gilead Sciences.¹

BIC is an integrase strand transfer inhibitor that has a higher barrier to resistance and is only used in combination. LEN has been approved as a method of pre-exposure prophylaxis but has also been used to treat multi-drug-resistant HIV in adults, with its use approved in multiple countries.

Participants of the ARTISTRY-1 trial were aged 18 years or older,² were virally suppressed for at least 6 months before screening, and were on a stable, complex ART regimen for at least 6 months due to either intolerance, previous viral resistance, or a contraindication to existing single-tablet regimens. Participants were recruited from Australia, Canada, the US, the Dominican Republic, and Puerto Rico.

For the phase 3 part of the study, participants were randomized 2:1 to either BIC/LEN or continued their baseline complex regimen. The study looked for a primary end point of viral suppression of less than 50 copies/mL after 48 weeks, as well as, change in baseline CD4 cell count and the occurrence of treatment-emergent adverse events (TEAEs).

In new results whose details will be revealed at a later date, researchers found that the primary efficacy end point of ARTISTRY-1 was met through 48 weeks and was well-tolerated in the patients.

“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,” said Chloe Orkin, MBE, clinical professor of Infection and Inequities at Queen Mary University of London.¹

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 14, 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. Mounzer K, Slim J, Ramgopal M, et al. 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;80(4):881-888. doi:10.1093/cid/ciae522