Gilead’s Single-Tablet Regimen of Bictegravir and Lenacapavir maintained virological suppression in people with HIV who switched antiretroviral therapy
The presentation of new Phase 3 ARTISTRY-1 and ARTISTRY-2 trial data at CROI 2026 showed 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.
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.
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.