FDA Approves Bixlenvo Once-Daily Single-Tablet Regimen for Virologically Suppressed Adults With HIV

The FDA has approved bictegravir/lenacapavir (Bixlenvo; Gilead Sciences), a once-daily single-tablet regimen for adults with HIV-1 who are virologically suppressed on a stable antiretroviral regimen. The approval introduces a treatment-switch option designed to maintain viral suppression while reducing pill burden for eligible patients, including some who have required complex multidrug regimens because of resistance, tolerability concerns, contraindications, or drug interactions.¹

Bixlenvo contains bictegravir 75 mg, an integrase strand transfer inhibitor with a high barrier to resistance, and lenacapavir 50 mg, a first-in-class capsid inhibitor. It is indicated to replace an existing regimen in adults with HIV-1 RNA below 50 copies/mL who have no known or suspected resistance to either component.¹

ARTISTRY-1 Supports Simplification From Complex Regimens

The approval was supported by the phase 3 ARTISTRY-1 (NCT05502341) and ARTISTRY-2 (NCT06333808) trials. Both evaluated whether patients with sustained virologic suppression could switch to bictegravir/lenacapavir without compromising viral control.¹

ARTISTRY-1 enrolled adults receiving complex antiretroviral regimens and randomly assigned them 2:1 to switch to bictegravir/lenacapavir or continue their baseline therapy. At week 48, HIV-1 RNA of at least 50 copies/mL was reported in 1% of participants receiving bictegravir/lenacapavir and 1% of those continuing their complex regimen, meeting the study’s noninferiority criterion (difference -0.3%; 95.002% CI, -2.3 to 1.8). CD4 cell counts remained stable, and no treatment-emergent resistance was detected.²

The study population reflected patients with substantial treatment experience. Participants had received HIV therapy for a median of 28 years, and the median age was 60 years. At baseline, participants took between 2 and 11 pills per day, with approximately 40% administering antiretroviral therapy more than once daily. Historical nucleoside reverse transcriptase inhibitor resistance was present in 67% of participants, and 81% were receiving a complex regimen because of antiretroviral resistance.^1,2

Switching to bictegravir/lenacapavir also improved selected fasting lipid measures and patient-reported treatment satisfaction. Median total cholesterol declined by 15 mg/dL in the switch group compared with an increase of 2 mg/dL among participants who remained on their baseline regimen. Treatment satisfaction increased by a mean of 7 points after the switch, whereas the comparison group reported no change.²

ARTISTRY-2 Demonstrates Comparable Viral Control to Biktarvy

ARTISTRY-2 compared bictegravir/lenacapavir with bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy; Gilead Sciences) in virologically suppressed adults. Participants receiving Biktarvy were randomly assigned 2:1 to switch to bictegravir/lenacapavir or remain on their existing treatment.³

At week 48, 1.3% of patients receiving bictegravir/lenacapavir had HIV-1 RNA of at least 50 copies/mL compared with 1.0% of patients continuing Biktarvy, establishing noninferiority. CD4 cell counts remained stable in both groups. No capsid resistance mutations emerged, although an isolated integrase substitution without phenotypic resistance was detected in 1 participant receiving bictegravir/lenacapavir. Body mass index remained stable after the treatment switch.³

Drug-related adverse events occurred in 10.0% of participants receiving bictegravir/lenacapavir and 12.0% of those continuing Biktarvy. No serious drug-related adverse events were reported, and 1.6% of participants in each group discontinued treatment because of adverse events.³

Dosing and Pharmacist Considerations

Bixlenvo requires a 2-day initiation regimen with oral lenacapavir (Sunlenca; Gilead Sciences). On days 1 and 2, patients take 1 Bixlenvo tablet with 2 oral Sunlenca 300-mg tablets. Beginning on day 3, patients take 1 Bixlenvo tablet once daily, with or without food. If more than 7 days have passed since the previous maintenance dose, the initiation regimen should be restarted when continued treatment remains clinically appropriate.¹

The most common adverse reactions in the ARTISTRY program were headache, reported in 4% of participants; nausea, reported in 3%; and diarrhea, reported in 2%. Bixlenvo is contraindicated with dofetilide and strong cytochrome P450 3A inducers. Pharmacists should perform a complete interaction assessment because CYP3A, UGT1A1, and P-glycoprotein modulators can alter exposure to the regimen’s components.^1,4

For eligible patients, the approval provides a route from complicated therapy to a single daily tablet without sacrificing virologic control. Pharmacists can support safe implementation by confirming resistance history, reviewing interacting medications, counseling patients on the 2-day initiation schedule, and reinforcing adherence during the transition.

REFERENCES

1. U.S. FDA approves Gilead’s Bixlenvo, a new once-daily single tablet option for virologically suppressed adults with HIV, including those on complex regimens. News release. Gilead Sciences. Published August 27, 2026. Accessed August 28, 2026. https://www.gilead.com/news/news-details/2026/u-s--fda-approves-gileads-bixlenvo-a-new-once-daily-single-tablet-option-for-virologically-suppressed-adults-with-hiv-including-those-on-complex-regimens

2. Orkin C, Ruane PJ, Hedgcock M, et al. Switch to single-tablet bictegravir-lenacapavir from a complex HIV regimen (ARTISTRY-1): a randomised, open-label, phase 3 clinical trial. Lancet. 2026;407(10535):1249-1258. doi:10.1016/S0140-6736(26)00307-7

3. Meissner EG, Ramgopal M, Ruane PJ, et al. Safety and efficacy of switching to bictegravir-lenacapavir versus continuing bictegravir-emtricitabine-tenofovir alafenamide in virologically suppressed people with HIV-1 (ARTISTRY-2): a double-blind, multicentre, randomised, controlled, phase 3, non-inferiority trial. Lancet HIV. 2026;13(8):e538-e547. doi:10.1016/S2352-3018(26)00078-0

4. Gilead Sciences. Bixlenvo prescribing and safety information. Accessed August 28, 2026. https://www.gilead.com/-/media/files/pdfs/medicines/hiv/bixlenvo/bixlenvo_pi.pdf