FDA Approves Bixlenvo, a Single Tablet Option for Adults With HIV

The FDA approved bictegravir 75 mg/lenacapavir 50 mg (Bixlenvo) as a once daily single-tablet regimen for virologically suppressed adults with HIV.¹

The approval covers patients on complex, multidrug regimens who have not been able to use currently available single tablets regimens because of pre-existing resistance or tolerability issues. Gilead described Bixlenvo as the smallest single regimen currently available for HIV treatment.¹

"Bixlenvo offers a new once-daily single tablets regimen designed for the evolving needs of people with HIV," Chloe Orkin, MBE, clinical professor of infection and inequities at Queen Mary University of London, said in a news release.¹ "The approval is a significant advancement in HIV treatment, especially for individuals unable to benefit from guideline-recommended single tablets regimen due to challenges like pre-existing resistance or tolerability. It expands tailored, simplified dosing to people whose needs were not fully met by existing single tablet therapies."

Trial Data Behind the Approval

Bictegravir/lenacapavir pairs bictegravir, a guideline-recommended integrase strand transfer inhibitor with a high barrier to resistance, with lenacapavir, a first-in-class capsid inhibitor with a novel mechanism of action and no cross-resistance to other antiretroviral classes.¹

The approval was supported by 48-week data from the phase 3 ARTISTRY-1 (NCT05502341) and ARTISTRY-2 (NCT06333808) trials, which Gilead said were generally well tolerated with no significant or new safety concerns. The data were also presented at the 33rd Conference on Retroviruses and Opportunistic Infections (CROI 2026).¹

Ahead of the approval, Gilead framed the ARTISTRY program as central to its HIV pipeline. "The ARTISTRY trials represent the latest example of Gilead's commitment to advancing HIV treatment through continuous scientific innovation," Jared Baeten, MD, PhD, senior vice president of clinical development and virology therapeutic area head at Gilead Sciences, said in a February news release announcing the trial results.²

ARTISTRY-1 randomized participants with HIV who were virologically suppressed on complex regimens, 2:1, to switch to bictegravir/lenacapavir or remain on their existing therapy. At week 48, 0.8% of participants who switched had HIV-1 RNA of 50 copies/mL or higher, compared with 1.1% of those who continued their complex regimens.²

CD4 cell counts stayed stable in both groups, and no participant developed treatment-emergent resistance. Participants who switched also had a median total cholesterol reduction of 15 mg/dL, compared with an increase of 2 mg/dL in those who stayed on complex regimens, and their treatment-satisfaction scores rose 7 points from baseline on the HIV Treatment Satisfaction Questionnaire, Status measure, and scores in the comparator group did not change.²

ARTISTRY-1 enrolled the oldest study population in a phase 3 registrational HIV treatment trial to date, with a median participant age of 60 years, a median HIV treatment duration of 28 years, and a baseline pill burden of 2 to 11 pills daily. About 40% of participants were taking antiretroviral therapy more than once a day. Most participants, 81%, were on a complex regimen because of antiretroviral resistance, and 67% had documented resistance to nucleoside reverse transcriptase inhibitors.¹

Earlier phase 2 data from ARTISTRY-1 described a somewhat different profile for that portion of the study population, showing a median HIV treatment duration of 27 years and a median of 3 pills daily before the switch, with adherence exceeding 99% by pill count and participants whose estimated glomerular filtration rates ran as low as 15 to 30 mL/min.³

ARTISTRY-2 compared bictegravir/lenacapavir with bictegravir/emtricitabine/tenofovir alafenamide (Biktarvy) in a double-blind, randomized design among adults already virologically suppressed on Biktarvy. At week 48, 1.3% of the bictegravir/lenacapavir group and 1.0% of the Biktarvy group had HIV-1 RNA of 50 copies/mL or higher, with no capsid mutations detected and body mass index stable in both arms.²

"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," Eric Meissner, MD, PhD, associate professor and director of HIV and hepatitis patient care and research at the Medical University of South Carolina, said in the February release.² "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."

Dosing, Safety, and Pharmacist Considerations

Bixlenvo requires a 2-day loading regimen before patients move to once-daily maintenance dosing. On day 1 and day 2, patients take one Bixlenvo tablet (75 mg/50 mg) along with 2 Sunlenca tablets (300 mg each, for a 600-mg total daily dose). Starting on day 3, patients take Bixlenvo alone, once daily, with or without food.¹

Patients who miss an initiation dose should take it as soon as possible, but should not take both the day 1 and day 2 Sunlenca doses on the same day. If more than 7 days elapse since the last maintenance dose, the initiation regimen may need to be restarted from day 1 if clinically appropriate.¹

Across trials, the most common adverse reactions occurring in more than 2% of patients, all grades, were headache (4%), nausea (3%), and diarrhea (2%). Drug-related adverse events were more frequent in the bictegravir/lenacapavir groups than in the comparator groups, at 14.3% versus 1.6% in ARTISTRY-1 and 10.4% versus 12.0% in ARTISTRY-2, though serious drug-related events and discontinuations due to adverse events were uncommon in both trials.^1,2

Bictegravir/lenacapavir is contraindicated with dofetilide and with strong CYP3A inducers. Drugs that combine strong CYP3A inhibition with UGT1A1 inhibition, or that combine P-glycoprotein, UGT1A1, and strong CYP3A inhibition, can significantly raise concentrations of its components, while strong or moderate CYP3A inducers can significantly decrease them.¹

Clinicians should monitor viral load closely in pregnant patients, since clinical studies found lower bictegravir exposures during pregnancy. Gilead has established an Antiretroviral Pregnancy Registry to track outcomes, and patients with HIV should be counseled about the potential risks of breastfeeding.¹

For pharmacists, the drug-interaction profile and the 2-day initiation sequence make Bixlenvo a regimen that calls for close counseling at dispensing, particularly for patients switching from multidrug regimens who may be used to a different pill schedule. Bictegravir/lenacapavir remains approved only in the United States.¹

REFERENCES

1. Gilead Sciences. 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. 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. Gilead Sciences. Gilead's single-tablet regimen of bictegravir and lenacapavir maintained virological suppression in people with HIV who switched antiretroviral therapy. News release. Gilead Sciences. February 25, 2026. Accessed August 28, 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

3. Gallagher A. Results show single-tablet regimen of bictegravir/lenacapavir maintains virological suppression of HIV. Drug Topics. February 27, 2026. Accessed August 28, 2026. https://www.drugtopics.com/view/results-show-single-tablet-regimen-of-bictegravir-lenacapavir-maintains-virological-suppression-of-hiv