Bictegravir/lenacapavir single-tablet once-daily regimen shows promise for HIV treatment
For many people living with HIV, being able to take a once-daily medication to treat HIV and maintain a suppressed viral load has been game-changing. Although single-tablet regimens exist, many people living with HIV aren’t able to take them because they have viral resistance, medication intolerance, or some other contraindication.
In November, Gilead Sciences released Phase 3 study results for the ARTISTRY-1 study which demonstrates promise for a once-daily single-tablet regimen that may benefit people living with HIV on complex antiretroviral therapies (ART) if and when the medication becomes commercially available.
“What is exciting about these results is that this new combination medication really did allow people to simplify from more complex regimens,” said Hyman Scott, MD, MPH, medical director of SFAF. “This study included people who were on multiple HIV medications, including those with multi-drug resistant HIV, and they were really able to simplify their regimen.”
The medication, a combination of the integrase strand transfer inhibitor bictegravir (75 mg) plus the capsid inhibitor lenacapavir (50 mg), was tested in a fixed-dose tablet with people living with HIV who were stable on their HIV treatment and were categorized as being on a complex ART regimen for more than six months.
In the Phase 3 portion of the study, which lasted for 48 weeks, a total of 557 participants were randomized to receive either the bictegravir/lenacapavir therapy (370 people) or to continue their existing HIV treatment (187 people).
Participants in the study were taking between 2 and 11 pills per day for HIV treatment, and about 40% were taking ARVs more than once per day. Many people included in the study had extensive HIV treatment experience: the median duration of HIV treatment was 28 years, and the median number of previous ART regimens was 7. Most were over age 50 and experienced co-existing health conditions including high cholesterol, high blood pressure, and diabetes.
The study met its primary endpoint: the bictegravir/lenacapavir treatment was found to be statistically “non-inferior” to existing multi-tablet regimens, which means that the new single-tablet regimen worked just as well as the more complex regimens.
Dr. Scott said he is looking forward to seeing more details from the study and results, and learning more about how clinically complex the ART regimens were of people who were able to successfully switch to the bictegravir/lenacapavir medication.
“This study did include some people who they classified as having a ‘complex regimen’ even though they were taking two or more tablets once per day–which I wouldn’t necessarily categorize as clinically complex. It will be interesting to see what the diversity in the regimens was, and if there were any differences in outcomes.”
What sets this new medication apart from existing one-tablet, complete two-drug regimens on the market is the ability for people with pre-existing drug resistance to take it.
“We do have another single tablet regimen, Dovato, that is only two drugs,” said Dr. Scott. “And it works really well for people to maintain viral suppression. But we would not use Dovato for someone who has pre-existing resistance, and so that’s where this new two drug regimen may provide another option.”
Gilead reports that participants tolerated the new medication well, and that there were no significant or new safety concerns identified.
References:
November, 2025. Gilead’s Investigational Single-Tablet Regimen of Bictegravir and Lenacapavir for HIV-1 Treatment Meets Primary Endpoint in Phase 3 ARTISTRY-1 Trial. (Press release)
Mounzer, K. and colleagues, 2025. 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). Clinical Infectious Diseases.
Hedgcock, M. and colleagues, 2025. Demographic and clinical characteristics of Phase 3 participants in ARTISTRY-1, an open-label study comparing a bictegravir/lenacapavir single tablet regimen with complex antiretroviral therapy regimens. 20th European AIDS Conference.
