The US Food and Drug Administration approved bictegravir and lenacapavir (Bixlenvo) to replace current antiretroviral therapy in adults with HIV-1 who have HIV-1 RNA levels below 50 copies/mL while receiving a stable antiretroviral regimen and have no known or suspected resistance to either component, according to a press release from Gilead Sciences.
The once-daily tablet combines bictegravir 75 mg, an integrase strand transfer inhibitor, with lenacapavir 50 mg, a capsid inhibitor. According to Gilead, bictegravir has a high barrier to resistance, and lenacapavir has no cross-resistance to other antiretroviral therapies.
The approval was based on results from the phase 3 ARTISTRY-1 and ARTISTRY-2 trials, which evaluated bictegravir and lenacapavir in adults with HIV who were virologically suppressed. The trials included patients who switched from complex multitablet regimens or from bictegravir, emtricitabine, and tenofovir alafenamide. At 48 weeks, both trials showed comparable maintenance of virologic suppression with bictegravir and lenacapavir, according to Gilead. The company reported that the regimen was generally well tolerated, with no new safety concerns identified.
ARTISTRY-1 participants had a median age of 60 years and a median HIV treatment duration of 28 years. At baseline, participants were taking 2 to 11 pills per day, and approximately 40% received antiretroviral therapy more than once daily. Overall, 67% had nucleoside reverse transcriptase inhibitor resistance, and 81% were receiving a complex regimen because of antiretroviral resistance. Following the switch to bictegravir and lenacapavir, participants showed improvements in some fasting lipid measures and participant-reported treatment satisfaction. ARTISTRY-2 showed no significant change in weight following the switch to bictegravir and lenacapavir.
The most common adverse reactions reported in clinical trials were headache, nausea, and diarrhea. Concomitant administration of bictegravir and lenacapavir is contraindicated with dofetilide and strong CYP3A inducers.
The 2-day initiation regimen consists of bictegravir and lenacapavir plus additional lenacapavir tablets. Beginning on day 3, patients take 1 bictegravir and lenacapavir tablet orally once daily, with or without food.
Source: Gilead Sciences
