Bictegraviremtricitabinetenofovir

Bictegraviremtricitabinetenofovir is a fixed-dose combination antiretroviral therapy used in the treatment of HIV-1 infection. It combines three active agents: bictegravir, an integrase strand transfer inhibitor; emtricitabine, a nucleoside reverse transcriptase inhibitor; and tenofovir alafenamide, a prodrug of tenofovir and another nucleoside reverse transcriptase inhibitor. The formulation is provided as a single tablet taken once daily, with or without food, as part of combination antiretroviral therapy.

Indications and use

The combination is indicated for the treatment of HIV-1 infection in adults and certain pediatric patients as part of combination ART. It is commonly used as a complete regimen for therapy-naive adults and as a switch option for virologically suppressed patients under appropriate clinical guidance. It is not intended for treatment of HIV-2 infection. Treatment decisions consider viral resistance, prior ART exposure, and comorbid conditions.

Dosing and administration

The standard dosing is one tablet once daily. It should be taken consistently, with or without food. The regimen is generally not recommended for individuals with creatinine clearance below a specified threshold (reduced or avoided with severe renal impairment). Concomitant use with certain drugs or supplements may require dose adjustments or avoidance.

Safety and adverse effects

Common adverse effects include diarrhea, nausea, and fatigue. As with other antiretrovirals, potential renal and bone safety considerations exist, particularly with long-term use, though tenofovir alafenamide is associated with less renal and bone toxicity than tenofovir disoproxil fumarate in some regimens. Patients should be monitored regularly for kidney function and other adverse effects, and interactions with other medications should be reviewed.

History and context

Bictegraviremtricitabinetenofovir was developed by pharmaceutical manufacturers and approved by regulatory agencies in the late 2010s as part of a move toward single-tablet regimens with high barriers to resistance.