Biktarvy represents a significant advancement in the treatment of HIV-1 infection, offering a complete antiretroviral regimen in a single, once-daily tablet. It combines three potent antiretroviral agents—bictegravir, emtricitabine, and tenofovir alafenamide—into a fixed-dose combination designed to achieve and maintain viral suppression with a high barrier to resistance. This regimen is indicated for use in both treatment-naïve adults and virologically suppressed adults seeking to replace their current antiretroviral therapy, providing a streamlined approach to long-term HIV management. Its development reflects a continued commitment to improving patient adherence, reducing pill burden, and minimizing long-term toxicities associated with lifelong therapy.

Features

• Fixed-dose combination tablet containing bictegravir 50 mg, emtricitabine 200 mg, and tenofovir alafenamide 25 mg.
• Once-daily oral administration, independent of food.
• Formulated with tenofovir alafenamide (TAF), a targeted prodrug of tenofovir that achieves high intracellular concentrations with lower systemic exposure.
• Integrates an unboosted integrase strand transfer inhibitor (INSTI) with a dual NRTI backbone.
• High genetic barrier to resistance, supported by in vitro and clinical trial data.
• Available in 30-count bottles with a child-resistant closure.

Benefits

• Achieves rapid and durable viral suppression, with high rates of virologic success in clinical trials.
• Simplifies treatment regimens by combining three agents into one tablet, enhancing adherence and quality of life.
• Demonstrates a favorable renal and bone safety profile compared to regimens containing tenofovir disoproxil fumarate (TDF).
• Minimizes drug-drug interaction potential due to the absence of a pharmacokinetic enhancer (e.g., cobicistat or ritonavir).
• Supports long-term management with a well-tolerated side effect profile in a broad patient population.
• Reduces the risk of resistance development, supporting sustained treatment efficacy.

Common use

Biktarvy is indicated for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 25 kg who have no antiretroviral treatment history or who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen for at least three months with no history of treatment failure and no known substitutions associated with resistance to the individual components of Biktarvy. It is not recommended for use in patients with severe renal impairment (CrCl <30 mL/min) or severe hepatic impairment.

Dosage and direction

The recommended dosage of Biktarvy is one tablet taken orally once daily, with or without food. It should be swallowed whole and not chewed, crushed, or split. For pediatric patients weighing at least 25 kg, the same once-daily dosing applies. Dosage adjustment is not required in patients with mild to moderate renal impairment (CrCl ≥30 mL/min) or mild to moderate hepatic impairment (Child-Pugh Class A or B). Adherence to the prescribed dosing schedule is critical to maintain virologic suppression and prevent the development of resistance.

Precautions

Prior to initiating Biktarvy, test for hepatitis B virus (HBV) coinfection, as post-treatment exacerbation of hepatitis may occur in patients coinfected with HIV-1 and HBV after discontinuation of antiretroviral therapy. Assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein at baseline and during therapy as clinically appropriate. Monitor for immune reconstitution syndrome, which may necessitate further evaluation and management. Use with caution in patients with a history of bone pathology or risk factors for renal impairment.

Contraindications

Biktarvy is contraindicated in patients with a known hypersensitivity to any component of the product. Coadministration with rifampin is contraindicated due to significant decreases in bictegravir plasma concentrations, which may lead to loss of virologic response and possible resistance. Do not use with other products containing emtricitabine, tenofovir alafenamide, tenofovir disoproxil fumarate, or lamivudine.

Possible side effects

The most common adverse reactions (all grades, incidence ≥5%) in clinical trials were diarrhea, nausea, and headache. Serious side effects may include exacerbation of hepatitis B in coinfected patients, immune reconstitution syndrome, and lactic acidosis/severe hepatomegaly with steatosis. Renal adverse events, including declines in creatinine clearance, have been reported, though less frequently than with TDF-containing regimens. Less common but notable effects include rash and sleep disturbances.

Drug interaction

Biktarvy may interact with drugs that induce UGT1A1 or CYP3A, such as rifampin, carbamazepine, and St. John’s wort, leading to reduced bictegravir concentrations. Coadministration with polyvalent cations (e.g., antacids containing aluminum, magnesium, or calcium; laxatives; sucralfate; buffered medications) may chelate bictegravir and reduce its absorption—administer Biktarvy at least 2 hours before or 6 hours after these products. Use with drugs that reduce renal function or compete for active tubular secretion may increase concentrations of emtricitabine and tenofovir.

Missed dose

If a dose is missed and it is within 18 hours of the usual dosing time, the patient should take Biktarvy as soon as possible and resume the normal dosing schedule. If more than 18 hours have passed, the patient should skip the missed dose and take the next dose at the regularly scheduled time. The patient should not take a double dose to make up for a missed dose. Consistently missed doses may increase the risk of virologic failure and resistance.

Overdose

There is no specific antidote for overdose with Biktarvy. Treatment should consist of general supportive measures, including monitoring of vital signs and observation of the patient’s clinical status. Hemodialysis may remove emtricitabine and tenofovir alafenamide (and its metabolites), but is unlikely to significantly remove bictegravir due to high protein binding. If overdose occurs, contact a Poison Control Center for the most current guidance.

Storage

Store Biktarvy tablets at room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Keep in the original container to protect from moisture. Keep tightly closed and out of reach of children and pets. Do not use if the seal over the bottle opening is broken or missing.

Disclaimer

This information is intended for healthcare professionals and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of a qualified healthcare provider with any questions regarding a medical condition or treatment options. Do not disregard professional medical advice or delay in seeking it because of something you have read in this document. The full prescribing information should be consulted before initiating therapy.

Reviews

Clinical trials and real-world evidence have consistently demonstrated the efficacy, safety, and tolerability of Biktarvy. In Phase 3 studies, Biktarvy achieved high rates of virologic suppression (HIV-1 RNA <50 copies/mL) at 48 and 144 weeks, with responses non-inferior to comparator regimens. Real-world analyses support these findings, noting high adherence rates and patient satisfaction due to the single-tablet regimen. Healthcare providers frequently cite its favorable safety profile, minimal interactions, and convenience as key advantages in both naive and switch scenarios.