Biktarvy represents a significant advancement in the treatment of HIV-1 infection, offering a complete antiretroviral regimen within a single, once-daily tablet. It combines three potent 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 integrase strand transfer inhibitor (INSTI)-based regimen is indicated for 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 optimizing efficacy while minimizing the treatment burden and potential 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), which demonstrates enhanced delivery to lymphoid tissues and reduced systemic tenofovir exposure compared to tenofovir disoproxil fumarate (TDF).
• High genetic barrier to resistance, supported by the pharmacokinetic boosting effect of bictegravir.
• Approved for use in treatment-naïve adults and as a replacement therapy for virologically suppressed adults with no history of treatment failure or known resistance to any component.

Benefits

• Achieves rapid and durable viral suppression, with high rates of virological success demonstrated in pivotal clinical trials.
• Simplifies treatment regimens by combining three antiretroviral agents into a single tablet, potentially improving adherence and quality of life.
• Favorable renal and bone safety profile compared to regimens containing tenofovir disoproxil fumarate, due to the targeted action of tenofovir alafenamide.
• Low potential for drug-drug interactions, though certain coadministrations require caution or are contraindicated.
• Supports long-term management goals with a well-tolerated side effect profile for most patients.

Common use

Biktarvy is primarily prescribed for the treatment of HIV-1 infection in adults. It is used both as initial therapy in antiretroviral-naïve individuals and as a switch option for those who are already virologically suppressed on a stable antiretroviral regimen and have no history of treatment failure or known mutations associated with resistance to bictegravir, emtricitabine, or tenofovir. It is not a cure for HIV infection and does not reduce the risk of transmitting HIV to others.

Dosage and direction

The recommended dosage of Biktarvy is one tablet taken orally once daily, with or without food. It is critical that patients take Biktarvy consistently at approximately the same time each day to maintain stable drug levels. Tablets should be swallowed whole and not crushed, chewed, or split. Dosage adjustment is not required in patients with estimated creatinine clearance ≥30 mL/min. Use is not recommended in patients with severe renal impairment (CrCl <30 mL/min) or end-stage renal disease requiring dialysis.

Precautions

Prior to initiating Biktarvy, test for hepatitis B virus (HBV) coinfection, as post-treatment exacerbation of hepatitis may occur. 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. Although the risk is reduced with TAF, long-term bone and renal monitoring remains advisable.

Contraindications

Biktarvy is contraindicated in patients with a known hypersensitivity to any component of the formulation. Coadministration with rifampin is contraindicated due to significant decreases in bictegravir plasma concentrations, which may lead to loss of virologic response and possible resistance. Concomitant use with other strong inducers of UGT1A1 or CYP3A enzymes (e.g., rifapentine, St. John’s wort) is not recommended.

Possible side effects

The most common adverse reactions (≥5% incidence) in clinical trials were diarrhea, nausea, and headache. Serious side effects may include exacerbation of hepatitis B in coinfected patients, lactic acidosis/severe hepatomegaly with steatosis, and renal impairment, including acute renal failure and Fanconi syndrome. Immune reconstitution syndrome and redistribution/accumulation of body fat have been reported. Less common effects include insomnia, fatigue, and dizziness.

Drug interaction

Biktarvy has a low potential for interactions but may be affected by drugs that induce UGT1A1 or CYP3A. Coadministration with the following requires caution or alternative agents: antacids containing aluminum, magnesium, or calcium (administer Biktarvy 2 hours before or 6 hours after); supplements or drugs containing polyvalent cations (e.g., iron, calcium); certain anticonvulsants (carbamazepine, oxcarbazepine, phenobarbital, phenytoin); and certain HIV protease inhibitors. Consult full prescribing information before coadministration with other antiretrovirals or narrow therapeutic index drugs.

Missed dose

If a dose is missed and it is within 18 hours of the usual time, the patient should take Biktarvy as soon as possible and then 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. Patients should not take a double dose to make up for a missed dose.

Overdose

There is limited experience with overdose of Biktarvy. Management should consist of general supportive measures, including monitoring of vital signs and observation of clinical status. Since tenofovir is efficiently removed by hemodialysis, removal of bictegravir or emtricitabine by dialysis is unlikely, but hemodialysis may be considered in cases of significant tenofovir overdose.

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 out of reach of children and pets.

Disclaimer

This information is intended for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always seek the advice of a qualified healthcare provider with any questions regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of information provided here.

Reviews

Clinical trial data and real-world evidence consistently support the efficacy, tolerability, and convenience of Biktarvy. In phase 3 studies, Biktarvy demonstrated non-inferiority to comparator regimens with high virologic suppression rates (e.g., 89%–92% at Week 144) and a favorable safety profile. Providers report high patient satisfaction due to the once-daily, single-tablet regimen and low incidence of significant side effects. Long-term data continue to reinforce its role as a cornerstone of modern antiretroviral therapy.