Biktarvy represents a significant advancement in the treatment of HIV-1 infection, offering a complete, once-daily, single-tablet regimen for adults and pediatric patients weighing at least 25 kg. This fixed-dose combination integrates three potent antiretroviral agents—bictegravir, emtricitabine, and tenofovir alafenamide—into a highly effective and well-tolerated therapeutic option. It is indicated for both treatment-naïve patients and as a replacement for a stable antiretroviral regimen in those who are virologically suppressed, providing a streamlined approach to long-term viral suppression. Its development reflects a continued commitment to reducing pill burden and minimizing potential long-term toxicities, thereby supporting improved adherence and quality of life.

Features

• Fixed-dose combination tablet containing bictegravir 50 mg, emtricitabine 200 mg, and tenofovir alafenamide 25 mg.
• Once-daily oral administration, independent of food, enhancing convenience and adherence.
• Formulated with tenofovir alafenamide, which demonstrates improved renal and bone safety profiles compared to tenofovir disoproxil fumarate.
• High barrier to resistance, supported by the integrase strand transfer inhibitor (INSTI) class properties of bictegravir.
• Approved for use in adults and pediatric patients weighing at least 25 kg.

Benefits

• Achieves and maintains virologic suppression with a high efficacy rate in clinical trials, reducing HIV-1 RNA to undetectable levels.
• Minimizes pill burden through a single-tablet regimen, supporting long-term adherence and reducing the risk of treatment failure.
• Exhibits a favorable safety and tolerability profile, with low incidence of neuropsychiatric and weight-related adverse events compared to some other INSTIs.
• Lowers potential for renal and bone toxicity due to the tenofovir alafenamide component, benefiting long-term health outcomes.
• Provides a robust treatment option with a high genetic barrier to resistance, reducing the likelihood of virologic breakthrough.
• Suitable for a broad patient population, including those switching from other regimens, facilitating simplified disease management.

Common use

Biktarvy is primarily prescribed for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 25 kg. It is used both as initial therapy in antiretroviral-naïve individuals and as a replacement regimen for those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and no known resistance to any of its components. Its use is grounded in guidelines from major health organizations, which recommend integrase strand transfer inhibitor-based regimens for first-line treatment due to their potency and tolerability.

Dosage and direction

The recommended dosage of Biktarvy is one tablet taken orally once daily, with or without food. It is crucial to maintain consistent dosing timing to ensure stable drug levels. For pediatric patients, administration is weight-based; it is approved for those weighing at least 25 kg, with the same once-daily, one-tablet regimen. No dosage adjustment is required in patients with estimated creatinine clearance ≥30 mL/min. In cases of severe renal impairment (CrCl <30 mL/min) or end-stage renal disease, Biktarvy is not recommended due to lack of data and potential for increased tenofovir exposure.

Precautions

Prior to initiating Biktarvy, test for hepatitis B virus (HBV) coinfection, as discontinuation may lead to acute exacerbation of hepatitis. 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 depression or other psychiatric disorders, as INSTIs have been associated with neuropsychiatric events. Consider the potential for weight gain, which has been observed with some antiretroviral regimens.

Contraindications

Biktarvy is contraindicated in patients with a previous hypersensitivity reaction to any of its components. Concomitant use with rifampin is contraindicated due to significant decreases in bictegravir and tenofovir concentrations, which may lead to loss of virologic response and possible resistance. It is also contraindicated with other strong inducers of UGT1A1 or CYP3A, such as rifapentine, St. John’s wort, and certain anticonvulsants, due to the risk of reduced efficacy.

Possible side effects

The most common adverse reactions (incidence ≥5%) in clinical trials were diarrhea, nausea, and headache. Less common but potentially serious side effects include lactic acidosis/severe hepatomegaly with steatosis, exacerbations of HBV in coinfected patients, and renal impairment, including acute renal failure and Fanconi syndrome. Instances of immune reconstitution syndrome and weight increase have been reported. Neuropsychiatric events, such as depression, insomnia, and suicidal ideation, though less frequent, have been associated with INSTI class drugs and should be monitored.

Drug interaction

Biktarvy may interact with drugs that induce or inhibit CYP3A and UGT1A1. Coadministration with carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, and St. John’s wort is not recommended. Antacids containing aluminum, magnesium, or calcium should be administered at least 2 hours before or 6 hours after Biktarvy. Supplements or drugs containing polyvalent cations (e.g., iron, calcium) may reduce bictegravir absorption; administer simultaneously only with food or separate by 2 hours. Use with caution alongside drugs that reduce renal function or compete for active tubular secretion, such as acyclovir, cidofovir, ganciclovir, valacyclovir, and high-dose or multiple NSAIDs, due to potential increases in tenofovir concentrations.

Missed dose

If a dose is missed within 18 hours of the usual time, the patient should take Biktarvy as soon as possible and resume the normal dosing schedule. If more than 18 hours have passed, the missed dose should be skipped, and the next dose taken at the regularly scheduled time. Patients should not take a double dose to make up for a missed one. Consistent adherence is critical to maintaining virologic suppression and preventing the development of resistance.

Overdose

There is limited experience with overdose of Biktarvy. In the event of overdose, monitor the patient for evidence of toxicity and provide supportive treatment, which may include monitoring of vital signs and ECG. Since tenofovir alafenamide is extensively protein-bound, it is unlikely to be significantly removed by dialysis; however, the removal of emtricitabine by hemodialysis has been documented. Management should focus on symptomatic and supportive care, with attention to potential renal, gastrointestinal, and metabolic effects.

Storage

Store Biktarvy tablets at room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Keep in the original container to protect from moisture, and keep the bottle tightly closed. Do not remove the desiccant. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the label.

Disclaimer

This information is intended for educational purposes 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 before starting any new treatment. Do not disregard professional medical advice or delay in seeking it because of something you have read here. The efficacy and safety of Biktarvy may vary based on individual patient factors, including comorbidities, concomitant medications, and adherence.

Reviews

In clinical trials and real-world evidence, Biktarvy has demonstrated high rates of virologic suppression and a favorable tolerability profile. Study 1489 and 1490, which involved treatment-naïve adults, showed that 92.4% and 89.4% of participants achieved HIV-1 RNA <50 copies/mL at Week 48, respectively, with low discontinuation rates due to adverse events. In switch studies, such as Study 1878, Biktarvy maintained suppression in 99% of participants at Week 48. Patients and providers frequently report satisfaction with the convenience, efficacy, and minimal side effects, though individual experiences with weight gain or neuropsychiatric symptoms vary. Long-term data continue to support its role as a cornerstone of modern antiretroviral therapy.