In recognition of World AIDS Day 2024, our latest edition of the Guidelines+ Monographs Series will delve into the medication bictegravir, emtricitabine, and tenofovir alafenamide, marketed under the brand name Biktarvy®  by Gilead Sciences, Inc. Biktarvy is a three-drug combination of bictegravir (BIC), a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI), and emtricitabine (FTC) and tenofovir alafenamide (TAF), both HIV-1 nucleoside analog reverse transcriptase inhibitors (NRTIs), and is indicated as a complete regimen for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 14 kg who have no antiretroviral treatment history or to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known or suspected substitutions associated with resistance to bictegravir or tenofovir. It was initially approved in 2018.

In the following sections, we will provide a comprehensive overview of bictegravir, emtricitabine, and tenofovir alafenamide and analyze its positioning across various guidelines for its approved indications.

Note* – This Guidelines+ Monographs for bictegravir, emtricitabine, and tenofovir alafenamide (Biktarvy) is current as of December 2024. Consult our clinical guidelines library and/or or medication information lookup tool to ensure you are always accessing the most current information.

Medication Overview:

  • Brand name: Biktarvy
  • Generic name: bictegravir, emtricitabine, and tenofovir alafenamide 
  • Manufacturer(s): Gilead Sciences, Inc
  • Initial FDA Approval: February 2018

Indications and FDA Approval Details

Indicated ConditionIndicated Age RangeDate Approved
HIV-1 infectionFor the treatment of HIV-1 who have no antiretroviral treatment historyAdultsFebruary 2018
HIV-1 infectionFor the treatment of HIV-1 who have no antiretroviral treatment historyPediatric patients weighing at least 14 kgOctober 2021
HIV-1 infectionTo treat people with HIV (PWH) who have suppressed viral loads with known or suspected M184V/I resistance, a common form of treatment resistance.AdultsFebruary 2024

Dosage and Administration

  • Testing: Prior to or when initiating BIKTARVY test for hepatitis B virus infection. Prior to or when initiating BIKTARVY, and during treatment, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, also assess serum phosphorus. 
  • Recommended dosage in adults and pediatric patients weighing at least 25 kg, or virologically-suppressed adults with estimated creatinine clearance below 15 mL/min receiving chronic hemodialysis: One tablet containing 50 mg BIC, 200 mg FTC, and 25 mg TAF taken once daily with or without food. 
  • Recommended dosage in pediatric patients weighing at least 14 kg to less than 25 kg: One tablet containing 30 mg BIC, 120 mg FTC, and 15 mg TAF taken once daily with or without food. 
  • Recommended dosage in pregnant individuals who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known substitutions associated with resistance to the individual components of BIKTARVY: One tablet containing 50 mg BIC, 200 mg FTC, and 25 mg TAF taken orally once daily with or without food. 
  • Renal impairment: BIKTARVY is not recommended in patients with estimated creatinine clearance of 15 to below 30 mL/min, or below 15 mL/min who are not receiving chronic hemodialysis, or below 15 mL/min who have no antiretroviral treatment history. 
  • Hepatic impairment: BIKTARVY is not recommended in patients with severe hepatic impairment. 

WARNING: POST TREATMENT ACUTE EXACERBATION OF HEPATITIS B

See full prescribing information for complete boxed warning.

  • Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF), and may occur with discontinuation of BIKTARVY. Closely monitor hepatic function in these patients. If appropriate, anti-hepatitis B therapy may be warranted.

Warnings and Precautions

  • Immune reconstitution syndrome: May necessitate further evaluation and treatment. 
  • New onset or worsening renal impairment: Assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein when initiating BIKTARVY and during therapy as clinically appropriate in all patients. Also assess serum phosphorus in patients with chronic kidney disease. 
  • Lactic acidosis/severe hepatomegaly with steatosis: Discontinue treatment in patients who develop symptoms or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity.

Adverse Reactions

  • Most common adverse reactions (incidence greater than or equal to 5%, all grades) are diarrhea, nausea, and headache.

Now that we’ve covered the basic monograph information for Biktarvy, let’s take a closer look at how it is currently recommended in various clinical practice guidelines.

Specific Inclusions of Bictegravir, Emtricitabine, & Tenofovir Alafenamide in the Guidelines

  • Use of Antiretroviral Agents in Pediatric HIV Infection
    • Authoring Organization: United States Department of Health and Human Services (HHS)
    • Publication: April 12, 2023
    • Preferred Regimens for Children Aged ≥2 Years to ≤12 Years Who Are Able to Swallow Pills
      • The Panel recommends initiating ART with a once-daily, single-tablet regimen of BIC/FTC/TAF (Biktarvy) for children weighing ≥14 kg. Two different strengths of BIC/FTC/TAF tablets are available, with the lower-strength tablet for children weighing ≥14 kg and <25 kg. The product label states that for children who are unable to swallow a whole tablet, the BIC/FTC/TAF tablet can be split and each part taken separately, as long as all parts are ingested within approximately 10 minutes.
    • Recommended Regimens for Children and Adolescents Aged ≥12 Years
      • The Preferred regimens (BIC/FTC/TAF and DTG/ABC/3TC) are consistent with the Panel’s recommendations for the 2- to 12-year age group and are available as FDC single-tablet regimens that contain the appropriate dose of the three drugs for the specified weight. These FDC regimens are also the same as those recommended for use in adults and adolescents without delay in pubertal onset, allowing for the continuation of the same initial Preferred regimen as patients transition through puberty in adolescence to adulthood.

  • Use of Antiretroviral Agents in Adults and Adolescents Living with HIV
    • Authoring Organization: HHS
    • Publication: December 06, 2023
    • The Panel on Antiretroviral Guidelines for Adults and Adolescents (the Panel) now recommends initial ARV regimens based on an oral second generation INSTI plus two NRTIs—bictegravir (BIC)/tenofovir alafenamide (TAF)/emtricitabine (FTC) (AI) or dolutegravir (DTG) plus TAF/FTC or tenofovir disoproxil fumarate (TDF)/ FTC or TDF/lamivudine (3TC) (AI)—for most people with HIV.

  • Antiretroviral Drugs for Treatment and Prevention of HIV Infection in Adults
    • Authoring Society: International Antiviral Society–USA (IAS-USA)
    • Publication: November 30, 2022
    • Recommended Initial Antiretroviral Therapy (ART) Regimens for Most People With HIV
    • The following are recommended (in alphabetical order) for most people with HIV:
      • BIC/TAF/FTC (evidence rating: AIa)
      • Dolutegravir plus TXF/XTC (evidence rating: AIa)
      • DTG/3TC (only if HIV RNA <500 000 copies/mL and HBV coinfection not present). This regimen should not be used for rapid initiation when genotype, HIV RNA, and HBV serology results are not yet available (evidence rating: AIa)

This concludes our Guidelines+ Monographs for bictegravir, emtricitabine, & tenofovir alafenamide (Biktarvy). This list is current as of December 2024 and may be updated over time as new indications are approved and/or new guidelines published or updated. Sign up for alerts and stay informed on the latest published guidelines and articles.

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