Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection

Drugs. 2018 Nov;78(17):1817-1828. doi: 10.1007/s40265-018-1010-7.


Bictegravir is a new integrase strand transfer inhibitor (INSTI) with a high genetic barrier to the development of HIV-1 resistance. The drug is co-formulated with the nucleos(t)ide reverse transcriptase inhibitors emtricitabine and tenofovir alafenamide (AF) in a single-tablet regimen (STR) for the once-daily treatment of HIV-1 infection in adults (bictegravir/emtricitabine/tenofovir AF; Biktarvy®). In phase 3 trials, bictegravir/emtricitabine/tenofovir AF was noninferior to dolutegravir-based therapy (dolutegravir/abacavir/lamivudine or dolutegravir plus emtricitabine/tenofovir AF) in establishing virological suppression in treatment-naïve adults through 96 weeks' treatment and, similarly, was noninferior to ongoing dolutegravir/abacavir/lamivudine or boosted elvitegravir- or protease inhibitor (PI)-based therapy in preventing virological rebound over 48 weeks in treatment-experienced patients. No resistance emerged to any of the antiretrovirals in the STR. Bictegravir/emtricitabine/tenofovir AF is generally well tolerated, requires no prior HLA-B*5701 testing (making it more suitable for 'rapid start' treatment), fulfils the antiretroviral regimen requirement for patients with hepatitis B virus (HBV) co-infection (i.e. contains tenofovir AF and emtricitabine, both of which are active against HBV) and can be used in renally impaired patients with creatinine clearance (CRCL) ≥ 30 mL/min. Thus, although cost-effectiveness analyses would be beneficial, current data indicate that bictegravir/emtricitabine/tenofovir AF is a convenient initial and subsequent treatment option for adults with HIV-1 infection, including those co-infected with HBV, and provides the first non-pharmacologically boosted, INSTI-based, triple-combination STR suitable for patients with CRCL 30-50 mL/min.

Publication types

  • Review

MeSH terms

  • Adenine / analogs & derivatives*
  • Adenine / pharmacology
  • Adenine / therapeutic use
  • Adult
  • Anti-HIV Agents* / pharmacology
  • Anti-HIV Agents* / therapeutic use
  • Dideoxynucleosides / pharmacology
  • Dideoxynucleosides / therapeutic use
  • Dose-Response Relationship, Drug
  • Drug Combinations
  • Emtricitabine / pharmacology*
  • Emtricitabine / therapeutic use
  • HIV Infections / drug therapy*
  • Heterocyclic Compounds, 4 or More Rings / pharmacology*
  • Heterocyclic Compounds, 4 or More Rings / therapeutic use
  • Humans
  • Lamivudine / pharmacology
  • Lamivudine / therapeutic use
  • Reverse Transcriptase Inhibitors* / pharmacology
  • Reverse Transcriptase Inhibitors* / therapeutic use
  • Treatment Outcome


  • Anti-HIV Agents
  • Dideoxynucleosides
  • Drug Combinations
  • Heterocyclic Compounds, 4 or More Rings
  • Reverse Transcriptase Inhibitors
  • abacavir, lamivudine drug combination
  • bictegravir
  • Lamivudine
  • GS-7340
  • Emtricitabine
  • Adenine