The potential role of bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC/TAF) single-tablet regimen in the expanding spectrum of fixed-dose combination therapy for HIV

HIV Med. 2020 Mar;21 Suppl 1:3-16. doi: 10.1111/hiv.12833.

Abstract

Single-tablet regimens (STRs) of highly safe and effective combination antiretroviral therapy (cART) have had a significant beneficial impact on the clinical outcomes and lives of people living with HIV (PLHIV). As a consequence, healthcare professionals caring for PLHIV in high-income countries have increasingly focused on issues beyond those related to HIV itself, i.e. HIV-related neurological disease, or associated opportunistic infections, which include co-infections, and primarily age- and lifestyle-related comorbidities such as cardiovascular disease, diabetes mellitus, renal impairment, osteoporosis and frailty. This review considers drug side effects and comorbidities seen in PLHIV and evaluates the role of a recently licensed STR - bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC/TAF) - in mitigating some of those challenges. Factors that need to be evaluated for initial cART regimens include: pretreatment CD4 cell count; plasma HIV RNA; HIV drug resistance; hepatitis B co-infection; HLA-B*5701 status; drug-drug interactions; pregnancy and pregnancy potential; psychiatric and physical comorbidities such as renal or bone disease, as well as simplicity and adherence-friendliness, all of which need to be considered in all lines of therapy. BIC/FTC/TAF constitutes a new STR that includes an unboosted integrase strand transfer inhibitor with a high barrier against resistance with TAF and FTC. Its virological efficacy was non-inferior to dolutegravir-based regimens previously recommended by most guidelines for treatment initiation in large double-blind, randomised clinical trials in treatment-naïve or switch patients over 96 weeks. Tolerability and pharmacological properties of the regimen make it a useful tool to address several of the clinical management issues raised above.

Keywords: bictegravir; emtricitabine; single-tablet regimen; tenofovir alafenamide.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adenine / adverse effects
  • Adenine / analogs & derivatives*
  • Adenine / therapeutic use
  • Alanine
  • Anti-HIV Agents / adverse effects*
  • Anti-HIV Agents / therapeutic use
  • CD4 Lymphocyte Count
  • Comorbidity
  • Drug Combinations
  • Emtricitabine
  • Equivalence Trials as Topic
  • HIV Infections / blood
  • HIV Infections / drug therapy*
  • Heterocyclic Compounds, 4 or More Rings / adverse effects*
  • Heterocyclic Compounds, 4 or More Rings / therapeutic use
  • Humans
  • Piperazines
  • Pyridones
  • Risk Factors
  • Socioeconomic Factors
  • Tablets
  • Tenofovir / adverse effects*
  • Tenofovir / therapeutic use

Substances

  • Anti-HIV Agents
  • Drug Combinations
  • Heterocyclic Compounds, 4 or More Rings
  • Piperazines
  • Pyridones
  • Tablets
  • bictegravir, emtricitabine, tenofovir alafenamide, drug combination
  • Tenofovir
  • Emtricitabine
  • Adenine
  • Alanine