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

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.

Efficacy and safety of switching to bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed Asian adults living with HIV: A pooled analysis from three international phase III randomized trials

“…Interestingly, although 35% of the B/F/TAF‐switched Asian participants discontinued baseline TDF (thereby losing access to the demonstrated lipid‐lowering effect of TDF 26 ), the Asian B/F/TAF arm exhibited no blood lipid elevation, and the switch to B/F/TAF showed neutral to favourable changes in blood lipid overall. This might in part reflect the effects of the discontinuation of a booster and its corresponding replacement by BIC (which is lipid neutral 27 ) in participants who switched from baseline regimens containing both TDF and a booster.…”

A Step Closer to the “Fourth 90”: A Practical Narrative Review of Diagnosis and Management of Nutritional Issues of People Living with HIV

“…Among nucleoside reverse transcriptase inhibitors (NRTIs), abacavir was traditionally related to an increased risk of cardiovascular disease in HIV-positive patients, which has been associated with mechanisms of endothelial disfunction and imbalance in platelets' activation and aggregation processes [41]. Although the impact on the cardiovascular system of exposure to abacavir remains controversial, several alternative therapeutic strategies are currently available to avoid this risk, above all opting for agents of the same class with different toxicity profiles, such as combination regimens based on tenofovir disoproxile fumarate (TDF) rather than tenofovir alafenamide (TAF) [42,43]. In recent years, the advent of highly efficient antiretroviral drug classes such as protease inhibitors (PIs) and, lately, integrase strand transfer inhibitors (INSTIs), allowed the creation of combined antiretroviral regimens that avoided NTRI-related cardiovascular toxicity along with maintaining high control on viral replication also in experienced subjects.…”

Bictegravir/emtricitabine/tenofovir alafenamide-induced acute pancreatitis: a case report

“…Bictegravir is a novel, unboosted, integrase inhibitor approved for the treatment of adults with human immunodeficiency virus (HIV) infection as a single tablet regimen co-formulated with emtricitabine and tenofovir alafenamide (BIC/FTC/TAF). 1 In Phase 3 studies, more grades 3 and 4 laboratory abnormalities were found in the BIC/FTC/TAF arm, mainly driven by frequent, transient increase in serum amylase often associated with normal lipase. No episodes of pancreatitis were, however, reported.…”