Abstract

Human immunodeficiency virus (HIV) infection remained a substantial global health challenge, with approximately 
39 million people living with HIV worldwide as of 2022. The advent of integrase strand transfer inhibitors (INSTIs) 
has transformed antiretroviral therapy (ART), offering enhanced virologic suppression with favorable tolerability 
profiles. Bictegravir (BIC), a second-generation unboosted INSTI, had emerged as a cornerstone of contemporary 
single-tablet regimens (STRs) for treatment-naive adults. This narrative review critically examined the virologic 
efficacy, metabolic tolerability, and safety profile of bictegravir-based STRs in antiretroviral-naive patients. A 
comprehensive literature search was conducted using PubMed, Embase, and Web of Science databases from January 
2017 to November 2024, focusing on randomized controlled trials, observational cohorts, and mechanistic studies 
evaluating bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF). Evidence from pivotal phase III trials 
demonstrated that BIC-based STRs achieve virologic suppression rates exceeding 92% at 48 weeks, with sustained 
efficacy through 144 weeks and beyond. Compared with dolutegravir-based and boosted INSTI regimens, 
bictegravir exhibited non-inferior virologic outcomes while demonstrating superior weight neutrality, minimal 
drug-drug interactions due to its unboosted formulation, and a high genetic barrier to resistance. The favorable 
pharmacokinetic profile, characterized by high plasma protein binding and minimal renal elimination, contributes to 
once-daily dosing convenience and reduced metabolic perturbations. Bictegravir-based STRs represented a highly 
effective, well-tolerated first-line option for treatment-naive adults, combining potent virologic suppression with 
metabolic safety and simplified administration that enhances long-term adherence and clinical outcomes.