Pharmacokinetic evaluation of bictegravir + emtricitabine + tenofovir alafenamide in HIV treatment

Introduction: The combination of bictegravir, emtricitabine, and tenofovir alafenamide (BIC/FTC/TAF) represents a valid option of antiretroviral therapy (ART) as first line regimen both in ART-naïve and -experienced people with HIV (PWH). This review evaluates the pharmacokinetic profiles of these drugs and their clinical implications. Areas covered: This article discusses the pharmacokinetics and pharmacodynamics of BIC/FTC/TAF. It covers their efficacy, safety, tolerability, and potential drug-drug interactions. It also examines the benefits of this combination therapy, including improved adherence due to once-daily dosing and reduced toxicity compared to previous therapies. The review includes data from phase III trials and real-world studies, with a focus on treatment outcomes in diverse populations. Expert opinion: BIC/FTC/TAF’s high genetic barrier to resistance and independence from boosting agents represent strengths from the pharmacokinetic perspective. The combination’s once-daily, single-tablet regimen ensures consistent therapeutic drug levels and makes this regimen a viable treatment choice even for those with suboptimal adherence. With clinical trial data demonstrating efficacy and safety, as well as ease of use, BIC/FTC/TAF plays a central role in international guidelines. As the HIV treatment landscape continues to evolve, this regimen will remain a cornerstone of oral ART and may serve as a model for future therapies.