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

Elena Bruzzesi, Camilla Muccini, Antonella Castagna
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Abstract

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.

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比特拉韦+恩曲他滨+替诺福韦-阿拉非那胺在艾滋病治疗中的药代动力学评估。
简介联用比特拉韦、恩曲他滨和替诺福韦-阿拉非酰胺(BIC/FTC/TAF)是抗逆转录病毒疗法(ART)的有效选择,可作为抗逆转录病毒疗法(ART)治疗艾滋病病毒感染者(PWH)的一线方案。本综述评估了这些药物的药代动力学特征及其临床意义:本文讨论了 BIC/FTC/TAF 的药代动力学和药效学。文章涵盖了这些药物的疗效、安全性、耐受性以及潜在的药物间相互作用。文章还探讨了这种联合疗法的益处,包括与以前的疗法相比,每日一次给药提高了依从性,降低了毒性。综述包括 III 期试验和实际研究的数据,重点关注不同人群的治疗效果:从药代动力学的角度来看,BIC/FTC/TAF 的耐药基因屏障高,且不受增效剂的影响,这些都是其优势所在。从药代动力学的角度来看,BIC/FTC/TAF 的高遗传抗性屏障和独立于促进剂的特性是其优势所在。该组合的每日一次、单片剂治疗方案可确保稳定的治疗药物水平,即使对于依从性不佳的患者来说,该治疗方案也是一种可行的治疗选择。临床试验数据表明,BIC/FTC/TAF 具有疗效和安全性,而且易于使用,因此在国际指南中发挥着重要作用。随着艾滋病治疗领域的不断发展,该疗法仍将是口服抗逆转录病毒疗法的基石,并可能成为未来疗法的典范。
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