a Lady Davis Institute for Medical Research, Jewish General Hospital , McGill University AIDS Centre , Montréal , Québec , Canada.
b Department of Microbiology and Immunology, Faculty of Medicine , McGill University , Montréal , Québec , Canada.
Expert Opin Pharmacother. 2019 Mar;20(4):385-397. doi: 10.1080/14656566.2018.1560423. Epub 2019 Jan 30.
Current antiretroviral therapy is more effective and simpler than in previous times due to the development of new drugs with improved pharmacokinetic and pharmacodynamic profiles and the advent of single pill regimens with low toxicity that facilitate long-term adherence. The recent approval of the novel potent integrase strand-transfer inhibitor bictegravir (BIC) co-formulated with emtricitabine (FTC) and tenofovir alafenamide (TAF) in a fixed daily dose pill, B/F/TAF, adds to the list of single-tablet regimens available to treat HIV infection. Areas covered: This review provides an overview of the pharmacological and clinical information obtained from MEDLINE/PubMed publications and the latest international conferences. Expert opinion: BIC is a potent antiretroviral with an improved resistance profile over previous integrase inhibitors. Its combination with the new tenofovir prodrug TAF and FTC creates an effective regimen B/F/TAF for treatment-naïve patients and for those switching from another successful combination. B/F/TAF's favorable pharmacokinetic profile, simple dose, low pill burden, and few drug-drug interactions or treatment-related adverse events, will make it one of the preferred regimens in the future.
目前的抗逆转录病毒疗法比以往更加有效和简单,这要归功于新药物的发展,这些药物具有改善的药代动力学和药效学特征,以及毒性低的单一片剂方案的出现,这有助于长期坚持治疗。最近批准的新型强效整合酶链转移抑制剂比替拉韦(BIC)与恩曲他滨(FTC)和丙酚替诺福韦(TAF)联合固定剂量每日一片的复方制剂(B/F/TAF),增加了可用于治疗 HIV 感染的单一片剂方案的选择。
本文综述了从 MEDLINE/PubMed 出版物和最新国际会议获得的关于 BIC 的药理学和临床信息。
BIC 是一种有效的抗逆转录病毒药物,其耐药谱优于以前的整合酶抑制剂。它与新的替诺福韦前药 TAF 和 FTC 联合使用,为初治患者和那些从其他成功联合方案转换的患者创造了一种有效的 B/F/TAF 方案。B/F/TAF 良好的药代动力学特征、简单的剂量、低的药物负担、较少的药物相互作用或与治疗相关的不良事件,将使其成为未来的首选方案之一。