比克替拉韦/恩曲他滨/替诺福韦艾拉酚胺固定剂量复方制剂概况及其在治疗HIV-1感染中的潜力：迄今的证据
Profile of bictegravir/emtricitabine/tenofovir alafenamide fixed dose combination and its potential in the treatment of HIV-1 infection: evidence to date.
作者信息
Hill Lucas, Smith Shawn R, Karris Maile Young
机构信息
University of California San Diego Skaggs School of Pharmacy and Pharmaceutical Sciences, San Diego, CA, USA,
Department of Medicine, University of California San Diego, San Diego, CA, USA.
出版信息
HIV AIDS (Auckl). 2018 Oct 29;10:203-213. doi: 10.2147/HIV.S145529. eCollection 2018.
Abstract
Modern pharmacologic management of people living with HIV involves the use of fixed dose combinations of antiretrovirals that are simple to take, well tolerated, and highly effective. Specific recent pharmacologic advancements include 1) the second-generation integrase strand transfer inhibitors (dolutegravir and bictegravir) that consistently show less side effects, high tolerability, minimal drug interactions, and rapid rates of HIV viral load decline and 2) tenofovir alafenamide, a prodrug of tenofovir that concentrates in lymphoid tissue and minimizes off target effects. Bictegravir/emtricitabine/tenofovir alafenamide or B/F/TAF is a recently approved fixed dose combination that incorporates these new advancements in the management of HIV. This review focuses on the data supporting the use of B/F/TAF, reviews clinically relevant findings, and highlights the unanswered questions that may limit its clinical utility.
摘要
现代对HIV感染者的药物治疗包括使用固定剂量的抗逆转录病毒药物组合，这些组合服用简便、耐受性良好且高效。近期具体的药物进展包括：1）第二代整合酶链转移抑制剂（多替拉韦和比克替拉韦），其始终显示出较少的副作用、高耐受性、最小的药物相互作用以及HIV病毒载量快速下降；2）替诺福韦艾拉酚胺，替诺福韦的前体药物，它集中在淋巴组织中并将脱靶效应降至最低。比克替拉韦/恩曲他滨/替诺福韦艾拉酚胺（B/F/TAF）是最近批准的一种固定剂量组合，它将这些新进展纳入了HIV的治疗中。本综述重点关注支持使用B/F/TAF的数据，回顾临床相关发现，并突出可能限制其临床应用的未解决问题。
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Lancet. 2017 Nov 4;390(10107):2073-2082. doi: 10.1016/S0140-6736(17)32340-1. Epub 2017 Aug 31.
2
Bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir, abacavir, and lamivudine for initial treatment of HIV-1 infection (GS-US-380-1489): a double-blind, multicentre, phase 3, randomised controlled non-inferiority trial.比克替拉韦、恩曲他滨和替诺福韦艾拉酚胺与多替拉韦、阿巴卡韦和拉米夫定用于治疗人类免疫缺陷病毒 1 型感染的初始治疗（GS-US-380-1489）：一项双盲、多中心、3 期、随机、对照非劣效性试验。
Lancet. 2017 Nov 4;390(10107):2063-2072. doi: 10.1016/S0140-6736(17)32299-7. Epub 2017 Aug 31.
3
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Lancet HIV. 2017 Apr;4(4):e154-e160. doi: 10.1016/S2352-3018(17)30016-4. Epub 2017 Feb 15.
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