Di Perri Giovanni
Infectious Diseases Unit, Department of Medical Sciences, University of Torino, Amedeo di Savoia Hospital, Torino, Italy.
Infez Med. 2019 Dec 1;27(4):365-373.
The fourth HIV strand-transfer integrase inhibitor (INSTI) has been released into the market as part of a single-tablet-regimen (STR) consisting of bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC/TAF). The newest component is thus BIC, a booster-free INSTI with pharmacological characteristics similar to those of dolutegravir (DTG), including high intrinsic antiretroviral potency. The BIC-containing STR underwent clinical development in both treatment-naive and virologically suppressed patients and was found non-inferior to DTG-based comparator arms. In the currently evolving therapeutic scenario, the BIC/FTC/TAF STR regimen represents the smartest response on the side of triple conventional regimens, while new 2-drug regimens have received regulatory approval and nowadays epitomize the search for simpler and lighter antiretroviral regimens. The overall characteristics of BIC/FTC/TAF, however, make this therapeutic option quite comparable in terms of simplicity to the newly approved dual regimens, and the main reasons (e.g., toxicity) accounting in the past for the search of regimens consisting of less than three drugs are no longer in place.
第四种HIV链转移整合酶抑制剂（INSTI）已作为由比克替拉韦/恩曲他滨/替诺福韦艾拉酚胺（BIC/FTC/TAF）组成的单片复方制剂（STR）的一部分投放市场。因此，最新成分是BIC，一种无需增效剂的INSTI，其药理学特性与多替拉韦（DTG）相似，包括高内在抗逆转录病毒效力。含BIC的STR在初治患者和病毒学抑制患者中都进行了临床开发，结果发现其不劣于基于DTG的对照组。在当前不断发展的治疗方案中，BIC/FTC/TAF STR方案是传统三联方案中最明智的选择，而新的二联方案已获得监管批准，如今代表了对更简单、更轻松的抗逆转录病毒方案的探索。然而，BIC/FTC/TAF的总体特性使得该治疗方案在简单性方面与新批准的二联方案相当，而且过去导致寻求少于三种药物组成的方案的主要原因（例如毒性）已不复存在。
