Department of Pharmaceutical Sciences, University of Colorado Skaggs School of Pharmacy and Pharmaceutical Sciences, Aurora, Colorado.
Department of Pharmacy Practice, Nova Southeastern University, Fort Lauderdale, Florida.
Pharmacotherapy. 2019 May;39(5):576-598. doi: 10.1002/phar.2246. Epub 2019 Apr 1.
The era of the integrase strand transfer inhibitors (INSTIs) for the treatment of human immunodeficiency virus (HIV) infection began with raltegravir in 2007. Since that time, several other INSTIs have been introduced including elvitegravir, dolutegravir, and, most recently, bictegravir, that have shown great utility as part of antiretroviral regimens in both treatment-naive and treatment-experienced patients. At present, antiretroviral guidelines fully endorse the INSTI class as part of all first-line treatment regimens. After 10 years of experience with INSTIs, newer agents are on the horizon such as cabotegravir and MK-2048 for potential use as either HIV pre-exposure prophylaxis or maintenance therapy. This review provides a brief overview of the INSTI class including agents currently available and those still in development, reviews available data from both completed and ongoing clinical trials, and outlines simplification strategies using INSTIs.
整合酶 strand 转移抑制剂（INSTIs）治疗人类免疫缺陷病毒（HIV）感染的时代始于 2007 年的拉替拉韦。自那时以来，已经引入了其他几种 INSTIs，包括艾维雷格、多替拉韦和最近的比克替拉韦，它们在治疗初治和治疗经验丰富的患者的抗逆转录病毒方案中显示了很大的作用。目前，抗逆转录病毒指南完全支持 INSTI 类药物作为所有一线治疗方案的一部分。在 INSTIs 应用 10 年后，新的药物正在出现，如卡博特韦和 MK-2048，可能用于 HIV 暴露前预防或维持治疗。这篇综述简要概述了 INSTI 类药物，包括目前可用的和仍在开发中的药物，回顾了已完成和正在进行的临床试验的可用数据，并概述了使用 INSTIs 的简化策略。
