1st Internal Medicine Department, Laiko General Hospital, National and Kapodistrian University of Athens, Agiou Thoma 17, Goudi, Athens, Greece.
Fourth Department of Medicine, Attikon General Hospital, National and Kapodistrian University of Athens, Athens, Greece.
Curr Pharm Des. 2017;23(18):2552-2567. doi: 10.2174/1381612823666170329142059.
Integrase strand transfer inhibitors (INSTIs) belong to a novel class of antiretroviral agents that have emerged as the new first-line treatments. Three such compounds are currently available, raltegravir, elvitegravir, dolutegravir and two more under development, bictegravir and cabotegravir. These compounds share the same mode of action but exhibit different pharmacokinetic/ pharmacodynamic properties, and drug-drug interactions. A series of studies in the past decade have established their efficacy compared to previous regimens, both in treatment- naïve and experienced patients. INSTIs have demonstrated a favorable safety profile with fewer adverse events and low rates of virological failure. Emergence of resistance to these agents, however, is a worrying concern, particularly for elvitegravir and raltegravir that display a lower genetic barrier than dolutegravir. On-going trials aim at establishing INSTIs as part of dual-drug HIV treatments or even monotherapy. New long-acting, injectable formulations are under investigation for treatment or prevention.
整合酶链转移抑制剂（INSTIs）属于一类新型抗逆转录病毒药物，已成为新的一线治疗药物。目前有三种此类化合物，即拉替拉韦、艾维雷格、多替拉韦，还有两种正在开发中，即比克替拉韦和卡博替拉韦。这些化合物具有相同的作用机制，但表现出不同的药代动力学/药效学特性和药物相互作用。过去十年中的一系列研究已经证实了它们与之前的治疗方案相比的疗效，无论是在初治患者还是经验丰富的患者中。INSTIs 具有良好的安全性，不良事件较少，病毒学失败率较低。然而，这些药物的耐药性的出现令人担忧，特别是对于艾维雷格和拉替拉韦，它们的遗传屏障比多替拉韦低。正在进行的试验旨在将 INSTIs 作为双药 HIV 治疗甚至单药治疗的一部分。正在研究新的长效、注射制剂用于治疗或预防。
