HIV整合酶抑制剂临床应用研究进展

Research progress on the clinical application of HIV integrase inhibitors

整合酶抑制剂(integrase inhibitors,INSTIs)是治疗人类免疫缺陷病毒(human immunodeficiency virus,HIV)感染者的最新一类药物。自2007年以来,已经有5种INSTIs上市:拉替拉韦(Raltegravir,RAL)、艾维雷韦(Elvitegravir,EVG)、多替拉韦(Dolutegravir,DTG)、比克替拉韦(Bictegravir,BIC)和卡博特韦(Cabotegravir,CAB),这些药物均获得美国食品药品监督管理局(Food and Drug Administration,FDA)批准用于HIV感染者的起始抗逆转录病毒治疗(antiretroviral therapy,ART)。与其他类型抗病毒药物相比,INSTIs具有更好的疗效性及耐受性,因此全球众多国家把包含INSTIs的治疗方案列为HIV抗病毒治疗的优选方案。近年来,随着INSTIs的广泛使用,一些研究数据表明,INSTIs可能存在一些不良反应,比如出现中枢神经系统症状、血脂代谢异常、体重增加、肝肾功能异常等。本综述总结了目前用于成人HIV感染者的INSTIs,强调了5种INSTIs的临床疗效及其不良反应。

Integrase inhibitors(INSTIs)are the newest class of antiretroviral drug which are available to people living with the human immunodeficiency virus(HIV).Since 2007,five types of INSTIs have been marketed:Raltegravir,Elvitegravir,Dolutegravir,Bictegravir and Cabotegravir,all of which were approved by the US Food and Drug Administration(FDA)for use in the initiation of antiretroviral therapy(ART)in treatment-naïve individuals.Compared with other types of antiretroviral drugs,INSTIs have better efficacy and tolerability,so many countries around the world have listed INSTIs-containing regimens as the preferred regimen for HIV ART.In recent years,with the widespread use of INSTIs,some research data suggest that INSTIs may have some adverse effects(AEs),such as central nervous system symptoms,abnormal lipid metabolism,weight gain,abnormal liver and kidney function,etc.This review summarizes the current use of INSTIs in people living with the HIV,and highlights the clinical efficacy and their AEs among the five types of INSTIs in China.