Approved HIV reverse transcriptase inhibitors in the past decade  

作　　者：Guangdi Li Yali Wang Erik De Clercq 

机构地区：[1]Hunan Provincial Key Laboratory of Clinical Epidemiology,Xiangya School of Public Health,Central South University,Changsha 410078,China [2]Rega Institute for Medical Research,Department of Microbiology,Immunology and Transplantation,KU Leuven,Leuven B-3000,Belgium

出　　处：《Acta Pharmaceutica Sinica B》2022年第4期1567-1590,共24页药学学报（英文版）

基　　金：This work was funded by the National Nature Science Foundation of China(31871324,81730064,31571368,China);the Hunan Youth Elite Project(2018RS3006,China);the National Science and Technology Major Project(2018ZX10715004,China).

摘　　要：HIV reverse transcriptase(RT)inhibitors are the important components of highly active antiretroviral therapies(HAARTs)for anti-HIV treatment and pre-exposure prophylaxis in clinical practice.Many RT inhibitors and their combination regimens have been approved in the past ten years,but a review on their drug discovery,pharmacology,and clinical efficacy is lacking.Here,we provide a comprehensive review of RT inhibitors(tenofovir alafenamide,rilpivirine,doravirine,dapivirine,azvudine and elsulfavirine)approved in the past decade,regarding their drug discovery,pharmacology,and clinical efficacy in randomized controlled trials.Novel RT inhibitors such as islatravir,MK-8504,MK-8507,MK8583,IQP-0528,and MIV-150 will be also highlighted.Future development may focus on the new generation of novel antiretroviral inhibitors with higher bioavailability,longer elimination half-life,more favorable side-effect profiles,fewer drug–drug interactions,and higher activities against circulating drug-resistant strains.

关 键 词：HIV treatment HAART NRTI NNRTI Clinical efficacy 

分 类 号：R978.7[医药卫生—药品]