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.
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).
