抗HIV新药raltegravir  

A new antiretroviral agent against HIV:raltegravir

作　　者：谭艳梅[1] 刘川[1] 赵桂森[1] 

机构地区：[1]山东大学药学院药物化学教研室,济南250012

出　　处：《中国新药杂志》2007年第21期1812-1815,共4页Chinese Journal of New Drugs

基　　金：国家自然科学基金(20472045)

摘　　要：整合酶(integrase)是HIV病毒复制的必需酶,因而成为抗HIV药物设计的一个合理靶点。目前尚无整合酶抑制剂类药物上市,raltegravir是第一个进入Ⅲ期临床的此类药物。与上市的抗HIV药物相比,具有更高或相近的抗逆转录病毒的活性,无交叉耐药性,毒副作用小,有可能成为第一个上市的整合酶抑制剂。现对其作用机制、临床前研究、药动学、临床应用及安全性等做一综述。Integrase is essential for retroviral replication of human immunodeficiency virus and the rational target of the design of anti-HIV drug. To date, no IN inhibitor is approved by FDA for clinical use, rahegravir is the first one to enter into Phase III clinical trials. Compared with the anti-HIV drugs in the market, raltegravir is not only more or equal potent, but also no cross resistant, weak toxicity and side effect, et al. It may be the first approved integrase inhibitor for anti-HIV. This article reviews raltegravir in action mechanism, preclinical research ,clinical research, pharmacokinetic research and safety.

关 键 词：抗HIV药 整合酶抑制剂 RALTEGRAVIR 

分 类 号：R978.7[医药卫生—药品]