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CCR5 antagonists: a new class of antiretrovirals

机译：CCR5拮抗剂：一类新的抗逆转录病毒

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Inhibition of CCR5 co-receptor which is also a chemokine receptor, is a new way for inhibition of HIV-1 replication. Small antagonist molecules exert non competitive inhibition of the HIV co-receptor CCR5, which is essential for HIV entry. The CCR5 antagonists aplaviroc (GlaxoSmithKine), vicriviroc (Schering-Plough), and maraviroc (Pfizer) have reached phases III of clinical development. The development of aplaviroc was stopped because of its hepatotoxicity in some of the HIV-infectcd patients. In ACTG 5211 and MOTIVATE trials, treatment-experienced subjects who added respectively vicriviroc and maraviroc demonstrated substantially greater reductions in plasma HIV-1 RNA levels than those who received the placebo maraviroc currently having obtained European authorization. The place of this new class in the strategies of initial, switch or rescue treatment remains to be clarified. The limitations of the use of these small molecules depend on their mechanism of action : obligation for monitoring the evolution of coreceptor usage, risk of failure by emergence of pre-existing strains with CXCR4 (X4) tropism or by resistant strains with CCR5 tropism, potential risks related to blocking of the physiological functions of this chemokine receptor. (C)2008 Elsevier Masson SAS. Tous droits reserves.
机译：抑制CCR5的CCR5共受体，其也是趋化因子受体，是抑制HIV-1复制的新方法。小拮抗剂分子对艾滋病毒共同受体CCR5的不竞争性抑制，这对于HIV进入至关重要。 CCR5拮抗剂APLAVIROC（Glaxosmithkine），ViCriviroc（Schering-Plow）和马拉维毒（Pfizer）已达到临床开发的阶段。由于其一些HIV-Infeccd患者的肝毒性，因此停止了Aplaviroc的发展。在Actg 5211和激发试验中，分别增加的治疗经验丰富的受试者分别的viCriroc和Maraviroc的血浆HIV-1 RNA水平的减少显着增加，而那些接受目前获得欧洲授权的安慰剂马鞭病的血浆患者水平则减少。在初始，交换机或救援治疗的策略中，这一新课程的地方仍有待澄清。这些小分子使用的局限取决于它们的行动机制：监测团簇使用的演变，通过用CXCR4（X4）的抗性或通过CCR5抗性的抗性菌株出现预先存在的菌株，潜在的菌株的义务与阻断该趋化因子受体的生理功能相关的风险。 （c）2008 Elsevier Masson SAS。艺术店储备。

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