Adis, a Wolters Kluwer Business, Auckland, New Zealand.
Drugs. 2010 Jun 18;70(9):1189-213. doi: 10.2165/11203940-000000000-00000.
Maraviroc (Celsentri; Selzentry) is a CCR5 coreceptor antagonist used in the treatment of CCR5-tropic HIV-1 infection. Administered orally twice daily, maraviroc, in combination with optimized background therapy regimens, showed good virological and immunological efficacy over 48 weeks in antiretroviral treatment-experienced patients aged > or = 16 years with CCR5-tropic HIV-1 infection, in the randomized, double-blind, placebo-controlled, multicentre, MOTIVATE 1 and MOTIVATE 2 studies. Initial data indicate that the efficacy of maraviroc in this patient population is sustained for up to 96 weeks. In the MERIT study in antiretroviral therapy-naive patients aged > or = 16 years with CCR5-tropic HIV-1 infection, maraviroc was noninferior to efavirenz (each in combination with zidovudine/lamivudine) for one primary virological endpoint (HIV-1-RNA levels < 400 copies/mL), but not for the other primary endpoint (HIV-1 RNA levels < 50 copies/mL) in the primary analysis at 48 weeks. However, in a subsequent analysis, which used a more sensitive tropism testing assay than the one originally used and retrospectively excluded patients with non CCR5-tropic HIV-1 infection who were ineligible for inclusion in the study, maraviroc demonstrated noninferiority to efavirenz on both primary virological endpoints. Maraviroc showed sustained virological efficacy in this patient population and improved immunological markers for up to 96 weeks. Maraviroc was generally well tolerated by both treatment-experienced and treatment-naive patients with CCR5-tropic HIV-1 infection. Thus, maraviroc, as a component of antiretroviral combination therapy regimens, is an important option for use in treatment-experienced adults with CCR5-tropic HIV-1 infection. Available data indicate that maraviroc may also have a role in treatment-naive adults with CCR5-tropic HIV-1 infection, a population in whom CCR5-tropic HIV-1 is often the major quasispecies.
马拉维若（Celsentri；Selzentry）是一种 CCR5 核心受体拮抗剂，用于治疗 CCR5 嗜性 HIV-1 感染。马拉维若每日口服两次，与优化的背景治疗方案联合使用，在接受过抗逆转录病毒治疗的、年龄≥16 岁的 CCR5 嗜性 HIV-1 感染患者中，在随机、双盲、安慰剂对照、多中心的 MOTIVATE 1 和 MOTIVATE 2 研究中，48 周时具有良好的病毒学和免疫学疗效。初步数据表明，在该患者人群中，马拉维若的疗效可持续长达 96 周。在初治患者（年龄≥16 岁的 CCR5 嗜性 HIV-1 感染患者）中，MERIT 研究中，马拉维若与依非韦伦（均与齐多夫定/拉米夫定联合使用）在一个主要病毒学终点（HIV-1-RNA 水平<400 拷贝/ml）上无差异，但在主要分析中在 48 周时在另一个主要终点（HIV-1 RNA 水平<50 拷贝/ml）上无差异。然而，在随后的分析中，该分析使用了一种比最初使用的更敏感的病毒学分析检测方法，并回顾性地排除了不符合纳入研究条件的非 CCR5 嗜性 HIV-1 感染患者，马拉维若在两个主要病毒学终点上均显示出与依非韦伦相当的非劣效性。马拉维若在该患者人群中表现出持续的病毒学疗效，免疫标志物改善长达 96 周。马拉维若在接受过治疗和初治的 CCR5 嗜性 HIV-1 感染患者中总体耐受性良好。因此，马拉维若作为抗逆转录病毒联合治疗方案的一部分，是治疗 CCR5 嗜性 HIV-1 感染成人的重要选择。现有数据表明，马拉维若在 CCR5 嗜性 HIV-1 感染的初治成人中也可能有作用，这一人群中 CCR5 嗜性 HIV-1 通常是主要准种。
