Fadel Hind, Temesgen Zelalem
Department of Internal Medicine, Mayo Clinic, Rochester, Minnesota, USA.
Drugs Today (Barc). 2007 Nov;43(11):749-58. doi: 10.1358/dot.2007.43.11.1131763.
Maraviroc, first in a new pharmacological class of antiretroviral agents known as CCR5 antagonists, has been approved by the U.S. Food and Drug Administration for the treatment of HIV-infected adult patients who are infected with only CCR5-tropic HIV-1 virus and who have HIV-1 strains resistant to multiple antiretroviral agents. Maraviroc has demonstrated in vitro activity against a wide range of CCR5 tropic clinical isolates, including those resistant to the four currently existing drug classes of antiretroviral agents. In the two pivotal phase III studies, MOTIVATE-1 and -2, maraviroc, in combination with optimized background therapy (OBT), demonstrated superior virologic and immunologic treatment outcomes than OBT alone in treatment-experienced patients infected with CCR5-tropic HIV-1. In these studies, maraviroc also demonstrated acceptable safety and tolerability profiles with adverse events and discontinuation rates in general comparable to those noted in the placebo arms.
马拉维若作为一类名为CCR5拮抗剂的新型抗逆转录病毒药物中的首个药物,已获美国食品药品监督管理局批准,用于治疗仅感染CCR5嗜性HIV-1病毒且其HIV-1毒株对多种抗逆转录病毒药物耐药的成年HIV感染者。马拉维若已在体外实验中显示出对多种CCR5嗜性临床分离株具有活性,包括对目前现有的四类抗逆转录病毒药物耐药的分离株。在两项关键的III期研究MOTIVATE-1和MOTIVATE-2中,马拉维若联合优化背景治疗(OBT),在感染CCR5嗜性HIV-1的经治患者中,显示出比单独使用OBT更优的病毒学和免疫学治疗效果。在这些研究中,马拉维若还显示出可接受的安全性和耐受性,其不良事件和停药率总体上与安慰剂组相当。