Veljkovic Nevena, Vucicevic Jelica, Tassini Sabrina, Glisic Sanja, Veljkovic Veljko, Radi Marco
University of Belgrade, Institute of Nuclear Sciences VINCA, Center for Multidisciplinary Research , P.O. Box 522, Belgrade , Serbia +381 11 3408154 ; + 381 11 7440100 ;
Expert Opin Drug Discov. 2015 Jun;10(6):671-84. doi: 10.1517/17460441.2015.1041497. Epub 2015 Apr 30.
Maraviroc is a first-in-class antiretroviral (ARV) drug acting on a host cell target (CCR5), which blocks the entry of the HIV virus into the cell. Maraviroc is currently indicated for combination ARV treatment in adults infected only with CCR5-tropic HIV-1.
This drug discovery case history focuses on the key studies that led to the discovery and approval of maraviroc, as well as on post-launch clinical reports. The article is based on the data reported in published preclinical and clinical studies, conference posters and on drug package data.
The profound understanding of HIV's entry mechanisms has provided a strong biological rationale for targeting the chemokine receptor CCR5. The CCR5-antagonist mariviroc, with its unique mode of action and excellent safety profile, is an important therapeutic option for HIV patients. In general, the authors believe that targeting host factors is a useful approach for combating new and re-emerging transmissible diseases, as well as pathogens that easily become resistant to common antiviral drugs. Maraviroc, offering a potent and safe cellular receptor-mediated pharmacological response to HIV, has paved the way for the development of a new generation of host-targeting antivirals.
马拉维罗是一种作用于宿主细胞靶点（CCR5）的一流抗逆转录病毒（ARV）药物，可阻止HIV病毒进入细胞。马拉维罗目前适用于仅感染CCR5嗜性HIV-1的成人的联合抗逆转录病毒治疗。
本药物研发案例历史聚焦于促成马拉维罗发现与获批的关键研究以及上市后的临床报告。本文基于已发表的临床前和临床研究、会议海报以及药品包装数据中报告的数据。
对HIV进入机制的深入理解为靶向趋化因子受体CCR5提供了有力的生物学依据。CCR5拮抗剂马拉维罗具有独特的作用方式和出色的安全性，是HIV患者的重要治疗选择。总体而言，作者认为靶向宿主因子是对抗新出现和再次出现的传染病以及易对常见抗病毒药物产生耐药性的病原体的有用方法。马拉维罗对HIV提供了有效且安全的细胞受体介导的药理反应，为新一代靶向宿主的抗病毒药物的开发铺平了道路。
