期刊
EXPERT OPINION ON DRUG DISCOVERY
卷 10, 期 6, 页码 671-684出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/17460441.2015.1041497
关键词
antiretroviral therapy; CCR5-receptor antagonist; entry inhibitor; HIV-1; maraviroc
资金
- Ministry of Education, Science and Technological Development of the Republic of Serbia [173001, 172033]
- European COST Action (GLISTEN) [CM1207]
- Chiesi Foundation
Introduction: 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. Areas covered: 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. Expert opinion: 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.
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