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Expert Opin Drug Discov. 2015 Jun;10(6):671-84. doi: 10.1517/17460441.2015.1041497. Epub 2015 Apr 30.

Preclinical discovery and development of maraviroc for the treatment of HIV.

Author information

1
University of Belgrade, Institute of Nuclear Sciences VINCA, Center for Multidisciplinary Research , P.O. Box 522, Belgrade , Serbia +381 11 3408154 ; + 381 11 7440100 ; nevenav@vinca.rs.

Abstract

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.

KEYWORDS:

CCR5-receptor antagonist; HIV-1; antiretroviral therapy; entry inhibitor; maraviroc

PMID:
25927601
DOI:
10.1517/17460441.2015.1041497
[Indexed for MEDLINE]

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