Oral CCR5 inhibitors: will they make it through?

Expert Opinion on Investigational Drugs
Priscilla BiswasGiuseppe Tambussi

Abstract

The therapeutic armamentarium against HIV has recently gained a drug belonging to a novel class of antiretrovirals, the entry inhibitors. The last decade has driven an in-depth knowledge of the HIV entry process, unravelling the multiple engagements of the HIV envelope proteins with the cellular receptorial complex that is composed of a primary receptor (CD4) and a co-receptor (CCR5 or CXCR4). The vast majority of HIV-infected subjects exhibit biological viral variants that use CCR5 as a co-receptor. Individuals with a mutated CCR5 gene, both homo- and heterozygotes, appear to be healthy. For these and other reasons, CCR5 represents an appealing target for treatment intervention, although certain challenges can not be ignored. Promising small-molecule, orally bioavailable CCR5 antagonists are under development for the treatment of HIV-1 infection.

References

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Citations

Sep 2, 2008·Expert Opinion on Drug Safety·Jetske M Emmelkamp, Jürgen K Rockstroh
May 3, 2007·Expert Opinion on Pharmacotherapy·Priscilla BiswasAdriano Lazzarin
Nov 14, 2006·Biologicals : Journal of the International Association of Biological Standardization·Ian McGowan
Apr 19, 2015·Journal of Translational Medicine·Francesca SironiPriscilla Biswas
May 3, 2007·Cytometry. Part B, Clinical Cytometry·Priscilla BiswasGiuseppe Tambussi

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