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Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00744-17. doi: 10.1128/AAC.00744-17. Print 2017 Aug.

MK-8591 (4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine) Exhibits Potent Activity against HIV-2 Isolates and Drug-Resistant HIV-2 Mutants in Culture.

Author information

1
Center for Emerging and Reemerging Infectious Diseases and Department of Medicine, Division of Allergy and Infectious Diseases, University of Washington, Seattle, Washington, USA.
2
Center for Emerging and Reemerging Infectious Diseases and Department of Medicine, Division of Allergy and Infectious Diseases, University of Washington, Seattle, Washington, USA smithra@u.washington.edu.
3
Service des Maladies Infectieuses et Tropicales, CHNU de Fann, Dakar, Senegal.
4
Merck & Co., Inc., West Point, Pennsylvania, USA.
5
Department of Global Health, University of Washington, Seattle, Washington, USA.

Abstract

There is a pressing need to identify more effective antiretroviral drugs for HIV-2 treatment. Here, we show that the investigational compound MK-8591 (4'-ethynyl-2-fluoro-2'-deoxyadenosine [EFdA]) is highly active against group A and B isolates of HIV-2; 50% effective concentrations [EC50] for HIV-2 were, on average, 4.8-fold lower than those observed for HIV-1. MK-8591 also retains potent activity against multinucleoside-resistant HIV-2 mutants (EC50 ≤ 11 nM). These data suggest that MK-8591 may have antiviral activity in HIV-2-infected individuals.

KEYWORDS:

4′-ethynyl-2-fluoro-2′-deoxyadenosine; EFdA; HIV-1; HIV-2; MK-8591; NRTI; antiretroviral therapy; drug resistance

PMID:
28559249
PMCID:
PMC5527656
DOI:
10.1128/AAC.00744-17
[Indexed for MEDLINE]
Free PMC Article

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