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

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 (click to view)

Wu VH, Smith RA, Masoum S, Raugi DN, Ba S, Seydi M, Grobler JA, Gottlieb GS,


Wu VH, Smith RA, Masoum S, Raugi DN, Ba S, Seydi M, Grobler JA, Gottlieb GS, (click to view)

Wu VH, Smith RA, Masoum S, Raugi DN, Ba S, Seydi M, Grobler JA, Gottlieb GS,

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Antimicrobial agents and chemotherapy 2017 07 2561(8) pii 10.1128/AAC.00744-17

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.

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