MK-8591 (4′-ethynyl-2-fluoro-2′-deoxyadenosine) exhibits potent activity against HIV-2 isolates and drug-resistant HIV-2 mutants in culture

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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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Wu, V. H., Smith, R. A., Masoum, S., Raugi, D. N., Ba, S., Seydi, M., … Gottlieb, G. S. (2017). MK-8591 (4′-ethynyl-2-fluoro-2′-deoxyadenosine) exhibits potent activity against HIV-2 isolates and drug-resistant HIV-2 mutants in culture. Antimicrobial Agents and Chemotherapy, 61(8). https://doi.org/10.1128/AAC.00744-17

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