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New classes of HIV inhibitors that can suppress drugresistant viral variants and exhibit longlasting activity are needed. Here, Yant et al. report the identification of GSCA1, a smallmolecule inhibitor of… Click to show full abstract
New classes of HIV inhibitors that can suppress drugresistant viral variants and exhibit longlasting activity are needed. Here, Yant et al. report the identification of GSCA1, a smallmolecule inhibitor of the HIV-1 capsid protein. In vitro, GSCA1 exhibited potent inhibitory activity against all major HIV-1 types, including viral variants resistant to the antiretroviral (ARV) therapies currently in clinical use. In a humanized mouse model of HIV-1 infection, 12 weeks of subcutaneous GSCA1 treatment achieved durable HIV-1 suppression, demonstrating superior activity to rilpivirine — a licensed longacting ARV.
Journal Title: Nature Reviews Drug Discovery
Year Published: 2019
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