New approaches to treating HIV infection are needed, given the development of multidrug resistance and current daily antiretroviral regimens. Here, Link et al. present the small molecule GS-6207, which targets the HIV-1 capsid protein to disrupt viral replication. In vitro, GS-6207 exhibited picomolar antiviral activity against all subtypes of HIV-1 tested and displayed synergy when combined with other antiretroviral agents, without cross-resistance or cytotoxicity. In 40 healthy participants, a single subcutaneous injection of GS-6207 was safe and well tolerated, remaining active for more than 24 weeks. In 32 patients with untreated HIV-1 infection, a single dose of GS-6207 reduced viral load by the ninth day.
Nature Reviews Drug Discovery 19, 512 (2020)