A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model.

ABSTRACT: People living with HIV (PLWH) have expressed concern about the life-long burden and stigma associated with taking pills daily and can experience medication fatigue that might lead to suboptimal treatment adherence and the emergence of drug-resistant viral variants, thereby limiting future treatment options^1-3. As such, there is strong interest in long-acting antiretroviral (ARV) agents that can be administered less frequently⁴. Herein, we report GS-CA1, a new archetypal small-molecule HIV capsid inhibitor with exceptional potency against HIV-2 and all major HIV-1 types, including viral variants resistant to the ARVs currently in clinical use. Mechanism-of-action studies indicate that GS-CA1 binds directly to the HIV-1 capsid and interferes with capsid-mediated nuclear

SUBMITTER: Yant SR 

PROVIDER: S-EPMC7396128 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature