Daily oral antiretroviral therapies (ART) provide many life-saving treatment options for millions of people with HIV (PWH) and have shown to be effective in preventing new infections. Nonetheless, new classes of antiretroviral agents are continually needed to treat people with multidrug resistant HIV-1 and long acting agents can help people with suboptimal adherence to daily oral regimens. The HIV-1 capsid protein is a novel and attractive target for therapeutic intervention due to its essential role at multiple steps in the viral replication cycle. Lenacapavir is a potent, investigational first-in-class small molecule capsid inhibitor in development as a long acting agent for the treatment and prevention of HIV infection. In heavily treatment experienced and treatment naïve PWH, lenacapavir in combination with other antiretroviral agents led to high rates of virologic suppression. Herein we describe the identification of the lenacapavir core structure via the use of structure-based drug design during both early- and mid-stage drug discovery efforts.

Core exploration in the discovery of Lenacapavir - a first-in-class long acting HIV capsid inhibitor

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ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.