Drug intelligence / Profile preview

GS-3242 + lenacapavir

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Subcutaneous
01

Overview

GS-3242 + lenacapavir is an investigational, long-acting combination therapy being developed by Gilead Sciences for the treatment of HIV-1 infection. The regimen consists of GS-3242, a novel long-acting integrase strand transfer inhibitor (INSTI), and lenacapavir, a first-in-class capsid inhibitor. This combination is designed for twice-yearly subcutaneous administration, aiming to provide a complete antiretroviral regimen with a significantly reduced dosing frequency compared to standard daily oral therapies. GS-3242 works by blocking the integration of viral DNA into the host cell genome, while lenacapavir (Sunlenca) interferes with multiple stages of the HIV life cycle by binding to the viral capsid protein (p24), including capsid-mediated nuclear import, viral assembly, and release.

02

Targets

Integrase allosteric pocket (HIV)p24 (HIV-1 capsid protein p24)

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