Lenacapavir CAS# 2189684-44-2 HIV-1衣壳抑制剂GS-6207

Lenacapavir (GS-6207) is a first-in-class, long-acting capsid inhibitor targeting HIV-1. In preclinical studies, it bound the HIV-1 capsid protein with subnanomolar affinity (Kd ~0.43 nM), disrupting both capsid assembly and disassembly processes critical for viral replication. It showed potent antiviral activity across diverse HIV-1 subtypes, with EC50 values in the picomolar range (30–500 pM), including against strains resistant to other antiretroviral classes. In humanized mouse models, lenacapavir achieved durable viral suppression with infrequent subcutaneous dosing. Pharmacokinetic studies in animals demonstrated sustained plasma levels and long half-life, supporting extended dosing intervals. These findings justified its advancement into clinical development.