is the first of a new class of drug called capsid inhibitors to be FDA-approved for treating HIV-1
is a novel, first-in-class, multistage, selective inhibitor of HIV capsid protein
blocks the HIV-1 virus' protein shell and interferes with essential steps of the virus' evolution
binds to the HIV-1 capsid to potently inhibits HIV-1 replication in vitro and in vivo (1)
in clinical studies, lenacapavir has demonstrated successful antiviral activity and adequate pharmacokinetic exposure for up to 6 months after a single subcutaneous injection (2)
by binding to two neighbouring subunits of the HIV capsid protein, lenacapavir interferes with their interactions essential for multiple phases of the viral replication cycle (1,2) and include:
capsid-mediated nuclear uptake of preintegration complexes,
virion production and proper capsid core formation
virus produced in the presence of lenacapavir displays improperly shaped capsids that can enter new target cells but cannot replicate
Reference:
Selyutina A, Hu P, Miller S, Simons LM, Yu HJ, Hultquist JF, Lee K, KewalRamani VN, Diaz-Griffero F. GS-CA1 and lenacapavir stabilize the HIV-1 core and modulate the core interaction with cellular factors. iScience. 2021 Dec 9;25(1):103593
Dvory-Sobol H, Shaik N, Callebaut C, Rhee MS. Lenacapavir: a first-in-class HIV-1 capsid inhibitor. Curr Opin HIV AIDS. 2022 Jan 1;17(1):15-21.
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