Synonyms: GS-6207 | GS6207 | Sunlenca®
lenacapavir is an approved drug (EMA & FDA (2022))
Compound class:
Synthetic organic
Comment: Lenacapavir (GS-6207) is a novel long-acting anti-HIV lead that binds to the virus' at a conserved interface between capsid protein monomers [2]. This mechanism disrupts early and late phases of the viral replication cycle [1] [3]. PDB entry 6V2F shows the crystal structure of lenacapavir-bound HIV capsid hexamer.
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Bioactivity Comments |
Picomolar concentrations of GS-6207 produced antiviral activity against all of the HIV-1 subtypes that were tested [2]. The EC50 is 105 pM in MT-4 cells infected with HIV-1, and 32 pM in primary human CD4+ T cells. GS-6207 is highly stable in vivo, and sustains antiviral activity for more than 6 months, and is activive against HIV-1 variants that are resistant to current drug classes. |