GSK3640254 Is a Novel HIV-1 Maturation Inhibitor with an Optimized Virology Profile.

ABSTRACT: HIV-1 maturation inhibitors (MIs) offer a novel mechanism of action and potential for use in HIV-1 treatment. Prior MIs displayed clinical efficacy but were associated with the emergence of resistance and some gastrointestinal tolerability events. Treatment with the potentially safer next-generation MI GSK3640254 (GSK'254) resulted in up to a 2-log₁₀ viral load reduction in a phase IIa proof-of-concept study. In vitro experiments have defined the antiviral and resistance profiles for GSK'254. The compound displayed strong antiviral activity against a library of subtype B and C chimeric viruses containing Gag polymorphisms and site-directed mutants previously shown to affect potency of earlier-generation MIs, with a mean protein-binding adjusted 90% effective concentration

SUBMITTER: Dicker I 

PROVIDER: S-EPMC8765437 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature