Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability.

ABSTRACT: Protease inhibitors (PIs) remain an important component of antiretroviral therapy for the treatment of HIV-1 infection due to their high genetic barrier to resistance development. Nevertheless, the two most commonly prescribed HIV PIs, atazanavir and darunavir, still require co-administration with a pharmacokinetic boosting agent to maintain sufficient drug plasma levels which can lead to undesirable drug-drug interactions. Herein, we describe GS-9770, a novel investigational non-peptidomimetic HIV PI with unboosted once-daily oral dosing potential due to improvements in its metabolic stability and its pharmacokinetic properties in preclinical animal species. This compound demonstrates potent inhibitory activity and high on-target selectivity for recombinant HIV-1 protease versus other asp

SUBMITTER: Mulato A 

PROVIDER: S-EPMC10989020 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature