GSK2556286 Is a Novel Antitubercular Drug Candidate Effective <i>In Vivo</i> with the Potential To Shorten Tuberculosis Treatment.

ABSTRACT: As a result of a high-throughput compound screening campaign using Mycobacterium tuberculosis-infected macrophages, a new drug candidate for the treatment of tuberculosis has been identified. GSK2556286 inhibits growth within human macrophages (50% inhibitory concentration [IC₅₀] = 0.07 μM), is active against extracellular bacteria in cholesterol-containing culture medium, and exhibits no cross-resistance with known antitubercular drugs. In addition, it has shown efficacy in different mouse models of tuberculosis (TB) and has an adequate safety profile in two preclinical species. These features indicate a compound with a novel mode of action, although still not fully defined, that is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and drug-se

SUBMITTER: Nuermberger EL 

PROVIDER: S-EPMC9211396 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature