Efficacy of Human Exposures of Gepotidacin (GSK2140944) against Escherichia coli in a Rat Pyelonephritis Model.

ABSTRACT: Gepotidacin is a first-in-class triazaacenaphthylene antibacterial that inhibits bacterial type II topoisomerases and has in vitro activity against a range of bacterial pathogens, including Escherichia coli Urinary tract infections often progress to pyelonephritis and are a worldwide problem due to the prevalence of multidrug-resistant E. coli strains. This study evaluated the in vivo efficacy of gepotidacin against four strains of multidrug-resistant E. coli in a rat pyelonephritis model. Infected rats received controlled intravenous infusions of gepotidacin every 12 h for 4 days that recreated human systemic exposures from oral gepotidacin (800 or 1,500 mg twice daily for 4 days). Liquid chromatography-tandem mass spectrometry analysis of blood samples

SUBMITTER: Hoover JL 

PROVIDER: S-EPMC6591613 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature