Cethromycin Pharmacokinetics and Pharmacodynamics for Single Dose Cure of <i>Plasmodium berghei</i> Liver Stages.

ABSTRACT: Cethromycin combines a quinoline nucleus and a macrolide for broad spectrum antibacterial and antiprotozoan activity. Here we characterized the murine pharmacokinetics and Plasmodium berghei lifecycle stage pharmacodynamics for the cethromycin base. Liver pharmacokinetic studies in mice show peak mM drug levels in the liver with 20 hour sustained levels above 10 μM. Peak concentrations in the liver were double the lung and about 440 times that of plasma. Immunofluorescence imaging of in vitro cethromycin-treated infected hepatocytes shows complete ablation of the apicoplast. We observed complete cure of P. berghei liver stage infection by single oral dose of 60 mg/kg in mice which is equivalent to the 5 mg/kg human dose of 300 mg a day used in bacterial pneumonia studi

SUBMITTER: Kennedy G 

PROVIDER: S-EPMC11844388 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature