Delpazolid

A novel oxazolidinone antibiotic that shows good antibacterial activity (MSSA MIC50=1 ug/mL) ; potently inhibits MSSA and MRSA clinical isolates with MIC of 0.5-2 and 0.5-4 ug/mL, respectively; shows more-potent protective effects (MSSA ED50=4.53 mg/kg) than Linezolid against systemic infections caused by Gram-positive and Gram-negative bacteria in mice model.Bacterial Infection Preclinical (In Vitro) :Delpazolid (LCB01-0371), at concentrations of 1xMIC and 2xMIC, has bacteriostatic activity against MSSA and MRSA after 24 h. At concentrations of 4xMIC and 8xMIC, Delpazolid shows bacteriostatic activity, but there is no regrowth at concentrations of 4xMIC and 8xMIC after 24 h of incubation. The survival of M. abscessus is greatly decreased in the presence of Delpazolid (LCB-0371) (MIC50=1.2 μg/mL) . Delpazolid dramatically decreases the number of intracellular mycobacteria present at 2 days after infection at concentrations of 0.1, 1, and 10 μg/mL. (In Vivo) :When administered orally, Delpazolid (LCB01-0371) shows potent protective effects against systemic infections caused by Gram-positive and Gram-negative bacteria. Against infection caused by S. aureus Giorgio (MSSA), the ED50 of Delpazolid is 4.53 mg/kg of body weight. Against S. aureus p125 (MRSA), the ED50 of Delpazolid is 2.96 mg/kg. When Delpazolid (LCB-0371) is administered at 100 mg/kg daily (by gavage), the colony-forming unit (CFU) counts tend to be decreased in the lungs of mice at 7 days after infection.