Abstract
LCB01-0062, a novel oxazolidinone, has potent antibacterial activity against clinical isolates of Gram-positive bacteria. The in vitro activity of LCB01-0062 was compared with that of linezolid, oxacillin, erythromycin, ciprofloxacin, vancomycin and quinupristin/dalfopristin. Among the tested agents, LCB01-0062 showed the most potent antibacterial activity against meticillin-resistant Staphylococcus aureus, meticillin-resistant coagulase-negative staphylococci and vancomycin-resistant enterococci. LCB01-0062 was 4–8-fold more active than linezolid, the first oxazolidinone drug, against Gram-positive bacteria. The time–kill curves of LCB01-0062 were analysed at concentrations of 0.5×, 1×, 2×, 4× and 8× the minimum inhibitory concentration against S. aureus strains. LCB01-0062 showed bacteriostatic activity during 24h. LCB01-0062 was also more effective than linezolid against S. aureus in a systemic mouse model of infection.
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