Jin-Hwan KWAK
Handong Global University, Korea
Title: In vitro and In vivo Activities of LCB01-0648 and LCB01-0699 against Staphylococci
Biography
Biography: Jin-Hwan KWAK
Abstract
LCB01-0648 is a new oxazolidinone, which is under preclinical development. In this study, we tested in vitro and in vivo activity of LCB01-0648 against staphylococci. In vitro activity of LCB01-0648 against MSSA, MRSA and LRSA, was evaluated by the agar dilution method as described by the CLSI, and compared with those of linezolid, oxacillin, erythromycin, ciprofloxacin, sparfloxacin, moxifloxacin, gemifloxacin and vancomycin. The MIC90 of LCB01-0648, at which 90% of bacterial strains are inhibited, was 0.5 μg/ml against MSSA, MRSA and was below 4 μg/ml against LRSA. In vitro activity of CB01-0648 was 4-fold more active than linezolid against MSSA and MRSA. Especially, the antibacterial activity of LCB01-0648 had good antibacterial activities against linezolid-resistant or -intermediate S. aureus. LCB01-0648, at the concentration of 8X MIC, showed a bactericidal activity against MSSA and MRSA. In vivo activity of LCB01-0699 which is the active prodrug of LCB01-0648 was also compared with that of linezolid against systemic infections caused by MSSA, MRSA and LRSA in mice. LCB01-0699 was more effective than linezolid against systemic infections. In conclusion, LCB01-0648 had potent in vitro and in vivo activity against drug resistant Gram-positive pathogen, including MRSA and LRSA. These results indicate that LCB01-0648 could be a good candidate for further pre-clinical studies.