TOC-50

In vitro and in vivo antibacterial activities of TOC-50, a new parenteral cephalosporin, were assessed against Enterococcus faecalis. In vitro, TOC-50 had excellent activity, stronger than that of penicillin G, sulbactam/ampicillin, tazobactam/piperacillin, the cephalosporins tested, imipenem, vancomycin, gentamicin, tobramycin, arbekacin, amikacin, minocycline and ofloxacin against clinically isolated strains. In addition, TOC-50 was more active than penicillin G, sulbactam/ampicillin and imipenem against vancomycin-resistant E. faecalis NCTC 12201. In terms of bactericidal effect against the same strain, TOC-50 was superior to sulbactam/ampicillin and imipenem. In murine systemic infection models, TOC-50 had a potent protective activity against E. faecalis 42. Its protective activity was stronger than that of imipenem or vancomycin.

The in vitro activity of TOC-50, a new parenteral cephalosporin, was assessed against methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). TOC-50 showed excellent activity, which was stronger than that of methicillin, cloxacillin, the cephalosporins tested, imipenem, gentamycin, minocycline, ofloxacin and ciprofloxacin against MRSA and had a minimum inhibitory concentration (MIC) comparable to that of vancomycin (the MICs of TOC-50 and vancomycin for growth inhibition of 90% of the strains tested were 3.13 and 1.56 micrograms/ml, respectively). Against MRSE, TOC-50 exhibited excellent activity, which was stronger than that of methicillin, ampicillin, the cephalosporins tested and imipenem, and was twice as active as vancomycin. In terms of the bactericidal effect against MRSA, TOC-50 was superior to vancomycin.