LB10517 is a new
injectable cephalosporin with a broad spectrum of antibacterial activity against Gram-positive and Gram-negative bacteria.
LB10517 inhibited 90% of
methicillin-susceptible Staphylococcus aureus (MSSA) at 0.25 mg/L (MIC90), and was 8-fold more active than
cefpirome.
LB10517 was two- or four-fold more active than
cefpirome against
methicillin-susceptible Staphylococcus epidermidis (MSSE), Streptococcus pyogenes and Enterococcus faecalis. Both methicillin-resistant S. aureus (MRSA) and methicillin-resistant S. epidermidis (MRSE) were highly resistant to all compounds.
LB10517 activity against most Enterobacteriaceae was comparable to or greater than that of
cefpirome, and it also showed high activity against Pseudomonas aeruginosa. In a mouse septicaemia model,
LB10517 exhibited excellent protective effects. In a
respiratory tract infection model, the protective effect of
LB10517 was comparable to that of
cefpirome and
ceftazidime. It was highly stable to hydrolysis by
beta-lactamases, showing better physiological efficiency for TEM-9 than the other test compounds.
LB10517 had the most potent antibacterial activity against
beta-lactamase producing resistant strains.
LB10517 did not induce
beta-lactamase production in Enterobacter cloacae 1194E.