In-vitro and in-vivo antibacterial activity of LB10517, a novel catechol-substituted cephalosporin with a broad antibacterial spectrum

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Abstract
LB10517 is a new injectable cephalosporin with a broad spectrum of antibacterial activity against Gram-opositive 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 β-lactamases, showing better physiological efficiency for TEM-9 than the other test compounds. LB10517 had the most potent antibacterial activity against β-lactamase producing resistant strains. LB10517 did not induce β-lactamase production in Enterobacter cloacae 1194E.

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