Cefozopran

Cefozopran (SCE-2787) is a potent antibiotic with broad-spectrum antibacterial activity. Cefozopran binds PBPs, induces cell wall destruction, cell elongation, filamentation, irregular septa formation, and bactericidal, bacteriolytic activity. Cefozopran reduces bacterial counts and eradicates bacteria in mouse respiratory, urinary, and thigh muscle infections. Cefozopran can be used for the research of bacterial infections^[1][2][3][4]. In Vitro:Cefozopran (20 h) potently inhibits growth of Streptococcus pyogenes, Staphylococcus aureus, Enterococcus faecalis, and shows particularly strong activity against Streptococcus species, Enterobacteriaceae (except Proteus vulgaris), and Methicillin (HY-121544)-susceptible staphylococci^[4].
Cefozopran (20 h) inhibits growth of various laboratory aerobic bacterial strains, with MIC values ranging from 0.1 μg/mL to 50 μg/mL, and shows limited activity against tested anaerobic strains^[4].
Cefozopran (20 h) is highly active against Ceftazidime (HY-B0593)-resistant Citrobacter freundii (MIC₉₀ = 3.13 μg/mL) and Enterobacter cloacae (MIC₉₀ = 12.5 μg/mL), but shows cross-resistance with Ceftazidime against Ceftazidime-resistant Pseudomonas aeruginosa (MIC₉₀ >100 μg/mL)^[4].
Cefozopran (200 μM) is highly resistant to hydrolysis by most common β-lactamases, including Bush group 1, 2a, 2b, and 2c enzymes, but is hydrolyzed to varying degrees by Bush group 2b', 2d, and 2e enzymes^[4].
Cefozopran dihydrochloride has low affinity for all tested β-lactamases, with K_m/K_i values all >100 μM, indicating minimal interaction with these enzymes^[4]. In Vivo:Cefozopran (5-80 mg/kg; s.c.; twice daily; 5 days) exhibits potent efficacy against acute K. pneumoniae respiratory tract infection in mice^[2].
Cefozopran (20-80 mg/kg; s.c.; twice daily; 7 days) effectively eradicates chronic K. pneumoniae respiratory tract infection in mice^[2].
Cefozopran (1.56-100 mg/kg; s.c.; twice daily; 5 days; tarting 3 days after infection) demonstrates potent efficacy against P. aeruginosa urinary tract infection in mice^[2].
Cefozopran (0.625-200 mg/kg; s.c.; dose at 2, 18, 26 hours post-infection) shows strong efficacy against MSSA thigh muscle abscess infection in mice^[2].