Resistance to antimicrobials is a significant and growing problem, limiting treatment options, especially for serious Gram-positive
infections.
Ceftobiprole is a novel broad-spectrum
cephalosporin that is active in vitro against streptococci and staphylococci, including
penicillin-resistant strains of pneumococci and methicillin-resistant Staphylococcus aureus (MRSA). It maintains the activity of extended-spectrum
cephalosporins against Gram-negative bacteria, including Enterobacteriaceae. The in-vivo activity of
ceftobiprole has been demonstrated in mouse
sepsis and subcutaneous
abscess models of
infection. Its activity also has been examined in several discriminative models of
infection that mimic specific diseases in humans and permit testing of antimicrobial activity under a variety of defined pharmacokinetic conditions. These include experimental
pneumonia in mice, a
tissue cage model of
foreign body infection in rats, and
endocarditis models in rats and rabbits. In these models,
ceftobiprole exhibits activity equivalent or superior to that of comparators against MRSA, including
vancomycin-intermediate strains. These models also confirm the in-vivo activity of
ceftobiprole against Gram-negative bacteria that are susceptible in vitro. The results from animal models support the evaluation of the clinical efficacy of
ceftobiprole in humans and also predict clinical efficacy in the empirical treatment of severe
infections. The broad spectrum of activity may allow
ceftobiprole to be used as monotherapy for serious hospital-acquired
infections where combination
therapy would otherwise be required.