Ceftobiprole medocaril is a new injectable cephalosporin antibiotic
with broad-spectrum activity against a wide range of difficult-to-treat
Gram-positive and Gram-negative hospital- and community-acquired
infections including MRSA. It was launched in Canada for the treatment of cSSSI, including diabetic foot infection. Ceftobiprole
medocaril is a water-soluble pro-drug of ceftobiprole, which is a
pyrrolidinone-3-ylidenemethyl cephem with a 3-pyrrolidinyl side chain.
The pro-drug is derived by the attachment of a carbamoyl ester group on
the pyrrolidine nitrogen of ceftobiprole. Like all beta-lactam antibiotics,
ceftobiprole produces its bactericidal effects by inhibiting cell wall synthesis through the prevention of the cross-linking of peptides on the
mucosaccharide chains that make up the cell wall. This is accomplished
by binding to and inhibiting the penicillin-binding proteins (PBPs). As
a result, bacterial cell walls are weakened and susceptible to osmotic
pressure and cell lysis. The broad-spectrum activity of ceftobiprole is due
to the inhibition of PBPs in both Gram-positive and Gram-negative
bacteria. In addition, ceftobiprole inhibits PBP2x in penicillin-resistant Streptococcus pneumoniae as well as PBP3 and other PBPs in certain Gram-negative bacteria such as Escherichia coli and Pseudomonas aeruginosa.Among Gram-positive pathogens, it has excellent activity against coagulase-negative staphylococci (both methicillin-susceptible and methicillin-resistant strains), S. pneumoniae (including penicillinresistant strains) and other streptococcal species, and Enterococcus faecalis (MIC90 4 mg/mL).Ceftobiprole is also active in vitro against a broad range of aerobic Gram-negative bacilli, including P. aeruginosa, against which its activity is similar to that of cefepime.
