Ceftobiprole Medocaril Sodium is the prodrug that is rapidly converted in vivo to Ceftobiprole, its active form by type A plasma esterases. Ceftobiprole is a a broad-spectrum, beta-lactam, fifth-generation Cephalosporin. It has a high binding affinity for penicillin binding proteins in many Gram-positive and Gram-negative bacteria.
| Mechanism of Action | Cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases. Ceftobiprole Medocaril Sodium has a high affinity for PBP2a conferrring methicillin-resistance in S. aureus, PBP2x conferring penicillin-resistance in S. pneumoniae, and PBP5 in Enterococcus faecalis. |
| Spectrum | Broad-range against Gram-positive and Gram-negative bacteria. It is active in vitro against S. aureus (most MRSA), vancomycin-intrmediate S. aureus (VISA), and vancomycin-resistant S. aureus (VRSA). S. pneumoniae, and Enterobacteriaceae. It is not active against anaerobic bacteria. |
| Microbiology Applications | Ceftobiprole Medocaril Sodium has activity against Streptococcus pneumoniae, Enterococcus faecalis. H. influenzae, and P aeruginosa. Resistance among Staphyloccus and streptococcus is uncommon. However, resistance in Enterobacteriaceae is conferred by B-lactamases. |
| Molecular Formula | C26H26N8O11S2 ∙ Na |
| References | Kisgen J and Whitney D (2008) Ceftobiprole, a broad-spectrum Cephalosporin with activity against Methicillin-Resistant Staphylococcus aureus (MRSA). P.T. 33 (11): 631-634 PMID 19750059 Livermore DM (2006) Can β-lactams be re-engineered to beat MRSA? CMI 12(s2):11-16 PMID 16524423 Scheeren TW (2015) Ceftobiprole medocaril in the treatment of hospital-acquired pneumonia. Future. Microbiol. 10(12):1913-1928 PMID 26573022 Stein RA, Goetz RM and Ganea GM (2009) Ceftobiprole: A new beta-lactam antibiotic. Int. J. Clin. Pract. 63(6):930-943 PMID 19490203 Yin L, Calhoun JH, Thomas JK, Shapiro S and Schmitt-Hoffmann A (year) Efficacies of Ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus. Antimicrob. Agents Chemother. 52 (5) 1618-1622 PMID 18332175 |
