Ceftobiprole is a a broad-spectrum, β-lactam, fifth-generation Cephalosporin antibiotic. It has activity against Gram-positive and Gram-negative bacteria. It has activity against methicillin-resistant Staphylococcus aureus (MRSA). Ceftobiprole inhabits PBP1 (penicillin-binding protein 1), PBP2 and ß-lactam resistance determinant PBP2a.
Ceftobiprole is slightly soluble in DMSO.
We also offer:
- Ceftobiprole Medocaril Sodium (C236)
| Molecular Formula |
C20H22N8O6S2 |
| 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. |
| Spectrum |
Ceftobiprole has in vitro activity against Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus. |
| Microbiology Applications |
Ceftobiprole exhibits bactericidal activity via inhibition of bacterial cell wall synthesis. This activity is mediated through binding to essential penicillin-binding proteins (PBPs) and inhibiting their transpeptidase activity, which is essential for the synthesis of the peptidoglycan layer of the bacterial cell wall. Ceftobiprole has demonstrated in vitro activity against both Gram-positive and Gram-negative bacteria. In Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), Ceftobiprole binds to PBP2a. Ceftobiprole also binds to PBP2b in Streptococcus pneumoniae, (penicillin-intermediate), PBP2x in S. pneumoniae (penicillin resistant), and to PBP5 in Enterococcus faecalis. Ceftobiprole is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram-positive and Gram-negative microbial isolates. Medical microbiologists use AST results to recommend antibiotic treatment options. Representative MIC values include: Staphyloccus aureus (methicillin-resistant) 0.5 － 4 µg/ml For list of Ceftobiprole MIC values, click here |
| References |
El Solh A. Ceftobiprole: a new broad spectrum cephalosporin. Expert Opin Pharmacother. 2009 Jul;10(10):1675-86 PMID: 19527192 Stein RA, Goetz RM and Ganea GM (2009) Ceftobiprole: A new beta-lactam antibiotic. Int. J. Clin. Pract. 63(6):930-943 PMID 19490203 Zhanel GG, Lam A, Schweizer F, Thomson K, Walkty A, Rubinstein E, Gin AS, Hoban DJ, Noreddin AM, Karlowsky JA. Ceftobiprole: a review of a broad-spectrum and anti-MRSA cephalosporin. Am. J. Clin. Dermatol. 2008;9(4):245-54 PMID: 18572975 |
