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Updated: Jan 21, 2026
Expression, Purification, and Antimicrobial Activity of S100A12
Published on: May 13, 2017
Mechanisms of action and antimicrobial activity of ceftobiprole
M I Morosini, M Díez-Aguilar, R Cantón1
1Rafael Cantón, Servicio de Microbiología. Hospital Ramón y Cajal e Instituto Ramón y Cajal de Investigación Sanitaria (IRYCIS). Madrid. Spain. rafael.canton@salud.madrid.org.
Abstract:
Ceftobiprole, a novel last generation parenteral cephalosporin, has an extended spectrum of activity, notably against methicillin-resistant Staphylococcus aureus (MRSA), ampicillin-susceptible enterococci, penicillin-resistant pneumococci, Enterobacterales and susceptible Pseudomonas aeruginosa. It exerts an inhibitory action on essential peptidoglycan transpeptidases, interfering with cell wall synthesis. The inhibitory action of ceftobiprole through binding to abnormal PBPs like PBP2a in methicillin-resistant staphylococci and PBP2b and PBP2x in the case of β-lactam-resistant pneumococci, ultimately leads to rapid bacterial cell death. In the case of Enterobacterales, ceftobiprole retains activity against narrow spectrum β-lactamases but is hydrolysed by their extended-spectrum counterparts, overexpressed Amp C, and carbapenemases. It is also affected by certain efflux pumps from P. aeruginosa. For anaerobic bacteria, ceftobiprole is active against Gram-positive Clostridioides difficile and Peptococcus spp. and Gram-negative Fusobacterium nucleatum but not against Bacteroides group or other anaerobic Gram-negatives. In in vitro studies, a low propensity to select for resistant subpopulations has been demonstrated. Currently, ceftobiprole is approved for the treatment of community-acquired pneumonia and hospital-acquired pneumonia with the exception of ventilator-associated pneumonia. Ceftobiprole's place in therapy appears to lie mainly in its combined activity against Gram-positive organisms, such as S. aureus and S. pneumoniae alongside that against Gram-negative organisms such as P. aeruginosa.
Insights
Ceftobiprole is a novel cephalosporin effective against resistant bacteria like MRSA and penicillin-resistant pneumococci. It shows promise for treating certain pneumonias by inhibiting bacterial cell wall synthesis.
Area of Science:
- Pharmacology and Microbiology
- Infectious Diseases
- Antibiotic Resistance
Background:
- Ceftobiprole is a fifth-generation cephalosporin with broad-spectrum antimicrobial activity.
- It targets essential bacterial enzymes involved in cell wall synthesis.
- Emerging antibiotic resistance necessitates novel therapeutic agents.
Purpose of the Study:
- To evaluate the spectrum of activity and mechanism of action of ceftobiprole.
- To assess ceftobiprole's efficacy against key resistant pathogens.
- To determine ceftobiprole's potential role in treating bacterial infections.
Main Methods:
- In vitro susceptibility testing against various bacterial strains.
- Analysis of ceftobiprole's interaction with penicillin-binding proteins (PBPs).
- Assessment of resistance development potential.
Main Results:
- Ceftobiprole demonstrates potent activity against methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae, and susceptible Pseudomonas aeruginosa.
- It effectively inhibits bacterial cell wall synthesis by targeting specific PBPs.
- Activity is retained against some extended-spectrum beta-lactamases but not carbapenemases; affected by certain efflux pumps.
- Shows activity against Gram-positive anaerobes like Clostridioides difficile but not Bacteroides species.
- Demonstrated a low propensity to select for resistant subpopulations in vitro.
Conclusions:
- Ceftobiprole offers a valuable therapeutic option for infections caused by challenging Gram-positive and Gram-negative pathogens.
- Its mechanism of action and spectrum of activity position it as an important agent in combating antibiotic resistance.
- Approved for community-acquired and hospital-acquired pneumonia (excluding VAP), its utility lies in combined Gram-positive and Gram-negative coverage.
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