Ceftobiprole medocaril
Trade names Zevtera, Mabelio
Routes of administration Intravenous
Drug class Cephalosporin antibacterial
Ceftobiprole is the active moiety of the prodrug ceftobiprole medocaril and is available for intravenous treatment only.
It is mainly excreted via the kidney.
Ceftobiprole, is a fifth-generation cephalosporin antibacterial used for the treatment of hospital-acquired pneumonia (excluding ventilator-associated pneumonia) and community-acquired pneumonia.
It exerts its antibacterial activity by binding to important penicillin-binding proteins and inhibiting their transpeptidase activity which is essential for the synthesis of bacterial cell walls.
Ceftobiprole has high affinity for penicillin-binding protein 2a of methicillin-resistant Staphylococcus aureus strains and retains its activity against strains that express divergent mecA gene homologues.
Ceftobiprole also binds to penicillin-binding protein 2b in Streptococcus pneumoniae, to penicillin-binding protein 2x in Streptococcus pneumoniae (penicillin-resistant), and to penicillin-binding protein 5 in Enterococcus faecalis.
For adults with Staphylococcus aureus bloodstream infections, the most common manifestations of side effects include hypokalemia, vomiting, diarrhea, increased liver tests, increased blood creatinine, high blood pressure, leukopenia, fever, abdominal pain, fungal infection, headache and dyspnea.
For adults with acute bacterial skin and skin structure infections, the most common side effects include nausea, diarrhea, headache, injection site reaction, increased levels of hepatic enzymes, rash, vomiting and dysgeusia.
For adults with community-acquired bacterial pneumonia, the most common side effects include nausea, increased levels of hepatic enzymes, vomiting, diarrhea, headache, rash, insomnia, abdominal pain, phlebitis, high blood pressure and dizziness.
For children with community-acquired bacterial pneumonia, the most common side effects include vomiting, headache, increased levels of hepatic enzymes, diarrhea, infusion site reaction, phlebitis and fever.
Ceftobiprole is indicated for the treatment of adults with Staphylococcus aureus bacteremia including those with right-sided infective endocarditis; adults with acute bacterial skin and skin structure infections; and people with community-acquired bacterial pneumonia.
Ceftobiprole has antimicrobial activity against a broad range of Gram-positive and Gram-negative pathogens.
Among the Gram-positive pathogens- methicillin-resistant Staphylococcus aureus, methicillin-susceptible Staphylococcus aureus and coagulase-negative staphylococci, as well as against strains of methicillin-resistant Staphylococcus aureus with reduced susceptibility to linezolid, daptomycin or vancomycin.
It has also potent activity against Streptococcus pneumoniae, including penicillin-sensitive, penicillin-resistant and ceftriaxone-resistant strains, and Enterococcus faecalis, but not against Enterococcus faecium.
For Gram-negative pathogen activity against Haemophilus influenzae (including both ampicillin-susceptible and ampicillin-non-susceptible isolates), Pseudomonas aeruginosa and strains of Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis that do not produce extended-spectrum β-lactamases (ESBL).
Like all other cephalosporins, ceftobiprole was inactive against strains that produce extended-spectrum β-lactamases.
Ceftobiprole was non-inferior to ceftazidime plus linezolid in the treatment of hospital-acquired pneumonia (excluding ventilator-acquired pneumonia) and non-inferior to ceftriaxone with or without linezolid in the treatment of community-acquired pneumonia.
The efficacy of ceftobiprole medocaril in treating Staphylococcus aureus bacteremia. was evaluated in a randomized, controlled, double-blind, multinational, multicenter trial.
A total of 69.8% of participants who received ceftobiprole medocaril achieved overall success compared to 68.7% of participants who received the comparator.
The efficacy of ceftobiprole medocaril in treating acute bacterial skin and skin structure infections was evaluated in a randomized, controlled, double-blind, multinational trial..
In the trial, researchers randomly assigned 679 participants to receive either ceftobiprole medocaril or vancomycin plus aztreonam [the comparator]: 91.3% achieved an early clinical response within the necessary timeframe compared to 88.1% of participants who received the comparator.
The efficacy of ceftobiprole medocaril in treating adults with community-acquired bacterial pneumonia was evaluated in a randomized, controlled, double-blind, multinational, multicenter trial.
In the trial, randomly assigned 638 adults hospitalized with community-acquired bacterial pneumonia and requiring IV antibacterial treatment for at least 3 days to receive either ceftobiprole medocaril or ceftriaxone with optional linezolid.
Clinical cure rates at test-of-cure visit, which occurred 7-14 days after end-of-treatment: Of the participants who received ceftobiprole medocaril, 76.4% achieved clinical cure compared to 79.3% of participants who received the comparator.
Designations for the community-acquired bacterial pneumonia, acute bacterial skin and skin structure infections, and Staphylococcus aureus bacteremia indications.