Ceftobiprole: The First Broad-Spectrum Anti–methicillin-resistant Staphylococcus aureus Beta-Lactam

The chemistry, pharmacology, antimicrobial activity, pharmacokinetics, pharmacodynamics, efficacy, safety, and formulary considerations of ceftobiprole are reviewed. Ceftobiprole medocaril is a novel broad-spectrum cephalosporin antibiotic with unique activity against gram-positive bacteria, including methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, and Enterococcus faecalis. Spectrum of activity against gram-negative bacteria includes Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Enterobacter cloacae, and Pseudomonas aeruginosa. Ceftobiprole is not active against Acinetobacter baumannii and extended-spectrum β-lactamase-producing Enterobacteriaceae. Ceftobiprole at a dosage of 500 mg, infused intravenously over 1 hour every 12 hours, was noninferior to vancomycin in the treatment of complicated skin and skin structure infections (cSSSIs) caused by suspected or documented gram-positive pathogens with cure rates of 93.3% and 93.5%, respectively. Ceftobiprole at a dosage of 500 mg, infused intravenously over 2 hours every 8 hours, was noninferior to the combination of vancomycin and ceftazidime in the treatment of cSSSIs caused by suspected or documented gram-positive or gram-negative pathogens, with cure rates of 90.5% and 90.2%, respectively. Ceftobiprole has also been studied for the treatment of community- and hospital-acquired pneumonia. Clinical trials conducted so far have confirmed the relative safety of ceftobiprole, with nausea, vomiting, and caramel-like taste disturbance being the most common adverse events and allergic reactions the most serious adverse events. Ceftobiprole medocaril is currently approved in Canada and Switzerland for the treatment of cSSSIs. If approved by the food and drug administration, ceftobiprole may represent an attractive option for the treatment of cSSSIs and pneumonias as monotherapy.