Ceftobiprole is a novel parenteral cephalosporin with high affinity for most penicillin-binding proteins, including the mecA product penicillin-binding protein (PBP) 2a, rendering it active against methicillin-resistant staphylococci. Its in vitro activity against staphylococci and multiresistant pneumococci, combined with its Gram-negative spectrum comparable to that of other extended-spectrum cephalosporins, its stability against a wide range of β-lactamases and its pharmacokinetic and safety profile make ceftobiprole an attractive new antimicrobial agent. Because of its low water solubility, ceftobiprole is administered intravenously as a prodrug, ceftobiprole medocaril. Ceftobiprole medocaril is generally well tolerated (with the exception of a caramel-like taste disturbance). Ceftobiprole medocaril has been evaluated in two phase III clinical trials for the treatment of complicated skin infections and skin structure infections. Its broad spectrum of activity may allow ceftobiprole to be used as monotherapy for some infections where combination therapy would otherwise be required, especially regimens requiring coverage of methicillin-resistant Staphylococcus aureus (MRSA).
ASJC Scopus subject areas
- Pharmacology (medical)