Ceftobiprole, an investigational beta-lactam antibiotic, has been shown to have a broad spectrum of activity against Gram-positive and Gram-negative pathogens. Unlike currently available beta-lactams, ceftobiprole has been shown to be active against methicillin-resistant staphylococci because of its high affinity for penicillin-binding protein (PBP) 2' (2a). Ceftobiprole has undergone extensive evaluation in phase I studies to characterise dose, pharmacokinetics, and safety/tolerability. In an early phase II study, all 35 clinically evaluable patients (n = 40) with complicated skin and skin structure infections (cSSSIs) receiving intravenous ceftobiprole 750 mg twice-daily were cured, including four of four patients with methicillin-resistant Staphylococcus aureus (MRSA). Microbiological eradication was achieved in 91% (21/23) of evaluable patients. On the basis of these results, phase III studies of ceftobiprole for the treatment of cSSSIs were initiated. One study compared intravenous ceftobiprole (500 mg every 12 h) to intravenous vancomycin (1 g every 12 h) in patients with cSSSIs due to Gram-positive bacteria. Staphylococci were the predominant pathogens, and more than 25% of the microbiologically evaluable patients had infections caused by MRSA. In the clinically evaluable population, efficacy and adverse events were comparable between treatment arms. Additional clinical trials in cSSSI and pneumonia patients are underway to evaluate ceftobiprole for the treatment of infections due to both Gram-positive and Gram-negative bacteria. Ceftobiprole is the first cephalosporin to demonstrate clinical efficacy in patients with infections due to methicillin-resistant staphylococci and, if approved by regulatory authorities, is expected to be a useful addition to the armamentarium of agents for the treatment of complicated skin infections and pneumonia.