Ceftobiprole – a case study

Abstract

Ceftobiprole medocaril is a cephalosporin prodrug that is under investigation for treatment of complicated skin and skin-structure infections (cSSSIs) due to methicillin-resistant Staphylococcus aureus (MRSA) and hospital-acquired pneumonia (HAP), including ventilator-associated pneumonia due to suspected or proven MRSA. Ceftobiprole was designed to bind the penicillin-resistant targets in Gram-positive bacteria, resulting in potent bactericidal activity against methicillin-resistant MRSA and penicillin-resistant Streptococcus pneumoniae (PRSP). In microbiological studies, ceftobiprole has demonstrated a broad-spectrum profile, with activity against many Gram-positive bacteria and a variety of important pathogenic Gram-negative bacteria. Ceftobiprole medocaril is being studied in Phase III clinical trials for cSSSI, HAP and hospitalised community-acquired pneumonia (hCAP). Top-line Phase III results in the first cSSSI study (STRAUSS 1) showed a high cure rate and good tolerability. The second cSSSI trial (STRAUSS 2) is targeting infections caused by Gram-positive and Gram-negative bacteria, and includes patients with diabetic foot infections. Ceftobiprole is expected to combine the well-established advantages of the cephalosporin antibiotic class with an enhanced spectrum of action, including against resistant Gram-positive bacteria.

Keywords::

• carbapenem
• ceftobiprole
• cephalosporin
• methicillin-resistant Staphylococcus aureus
• MRSA
• penicillin-binding protein

Acknowledgements

The author thanks S Reinelt for preparing the structural models (Figure 6).