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.