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ceftobiprole medocaril
- Development stage
- Approved
- Lead developer
- Basilea Pharmaceutica
- Modality
- Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Ceftobiprole medocaril is a prodrug of ceftobiprole, a fifth-generation (next-generation) broad-spectrum cephalosporin antibiotic for intravenous use. It is active against both Gram-positive and Gram-negative bacteria, including multidrug-resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae, and Pseudomonas aeruginosa. Ceftobiprole exerts its bactericidal effect by binding to essential penicillin-binding proteins (PBPs)—notably PBP2a in MRSA, PBP2b and PBP2x in S. pneumoniae—and inhibiting their transpeptidase activity, which disrupts bacterial cell wall synthesis and leads to cell death. The drug is indicated for the treatment of Staphylococcus aureus bloodstream infections (bacteremia), including right-sided infective endocarditis; acute bacterial skin and skin structure infections (ABSSSI); and community-acquired bacterial pneumonia (CABP) in adults and children aged 3 months or older[1][3][5][6].
- Brand names
- Zevtera
- Other names
- ceftobiprole medocaril sodiumceftobiprole medocaril free acid
02
Targets
PBP2B (Penicillin-binding protein 2B)PBP2x (Penicillin-binding protein 2x)PBP1A (Penicillin-binding protein 1A)PBP5 (D-alanyl-D-alanine carboxypeptidase DacA)PBP2 (Penicillin-binding protein 2)
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