Ceftobiprole is a broad spectrum 5th-generation cephalosporin antibacterial indicated for certain kinds of pneumonia, bacteremia, and skin and skin structure infections, including those caused by MRSA. Ceftobiprole is a fifth-generation semisynthetic cephalosporin antibacterial which is available commercially as the prodrug ceftobiprole medocaril.
- Mechanism
- Curator reviewed · 5 references
Ceftobiprole, the active moiety of ceftobiprole medocaril, exhibits its bactericidal activity by inhibition of bacterial cell wall synthesis. This activity is mediated through binding to essential penicillin-binding proteins (PBPs) and inhibiting their transpeptidase activity, which is essential for the synthesis of the peptidoglycan layer of the bacterial cell wall.
Ceftobiprole has demonstrated in vitro activity against both Gram-positive and Gram-negative bacteria. In Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), Ceftobiprole binds to PBP2a. Ceftobiprole also binds to PBP2b in Streptococcus pneumoniae (penicillin-intermediate), PBP2x in S. pneumoniae (penicillin resistant), and to PBP5 in Enterococcus faecalis.
- Primary indication
- Ceftobiprole medocaril is an antibacterial indicated for the treatment of adult patients with Staphylococcus aureus bloodstream infections (bacteremia) (SAB), including those with right-sided infective endocarditis.Curator reviewed
- Formula / weight
- C20H22N8O6S2 · 534.57 g/mol (avg)
- Code names
- BAL-9141 · BAL-9141-000 · RO 63-9141
Resolves to
VOAZJEPQLGBXGO-SDAWRPRTSA-NSMILES[H][C@@]1(NC(=O)C(=N/O)\C2=NSC(N)=N2)C(=O)N2C(C(O)=O)=C(CS[C@]12[H])\C=C1/CCN(C1=O)[C@]1([H])CCNC1What you can answer from here — as of September 13, 2026
Which drugs share a target with Ceftobiprole, and which of those have an active Phase 3 trial?
Create a free account or log in to explore the full data card.
Create Account