Ceftobiprole medocaril

DB14733ApprovedSmall moleculeCephalosporins

Ceftobiprole medocaril 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 broad-spectrum agent with demonstrated activity against both Gram-positive and Gram-negative bacteria, including antibiotic-resistant strains of Staphylcoccus aureus (methicillin-resistant Staphylococcus aureus; MRSA).

Mechanism: 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.
Curator reviewed · 5 references
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 · 20 structured indications
Formula / weight: C₂₆H₂₆N₈O₁₁S₂ · 690.66 g/mol (avg)
First approval: Canada, 2008 · United States, 2025
Also known as: Ceftobiprole medocaril free acid
Brand names: Zevtera

Resolves to

Compound

UNIIYXV28V1B07CAS376653-43-9ChEMBLCHEMBL6175829ChEBI135968

Clinical / RWD

ATCJ01DI01

Structure

InChIKeyHFTSMHTWUFCYMJ-YIOMYIDASA-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])CCN(C1)C(=O)OCC1=C(C)OC(=O)O1

Targets

Q7DHH4mecAP72355pbp4P0A3M6penAP59676pbpX

Transporters

Q9Y6L6SLCO1B1Q9NPD5SLCO1B3Q92887ABCC2O95342ABCB11

What you can answer from here — as of September 12, 2026

4Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

4TransportersSubstrate / inhibitor direction, not just membership

Listed above

193Drug interactionsStructured to mechanism, not free text

12Clinical trialsPhase, status and sponsor resolved per trial

20Structured indicationsCondition, population, route and combination as fields, not prose

3ContraindicationsEach with its own population and attribute set

7Marketed productsAcross 5 countries and 6 labellers

1ATC codeIncluding every combination product, plus 14 drug categories

18+ReferencesStructured and connected to the statements they support

Which drugs share a target with Ceftobiprole medocaril, and which of those have an active Phase 3 trial?

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