Ceftobiprole, tradename Zevtera/Mabelio) is a fifth-generation cephalosporin for the treatment of hospital-acquired pneumonia and community-acquired pneumonia. 

Its antibacterial activity occurs by binding to important penicillin-binding proteins and inhibiting their transpeptidase activity which is essential for the synthesis of bacterial cell walls. 

The drug has high affinity for penicillin-binding protein 2a of methicillin-resistant Staphylococcus aureus strains and retains its activity against strains that express divergent mecA gene homologues (mecC or mecALGA251). 

Ceftobiprole also binds to penicillin-binding protein 2b in Streptococcus pneumonia, to penicillin-binding protein 2x in Streptococcus pneumoniae (penicillin-resistant), and to penicillin-binding protein 5 in Enterococcus faecalis.

Routes of administration Intravenous

Has in vitro antimicrobial activity against a broad range of Gram-positive and Gram-negative pathogens. 

Among the Gram-positive pathogens, it  

has good in vitro activity against methicillin-resistant Staphylococcus aureus, methicillin-susceptible Staphylococcus aureus and coagulase-negative staphylococci, as well as against strains of methicillin-resistant Staphylococcus aureus with reduced susceptibility to linezolid, daptomycin or vancomycin.

It has potent activity against Streptococcus pneumoniae (including penicillin-sensitive, penicillin-resistant and ceftriaxone-resistant strains) and Enterococcus faecalis, but not against Enterococcus faecium. 

For Gram-negative pathogens, ceftobiprole has shown good in vitro activity against Haemophilus influenzae, Pseudomonas aeruginosa and strains of Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis that do not produce extended-spectrum β-lactamases (ESBL). 

Like all other cephalosporins, ceftobiprolenis inactive against strains that produce extended-spectrum β-lactamases.

Randomized, double-blind, phase 3 clinical trials in patients with hospital-acquired and community-acquired pneumonia: Ceftobiprole was non-inferior to ceftazidime plus linezolid in the treatment of hospital-acquired pneumonia and non-inferior to ceftriaxone with or without linezolid in the treatment of community-acquired pneumonia.

Ceftobiprole is the active moiety of the prodrug ceftobiprole medocaril and is available for intravenous treatment only. 

The recommended dose is 500 mg as 2-hour infusion every 8 hours. 

It is mainly excreted renally. 

Dose adjustment is required for patients with renal impairment and for patients with end-stage renal disease, but no dose adjustment is needed by gender, ethnicity, age, obesity or hepatic impairment.

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