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Ceftobiprole
Systematic (IUPAC) name
(6R,7R)-7-[[(2Z)-2-(5-amino-1,2,4-thiadiazol-3-ylidene)- 2-nitroso-1-oxoethyl]amino]-8-oxo-3-[(E)-[2-oxo-1-[(3R)- 3-pyrrolidinyl]-3-pyrrolidinylidene]methyl]-5-thia-1- azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Identifiers
CAS number 209467-52-7
252188-71-9 (medocaril)
ATC code J01DI01 [1]
PubChem 6918430
Chemical data
Formula C 20H22N8O6S2  
Mol. mass 534.568 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Intravenous

Ceftobiprole (Zeftera/Zevtera) is a next generation (5th generation) cephalosporin antibiotic with activity against methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, Pseudomonas aeruginosa, and Enterococci.[2][3][4] It was discovered by Basilea Pharmaceutica[5] and was developed by Johnson & Johnson Pharmaceutical Research and Development.[6] It has been shown to be statistically non-inferior to the combination of vancomycin and ceftazidime for the treatment of skin and soft tissue infections.

It has been described as a "fifth generation" antibiotic,[7][8] though acceptance for this terminology is not universal.

Contents

Pharmacology

Ceftobiprole inhibits the 2a penicillin-binding protein (pbp) of Methicillin-resistant Staphylococcus aureus and the 2x pbp of Streptococcus pneumoniae[3] as well as the classic PBP-2 of MSSA. Ceftobiprole is resistant to staphylococcal β-lactamase.[5]

Dosing

Ceftobiprole cannot be given by mouth and so is given intravenously. It is not FDA approved to be used in children.[4]

Ceftobiprole has been approved for use in Canada and Switzerland, and is under review by regulatory authorities in the United States, the European Union, Australia, Russia and South Africa.[9] In Nov 2008 the US FDA declined to approve Ceftobiprole citing data integrity concerns with two of the supporting studies.[10]

Synonyms

  • RO0639141-000[5]
  • BAL9141[11]
  • Ceftobiprole medocaril

References

  1. ^ WHO International Working Group for Drug Statistics Methodology (August 27, 2008). "ATC/DDD Classification (FINAL): New ATC 5th level codes". WHO Collaborating Centre for Drug Statistics Methodology. http://www.whocc.no/atcddd/new_atc_ddd.html#ATCDDD_FINAL. Retrieved 2008-09-05.  
  2. ^ Yun HC, Ellis MW, Jorgensen JH (2007). "Activity of ceftobiprole against community-associated methicillin-resistant Staphylococcus aureus isolates recently recovered from US military trainees". Diagnostic Microbiology and Infectious Disease 59: 463. doi:10.1016/j.diagmicrobio.2007.06.023. PMID 17911001.  
  3. ^ a b Widmer A (2008). "Ceftobiprole: A new option for treatment of skin and soft-tissue infections due to methicillin-resistant Staphylococcus aureus". Clin Infect Dis 46: 656–8. doi:10.1086/526528.  
  4. ^ a b Noel GJ, Bush K, Bagchi P, Ianus J, Strauss RS (2008). "A randomized, double-blind trial comparing ceftobiprole medocaril with vancomycin plus ceftazidime plus ceftazidime for the treatment of patients with complicated skin and skin-structure infections". Clin Infect Dis 46: 647–55. doi:10.1086/526527.  
  5. ^ a b c Hebeisen P, Heinze-Krauss I, Angehrn P, et al. (2001). "In vitro and in vivo properties of Ro63-9141, a novel broad-spectrum cephalosporin with activity against methicillin-resistant staphylococci". Antimicrob Agents Chemother 45: 825–36. doi:10.1128/AAC.45.3.825-836.2001.  
  6. ^ Basilea.com
  7. ^ Widmer AF (March 2008). "Ceftobiprole: a new option for treatment of skin and soft-tissue infections due to methicillin-resistant Staphylococcus aureus". Clin. Infect. Dis. 46 (5): 656–8. doi:10.1086/526528. PMID 18225983. http://www.journals.uchicago.edu/doi/abs/10.1086/526528?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub%3dncbi.nlm.nih.gov.  
  8. ^ Kosinski MA, Joseph WS (July 2007). "Update on the treatment of diabetic foot infections". Clin Podiatr Med Surg 24 (3): 383–96, vii. doi:10.1016/j.cpm.2007.03.009. PMID 17613382. http://journals.elsevierhealth.com/retrieve/pii/S0891-8422(07)00026-2.  
  9. ^ Basilea superbug drug approved in Canada, Reuters News, June 30, 2008
  10. ^ http://www.dancewithshadows.com/pillscribe/ceftobiprole-antibiotic-to-fight-tougher-bacterial-infections-fails-to-win-approval-in-us/
  11. ^ Jones RN, Deshpande LM, Mutnick AH, Biedenbach DJ (2002). "In vitro evaluation of BAL9141, a novel parenteral cephalosporin active against oxacillin-resistant staphylococci". J Antimicrob Chemother 50: 915–932. doi:10.1093/jac/dkf249. http://jac.oxfordjournals.org/cgi/content/full/50/6/915?ijkey=44287b37747e341869bed979dc42b8250ff5c6ce.  
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