Cadazolid

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Cadazolid
Cadazolid.svg
Systematic (IUPAC) name
1-Cyclopropyl-6-fluoro-7-[4-({2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]phenoxy}methyl)-4-hydroxypiperidin-1-yl]-4-oxo-1,4-dihydroquinolin-3-carboxylic acid
Clinical data
Legal status
  • Investigational
Identifiers
CAS number 1025097-10-2
ATC code None
ChemSpider 30774277
Chemical data
Formula C29H29F2N3O8 
Mol. mass 585.55 g/mol

Cadazolid is an experimental antibiotic of the oxazolidinone class made by Actelion Pharmaceuticals Ltd. which is effective against Clostridium difficile, a major cause of drug resistant diarrhea in the elderly.[1] Current drug treatments for this infection involve orally delivered antibiotics, principally fidaxomicin, metronidazole and vancomycin; the last two drugs are the principal therapeutic agents in use, but fail in approximately 20 to 45% of the cases. The drug is in Phase III trials.[1] The drug works by inhibiting synthesis of proteins in the bacteria, thus inhibiting the production of toxins and the formation of spores.[2]

Structure[edit]

The chemical structure of cadazolid combines the pharmacophores of oxazolidinone and fluoroquinolone.[2]

Clinical trials[edit]

In a study published in the journal Anaerobe, cadazolid has been shown to be effective in vitro against 133 strains of Clostridium difficile all collected from Sweden.[3]

In phase I tests, sixty four male patients reacted favourably to cadazolid which primarily acted and remained in the colon while displaying little toxicity even in regimes involving large doses.[1]

References[edit]

  1. ^ a b c Boschert, Sherry (19 Sep 2012). "Promising C. difficile Antibiotic in Pipeline". Internal Medicine News. International Medical News Group. Retrieved 22 May 2013. 
  2. ^ a b "Cadazolid". .actelion.com. Retrieved 2013-05-22. 
  3. ^ "Anaerobe - In vitro activity of cadazolid against Clostridium difficile strains isolated from primary and recurrent infections in Stockholm, Sweden". ScienceDirect.com. 2013-02-26. Retrieved 2013-05-22.