Cadazolid

Cadazolid
Clinical data
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
ChemSpider
UNII
Chemical and physical data
Formula C29H29F2N3O8
Molar mass 585.55 g/mol
3D model (JSmol)

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] In its financial results for Q1 2018, Idorsia mentions that Actelion informed them that "following completion of Phase 3 data analysis of cadazolid - it has decided to discontinue the development of the compound." [3]

Structure

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

Clinical trials

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.[4]

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

  1. 1 2 3 Boschert, Sherry (19 September 2012). "Promising C. difficile Antibiotic in Pipeline". Internal Medicine News. International Medical News Group. Retrieved 22 May 2013.
  2. 1 2 "Cadazolid". .actelion.com. Retrieved 2013-05-22.
  3. ↑ "Idorsia announces financial results for the first quarter 2018". Idorsia. April 19, 2018.
  4. ↑ "Anaerobe - In vitro activity of cadazolid against Clostridium difficile strains isolated from primary and recurrent infections in Stockholm, Sweden". Anaerobe. 20: 32–35. 2013-02-26. doi:10.1016/j.anaerobe.2013.02.003. Retrieved 2013-05-22.


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