Cadazolid
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Systematic (IUPAC) name | |
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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 | |
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Identifiers | |
1025097-10-2 | |
None | |
ChemSpider | 30774277 |
Chemical data | |
Formula | C29H29F2N3O8 |
585.55 g/mol | |
SMILES
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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
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.[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
- ↑ 1.0 1.1 1.2 Boschert, Sherry (19 Sep 2012). "Promising C. difficile Antibiotic in Pipeline". Internal Medicine News. International Medical News Group. Retrieved 22 May 2013.
- ↑ 2.0 2.1 "Cadazolid". .actelion.com. Retrieved 2013-05-22.
- ↑ "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.