Tedizolid

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Tedizolid
Tedizolid.svg
Systematic (IUPAC) name
(5R)-3-{3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-1,3-oxazolidin-2-one
Clinical data
Legal status -only (US) Investigational
Routes Oral,IV
Pharmacokinetic data
Bioavailability 80%
Half-life longer then linezolid
Identifiers
CAS number 856866-72-3 N
ATC code None
ChemSpider 9409096 YesY
UNII 97HLQ82NGL YesY
KEGG D09685 YesY
ChEMBL CHEMBL1257051 N
Chemical data
Formula C17H15FN6O3 
Mol. mass 370.338 g/mol
 N (what is this?)  (verify)

Tedizolid (formerly torezolid[1]) is an oxazolidinone drug being developed by Cubist Pharmaceuticals following acquisition of Trius Therapeutics (originator: Dong-A Pharmaceuticals) for complicated skin and skin-structure infections (cSSSI), including those caused by methicillin-resistant Staphylococcus aureus (MRSA).[2]

The prodrug tedizolid is called "TR-701", while the active moiety is called "TR-700".[3][4]

Clinical trials[edit]

As of July 2012, tedizolid had completed one phase III trial, with another one under way. [5] Both trials compare a six-day regimen of tedizolid 200 mg once-daily against a ten-day regimen of linezolid 600 mg twice-daily. The results of the pivotal phase III trial ESTABLISH 1 were published in February 2013. It met the primary and both secondary endpoints.[6]

Tedizolid has been approved by the FDA on June 20, 2014 for the treatment of methicillin-resistant S. aureus skin infections. It can be taken both orally and given via IV injection.[7]

References[edit]

  1. ^ "Trius grows as lead antibiotic moves forward". 31 Oct 2011. 
  2. ^ "Trius Completes Enrollment In Phase 2 Clinical Trial Evaluating Torezolid (TR-701) In Patients With Complicated Skin And Skin Structure Infections". Jan 2009. 
  3. ^ PMID 19528279 In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
  4. ^ PMID 19218276 TR-700 in vitro activity against and resistance mutation frequencies among Gram-positive pathogens.
  5. ^ http://clinicaltrials.gov/ct2/results?flds=Xf&flds=a&flds=b&term=tedizolid&phase=2&fund=2&show_flds=Y
  6. ^ New MRSA treatment
  7. ^ [1]