Open Access Articles- Top Results for Radafaxine


Systematic (IUPAC) name
Clinical data
106083-71-0 7pxN
PubChem CID 9795056
ChemSpider 7970823 7pxY
UNII Q47741214K 7pxY
ChEMBL CHEMBL1172928 7pxY
Chemical data
Formula C13H18ClNO2
292.20 g/mol
 14pxN (what is this?)  (verify)

Radafaxine is drug candidate designated GW-353,162[1] by GlaxoSmithKline, investigated for treatment of restless leg syndrome and as an NDRI antidepressant. GlaxoSmithKline was targeting Radafaxine for regulatory filing in 2007,[2] but development was discontinued in 2006 due to "poor test results".[3]


It is a potent metabolite of bupropion, the compound in GlaxoSmithKline's Wellbutrin. More specifically, "hydroxybupropion" is an analogue of bupropion, and radafaxine is an isolated isomer ((2S,3S)-) of hydroxybupropion.[4]

Therefore, radafaxine builds on at least some of the properties of bupropion in humans.[5]


In various clinical trials, radafaxine has been studied as a treatment for clinical depression, obesity, and neuropathic pain. Radafaxine is described as a norepinephrine-dopamine reuptake inhibitor (NDRI).

Unlike bupropion (which has a much higher effect on dopamine reuptake), radafaxine seems to have a higher potency on norepinephrine. Radafaxine has about 70% of bupropion's efficacy in blocking dopamine reuptake, and 392% of efficacy in blocking norepinephrine reuptake, making it fairly selective for inhibiting the reuptake of norepinephrine over dopamine.[6][7] This, according to GlaxoSmithKline, may account for the increased effect of radafaxine on pain and fatigue.[8]

At least one study suggests that radafaxine has a low abuse potential similar to bupropion.[9]

See also


  1. ^ Restless Legs Syndrome: First Approval
  2. ^ {1} Reviews Novel Therapeutics For CNS Disorders And Confirms Strong Pipeline Momentum - News, Search Jobs, Events
  3. ^ GSK breakthrough on bird flu vaccine.
  4. ^ radafaxine at the US National Library of Medicine Medical Subject Headings (MeSH)
  5. ^ GlaxoSmithKline Reviews Novel Therapeutics for CNS Disorders and Confirms Strong Pipeline Momentum
  6. ^ Xu, H; Loboz, KK; Gross, AS; McLachlan, AJ (2007). "Stereoselective analysis of hydroxybupropion and application to drug interaction studies". Chirality 19 (3): 163–70. PMID 17167747. doi:10.1002/chir.20356. 
  7. ^ Bondarev, ML; Bondareva, TS; Young, R; Glennon, RA (2003). "Behavioral and biochemical investigations of bupropion metabolites". Eur J Pharmacol 474 (1): 85–93. PMID 12909199. doi:10.1016/S0014-2999(03)02010-7. 
  8. ^ Microsoft PowerPoint - slides_05_burch.ppt
  9. ^ Radafaxine

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