Radafaxine

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Radafaxine
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Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
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Chemical and physical data
FormulaC13H18ClNO2
Molar mass255.74 g/mol

Radafaxine is drug candidate designated 353162[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]

Chemistry

It is a potent metabolite of bupropion, the compound in GlaxoSmithKline's Wellbutrin. More specifically, "hydroxybupropion" is a hydroxy derivative of bupropion, and radafaxine is an isolated isomer of hydroxybupropion.[4]

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

Effects

Presently in various clinical trials, radafaxine is being 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 slightly higher effect on dopamine reuptake), radafaxine seems to have a higher potency on norepinephrine. This, according to GlaxoSmithKline, may account for the increased effect of radafaxine on pain and fatigue.[6]

At least one study suggests that radafaxine has a low abuse potential similar to bupropion.[7]

References



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