radafaxine

Radafaxine is a small molecule investigational drug developed as a norepinephrine–dopamine reuptake inhibitor (NDRI). It is an active metabolite of bupropion and was under development by GlaxoSmithKline in the 2000s for several neuropsychiatric indications including major depressive disorder, fibromyalgia, neuropathic pain, obesity, bipolar disorder, and restless legs syndrome. Radafaxine exhibits higher selectivity for inhibiting norepinephrine reuptake compared to dopamine reuptake—showing about 392% of the efficacy of bupropion in blocking norepinephrine reuptake and about 70% for dopamine. This selectivity may contribute to its effects on pain and fatigue. Clinical development reached up to phase II trials but was discontinued for all investigated indications[4][5][7].

Other names

radafaxine hydrochloride(S,S)-hydroxy bupropion(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethylmorpholin-2-olbupropion metabolite