Brasofensine

Brasofensine (NS-2214, BMS-204756) is a phenyltropane dopamine reuptake inhibitor that had been under development by Bristol-Myers Squibb and defunct company NeuroSearch for the treatment of Parkinson's and Alzheimer's diseases.

[1] From 1996 to 1999, Bristol-Myers Squibb (BMS) was involved in development and testing before exiting the collaboration with NeuroSearch.

[2] In animal models of Parkinson's disease, brasofensine was effective in stimulating locomotor activity and reversing akinesia.

[3] Phase II trials in humans were conducted in 1996 and brasofensine was shown to be both effective and well tolerated at a dose of 4 mg;[4] however, development was stopped after in vivo cis-anti isomerization of the 2α-methyloxime group was reported.

[5] In Parkison's disease, symptoms do not begin to manifest until there has been an 80% reduction in dopaminergic neurons, particularly in the substantia nigra brain region.