Drug intelligence / Profile preview

brasofensine

Development stage
Preclinical
Lead developer
NeuroSearch
Modality
Small Molecules
Administration
Oral
01

Overview

Brasofensine is a phenyltropane-derived small molecule that acts as a potent dopamine reuptake inhibitor. It was developed primarily for the treatment of Parkinson's disease and investigated for other indications such as depression and drug dependence. The drug works by inhibiting the synaptic dopamine transporter (DAT), thereby preventing the reuptake of dopamine into presynaptic neurons and prolonging dopaminergic signaling in the brain[1][2][4]. Brasofensine also exhibits some activity on serotonin and noradrenaline transporters[5]. Clinical trials demonstrated that it was well tolerated at doses up to 4 mg daily; however, its development was discontinued due to issues with in vivo isomerization of its oxime group[3][4].

Other names
brasofensine(E)-1R,2R,3S-3-(3,4-dichlorophenyl)-8-methyl-8-azabicyclo(3.2.1)octane-2-carbaldehyde O-methyloxime
02

Targets

NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)SERT (Sodium-dependent serotonin transporter)

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