Drug intelligence / Profile preview

tetrabenazine

Development stage
Approved
Lead developer
Valeant Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Tetrabenazine is a small molecule drug classified as a vesicular monoamine transporter 2 (VMAT2) inhibitor. It is primarily used for the symptomatic treatment of chorea associated with Huntington's disease and has also been used in other hyperkinetic movement disorders such as dystonias and tics[1][3][4][8]. Tetrabenazine works by reversibly inhibiting VMAT2 in presynaptic neurons, leading to decreased uptake of monoamines (dopamine, serotonin, norepinephrine, histamine) into synaptic vesicles and depletion of these neurotransmitters from nerve terminals[4][6][8]. This mechanism reduces involuntary movements but does not address psychiatric or cognitive symptoms of Huntington's disease. The drug was FDA approved on August 15, 2008[4].

Brand names
XenazineNitoman
Other names
TBZtetrabenazinum
02

Targets

DRD2 (Dopamine D2 Receptor)VMAT2 (Vesicular monoamine transporter 2)

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