Tetrabenazine is a vesicular monoamine transporter 2 (VMAT) inhibitor used for the management of chorea associated with Huntington's Disease. A drug formerly used as an antipsychotic but now used primarily in the symptomatic treatment of various hyperkinetic disorders.
- Mechanism
- Curator reviewed
Tetrabenazine is a reversible human vesicular monoamine transporter type 2 inhibitor (Ki = 100 nM). It acts within the basal ganglia and promotes depletion of monoamine neurotransmitters serotonin, norepinephrine, and dopamine from stores. It also decreases uptake into synaptic vesicles. Dopamine is required for fine motor movement, so the inhibition of its transmission is efficacious for hyperkinetic movement. Tetrabenazine exhibits weak in vitro binding affinity at the dopamine D2 receptor (Ki = 2100 nM).
- Primary indication
- Treatment of hyperkinetic movement disorders like chorea in Huntington's disease, hemiballismus, senile chorea, Tourette syndrome and other tic disorders, and tardive dyskinesiaCurator reviewed · 5 structured indications
- Formula / weight
- C19H27NO3 · 317.4226 g/mol (avg)
- First approval
- Canada, 2013 · United States, 2008
- Code names
- RO 1-9569
- Brand names
Resolves to
MKJIEFSOBYUXJB-UHFFFAOYSA-NSMILESCOC1=C(OC)C=C2C3CC(=O)C(CC(C)C)CN3CCC2=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Tetrabenazine, and which of those have an active Phase 3 trial?
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