Investigational Drug Details
| Drug ID: | D429 |
| Drug Name: | Tetrabenazine |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB04844 |
| DrugBank Description: | A drug formerly used as an antipsychotic but now used primarily in the symptomatic treatment of various hyperkinetic disorders. It is a monoamine depletor and used as symptomatic treatment of chorea associated with Huntington's disease. FDA approved on August 15, 2008. |
| PubChem ID: | 6018 |
| CasNo: | 58-46-8 |
| Repositioning for NAFLD: | Yes |
| SMILES: | COC1=C(OC)C=C2C3CC(=O)C(CC(C)C)CN3CCC2=C1 |
| Structure: |
|
| InChiKey: | MKJIEFSOBYUXJB-UHFFFAOYSA-N |
| Molecular Weight: | 317.4226 |
| DrugBank Targets: | Synaptic vesicular amine transporter; Dopamine D2 receptor |
| DrugBank MoA: | 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). |
| DrugBank Pharmacology: | Prolongation of the QTc interval has been observed at doses of 50 mg. In rats, it has been observed that tetrabenazine or its metabolites bind to melanin-containing tissues such as the eyes and skin. After a single oral dose of radiolabeled tetrabenazine, radioactivity was still detected in eye and fur at 21 days post dosing. |
| DrugBank Indication: | Treatment of hyperkinetic movement disorders like chorea in Huntington's disease, hemiballismus, senile chorea, Tourette syndrome and other tic disorders, and tardive dyskinesia |
| Targets: | |
| Therapeutic Category: | |
| Clinical Trial Progress: | |
| Latest Progress: |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Article ID | PMID | Source | Title |
|---|