Rx00232 - Tetrabenazine


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Rx00232
Primary Indication
Secondary Indication

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Disease prevalence from Electronic Health Records

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Disease A Disease B A∩B A∩¬B B∩¬A Odds-Ratio P-Value Adjusted P-Value
senile chorea chorea 182 182 182 22169.912 0 0.0
hemiballismus chorea 182 182 182 22169.912 0 0.0
tardive dyskinesia severe tardive dyskinesia 292 292 292 13818.233 0 0.0
Tourette syndrome juvenile Tourette's Syndrome 477 477 477 8458.96 0 0.0
Huntington's disease chorea 19 144 182 2925.197 2.18E-58 6.99e-55
chorea Huntington's disease 19 182 144 2925.197 2.18E-58 6.99e-55

Chemical, Pharmacological and Biological Annotations


ATC Code:
N07XX06
Brand:
Rubigen
Category:
Adrenergic Uptake Inhibitors
ChEBI ID:
9467
PubChem ID:
6018
KEGG Drug ID:
D08575
SMILE:
COC1=C(OC)C=C2C3CC(=O)C(CC(C)C)CN3CCC2=C1
InChI:
1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3
Classification:
Kingdom:
Organic Compounds
Superclass:
Heterocyclic Compounds
Class:
Isoquinolines and Derivatives
Subclass:
Indication:
Treatment of hyperkinetic movement disorders like chorea in Huntington's disease, hemiballismus, senile chorea, Tourette syndrome and other tic disorders, and tardive dyskinesia
Pharmacodynamics:
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...
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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...
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Mechanism:
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. ...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
+
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Inhibitor
P-glycoprotein inhibitor II:
Inhibitor
Renal organic cation transporter:
Inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Inhibitor
CYP450 2C19 substrate:
Non-inhibitor
CYP450 inhibitory promiscuity:
Low CYP Inhibitory Promiscuity
Ames test:
Non AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
2.8540 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Inhibitor

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Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
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Manhattan, New York City, NY
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