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Deutetrabenazine

Generic Name
Deutetrabenazine
Brand Names
Austedo
Drug Type
Small Molecule
Chemical Formula
C19H27NO3
CAS Number
1392826-25-3
Unique Ingredient Identifier
P341G6W9NB

Overview

Deutetrabenazine is a novel, highly selective vesicular monoamine transporter 2 (VMAT2) inhibitor indicated for the management of chorea associated with Huntington’s disease. It is a hexahydro-dimethoxybenzoquinolizine derivative and a deuterated Tetrabenazine . The presence of deuterium in deutetrabenazine increases the half-lives of the active metabolite and prolongs their pharmacological activity by attenuating CYP2D6 metabolism of the compound . This allows less frequent dosing and a lower daily dose with improvement in tolerability . Decreased plasma fluctuations of deutetrabenazine due to attenuated metabolism may explain a lower incidence of adverse reactions associated with deutetrabenazine . Deutetrabenazine is a racemic mixture containing RR-Deutetrabenazine and SS-Deutetrabenazine . Huntington's disease (HD) is a hereditary, progressive neurodegenerative disorder characterized by motor dysfunction, cognitive decline, and neuropsychiatric disturbances that interfere with daily functioning and significantly reduce the quality of life. The most prominent physical symptom of HD that may increase the risk of injury is chorea, which is an involuntary, sudden movement that can affect any muscle and flow randomly across body regions . Psychomotor symptoms of HD, such as chorea, are related to hyperactive dopaminergic neurotransmission . Deutetrabenazine depletes the levels of presynaptic dopamine by blocking VMAT2, which is responsible for the uptake of dopamine into synaptic vesicles in monoaminergic neurons and exocytotic release . As with other agents for the treatment of neurodegenerative diseases, deutetrabenazine is a drug to alleviate the motor symptoms of HD and is not proposed to halt the progression of the disease . In clinical trials of patients with HD, 12 weeks of treatment of deutetrabenazine resulted in overall improvement in mean total maximal chorea scores and motor signs than placebo . It was approved by FDA in April 2017 and is marketed under the trade name Austedo as oral tablets.

Indication

Deutetrabenazine is indicated in adults patients for the treatment of tardive dyskinesia and for chorea associated with Huntington's disease.

Associated Conditions

  • Chorea
  • Tardive Dyskinesia (TD)

Research Report

Published: Sep 7, 2025

Deutetrabenazine (Austedo®): A Comprehensive Pharmacological and Clinical Monograph

Executive Summary

Deutetrabenazine is a highly selective, reversible inhibitor of the vesicular monoamine transporter 2 (VMAT2) indicated for the management of hyperkinetic movement disorders, specifically chorea associated with Huntington's disease and tardive dyskinesia in adults. Marketed under the brand names Austedo® and Austedo XR®, its development marks a significant milestone in medicinal chemistry as the first deuterated drug to receive approval from the U.S. Food and Drug Administration (FDA). Its mechanism of action, shared with its non-deuterated predecessor tetrabenazine, involves the depletion of presynaptic monoamines such as dopamine, thereby reducing the excessive dopaminergic signaling implicated in these conditions.

The core innovation of deutetrabenazine lies in the strategic replacement of specific hydrogen atoms with deuterium, a stable isotope of hydrogen. This molecular modification leverages the kinetic isotope effect to create a stronger carbon-deuterium bond, which attenuates the rate of metabolism by the cytochrome P450 2D6 (CYP2D6) enzyme system. This rational design confers a superior pharmacokinetic profile characterized by a longer half-life of its active metabolites, more stable plasma concentrations, and reduced peak-to-trough variability.

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2021/01/19
Phase 2
Recruiting
2020/03/10
Phase 1
Terminated
2019/12/16
Phase 3
Terminated
2019/11/21
Phase 1
Active, not recruiting
2019/08/28
Phase 1
Recruiting
Second Affiliated Hospital, School of Medicine, Zhejiang University
2019/01/23
Phase 3
Completed
2018/06/27
Phase 3
Completed
2018/06/25
Phase 3
Terminated
2018/03/02
Phase 2
Completed
2016/02/04
Phase 1
Completed

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Teva Neuroscience, Inc.
68546-471
ORAL
12 mg in 1 1
10/9/2023
Teva Neuroscience, Inc.
68546-171
ORAL
9 mg in 1 1
10/9/2023
Teva Neuroscience, Inc.
68546-470
ORAL
6 mg in 1 1
10/9/2023
Teva Neuroscience, Inc.
68546-172
ORAL
12 mg in 1 1
10/9/2023
Teva Neuroscience, Inc.
68546-472
ORAL
24 mg in 1 1
10/9/2023
Teva Neuroscience, Inc.
68546-170
ORAL
6 mg in 1 1
10/9/2023

EMA Drug Approvals

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No EMA approvals found for this drug.

HSA Drug Approvals

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No HSA approvals found for this drug.

NMPA Drug Approvals

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No NMPA approvals found for this drug.

PPB Drug Approvals

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No PPB approvals found for this drug.

Health Canada Drug Approvals

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No Health Canada approvals found for this drug.

CIMA AEMPS Drug Approvals

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No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

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No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

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No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

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No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

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Authorization Date
No UK EMC drug information found for this drug.

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