U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry RACEMIC
Molecular Formula C19H27NO3
Molecular Weight 323.4603
Optical Activity ( + / - )
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DEUTETRABENAZINE

SMILES

CC(C)C[C@@]1([H])CN2CCc3cc(c(cc3[C@]2([H])CC1=O)OC([H])([H])[H])OC([H])([H])[H]

InChI

InChIKey=MKJIEFSOBYUXJB-WEZHFFAMSA-N
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/t14-,16-/m0/s1/i3D3,4D3

HIDE SMILES / InChI

Molecular Formula C19H27NO3
Molecular Weight 323.4603
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Deutetrabenazine (trade name Austedo) is a vesicular monoamine transporter 2 (VMAT2) inhibitor indicated for the treatment of chorea associated with Huntington’s disease. The drug was developed by Auspex Pharmaceuticals and is being commercialized by Teva Pharmaceuticals. Deutetrabenazine is a deuterated derivative of tetrabenazine. The incorporation of deuterium in place of hydrogen at the sites of primary metabolism results in metabolic clearance being slowed, allowing less frequent dosing and better tolerability.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: Q05940
Gene ID: 6571.0
Gene Symbol: SLC18A2
Target Organism: Homo sapiens (Human)
3.8 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
AUSTEDO

Approved Use

Austedo® is indicated for the treatment of chorea associated with Huntington’s disease

Launch Date

1.49109119E12
Primary
AUSTEDO

Approved Use

Austedo® is indicated for the treatment of ​tardive dyskinesia in adults

Launch Date

1.49109119E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.3 ng/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DEUTETRABENAZINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
0.26 ng × h/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DEUTETRABENAZINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Disc. AE: Suicidal ideation, Sudden cardiac death...
AEs leading to
discontinuation/dose reduction:
Suicidal ideation
Sudden cardiac death
Sources: Page: 209885Orig1s000MedR.pdf - p.116
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Disc. AE: Insomnia, Cardio-respiratory arrest...
AEs leading to
discontinuation/dose reduction:
Insomnia
Cardio-respiratory arrest
Psychomotor hyperactivity
Sources: Page: 209885Orig1s000MedR.pdf - p.116
6 mg 2 times / day multiple, oral
Recommended
Dose: 6 mg, 2 times / day
Route: oral
Route: multiple
Dose: 6 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Disc. AE: QT prolonged, Vesicular rash...
AEs leading to
discontinuation/dose reduction:
QT prolonged
Vesicular rash
Psychotic disorder
Schizophrenia exacerbated
Sources: Page: 209885Orig1s000MedR.pdf - p.116
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, 25 to 75 years
n = 58
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 25 to 75 years
Population Size: 58
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Disc. AE: Confusional state...
AEs leading to
discontinuation/dose reduction:
Confusional state
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.33
unhealthy, 32 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 32 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.33
Disc. AE: Mental status changes...
AEs leading to
discontinuation/dose reduction:
Mental status changes (grade 3, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.33
21 mg 2 times / day multiple, oral
Dose: 21 mg, 2 times / day
Route: oral
Route: multiple
Dose: 21 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.34
unhealthy, 44 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 44 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.34
Disc. AE: Depression...
AEs leading to
discontinuation/dose reduction:
Depression (grade 1, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.34
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.22
unhealthy, 49 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 49 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.22
Disc. AE: Hypersomnia...
AEs leading to
discontinuation/dose reduction:
Hypersomnia (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.22
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.35
unhealthy, 49 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 49 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.35
Disc. AE: Depression...
AEs leading to
discontinuation/dose reduction:
Depression (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.35
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.25
unhealthy, 51 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 51 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.25
Disc. AE: Communication disorder...
AEs leading to
discontinuation/dose reduction:
Communication disorder (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.25
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.32
unhealthy, 53 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 53 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.32
Disc. AE: Major depression...
AEs leading to
discontinuation/dose reduction:
Major depression (grade 3, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.32
24 mg 2 times / day multiple, oral
Dose: 24 mg, 2 times / day
Route: oral
Route: multiple
Dose: 24 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.29
unhealthy, 53 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 53 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.29
Disc. AE: Suicidal ideation...
AEs leading to
discontinuation/dose reduction:
Suicidal ideation (grade 1, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.29
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.26
unhealthy, 54 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 54 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.26
Disc. AE: Cognitive disorder...
AEs leading to
discontinuation/dose reduction:
Cognitive disorder (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.26
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.22
unhealthy, 56 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 56 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.22
Disc. AE: Dysphagia...
AEs leading to
discontinuation/dose reduction:
Dysphagia (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.22
9 mg 2 times / day multiple, oral
Dose: 9 mg, 2 times / day
Route: oral
Route: multiple
Dose: 9 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.24
unhealthy, 56 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 56 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.24
Disc. AE: Sudden cardiac death...
AEs leading to
discontinuation/dose reduction:
Sudden cardiac death (grade 3, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.24
21 mg 2 times / day multiple, oral
Dose: 21 mg, 2 times / day
Route: oral
Route: multiple
Dose: 21 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.31
unhealthy, 60 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 60 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.31
Disc. AE: Paranoia...
AEs leading to
discontinuation/dose reduction:
Paranoia (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.31
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.27
unhealthy, 60 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 60 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.27
Disc. AE: Chorea...
AEs leading to
discontinuation/dose reduction:
Chorea (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.27
15 mg 2 times / day multiple, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.28
unhealthy, 61 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 61 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.28
Disc. AE: Chorea...
AEs leading to
discontinuation/dose reduction:
Chorea (grade 3, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.28
21 mg 2 times / day multiple, oral
Dose: 21 mg, 2 times / day
Route: oral
Route: multiple
Dose: 21 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.30
unhealthy, 62 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 62 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.30
Disc. AE: Anxiety...
AEs leading to
discontinuation/dose reduction:
Anxiety (grade 2, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.30
36 mg 2 times / day multiple, oral
Highest studied dose
Dose: 36 mg, 2 times / day
Route: oral
Route: multiple
Dose: 36 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.36
unhealthy, 71 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 71 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.36
Disc. AE: Failure to thrive...
AEs leading to
discontinuation/dose reduction:
Failure to thrive (grade 3, 0.8%)
Sources: Page: 208082Orig1s000MedR.pdf - p.36
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Disc. AE: Somnolence, Disturbance in attention...
AEs leading to
discontinuation/dose reduction:
Somnolence (0.3%)
Disturbance in attention (0.3%)
Anxiety (0.7%)
Insomnia (0.3%)
Depression (0.7%)
Suicide attempt (0.3%)
Homicidal ideation (0.3%)
Fatigue (0.3%)
Asthenia (0.3%)
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
AEs

AEs

AESignificanceDosePopulation
Sudden cardiac death Disc. AE
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Suicidal ideation Disc. AE
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Cardio-respiratory arrest Disc. AE
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Insomnia Disc. AE
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Psychomotor hyperactivity Disc. AE
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Psychotic disorder Disc. AE
6 mg 2 times / day multiple, oral
Recommended
Dose: 6 mg, 2 times / day
Route: oral
Route: multiple
Dose: 6 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
QT prolonged Disc. AE
6 mg 2 times / day multiple, oral
Recommended
Dose: 6 mg, 2 times / day
Route: oral
Route: multiple
Dose: 6 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Schizophrenia exacerbated Disc. AE
6 mg 2 times / day multiple, oral
Recommended
Dose: 6 mg, 2 times / day
Route: oral
Route: multiple
Dose: 6 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Vesicular rash Disc. AE
6 mg 2 times / day multiple, oral
Recommended
Dose: 6 mg, 2 times / day
Route: oral
Route: multiple
Dose: 6 mg, 2 times / day
Sources: Page: 209885Orig1s000MedR.pdf - p.116
unhealthy, 18 to 75 years
n = 298
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 18 to 75 years
Sex: M+F
Population Size: 298
Sources: Page: 209885Orig1s000MedR.pdf - p.116
Confusional state Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, 25 to 75 years
n = 58
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 25 to 75 years
Population Size: 58
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Mental status changes grade 3, 0.8%
Disc. AE
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.33
unhealthy, 32 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 32 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.33
Depression grade 1, 0.8%
Disc. AE
21 mg 2 times / day multiple, oral
Dose: 21 mg, 2 times / day
Route: oral
Route: multiple
Dose: 21 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.34
unhealthy, 44 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 44 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.34
Hypersomnia grade 2, 0.8%
Disc. AE
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.22
unhealthy, 49 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 49 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.22
Depression grade 2, 0.8%
Disc. AE
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.35
unhealthy, 49 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 49 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.35
Communication disorder grade 2, 0.8%
Disc. AE
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.25
unhealthy, 51 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 51 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.25
Major depression grade 3, 0.8%
Disc. AE
18 mg 2 times / day multiple, oral
Recommended
Dose: 18 mg, 2 times / day
Route: oral
Route: multiple
Dose: 18 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.32
unhealthy, 53 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 53 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.32
Suicidal ideation grade 1, 0.8%
Disc. AE
24 mg 2 times / day multiple, oral
Dose: 24 mg, 2 times / day
Route: oral
Route: multiple
Dose: 24 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.29
unhealthy, 53 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 53 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.29
Cognitive disorder grade 2, 0.8%
Disc. AE
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.26
unhealthy, 54 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 54 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.26
Dysphagia grade 2, 0.8%
Disc. AE
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.22
unhealthy, 56 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 56 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.22
Sudden cardiac death grade 3, 0.8%
Disc. AE
9 mg 2 times / day multiple, oral
Dose: 9 mg, 2 times / day
Route: oral
Route: multiple
Dose: 9 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.24
unhealthy, 56 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 56 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.24
Paranoia grade 2, 0.8%
Disc. AE
21 mg 2 times / day multiple, oral
Dose: 21 mg, 2 times / day
Route: oral
Route: multiple
Dose: 21 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.31
unhealthy, 60 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 60 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.31
Chorea grade 2, 0.8%
Disc. AE
27 mg 2 times / day multiple, oral
Dose: 27 mg, 2 times / day
Route: oral
Route: multiple
Dose: 27 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.27
unhealthy, 60 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 60 years
Sex: F
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.27
Chorea grade 3, 0.8%
Disc. AE
15 mg 2 times / day multiple, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.28
unhealthy, 61 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 61 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.28
Anxiety grade 2, 0.8%
Disc. AE
21 mg 2 times / day multiple, oral
Dose: 21 mg, 2 times / day
Route: oral
Route: multiple
Dose: 21 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.30
unhealthy, 62 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 62 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.30
Failure to thrive grade 3, 0.8%
Disc. AE
36 mg 2 times / day multiple, oral
Highest studied dose
Dose: 36 mg, 2 times / day
Route: oral
Route: multiple
Dose: 36 mg, 2 times / day
Sources: Page: 208082Orig1s000MedR.pdf - p.36
unhealthy, 71 years
n = 119
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: 71 years
Sex: M
Population Size: 119
Sources: Page: 208082Orig1s000MedR.pdf - p.36
Asthenia 0.3%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Disturbance in attention 0.3%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Fatigue 0.3%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Homicidal ideation 0.3%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Insomnia 0.3%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Somnolence 0.3%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Suicide attempt 0.3%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Anxiety 0.7%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Depression 0.7%
Disc. AE
15 mg 2 times / day multiple, oral (mean)
Recommended
Dose: 15 mg, 2 times / day
Route: oral
Route: multiple
Dose: 15 mg, 2 times / day
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
unhealthy, mean age 5.59 years
n = 202
Health Status: unhealthy
Condition: Tardive dyskinesia
Age Group: mean age 5.59 years
Sex: M+F
Population Size: 202
Sources: Page: 209885Orig1s000OtherR.pdf - p.28 | 209885Orig1s000SumR.pdf - p.5
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
weak [Inhibition 20 uM]
weak [Inhibition 20 uM]
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: An in vivo drug-drug interaction (DDI) study conducted with SD-809, showed a 3-fold increase in total (α+β)-HTBZ exposures when a strong CYP2D6 inhibitor (paroxetine) was co-administered with SD-809.
Page: 4.0
no
no
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes
PubMed

PubMed

TitleDatePubMed
Breakthrough drugs for the interface between psychiatry and neurology.
2016 Apr
Patents

Patents

Sample Use Guides

In Vivo Use Guide
​The dose of Austedo is determined individually for each patient based on the reduction of chorea or tardive dyskinesia and tolerability. When first prescribed to patients who are not being switched from tetrabenazine (a related VMAT2 inhibitor), the recommended starting dose of Austedo is 6 mg administered orally once daily for patients with Huntington’s disease and 12 mg per day (6 mg twice daily) for patients with tardive dyskinesia.
Route of Administration: Oral
The in vitro binding affinity for the active metabolites of tetrabenazine (α- and β- dihydrotetrabenazine) and the deuterated versions of these metabolites to the vesicular monoamine transporter 2 (VMAT2) was examined in competitive binding assays. Deuterated α-dihydrotetrabenazine binds to VMAT2 with Ki of 3.8 nM, non-deuterated α-dihydrotetrabenazine binds with Ki of 3.1 nM.
Substance Class Chemical
Created
by admin
on Sat Jun 26 08:08:29 UTC 2021
Edited
by admin
on Sat Jun 26 08:08:29 UTC 2021
Record UNII
P341G6W9NB
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DEUTETRABENAZINE
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
DEUTETRABENAZINE [ORANGE BOOK]
Common Name English
(3RS,11BRS)-9,10-DI((2H3)METHOXY)-3-(2-METHYLPROPYL)-1,3,4,6,7,11B-HEXAHYDRO-2H-BENZO(A)QUINOLIZIN-2-ONE
Systematic Name English
AUSTEDO
Brand Name English
DEUTETRABENAZINE [WHO-DD]
Common Name English
SD-809
Code English
DEUTETRABENAZINE [INN]
Common Name English
DEUTETRABENAZINE [USAN]
Common Name English
2H-BENZO(A)QUINOLIZIN-2-ONE, 1,3,4,6,7,11B-HEXAHYDRO-9,10-DI(METHOXY-D3)-3-(2-METHYLPROPYL)-, (3R,11BR)-REL-
Systematic Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 383212
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
FDA ORPHAN DRUG 442314
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
Code System Code Type Description
FDA UNII
P341G6W9NB
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
NCI_THESAURUS
C174828
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
PUBCHEM
73442840
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
CAS
1392826-25-3
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
DRUG BANK
DB12161
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
WIKIPEDIA
Deutetrabenazine
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
RXCUI
1876905
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
EVMPD
SUB179485
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
DRUG CENTRAL
5226
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
INN
10069
Created by admin on Sat Jun 26 08:08:30 UTC 2021 , Edited by admin on Sat Jun 26 08:08:30 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
MINOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC