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Details

Stereochemistry ABSOLUTE
Molecular Formula C15H19NO2
Molecular Weight 245.3169
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TASIMELTEON

SMILES

CCC(=O)NC[C@@H]1C[C@H]1C2=C3CCOC3=CC=C2

InChI

InChIKey=PTOIAAWZLUQTIO-GXFFZTMASA-N
InChI=1S/C15H19NO2/c1-2-15(17)16-9-10-8-13(10)11-4-3-5-14-12(11)6-7-18-14/h3-5,10,13H,2,6-9H2,1H3,(H,16,17)/t10-,13+/m0/s1

HIDE SMILES / InChI

Molecular Formula C15H19NO2
Molecular Weight 245.3169
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=19579175

Tasimelteon, developed by Vanda Pharmaceuticals Inc under license from Bristol-Myers Squibb Co, is a melatonin receptor agonist. Tasimelteon differs structurally from melatonin and drugs with known melatonin agonist activity, in particular by its distinct aromatic group and linker. Tasimelteon bears also no structural relationship to any other approved active substance. Tasimelteon is presumably acts through activation of MT1 and MT2 G-protein coupled receptors, which are involved primarily in inhibition of neuronal firing and phase shift of circadian rhythms. Tasimelteon is approved for the treatment of Non24-Hour Sleep-Wake Disorder.

Originator

Curator's Comment: In May 2013 Vanda Pharmaceuticals submitted a New Drug Application to the Food and Drug Administration for Tasimelteon

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P49286
Gene ID: 4544.0
Gene Symbol: MTNR1B
Target Organism: Homo sapiens (Human)
0.0692 nM [Ki]
Target ID: P48039
Gene ID: 4543.0
Gene Symbol: MTNR1A
Target Organism: Homo sapiens (Human)
0.304 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
HETLIOZ

Approved Use

Indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (Non-24).

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
12 ng/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
394 ng/mL
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
873 ng/mL
150 mg 1 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
173 ng/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
33 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
261 ng/mL
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5 ng/mL
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
51 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
786 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
445 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
17 ng × h/mL
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1823 ng × h/mL
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
3797 ng × h/mL
150 mg 1 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
426 ng × h/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
59 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
611 ng × h/mL
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
8 ng × h/mL
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
96 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2269 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2304 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.49 h
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.78 h
150 mg single, oral
dose: 150 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.63 h
150 mg 1 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.37 h
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1.29 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.57 h
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1.75 h
1 mg single, oral
dose: 1 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1.44 h
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.75 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.06 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TASIMELTEON plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
Doses

Doses

DosePopulationAdverse events​
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Disc. AE: Supraventricular extrasystoles, Tachycardia...
AEs leading to
discontinuation/dose reduction:
Supraventricular extrasystoles (0.07%)
Tachycardia (0.07%)
Constipation (0.07%)
Fatigue (0.07%)
Oedema peripheral (0.07%)
Cholestasis (0.07%)
ALT increased (0.07%)
AST increased (0.07%)
GGT increased (0.07%)
Blood creatine increased (0.07%)
Hyperglycaemia (0.07%)
Headache (0.07%)
Loss of consciousness (0.07%)
Syncope (0.07%)
Transient ischaemic attack (0.07%)
Insomnia (0.14%)
Nightmare (0.14%)
Renal pain (0.07%)
Rash (0.07%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Disc. AE: Supraventricular extrasystoles, Vomiting...
AEs leading to
discontinuation/dose reduction:
Supraventricular extrasystoles (0.7%)
Vomiting (0.7%)
Headache (0.7%)
Syncope (0.7%)
Insomnia (0.7%)
Nightmare (1.3%)
Anger (0.7%)
Depression (0.7%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
1 mg 1 times / day multiple, oral
Studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Disc. AE: Local swelling, Disorientation...
AEs leading to
discontinuation/dose reduction:
Local swelling (0.07%)
Disorientation (0.07%)
Rash (0.07%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
10 mg 1 times / day multiple, oral
Studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Disc. AE: Diarrhoea, Gastritis...
AEs leading to
discontinuation/dose reduction:
Diarrhoea (0.07%)
Gastritis (0.07%)
Dizziness (0.07%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (0.07%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Disc. AE: Rash...
AEs leading to
discontinuation/dose reduction:
Rash (0.07%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Disc. AE: Ventricular arrhythmia, Gastritis...
AEs leading to
discontinuation/dose reduction:
Ventricular arrhythmia (0.9%)
Gastritis (0.9%)
Local swelling (0.9%)
Electrocardiogram ST segment elevation (0.9%)
Ataxia (0.9%)
Dizziness (0.9%)
Confusional state (0.9%)
Disorientation (0.9%)
Rash (0.9%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Disc. AE: Supraventricular extrasystoles, Ventricular arrhythmia...
AEs leading to
discontinuation/dose reduction:
Supraventricular extrasystoles (0.2%)
Ventricular arrhythmia (0.2%)
Diarrhoea (0.2%)
Dyspepsia (0.2%)
Gastritis (0.2%)
Hypoaesthesia oral (0.2%)
Vomiting (0.2%)
Local swelling (0.2%)
Somnolence (0.5%)
Ataxia (0.2%)
Dizziness (0.2%)
Headache (0.2%)
Syncope (0.2%)
Insomnia (0.5%)
Nightmare (0.5%)
Anger (0.2%)
Confusional state (0.2%)
Depression (0.2%)
Disorientation (0.2%)
Rash (0.2%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Disc. AE: Dyspepsia, Blood creatine increased...
AEs leading to
discontinuation/dose reduction:
Dyspepsia (0.07%)
Blood creatine increased (0.07%)
Somnolence (0.07%)
Insomnia (0.07%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 164
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 164
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Disc. AE: Diarrhoea, Dyspepsia...
AEs leading to
discontinuation/dose reduction:
Diarrhoea (0.6%)
Dyspepsia (0.6%)
Hypoaesthesia oral (0.6%)
Blood creatine phosphokinase increased (0.6%)
Somnolence (1.2%)
Insomnia (0.6%)
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
300 mg 1 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.20
healthy, 18-44 years
n = 11
Health Status: healthy
Age Group: 18-44 years
Sex: M+F
Population Size: 11
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.20
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.20
AEs

AEs

AESignificanceDosePopulation
ALT increased 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
AST increased 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Blood creatine increased 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Cholestasis 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Constipation 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Fatigue 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
GGT increased 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Headache 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Hyperglycaemia 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Loss of consciousness 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Oedema peripheral 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Rash 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Renal pain 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Supraventricular extrasystoles 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Syncope 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Tachycardia 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Transient ischaemic attack 0.07%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Insomnia 0.14%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Nightmare 0.14%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Anger 0.7%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Depression 0.7%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Headache 0.7%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Insomnia 0.7%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Supraventricular extrasystoles 0.7%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Syncope 0.7%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Vomiting 0.7%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Nightmare 1.3%
Disc. AE
20 mg 1 times / day multiple, oral
Recommended
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 151
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 151
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Disorientation 0.07%
Disc. AE
1 mg 1 times / day multiple, oral
Studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Local swelling 0.07%
Disc. AE
1 mg 1 times / day multiple, oral
Studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Rash 0.07%
Disc. AE
1 mg 1 times / day multiple, oral
Studied dose
Dose: 1 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Diarrhoea 0.07%
Disc. AE
10 mg 1 times / day multiple, oral
Studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Dizziness 0.07%
Disc. AE
10 mg 1 times / day multiple, oral
Studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Gastritis 0.07%
Disc. AE
10 mg 1 times / day multiple, oral
Studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Vomiting 0.07%
Disc. AE
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Rash 0.07%
Disc. AE
150 mg 1 times / day multiple, oral
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Ataxia 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Confusional state 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Disorientation 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Dizziness 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Electrocardiogram ST segment elevation 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Gastritis 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Local swelling 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Rash 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Ventricular arrhythmia 0.9%
Disc. AE
20 mg 1 times / day multiple, oral (max)
Studied dose
Dose: 20 mg, 1 times / day
Route: oral
Route: multiple
Dose: 20 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 114
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 114
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Anger 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Ataxia 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Confusional state 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Depression 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Diarrhoea 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Disorientation 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Dizziness 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Dyspepsia 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Gastritis 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Headache 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Hypoaesthesia oral 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Local swelling 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Rash 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Supraventricular extrasystoles 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Syncope 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Ventricular arrhythmia 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Vomiting 0.2%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Insomnia 0.5%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Nightmare 0.5%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Somnolence 0.5%
Disc. AE
25 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 25 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 429
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 429
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Blood creatine increased 0.07%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Dyspepsia 0.07%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Insomnia 0.07%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Somnolence 0.07%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
unhealthy, 18 - 92 years
n = 1346
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 1346
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.81
Blood creatine phosphokinase increased 0.6%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 164
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 164
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Diarrhoea 0.6%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 164
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 164
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Dyspepsia 0.6%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 164
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 164
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Hypoaesthesia oral 0.6%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 164
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 164
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Insomnia 0.6%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 164
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 164
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
Somnolence 1.2%
Disc. AE
50 mg 1 times / day multiple, oral
Studied dose
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
unhealthy, 18 - 92 years
n = 164
Health Status: unhealthy
Condition: 24-Hour Sleep-Wake Disorder
Age Group: 18 - 92 years
Sex: M+F
Population Size: 164
Sources: Page: nda/2014/205677Orig1s000MedR.pdf - p.84
OverviewDrug 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
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
no
no
yes
yes (co-administration study)
Comment: Rifampin, a strong CYP3A4 and moderate CYP2C8, CYP2C9/2C19 inducer, decreased the exposure of tasimelteon by approximately 90%.
Page: 8.0
yes
yes (co-administration study)
Comment: Rifampin, a strong CYP3A4 and moderate CYP2C8, CYP2C9/2C19 inducer, decreased the exposure of tasimelteon by approximately 90%.
Page: 8.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: Drug interaction studies with CY1A2 inhibitor, fluvoxamine and CYP3A4 inducer, rifampin resulted in 6.5 fold increase and 90% decrease in tasimelteon exposure respectively.
Page: 5.0
major
yes (co-administration study)
Comment: Drug interaction studies with CY1A2 inhibitor, fluvoxamine and CYP3A4 inducer, rifampin resulted in 6.5 fold increase and 90% decrease in tasimelteon exposure respectively.
Page: 5.0
minor
minor
minor
minor
no
no
no
no
no
no
no
no
no
no
no
no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Tasimelteon, a melatonin agonist for the treatment of insomnia and circadian rhythm sleep disorders.
2009 Jul
Sleep-promoting action of IIK7, a selective MT2 melatonin receptor agonist in the rat.
2009 Jun 26
Jet lag, circadian rhythm sleep disturbances, and depression: the role of melatonin and its analogs.
2010 Nov
Mechanism of action of tasimelteon in non-24 sleep-wake syndrome: treatment for a circadian rhythm disorder in blind patients.
2014 Dec
Tasimelteon: a selective and unique receptor binding profile.
2015 Apr
Tasimelteon for the treatment of non-24-hour sleep-wake disorder.
2015 Jan
Patents

Sample Use Guides

The recommended dosage of HETLIOZ is 20 mg per day taken before bedtime, at the same time every night. Because of individual differences in circadian rhythms, drug effect may not occur for weeks or months. HETLIOZ should be taken without food.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:58:06 GMT 2023
Edited
by admin
on Fri Dec 15 15:58:06 GMT 2023
Record UNII
SHS4PU80D9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TASIMELTEON
DASH   INN   MART.   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
TASIMELTEON [USAN]
Common Name English
HETLIOZ
Brand Name English
Tasimelteon [WHO-DD]
Common Name English
PROPANAMIDE, N-(((1R,2R)-2-(2,3-DIHYDRO-4-BENZOFURANYL)CYCLOPROPYL)METHYL)-
Systematic Name English
BMS-214778
Code English
VEC-162
Code English
BMS-214,778
Code English
HETLIOZ LQ
Brand Name English
N-[[(1R,2R)-2-(2,3-Dihydro-1-benzofuran-4-yl)cyclopropyl]methyl]propanamide
Systematic Name English
TASIMELTEON [VANDF]
Common Name English
TASIMELTEON [MI]
Common Name English
TASIMELTEON [MART.]
Common Name English
TASIMELTEON [ORANGE BOOK]
Common Name English
tasimelteon [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC N05CH03
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
NDF-RT N0000175743
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
FDA ORPHAN DRUG 297409
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
EU-Orphan Drug EU/3/10/841
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
EMA ASSESSMENT REPORTS HETLIOZ (AUTHORIZED: SLEEP DISORDERS, CICARDIAN RHYTHM)
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
NCI_THESAURUS C47795
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
FDA ORPHAN DRUG 301410
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
Code System Code Type Description
USAN
SS-70
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
DAILYMED
SHS4PU80D9
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
FDA UNII
SHS4PU80D9
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
PUBCHEM
10220503
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
CAS
609799-22-6
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
IUPHAR
7393
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
EPA CompTox
DTXSID70209826
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
CHEBI
79042
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
RXCUI
1490468
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY RxNorm
NCI_THESAURUS
C152515
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
SMS_ID
100000157714
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
DRUG CENTRAL
4820
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
MERCK INDEX
m10478
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY Merck Index
INN
8985
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
EVMPD
SUB166225
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
ChEMBL
CHEMBL2103822
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
DRUG BANK
DB09071
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
WIKIPEDIA
TASIMELTEON
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
MESH
C478745
Created by admin on Fri Dec 15 15:58:06 GMT 2023 , Edited by admin on Fri Dec 15 15:58:06 GMT 2023
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
MINOR
EXCRETED UNCHANGED
FECAL
TARGET -> AGONIST
METABOLIC ENZYME -> SUBSTRATE
MAJOR
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TARGET -> AGONIST
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> SUBSTRATE
MINOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC SINGLE- OR MULTIPLE-DOSE ADMINISTRATION

Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC