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

Details

Stereochemistry ABSOLUTE
Molecular Formula C10H14N2O2
Molecular Weight 194.2307
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SOLRIAMFETOL

SMILES

c1ccc(cc1)C[C@]([H])(COC(=N)O)N

InChI

InChIKey=UCTRAOBQFUDCSR-SECBINFHSA-N
InChI=1S/C10H14N2O2/c11-9(7-14-10(12)13)6-8-4-2-1-3-5-8/h1-5,9H,6-7,11H2,(H2,12,13)/t9-/m1/s1

HIDE SMILES / InChI

Molecular Formula C10H14N2O2
Molecular Weight 194.2307
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

ADX-N05, originally discovered by SK Holdings, is a selective dopamine and norepinephrine reuptake inhibitor (DNRI). ADX-N05 (Solriamfetol, sold under the brand name Sunosi) is approved in the US and is under regulatory review in the EU to improve wakefulness in adult patients with hypersomnia associated with narcolepsy or obstructive sleep apnoea.The US FDA has approved solriamfetol (Sunosi, Jazz Pharmaceuticals) for the treatment of excessive daytime sleepiness in adults with narcolepsy or obstructive sleep apnea.The dual-acting dopamine and norepinephrine reuptake inhibitor is approved for narcolepsy in once-daily 75 mg and 150 mg doses, and in obstructive sleep apnea in once-daily 37.5 mg, 75 mg, and 150 mg doses.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
2.9 µM [IC50]
4.4 µM [IC50]
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
499 ng/mL
75 mg single, oral
dose: 75 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLRIAMFETOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
5273 ng × h/mL
75 mg single, oral
dose: 75 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLRIAMFETOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.6 h
75 mg single, oral
dose: 75 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLRIAMFETOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Other AEs: Decreased appetite, Insomnia...
Other AEs:
Decreased appetite (9%)
Insomnia (5%)
Anxiety (6%)
Headache (16%)
Palpitations (2%)
Nausea (7%)
Dry mouth (4%)
Constipation (3%)
Agitation (<2%)
Bruxism (<2%)
Irritability (<2%)
Cough (<2%)
Hyperhidrosis (<2%)
Feeling jittery (<2%)
Thirst (<2%)
Chest discomfort (<2%)
Chest pain (<2%)
Weight decreased (<2%)
Sources:
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Disc. AE: Anxiety, Palpitations...
Other AEs: Headache, Nausea...
AEs leading to
discontinuation/dose reduction:
Anxiety (0.5%)
Palpitations (0.5%)
Restlessness (0.5%)
Other AEs:
Headache (13%)
Nausea (9%)
Decreased appetite (8%)
Anxiety (7%)
Dry mouth (4%)
Diarrhea (5%)
Sources:
37.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 37.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 37.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 58
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 58
Sources:
Other AEs: Headache, Nausea...
Other AEs:
Headache (7%)
Nausea (7%)
Decreased appetite (2%)
Anxiety (2%)
Dry mouth (2%)
Diarrhea (2%)
Sources:
75 mg 1 times / day steady, oral (mean)
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 120
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 120
Sources:
Other AEs: Headache, Nausea...
Other AEs:
Headache (9%)
Nausea (5%)
Decreased appetite (7%)
Anxiety (3%)
Dry mouth (3%)
Diarrhea (4%)
Sources:
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Other AEs: Decreased appetite, Anxiety...
Other AEs:
Decreased appetite (6%)
Anxiety (4%)
Irritability (3%)
Dizziness (2%)
Palpitations (3%)
Nausea (8%)
Diarrhea (4%)
Abdominal pain (3%)
Dry mouth (3%)
Feeling jittery (3%)
Chest discomfort (2%)
Hyperhidrosis (2%)
Bruxism (<2%)
Restlessness (<2%)
Disturbance in attention (<2%)
Tremor (<2%)
Cough (<2%)
Dyspnea (<2%)
Constipation (<2%)
Vomiting (<2%)
Weight decreased (<2%)
Sources:
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 396
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 396
Sources:
Other AEs: Blood pressure systolic increased, Blood pressure diastolic increased...
Other AEs:
Blood pressure systolic increased
Blood pressure diastolic increased
Heart rate increased
Sources:
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Other AEs: Insomnia, Headache...
Other AEs:
Insomnia (grade 1, 21.9%)
Headache (grade 1, 15.6%)
Hypervigilance (grade 1, 9.4%)
Decreased appetite (grade 1, 9.4%)
Nausea (grade 1, 9.4%)
Insomnia (grade 1, 21.9%)
Headache (grade 1, 12.5%)
Hypervigilance (grade 1, 12.5%)
Decreased appetite (grade 1, 9.4%)
Nausea (grade 1, 6.3%)
Sources:
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Disc. AE: Blood pressure increased, Nervousness...
Other AEs: Hypervigilance, Elevated mood...
AEs leading to
discontinuation/dose reduction:
Blood pressure increased (grade 1, 2.4%)
Nervousness (grade 1, 2.4%)
Other AEs:
Hypervigilance (42.9%)
Elevated mood (23.8%)
Dry mouth (21.4%)
Nausea (21.4%)
Feeling of relaxation (19%)
Decreased appetite (19%)
Hyperhidrosis (19%)
Insomnia (16.7%)
Headache (14.3%)
Restlessness (14.3%)
Palpitations (11.9%)
Paresthesia (7.1%)
Sources:
150 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy
n = 417
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Sex: M+F
Population Size: 417
Sources:
Disc. AE: Blood pressure increased, Hypertension...
AEs leading to
discontinuation/dose reduction:
Blood pressure increased (0.48%)
Hypertension (0.24%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Headache 16%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Palpitations 2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Constipation 3%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Dry mouth 4%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Insomnia 5%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Anxiety 6%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Nausea 7%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Decreased appetite 9%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Agitation <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Bruxism <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Chest discomfort <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Chest pain <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Cough <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Feeling jittery <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Hyperhidrosis <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Irritability <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Thirst <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Weight decreased <2%
112.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 112.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 112.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 161
Health Status: unhealthy
Condition: narcolepsy
Age Group: 18 to 75 years
Sex: M+F
Population Size: 161
Sources:
Anxiety 0.5%
Disc. AE
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Palpitations 0.5%
Disc. AE
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Restlessness 0.5%
Disc. AE
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Headache 13%
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Dry mouth 4%
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Diarrhea 5%
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Anxiety 7%
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Decreased appetite 8%
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Nausea 9%
150 mg 1 times / day steady, oral (mean)
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 218
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 218
Sources:
Anxiety 2%
37.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 37.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 37.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 58
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 58
Sources:
Decreased appetite 2%
37.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 37.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 37.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 58
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 58
Sources:
Diarrhea 2%
37.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 37.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 37.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 58
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 58
Sources:
Dry mouth 2%
37.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 37.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 37.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 58
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 58
Sources:
Headache 7%
37.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 37.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 37.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 58
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 58
Sources:
Nausea 7%
37.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 37.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 37.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 58
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 58
Sources:
Anxiety 3%
75 mg 1 times / day steady, oral (mean)
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 120
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 120
Sources:
Dry mouth 3%
75 mg 1 times / day steady, oral (mean)
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 120
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 120
Sources:
Diarrhea 4%
75 mg 1 times / day steady, oral (mean)
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 120
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 120
Sources:
Nausea 5%
75 mg 1 times / day steady, oral (mean)
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 120
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 120
Sources:
Decreased appetite 7%
75 mg 1 times / day steady, oral (mean)
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 120
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 120
Sources:
Headache 9%
75 mg 1 times / day steady, oral (mean)
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: steady
Dose: 75 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 120
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 120
Sources:
Chest discomfort 2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Dizziness 2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Hyperhidrosis 2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Abdominal pain 3%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Dry mouth 3%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Feeling jittery 3%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Irritability 3%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Palpitations 3%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Anxiety 4%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Diarrhea 4%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Decreased appetite 6%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Nausea 8%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Bruxism <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Constipation <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Cough <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Disturbance in attention <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Dyspnea <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Restlessness <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Tremor <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Vomiting <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Weight decreased <2%
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 235
Health Status: unhealthy
Condition: obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 235
Sources:
Blood pressure diastolic increased
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 396
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 396
Sources:
Blood pressure systolic increased
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 396
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 396
Sources:
Heart rate increased
87.5 mg 1 times / day steady, oral (mean)
Recommended
Dose: 87.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 87.5 mg, 1 times / day
Sources:
unhealthy, 18 to 75 years
n = 396
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Age Group: 18 to 75 years
Sex: M+F
Population Size: 396
Sources:
Headache grade 1, 12.5%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Hypervigilance grade 1, 12.5%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Headache grade 1, 15.6%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Insomnia grade 1, 21.9%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Insomnia grade 1, 21.9%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Nausea grade 1, 6.3%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Decreased appetite grade 1, 9.4%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Decreased appetite grade 1, 9.4%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Hypervigilance grade 1, 9.4%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Nausea grade 1, 9.4%
300 mg 1 times / day single, oral
Studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: single
Dose: 300 mg, 1 times / day
Sources:
healthy, 19 to 54 years
n = 32
Health Status: healthy
Age Group: 19 to 54 years
Sex: M+F
Population Size: 32
Sources:
Palpitations 11.9%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Headache 14.3%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Restlessness 14.3%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Insomnia 16.7%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Decreased appetite 19%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Feeling of relaxation 19%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Hyperhidrosis 19%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Dry mouth 21.4%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Nausea 21.4%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Elevated mood 23.8%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Hypervigilance 42.9%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Paresthesia 7.1%
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Blood pressure increased grade 1, 2.4%
Disc. AE
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Nervousness grade 1, 2.4%
Disc. AE
1200 mg 1 times / day single, oral
Highest studied dose
healthy, mean age 29.3 years
n = 42
Hypertension 0.24%
Disc. AE
150 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy
n = 417
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Sex: M+F
Population Size: 417
Sources:
Blood pressure increased 0.48%
Disc. AE
150 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
unhealthy
n = 417
Health Status: unhealthy
Condition: narcolepsy | obstructive sleep apnea
Sex: M+F
Population Size: 417
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



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
weak [IC50 146 uM]
weak [IC50 211 uM]
weak [IC50 360 uM]
Drug as victimTox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Effect of oral JZP-110 (ADX-N05) treatment on wakefulness and sleepiness in adults with narcolepsy.
2015 Sep
Effect of Oral JZP-110 (ADX-N05) on Wakefulness and Sleepiness in Adults with Narcolepsy: A Phase 2b Study.
2016 Jul 1
New developments in the management of narcolepsy.
2017

Sample Use Guides

The dual-acting dopamine and norepinephrine reuptake inhibitor is approved for narcolepsy in once-daily 75 mg and 150 mg doses, and in obstructive sleep apnea in once-daily 37.5 mg, 75 mg, and 150 mg doses.
Route of Administration: Oral
Solriamfetol binds to the dopamine transporter and norepinephrine transporter with low affinity (Ki=14.2 uM and 3.7 uM, respectively), and inhibits the reuptake of dopamine and norepinephrine with low potency (IC50 =2.9 uM and 4.4 uM, respectively). Solriamfetol has no appreciable binding affinity for the serotonin transporter (Ki=81.5 uM) and does not inhibit serotonin reuptake (IC50 > 100 uM).
Substance Class Chemical
Created
by admin
on Sat Jun 26 02:36:59 UTC 2021
Edited
by admin
on Sat Jun 26 02:36:59 UTC 2021
Record UNII
939U7C91AI
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SOLRIAMFETOL
USAN   INN  
Official Name English
(2R)-2-AMINO-3-PHENYLPROPYL CARBAMATE
Systematic Name English
SOLRIAMFETOL [ORANGE BOOK]
Common Name English
YKP-10A
Code English
R-228060
Code English
SOLRIAMFETOL [WHO-DD]
Common Name English
SUNOSI
Brand Name English
BENZENEPROPANOL, .BETA.-AMINO-, CARBAMATE (ESTER), (R)-
Systematic Name English
BENZENEPROPANOL, .BETA.-AMINO-, 1-CARBAMATE, (.BETA.R)-
Systematic Name English
JZP-110
Code English
SOLRIAMFETOL [INN]
Common Name English
ADX-N-05
Code English
SKL-N-05
Code English
SOLRIAMFETOL [USAN]
Common Name English
SOLRIAMFETOL [MI]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C78272
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
Code System Code Type Description
INN
10117
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
DRUG CENTRAL
5325
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
RXCUI
2121751
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
MERCK INDEX
M12132
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
FDA UNII
939U7C91AI
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
CAS
178429-62-4
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
PUBCHEM
10130337
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
DRUG BANK
DB14754
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
NCI_THESAURUS
C152389
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
LACTMED
Solriamfetol
Created by admin on Sat Jun 26 02:36:59 UTC 2021 , Edited by admin on Sat Jun 26 02:36:59 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TRANSPORTER -> INHIBITOR
WEAK
IC50
TRANSPORTER -> INHIBITOR
WEAK
IC50
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
Approximately 95% of the dose was recovered in urine as unchanged solriamfetol, 1% or less of the administered dose was recovered in urine as the minor inactive metabolite N-acetyl solriamfetol.
URINE
TARGET -> INHIBITOR
Ki
TARGET -> INHIBITOR
Ki
Related Record Type Details
METABOLITE INACTIVE -> PARENT
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
ORAL BIOAVAILABILITY PHARMACOKINETIC
Tmax PHARMACOKINETIC