Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C10H14N2O2 |
| Molecular Weight | 194.2304 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
N[C@@H](COC(N)=O)CC1=CC=CC=C1
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
| Molecular Formula | C10H14N2O2 |
| Molecular Weight | 194.2304 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | |
| 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.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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
Edited
Mon Oct 21 22:40:18 UTC 2019
by
admin
on
Mon Oct 21 22:40:18 UTC 2019
|
| Record UNII |
939U7C91AI
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C78272
Created by
admin on Mon Oct 21 22:40:18 UTC 2019 , Edited by admin on Mon Oct 21 22:40:18 UTC 2019
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
10117
Created by
admin on Mon Oct 21 22:40:18 UTC 2019 , Edited by admin on Mon Oct 21 22:40:18 UTC 2019
|
PRIMARY | |||
|
178429-62-4
Created by
admin on Mon Oct 21 22:40:18 UTC 2019 , Edited by admin on Mon Oct 21 22:40:18 UTC 2019
|
PRIMARY | |||
|
10130337
Created by
admin on Mon Oct 21 22:40:18 UTC 2019 , Edited by admin on Mon Oct 21 22:40:18 UTC 2019
|
PRIMARY | |||
|
C152389
Created by
admin on Mon Oct 21 22:40:18 UTC 2019 , Edited by admin on Mon Oct 21 22:40:18 UTC 2019
|
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
|
| 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 |
|
|
|||