solriamfetol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	5325	178429-62-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: solriamfetol sunosi JZP-110 ADX-N05 ARL-N05 SKL-N05	The mechanism of action of solriamfetol to improve wakefulness in patients with excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea is unclear. However, solriamfetol binds to the dopamine transporter and norepinephrine transporter with low affinity and inhibits the reuptake of dopamine and norepinephrine with low potency. Solriamfetol has no appreciable binding affinity for the serotonin transporter (Ki=81.5 μM) and does not inhibit serotonin reuptake (IC50 > 100 μM). Solriamfetol improves wakefulness in patients with excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea is unclear. However, its efficacy could be mediated through its activity as a dopamine and norepinephrine reuptake inhibitor (DNRI). Molecular weight: 194.23 Formula: C10H14N2O2 CLOGP: 0.63 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 78.34 ALOGS: -2 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

solriamfetol
sunosi
JZP-110
ADX-N05
ARL-N05
SKL-N05

The mechanism of action of solriamfetol to improve wakefulness in patients with excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea is unclear. However, solriamfetol binds to the dopamine transporter and norepinephrine transporter with low affinity and inhibits the reuptake of dopamine and norepinephrine with low potency. Solriamfetol has no appreciable binding affinity for the serotonin transporter (Ki=81.5 μM) and does not inhibit serotonin reuptake (IC50 > 100 μM). Solriamfetol improves wakefulness in patients with excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea is unclear. However, its efficacy could be mediated through its activity as a dopamine and norepinephrine reuptake inhibitor (DNRI).

Molecular weight: 194.23
Formula: C10H14N2O2
CLOGP: 0.63
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 78.34
ALOGS: -2
ROTB: 5

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Jan. 16, 2020	EMA	Jazz Pharmaceuticals Ireland Limited
March 20, 2019	FDA	JAZZ

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product administration interrupted	126.60	36.77	29	1774	4807	63482412
Anxiety	107.25	36.77	70	1733	217471	63269748
Drug ineffective	93.09	36.77	129	1674	1044636	62442583
Suicidal ideation	77.54	36.77	37	1766	62384	63424835
Surgery	62.67	36.77	27	1776	35885	63451334
Pre-existing condition improved	60.48	36.77	18	1785	8226	63478993
Sleep apnoea syndrome	51.13	36.77	22	1781	29111	63458108
Feeling jittery	48.04	36.77	17	1786	13386	63473833
Depression	40.77	36.77	38	1765	196454	63290765
Headache	38.45	36.77	66	1737	633175	62854044

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	110.88	55.79	64	308	456687	34499872

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product administration interrupted	89.03	40.38	17	673	3882	79739816

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N06BA14	NERVOUS SYSTEM PSYCHOANALEPTICS PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS Centrally acting sympathomimetics

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Narcolepsy	indication	60380001	DOID:8986
Obstructive sleep apnea syndrome	indication	78275009	DOID:0050848
Excessive daytime sleepiness - normal night sleep	indication	230489007
Monoamine oxidase inhibitor	contraindication	734595009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.22	acidic
pKa2	7.89	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	10351517	June 7, 2026	TO IMPROVE WAKEFULNESS IN ADULT PATIENTS WITH EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH NARCOLEPSY OR OBSTRUCTIVE SLEEP APNEA (OSA)
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	8877806	June 7, 2026	TO IMPROVE WAKEFULNESS IN ADULT PATIENTS WITH EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH NARCOLEPSY OR OBSTRUCTIVE SLEEP APNEA (OSA)
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	9604917	June 7, 2026	TO IMPROVE WAKEFULNESS IN ADULT PATIENTS WITH EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH NARCOLEPSY OR OBSTRUCTIVE SLEEP APNEA (OSA)
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	8440715	June 11, 2031	TO IMPROVE WAKEFULNESS IN ADULT PATIENTS WITH EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH NARCOLEPSY OR OBSTRUCTIVE SLEEP APNEA (OSA)
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	10512609	Sept. 5, 2037	TO IMPROVE WAKEFULNESS IN ADULT PATIENTS WITH EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH NARCOLEPSY OR OBSTRUCTIVE SLEEP APNEA (OSA)
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	10912754	June 1, 2038	TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH OBSTRUCTIVE SLEEP APNEA (OSA) IN AN ADULT THROUGH A DOSING REGIMEN THAT INCLUDES ORAL ADMINISTRATION OF 75 MG ONCE DAILY FOR AT LEAST 3 DAYS FOLLOWED BY 150 MG ONCE DAILY
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	10959976	June 1, 2038	TO IMPROVE WAKEFULNESS IN ADULT PATIENTS WITH EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH NARCOLEPSY OR OBSTRUCTIVE SLEEP APNEA (OSA) WITH A DOSING REGIMEN THAT INCLUDES A DOSE OF 75 MG ONCE DAILY FOR AT LEAST 3 DAYS FOLLOWED BY 150 MG ONCE DAILY
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	11648232	June 1, 2038	TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS WITH A DOSING REGIMEN THAT INCLUDES ORAL ADMINISTRATION OF 75 MG ONCE DAILY FOR AT LEAST 3 DAYS FOLLOWED BY 150 MG ONCE DAILY
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	11560354	March 6, 2039	TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS BY ADMINISTERING A COMPOSITION COMPRISING SOLRIAMFETOL HYDROCHLORIDE AND 2-CHLOROPROPANE, WHEREIN THE COMPOSITION COMPRISES LESS THAN ABOUT 5 PPM 2‑CHLOROPROPANE
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	10940133	March 19, 2040	TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH OBSTRUCTIVE SLEEP APNEA (OSA) IN A PATIENT WITH MODERATE RENAL IMPAIRMENT
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	11160779	March 19, 2040	TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS BY ADMINISTERING SOLRIAMFETOL TO A SUBJECT HAVING MILD, MODERATE, OR SEVERE RENAL IMPAIRMENT

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	June 17, 2024	NEW CHEMICAL ENTITY
EQ 75MG BASE	SUNOSI	AXSOME MALTA	N211230	June 17, 2019	RX	TABLET	ORAL	June 17, 2026	INDICATED TO IMPROVE WAKEFULNESS IN ADULT PATIENTS WITH EXCESSIVE DAYTIME SLEEPINESS ASSOCIATED WITH NARCOLEPSY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Ki	4.09	DRUG LABEL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Ki	5.43	DRUG LABEL
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN	INHIBITOR	Ki	4.85	DRUG LABEL

External reference:

ID	Source
939U7C91AI	UNII
C4726765	UMLSCUI
CHEMBL4297212	ChEMBL_ID
CHEMBL4297620	ChEMBL_ID
10130337	PUBCHEM_CID
DB14754	DRUGBANK_ID
D11315	KEGG_DRUG
10117	INN_ID
10342	IUPHAR_LIGAND_ID
017938	NDDF
787053002	SNOMEDCT_US
787070005	SNOMEDCT_US
4038551	VANDF
2121751	RXNORM
319330	MMSL
d09320	MMSL
C000623308	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	68727-350	TABLET, FILM COATED	75 mg	ORAL	NDA	26 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	68727-350	TABLET, FILM COATED	75 mg	ORAL	NDA	26 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	68727-351	TABLET, FILM COATED	150 mg	ORAL	NDA	26 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	68727-351	TABLET, FILM COATED	150 mg	ORAL	NDA	26 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	81968-350	TABLET, FILM COATED	75 mg	ORAL	NDA	31 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	81968-350	TABLET, FILM COATED	75 mg	ORAL	NDA	31 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	81968-350	TABLET, FILM COATED	75 mg	ORAL	NDA	31 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	81968-351	TABLET, FILM COATED	150 mg	ORAL	NDA	31 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	81968-351	TABLET, FILM COATED	150 mg	ORAL	NDA	31 sections
SUNOSI	HUMAN PRESCRIPTION DRUG LABEL	1	81968-351	TABLET, FILM COATED	150 mg	ORAL	NDA	31 sections