General
Preferred name
solriamfetol
Synonyms
ADX-N05 ()
R228060 ()
R-228060 ()
SOLRIAMFETOL HYDROCHLORIDE ()
SKL-N-05 ()
JZP-110 ()
YKP-10A ()
ADX-N-05 ()
Solriamfetol ()
JZP-110 hydrochloride ()
Sunosi ()
P&D ID
PD098074
CAS
178429-62-4
Tags
available
drug
Approved by
EMA
FDA
First approval
2019
Drug Status
approved
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
TOXICITY Age, gender, and race do not significantly affect solriamfetol pharmacokinetics and no dose adjustments were made in clinical trials for patients over 65 years[FDA Label].; ; Patients with renal failure experience increases in half life between 1.2 and 3.9 times that in healthy patients[FDA Label]. 21% of solriamfetol was removed by hemodialysis, however time to peak concentration was not affected[FDA Label].; ; Solriamfetol is not expected to lead to adverse effects in pregnancy[FDA Label]. Maternal and fetal toxicity was seen in animal studies at ≥4 and 5 times the maximum recommended human dose and teratogenicity was seen at 19 and ≥5 times the maximum recommended human dose[FDA Label].; ; Breastfed infants should be monitored for adverse reactions such as agitation, insomnia, anorexia, and reduced weight gain as solriamfetol is present in breast milk[FDA Label]. However, there is no currently available data on the effect of solriamfetol in breast milk on breast fed inants[FDA Label].; ; Safety and effectiveness of solriamfetol in pediatric patients has not been established in clinical studies[FDA Label].; ; Solriamfetol does not display different safety or effectiveness in geriatric populations[FDA Label].; ; Dosage adjustments are recommended for patients with eGFR <60mL/min/1.73m^2 and solriamfetol is not recommended for patients with an eGFR <15mL/min/1.73m^2[FDA Label].
PHARMACODYNAMICS Solriamfetol weakly binds to dopamine and norepinephrine transporters but not serotonin transporters[FDA Label][A176516]. Solriamfetol does not bind to dopamine, serotonin, norepinephrine, GABA, adenosine, histamine, orexin, benzodiazepines, or muscarinic and nicotinic receptors[FDA Label].; ; Solriamfetol is also associated with a mean increase of 21 beats per minute (BPM) in heart rate in patients taking 300mg (twice the maximum recommended dose) and 27 BPM in patients taking 900mg (six times the maximum recommended dose)[FDA Label]. 300mg of solriamfetol does not increase the QTcF interval to a clinically relevant degree[FDA Label].
DESCRIPTION Solriamfetol is a norepinephrine-dopamine reuptake inhibitor that was developed by Jazz Pharmaceuticals . (GtoPdb)
ABSORPTION Oral bioavailability of solriamfetol is approximately 95%[FDA Label]. Peak plasma concentration is reached in 2 hours (with a range of 1.25 to 3 hours) in fasted patients[FDA Label]. When solriamfetol is taken with a high fat meal, the time to peak plasma concentration increases to 3 hours[FDA Label].
METABOLISM Solriamfetol does not undergo significant metabolism in humans, though less than 1% of solriamfetol is metabolized to N-acetyl solriamfetol[FDA Label][A176516].
ROE 95% of solriamfetol is recovered in urine unchanged by metabolism[FDA Label]. Less than 1% of solriamfetol is recovered as N-acetyl solriamfetol[FDA Label][A176516].
INDICATION Solriamfetol is indicated for treatment of daytime sleepiness associated with obstructive sleep apnea and narcolepsy, but is not a treatment for the underlying airway obstruction in apnea patients[FDA Label][A176534,A176744].
MOA The specific mechanism of action is unknown but it may be through its activity as a dopamine and norepinephrine reuptake inhibitor[FDA Label][A176516].
HALF-LIFE 7.1 hours[FDA Label]. Other studies have found the mean half life to be 6.1 ± 1.2 hours in fasted subjects and 5.9 ± 1.2 hours in fed subjects[A176744].
Compound Sets
11
ChEMBL Approved Drugs
CHEMBL4297620
CHEMBL4297212
ChEMBL Drugs
CHEMBL4297620
CHEMBL4297212
Drug Repurposing Hub
DrugBank
DB14754
DrugBank Approved Drugs
DB14754
DrugCentral
5325
DrugCentral Approved Drugs
5325
Guide to Pharmacology
10342
NCATS Inxight Approved Drugs
939U7C91AI
ReFrame library
TargetMol Bioactive Compound Library
T7583
External IDs
29
Properties
(calculated by RDKit )
Molecular Weight
194.11
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
1
Aromatic Ring Count
1
cLogP
0.65
TPSA
78.34
Fraction CSP3
0.3
Chiral centers
1.0
Largest ring
6.0
QED
0.74
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Neuroscience
GPCR/G protein
Neuronal Signaling
Target
norepinephrine transporter (NET)
Dopamine Transporter
Dopamine Receptor
Indication
narcolepsy
MOA
dopamine reuptake inhibitor
Source data