Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C10H10N2O |
| Molecular Weight | 174.1996 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cc1cc(n(-c2ccccc2)n1)O
InChI
InChIKey=PLVBQEFRONZLHO-UHFFFAOYSA-N
InChI=1S/C10H10N2O/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-7,13H,1H3
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1689064: Hydroxyl Radical |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | RADICUT Approved UseImprovement of neurological symptoms, disorder of activities of daily living, and functional disorder associated with acute ischaemic stroke; Inhibition on progression of functional disorder in patients with amyotrophic lateral sclerosis (ALS). Launch Date1263427200000 |
|||
| Primary | RADICUT Approved UseImprovement of neurological symptoms, disorder of activities of daily living, and functional disorder associated with acute ischaemic stroke; Inhibition on progression of functional disorder in patients with amyotrophic lateral sclerosis (ALS). Launch Date1263427200000 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.48 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22762844/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2030.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30241688/ |
30 mg single, sublingual dose: 30 mg route of administration: Sublingual experiment type: SINGLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2354 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30241688/ |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1049.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28872908/ |
60 mg 1 times / day multiple, intravenous dose: 60 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
EDARAVONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.24 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22762844/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
5576.72 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30241688/ |
30 mg single, sublingual dose: 30 mg route of administration: Sublingual experiment type: SINGLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5981.91 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30241688/ |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1373.5 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28872908/ |
60 mg 1 times / day multiple, intravenous dose: 60 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
EDARAVONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.52 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22762844/ |
30 mg 2 times / day multiple, intravenous dose: 30 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2.83 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30241688/ |
30 mg single, sublingual dose: 30 mg route of administration: Sublingual experiment type: SINGLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.04 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30241688/ |
30 mg single, intravenous dose: 30 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
EDARAVONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
0.86 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28872908/ |
60 mg 1 times / day multiple, intravenous dose: 60 mg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
EDARAVONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
60 mg 1 times / day multiple, intravenous Recommended Dose: 60 mg, 1 times / day Route: intravenous Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, 58.8 years (range: 29 - 75 years) Health Status: unhealthy Age Group: 58.8 years (range: 29 - 75 years) Sex: M+F Sources: |
Disc. AE: Respiratory disorder, Respiratory failure... AEs leading to discontinuation/dose reduction: Respiratory disorder (0.5%) Sources: Respiratory failure (1.1%) Toxic skin eruption (0.5%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Respiratory disorder | 0.5% Disc. AE |
60 mg 1 times / day multiple, intravenous Recommended Dose: 60 mg, 1 times / day Route: intravenous Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, 58.8 years (range: 29 - 75 years) Health Status: unhealthy Age Group: 58.8 years (range: 29 - 75 years) Sex: M+F Sources: |
| Toxic skin eruption | 0.5% Disc. AE |
60 mg 1 times / day multiple, intravenous Recommended Dose: 60 mg, 1 times / day Route: intravenous Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, 58.8 years (range: 29 - 75 years) Health Status: unhealthy Age Group: 58.8 years (range: 29 - 75 years) Sex: M+F Sources: |
| Respiratory failure | 1.1% Disc. AE |
60 mg 1 times / day multiple, intravenous Recommended Dose: 60 mg, 1 times / day Route: intravenous Route: multiple Dose: 60 mg, 1 times / day Sources: |
unhealthy, 58.8 years (range: 29 - 75 years) Health Status: unhealthy Age Group: 58.8 years (range: 29 - 75 years) Sex: M+F Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| yes [IC50 121 uM] | ||||
| yes [IC50 13.6 uM] | ||||
| yes [IC50 2.74 uM] | ||||
| yes [IC50 72.3 uM] | ||||
| yes [IC50 84.5 uM] |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Protection by a radical scavenger edaravone against cisplatin-induced nephrotoxicity in rats. | 2002 Sep 13 |
|
| A free radical scavenger, edaravone, attenuates steatosis and cell death via reducing inflammatory cytokine production in rat acute liver injury. | 2003 Aug |
|
| Normalization by edaravone, a free radical scavenger, of irradiation-reduced endothelial nitric oxide synthase expression. | 2003 Aug 22 |
|
| Clinical usefulness of edaravone for acute liver injury. | 2003 Jul |
|
| A novel free radical scavenger, edarabone, protects against cisplatin-induced acute renal damage in vitro and in vivo. | 2003 Jun |
|
| Protective effect of edaravone against streptomycin-induced vestibulotoxicity in the guinea pig. | 2003 Mar 7 |
|
| Edaravone, a novel free radical scavenger, prevents liver injury and mortality in rats administered endotoxin. | 2003 Oct |
|
| Edaravone, a newly developed radical scavenger, protects against ischemia-reperfusion injury of the small intestine in rats. | 2004 Jan |
|
| Radical scavenger edaravone developed for clinical use ameliorates ischemia/reperfusion injury in rat kidney. | 2004 May |
|
| Edaravone protects against lung injury induced by intestinal ischemia/reperfusion in rat. | 2005 Feb 1 |
|
| Free radical scavenger (edaravone) prevents endotoxin-induced liver injury after partial hepatectomy in rats. | 2005 Jan |
|
| MCI-186 (edaravone), a free radical scavenger, attenuates hepatic warm ischemia-reperfusion injury in rats. | 2005 Jul |
|
| A radical scavenger, edaravone, protects canine kidneys from ischemia-reperfusion injury after 72 hours of cold preservation and autotransplantation. | 2005 Jul 27 |
|
| Edaravone, a novel radical scavenger, inhibits oxidative modification of low-density lipoprotein (LDL) and reverses oxidized LDL-mediated reduction in the expression of endothelial nitric oxide synthase. | 2005 Mar |
|
| The antioxidant edaravone attenuates pressure overload-induced left ventricular hypertrophy. | 2005 May |
|
| Effect of a novel free radical scavenger, edaravone, on puromycin aminonucleoside induced nephrosis in rats. | 2005 Oct |
|
| A free radical scavenger but not FGF-2-mediated angiogenic therapy rescues myonephropathic metabolic syndrome in severe hindlimb ischemia. | 2006 Apr |
|
| Edaravone inhibits rheumatoid synovial cell proliferation and migration. | 2006 Feb |
|
| Clinical analysis of 207 patients who developed renal disorders during or after treatment with edaravone reported during post-marketing surveillance. | 2007 Dec |
|
| Amelioration of hepatic ischemia/reperfusion injury in the remnant liver after partial hepatectomy in rats. | 2007 Dec |
|
| Edaravone inhibits the expression of vascular endothelial growth factor in human astrocytes exposed to hypoxia. | 2007 Dec |
|
| Edaravone reduces ischemia-reperfusion injury mediators in rat liver. | 2007 Jan |
|
| A case report of acute renal failure and fulminant hepatitis associated with edaravone administration in a cerebral infarction patient. | 2007 Jun |
|
| Edaravone neuroprotection effected by suppressing the gene expression of the Fas signal pathway following transient focal ischemia in rats. | 2007 Oct |
|
| Administration of free radical scavenger edaravone associated with higher frequency of hemorrhagic transformation in patients with cardiogenic embolism. | 2008 Jul |
|
| Edaravone protects against MPP+ -induced cytotoxicity in rat primary cultured astrocytes via inhibition of mitochondrial apoptotic pathway. | 2008 Sep |
|
| [Effects of edaravone on the expression of interleukin-1beta, nuclear factor-kappaB and neuron apoptosis in juvenile rat hippocampus after status convulsion]. | 2009 Aug |
|
| Expression of syndecan-2 in the amoeboid microglial cells and its involvement in inflammation in the hypoxic developing brain. | 2009 Feb |
|
| Protective effect of edaravone against tobramycin-induced ototoxicity. | 2009 Jan |
|
| [Effects of edaravone on IRE1 mRNA expression and neuronal apoptosis in the hippocampus of rats with status convulsivus]. | 2009 Jun |
|
| Protective effect of edaravone against PrP106-126-induced PC12 cell death. | 2010 Jul-Aug |
|
| Edaravone improves the expression of nerve growth factor in human astrocytes subjected to hypoxia/reoxygenation. | 2010 Mar |
|
| Protective effect of edaravone, a free-radical scavenger, on ischaemia-reperfusion injury in the rat testis. | 2010 Mar |
|
| Protective effects of the free radical scavenger edaravone on acute pancreatitis-associated lung injury. | 2010 Mar 25 |
|
| [Effects of edaravone on the expression of GRP78, Caspase-12, and neuron apoptosis in juvenile rat hippocampus after status convulsive]. | 2011 Jan |
|
| Edaravone, a novel antidote against lung injury and pulmonary fibrosis induced by paraquat? | 2011 Jan |
|
| Edaravone inhibits hypoxia-induced trophoblast-soluble Fms-like tyrosine kinase 1 expression: a possible therapeutic approach to preeclampsia. | 2014 Jul |
|
| Effects of Astragaloside IV combined with the active components of Panax notoginseng on oxidative stress injury and nuclear factor-erythroid 2-related factor 2/heme oxygenase-1 signaling pathway after cerebral ischemia-reperfusion in mice. | 2014 Oct |
|
| A novel pyrazolone-based derivative induces apoptosis in human esophageal cells via reactive oxygen species (ROS) generation and caspase-dependent mitochondria-mediated pathway. | 2015 Apr 25 |
|
| Change in soluble epoxide hydrolase (sEH) during cisplatin-induced acute renal failure in mice. | 2015 Aug |
|
| Ginsenoside Rd attenuates Aβ25-35-induced oxidative stress and apoptosis in primary cultured hippocampal neurons. | 2015 Sep 5 |
Sample Use Guides
30 mg of edaravone diluted with an appropriate volume of physiological saline, intravenously over 30 minutes twice a day in the morning and the evening (stroke); 60 mg of edaravone diluted with an appropriate volume of physiological saline, intravenously over 60 minutes once a day (amyotrophic lateral sclerosis).
Route of Administration:
Intravenous
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Systematic Name | English | ||
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C1509
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
||
|
WHO-ATC |
N07XX14
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
||
|
FDA ORPHAN DRUG |
478215
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
||
|
FDA ORPHAN DRUG |
754420
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
||
|
EU-Orphan Drug |
EU/3/15/1510
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
||
|
FDA ORPHAN DRUG |
465514
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
RADICUT
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | APPROVED JUNE 2015 | ||
|
DB12243
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
1921877
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
89-25-8
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
C005435
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
CHEMBL290916
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
1040016
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | USP-RS | ||
|
4021
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
942-32-5
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
ALTERNATIVE | |||
|
4102
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
EDARAVONE
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
201-891-0
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
19735-89-8
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
ALTERNATIVE | |||
|
7362
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
4156
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
SUB06453MIG
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
M8072
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | Merck Index | ||
|
213-390-4
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
ALTERNATIVE | |||
|
C74323
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
942-32-5
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY | |||
|
S798V6YJRP
Created by
admin on Sat Jun 26 05:08:30 UTC 2021 , Edited by admin on Sat Jun 26 05:08:30 UTC 2021
|
PRIMARY |
ACTIVE MOIETY
METABOLITE INACTIVE (PARENT)
METABOLITE INACTIVE (PARENT)
