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

Stem definitionDrug idCAS RN
4156 89-25-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • radicava
  • edaravone
  • edarabone
  • methylphenylpyrazolone
  • norantipyrine
  • norphenazone
  • radicut
Edaravone protects neurons from oxidative stress by scavenging free radicals that may cause cellular damage, and this mechanism is expected to be effective both in patients with acute cerebral infarction and in those with ALS
  • Molecular weight: 174.20
  • Formula: C10H10N2O
  • CLOGP: 1.33
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 32.67
  • ALOGS: -2.27
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.23 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.42 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.89 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.36 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 5, 2017 FDA MITSUBISHI TANABE PHARMA DEVELOPMENT AMERICA INC
None PMDA Mitsubishi Tanabe Pharma Corporation

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 99.47 45.54 53 465 325326 50279280
Cerebral infarction 79.89 45.54 22 496 21582 50583024

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 132.81 44.71 90 669 341994 29231774
Cerebral infarction 83.07 44.71 29 730 24646 29549122
Haemorrhagic infarction 51.40 44.71 9 750 421 29573347
Amyotrophic lateral sclerosis 44.85 44.71 9 750 882 29572886

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cerebral infarction 164.89 41.29 50 1058 40994 64456630
Death 121.46 41.29 84 1024 482621 64015003
Haemorrhagic infarction 63.99 41.29 11 1097 694 64496930
Haemorrhagic cerebral infarction 57.16 41.29 11 1097 1303 64496321
Hepatic function abnormal 48.15 41.29 23 1085 64290 64433334
No adverse event 43.88 41.29 17 1091 28544 64469080
Amyotrophic lateral sclerosis 42.91 41.29 9 1099 1641 64495983

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07XX14 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
OTHER NERVOUS SYSTEM DRUGS
Other nervous system drugs
MeSH PA D000975 Antioxidants
MeSH PA D002491 Central Nervous System Agents
MeSH PA D016166 Free Radical Scavengers
MeSH PA D018696 Neuroprotective Agents
MeSH PA D020011 Protective Agents
CHEBI has role CHEBI:22586 antioxidants
CHEBI has role CHEBI:48578 free radical scavengers

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Amyotrophic lateral sclerosis indication 86044005 DOID:332
Ischemic stroke indication 422504002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 0.5 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
30MG/100ML (0.3MG/ML) RADICAVA MITSUBISHI TANABE N209176 May 5, 2017 RX SOLUTION INTRAVENOUS May 5, 2022 NEW CHEMICAL ENTITY
60MG/100ML (0.6MG/ML) RADICAVA MITSUBISHI TANABE N209176 Nov. 15, 2018 RX SOLUTION INTRAVENOUS May 5, 2022 NEW CHEMICAL ENTITY
30MG/100ML (0.3MG/ML) RADICAVA MITSUBISHI TANABE N209176 May 5, 2017 RX SOLUTION INTRAVENOUS May 5, 2024 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS (ALS)
60MG/100ML (0.6MG/ML) RADICAVA MITSUBISHI TANABE N209176 Nov. 15, 2018 RX SOLUTION INTRAVENOUS May 5, 2024 FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Polyunsaturated fatty acid lipoxygenase ALOX15 Enzyme IC50 4.47 CHEMBL

External reference:

IDSource
D01552 KEGG_DRUG
4036711 VANDF
C0070694 UMLSCUI
CHEBI:31530 CHEBI
W1P PDB_CHEM_ID
CHEMBL290916 ChEMBL_ID
D000077553 MESH_DESCRIPTOR_UI
DB12243 DRUGBANK_ID
11994 IUPHAR_LIGAND_ID
7362 INN_ID
S798V6YJRP UNII
4021 PUBCHEM_CID
1921877 RXNORM
257218 MMSL
32736 MMSL
d08586 MMSL
017212 NDDF
736496005 SNOMEDCT_US
763587009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
RADICAVA HUMAN PRESCRIPTION DRUG LABEL 1 70510-2171 INJECTION 30 mg INTRAVENOUS NDA 28 sections
RADICAVA HUMAN PRESCRIPTION DRUG LABEL 1 70510-2171 INJECTION 30 mg INTRAVENOUS NDA 28 sections