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
Amyotrophic lateral sclerosis 159.12 51.52 24 570 1104 56290369
Cerebral infarction 135.99 51.52 34 560 22471 56269002
Death 112.24 51.52 59 535 341367 55950106

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
Amyotrophic lateral sclerosis 267.57 45.33 42 821 954 31695527
Death 161.66 45.33 106 757 360463 31336018
Cerebral infarction 127.12 45.33 41 822 25936 31670545
Haemorrhagic infarction 50.39 45.33 9 854 444 31696037

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
Amyotrophic lateral sclerosis 386.85 37.38 59 1204 1715 70925466
Cerebral infarction 271.81 37.38 75 1188 42934 70884247
Death 118.82 37.38 86 1177 509975 70417206
Haemorrhagic cerebral infarction 68.51 37.38 13 1250 1378 70925803
Haemorrhagic infarction 63.03 37.38 11 1252 731 70926450
Hepatic function abnormal 55.19 37.38 26 1237 67970 70859211
No adverse event 41.33 37.38 17 1246 32136 70895045
Paratonia 41.08 37.38 5 1258 23 70927158
Respiratory failure 40.02 37.38 29 1234 168706 70758475

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 | Suggest Off label Use Form| |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)
105MG/5ML RADICAVA ORS MITSUBISHI TANABE N215446 May 12, 2022 RX SUSPENSION ORAL May 12, 2025 NEW PRODUCT

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