edaravone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
S (Water solubility) 0.03 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.546 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.933 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 104.472 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 7.852 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 30.730 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 31.270 % High 1
herg hERG pIC50 4.018 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.837 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 7.586 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 16.860 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 50
kinase-selectivity-class AXL,GRK2 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.197 High 1
mh-clint Mouse hepatocyte intrinsic clearance 45.709 High 1
mppb Mouse plasma protein binding (% unbound) 34.520 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.365 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 26.320 % High 1
rh-clint Rat hepatocyte intrinsic clearance 20.045 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 95.200 % High 1
rppb Rat plasma protein binding (% unbound) 14.660 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 941.890 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 5, 2017 FDA MITSUBISHI TANABE PHARMA DEVELOPMENT AMERICA INC
April 4, 2001 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 186.99 42.81 90 817 456461 90171079
Cerebral infarction 112.50 42.81 30 877 26566 90600974
Disease progression 79.06 42.81 36 871 156579 90470961
Haemorrhagic cerebral infarction 49.07 42.81 8 899 633 90626907
Paratonia 43.96 42.81 5 902 23 90627517

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 234.67 41.12 150 1055 471035 42149095
Cerebral infarction 87.87 41.12 33 1172 31136 42588994
Amyotrophic lateral sclerosis 59.43 41.12 12 1193 1100 42619030
Disease progression 58.43 41.12 41 1164 143615 42476515
Haemorrhagic infarction 48.70 41.12 9 1196 517 42619613
Tracheostomy 48.39 41.12 10 1195 1027 42619103
Pneumonia aspiration 45.56 41.12 24 1181 50054 42570076
Haemorrhagic cerebral infarction 43.97 41.12 9 1196 882 42619248
Respiratory failure 43.89 41.12 33 1172 128099 42492031
Hepatic function abnormal 42.10 41.12 23 1182 51544 42568586

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 206.90 35.46 62 1721 51776 110535740
Death 198.25 35.46 128 1655 698741 109888775
Haemorrhagic cerebral infarction 94.60 35.46 17 1766 1478 110586038
Hepatic function abnormal 75.25 35.46 34 1749 89261 110498255
Haemorrhagic infarction 68.82 35.46 12 1771 877 110586639
Gastrostomy 68.38 35.46 13 1770 1537 110585979
Pneumonia aspiration 65.48 35.46 30 1753 81203 110506313
Respiratory failure 61.62 35.46 40 1743 215292 110372224
Amyotrophic lateral sclerosis 58.57 35.46 12 1771 2079 110585437
Subarachnoid haemorrhage 44.24 35.46 17 1766 29685 110557831
Tracheostomy 44.16 35.46 9 1774 1518 110585998
Cerebral haemorrhage 43.12 35.46 21 1762 64947 110522569
Cerebral hyperperfusion syndrome 41.82 35.46 6 1777 123 110587393
Paratonia 39.31 35.46 5 1778 39 110587477

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 D016166 Free Radical Scavengers
MeSH PA D018696 Neuroprotective Agents
MeSH PA D020011 Protective Agents
CHEBI has role CHEBI:22586 antioxidant
CHEBI has role CHEBI:48578 radical scavenger
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

N07XX Other nervous system drugs 23 drugs
amifampridinearimoclomoldeutetrabenazinedextromethorphaneplontersenfampridineinotersen laquinimodlevacetylleucineomaveloxolonepatisiranphenylbutanoic acid show all 23 →

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
105MG/5ML RADICAVA ORS SHIONOGI N215446 May 12, 2022 RX SUSPENSION ORAL 11478450 Nov. 1, 2039 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS
105MG/5ML RADICAVA ORS SHIONOGI N215446 May 12, 2022 RX SUSPENSION ORAL 12194025 Nov. 12, 2041 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS BY ADMINISTERING A LIQUID EDARAVONE COMPOSITION RELATIVE TO THE TIMING AND TYPE OF FOOD CONSUMPTION
105MG/5ML RADICAVA ORS SHIONOGI N215446 May 12, 2022 RX SUSPENSION ORAL 12310946 Nov. 12, 2041 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS BY ADMINISTERING A LIQUID EDARAVONE COMPOSITION RELATIVE TO THE TIMING AND TYPE OF FOOD CONSUMPTION
105MG/5ML RADICAVA ORS SHIONOGI N215446 May 12, 2022 RX SUSPENSION ORAL 12478611 Nov. 12, 2041 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS BY ADMINISTERING A LIQUID EDARAVONE COMPOSITION RELATIVE TO THE TIMING AND TYPE OF FOOD CONSUMPTION
105MG/5ML RADICAVA ORS SHIONOGI N215446 May 12, 2022 RX SUSPENSION ORAL 12527769 Nov. 12, 2041 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS BY ADMINISTERING A LIQUID EDARAVONE COMPOSITION RELATIVE TO THE TIMING AND TYPE OF FOOD CONSUMPTION
105MG/5ML RADICAVA ORS SHIONOGI N215446 May 12, 2022 RX SUSPENSION ORAL 12569469 Nov. 12, 2041 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS BY ADMINISTERING A LIQUID EDARAVONE COMPOSITION RELATIVE TO THE TIMING AND TYPE OF FOOD CONSUMPTION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
105MG/5ML RADICAVA ORS SHIONOGI N215446 May 12, 2022 RX SUSPENSION ORAL May 12, 2029 TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS (ALS)

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
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
387175 MMSL
d08586 MMSL
017212 NDDF
736496005 SNOMEDCT_US
763587009 SNOMEDCT_US
W1P PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Edaravone HUMAN PRESCRIPTION DRUG LABEL 1 0781-3527 INJECTION 30 mg INTRAVENOUS ANDA 24 sections
edaravone HUMAN PRESCRIPTION DRUG LABEL 1 39822-4500 INJECTION, SOLUTION 30 mg INTRAVENOUS ANDA 27 sections
edaravone HUMAN PRESCRIPTION DRUG LABEL 1 39822-4510 INJECTION, SOLUTION 60 mg INTRAVENOUS ANDA 27 sections
Edaravone HUMAN PRESCRIPTION DRUG LABEL 1 66794-259 INJECTION, SOLUTION 30 mg INTRAVENOUS ANDA 22 sections
Edaravone HUMAN PRESCRIPTION DRUG LABEL 1 66794-259 INJECTION, SOLUTION 30 mg INTRAVENOUS ANDA 22 sections
edaravone Human Prescription Drug Label 1 68083-500 INJECTION, SOLUTION 30 mg INTRAVENOUS ANDA 22 sections
edaravone Human Prescription Drug Label 1 68083-501 INJECTION, SOLUTION 60 mg INTRAVENOUS ANDA 22 sections
RADICAVA HUMAN PRESCRIPTION DRUG LABEL 1 70510-2171 INJECTION 30 mg INTRAVENOUS NDA 29 sections