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Drug

D0340 | Edaravone

Molecular Formula C10H10N2O
Molecular Weight 174.2
Structure
State solid
Clearance The mean total plasma drug clearance following an intravenous infusion of a single 30mg dose is 0.1L/min [A19139].
Volume of distribution The mean Vd value following an intravenous infusion of a single 30mg dose is 18.5L/kg [A19139].
Route of elimination About 0.7-0.9% of the dose is excreted as unchanged drug and 71.0-79.9% of the dose is excreted as metabolites (mostly as glucuronide conjugates) through mainly renal elimination.
Protein binding The in vitro binding rates of edaravone to human serum protein and albumin are 92% and 89-91%, respectively, with no concentration-dependence.
Half life The mean terminal elimination half-life of edaravone is 4.5 to 6 hours and the half-lives of its metabolites are 2 to 2.8 hours.
Absorption The peak plasma concentration of the parent drug is reached at the end of infusion, without accumulation of the drug with multiple dosing regimen. The mean Cmax value in healthy male adults is 888ng/mL for intravenous infusion. The values of AUC and Cmax are increased in a dose-proportional relationship. The oral bioavailability in mouse studies is 38% of the I.V. delivery [A19138].

N

N07XX14 Edaravone


[N07XX] Other nervous system drugs


[N07X] OTHER NERVOUS SYSTEM DRUGS


[N07] OTHER NERVOUS SYSTEM DRUGS


[N] Nervous system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 31.75±4.28 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 28.18 human HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 25.79±10.10 rat hepatocytes MMP assay decrease IC50 163

Pictogram Signal Statements Precautionary Statement Codes
Warning

Aggregated GHS information provided by 216 companies from 23 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


Reported as not meeting GHS hazard criteria by 15 of 216 companies. For more detailed information, please visit ECHA C&L website


Of the 21 notification(s) provided by 201 of 216 companies with hazard statement code(s):


H302 (26.87%): Harmful if swallowed [Warning Acute toxicity, oral]


H315 (50.25%): Causes skin irritation [Warning Skin corrosion/irritation]


H317 (66.67%): May cause an allergic skin reaction [Warning Sensitization, Skin]


H319 (24.38%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]


H335 (27.86%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure


Respiratory tract irritation]


H412 (42.79%): Harmful to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard]


H413 (17.41%): May cause long lasting harmful effects to aquatic life [Hazardous to the aquatic environment, long-term hazard]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


 P261, P264, P270, P271, P272, P273, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P333+P313, P337+P313, P362, P363, P403+P233, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)
Warning

H317: May cause an allergic skin reaction [Warning Sensitization, Skin]


 P261, P272, P280, P302+P352, P321, P333+P313, P363, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)


  • (MCI-186) 1-Fenyl-3-methyl-2-pyrazolin-5-on 1-Fenyl-3-methyl-2-pyrazolin-5-on [Czech]
    1-PEHNYL-3-METHYL-5-PYRAZALONE 1-Phenyl-3-methyl-2-pyrazolin-5-on 1-Phenyl-3-methyl-5-oxo-2-pyrazoline
    1-Phenyl-3-methyl-5-pyrazolone 1-Phenyl-3-methylpyrazolone 1-Phenyl-3-methylpyrazolone-5
    2 4-Dihydro-5-methyl-2-phenyl-3H-pyrazol-3-one 2,4-Dihydro-5-methyl-2-phenyl-3H-pyrazol-3-one 2,4-dihydro-2-phenyl-5-methyl-3H-pyrazol-3-one
    2-Pyrazolin-5-one, 3-methyl-1-phenyl- 3-METHYL-1-PHENYL-2-PYRAZOLIN-5-ONE 3-METHYL-1-PHENYL-2-PYRAZOLIN-5-ONE (MCI-186)
    3-Methyl-1-phenyl-1H-pyrazol-5(4H)-one 3-Methyl-1-phenyl-2-pyrazolin-5-one, 99% 3-Methyl-1-phenyl-2-pyrazoline-5-one
    3-Methyl-1-phenyl-2-pyrazoline-5-one, 99% 3-Methyl-1-phenyl-2-pyrazoline-5-one, SAJ special grade 3-Methyl-1-phenyl-2-pyrazoline-5-one, purum, >=98.0% (NT)
    3-Methyl-1-phenylpyrazol-5-one 3-methyl-1-phenyl-2-pyrazolin-5one 3-methyl-1-phenyl-4,5-dihydro-1H-pyrazol-5-one
    3H-Pyrazol-3-one, 2,4-dihydro-5-methyl-2-phenyl- 3H-Pyrazol-3-one,4-dihydro-5-methyl-2-phenyl- 4CA-0486
    4E-901 5-Methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one 5-Methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one #
    5-Methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one (Edaravone) 5-Pyrazolone, 3-methyl-1-phenyl- 5-methyl-2-phenyl-2,4-dihydro-3-pyrazolone
    5-methyl-2-phenyl-2,4-dihydro-pyrazol-3-one 5-methyl-2-phenyl-2,4-dihydropyrazol-3-one 89-25-8
    AB00375776_14 AB00375776_15 AB2000046
    AC-4745 ACT07289 AE-641/00371017
    AI3-03557 AK128848 AKOS000313817
    AM20060748 Antipyrine Related Compound A, United States Pharmacopeia (USP) Reference Standard BBL011741
    BCBcMAP01_000127 BCP26336 BCP9000635
    BCPP000246 BDBM50200541 BRD-K35458079-001-04-2
    BRD-K35458079-001-12-5 BRD-K35458079-001-23-2 BRN 0609575
    BSPBio_001235 BSPBio_002601 Bio1_000438
    Bio1_000927 Bio1_001416 Bio2_000448
    Bio2_000928 C.I. Developer 1 C13008
    CAS-89-25-8 CCG-39352 CCRIS 512
    CDS1_000986 CHEBI:31530 CHEMBL290916
    CI Developer 1 CS-1832 CTK3E8611
    D01552 DB-002517 DB12243
    DSSTox_CID_1130 DSSTox_GSID_21130 DSSTox_RID_75961
    DTXSID9021130 Developer Z DivK1c_001018
    DivK1c_002026 EC 201-891-0 EINECS 201-891-0
    Edaravone (MCI-186) Edaravone (USAN/JP17/INN) Edaravone [USAN:INN]
    F0391-0021 FT-0608243 HMS1362M17
    HMS1792M17 HMS1990M17 HMS2234M19
    HMS3266F04 HMS3403M17 HMS3411L05
    HMS3654L15 HMS3675L05 HMS503K17
    HMS557M18 HSDB 4102 HY-B0099
    IDI1_001018 IDI1_002203 InChI=1/C10H10N2O/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-6H,7H2,1H
    KBio1_001018 KBio2_000575 KBio2_000747
    KBio2_003143 KBio2_003315 KBio2_005711
    KBio2_005883 KBio3_001029 KBio3_001030
    KBio3_001821 KBioGR_000575 KBioGR_001502
    KBioSS_000575 KBioSS_000747 KS-00000X6I
    KSC448M1D LS-1892 M0687
    MCI-186 MCI-186, Radicut, 89-25-8 MFCD00003138
    MLS000069602 MLS001146878 MLS002415675
    MLS006011753 Maybridge1_005738 Methylphenylpyrazolone
    Monopyrazolone NCGC00018218-01 NCGC00018218-02
    NCGC00018218-03 NCGC00018218-04 NCGC00018218-05
    NCGC00018218-06 NCGC00018218-07 NCGC00018218-08
    NCGC00018218-10 NCGC00018218-17 NCGC00022665-02
    NCGC00022665-04 NCGC00022665-05 NCGC00022665-06
    NCGC00164015-01 NCGC00256515-01 NCGC00259296-01
    NCI-C03952 NE10266 NINDS_001018
    NSC 12 NSC-26139 NSC-2629
    NSC-758622 NSC26139 NSC2629
    NSC758622 Norantipyrine Norphenazone
    Opera_ID_1057 Pharmakon1600-01503635 Phenazone impurity A, European Pharmacopoeia (EP) Reference Standard
    Phenyl methyl pyrazolone Phenylmethylpyrazolone PubChem13301
    Q-200386 Q335099 QELUYTUMUWHWMC-UHFFFAOYSA-N
    RTR-028045 Radicava Radicava (TN)
    Radicut Radicut (TN) Radicut;MCI-186
    SB19128 SBI-0051836.P002 SC-13582
    SCHEMBL4704 SMR000059020 SPBio_001508
    SPECTRUM1503635 SR-01000000135 SR-01000000135-2
    SR-01000000135-3 SR-01000000135-5 ST012744
    ST2410773 STK201315 SW148216-2
    Spectrum2_001574 Spectrum3_000971 Spectrum4_001091
    Spectrum5_001217 Spectrum_000267 TR-028045
    Tocris-0786 Tox21_112077 Tox21_112077_1
    Tox21_201747 Tox21_302819 WLN: T5NMV DHJ BR& E1
    Z50145861 ZINC18203737 edaravone
    s1326

    DrugBank Name Edaravone
    DrugBank DB12243
    CAS Number 19735-89-8, 89-25-8, 94849-87-3
    PubChem Compound 4021
    KEGG Compound ID C13008
    KEGG Drug D01552
    PubChem.Substance 347828521
    ChEBI 31530
    ChemSpider 3881
    BindingDB 50200541.0
    Wikipedia Edaravone
    DPD 22947