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Drug

D0402 | Teriflunomide

Molecular Formula C12H9F3N2O2
Molecular Weight 270.21
Structure
State solid
Clearance After a single IV dose, teriflunomide has a total body clearance of 30.5 mL/h.
Volume of distribution After a single intravenous dose, the volume of distribution is 11 L.
Route of elimination Teriflunomide is eliminated unchanged and mainly through bile. Specifically 37.5% is eliminated in the feces and 22.6% in urine.
Protein binding Teriflunomide is extensively plasma protein bound(>99%).
Half life The median half-life is 18 to 19 days.
Absorption After oral administration of teriflunomide, maximum plasma concentrations are reached, on average, in 1-4 hours.
Trade names Aubagio
Description treatment of multiple sclerosis ; being the active metabolite of leflunomide; immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase

L

L04AA31 Teriflunomide


[L04AA] Selective immunosuppressants


[L04A] IMMUNOSUPPRESSANTS


[L04] IMMUNOSUPPRESSANTS


[L] Antineoplastic and immunomodulating agents

Toxicity Dose Time Species Model Method Action Positive criterion Reference
FUSION induce 295

Target Dose Time Species Model Method Action Positive criterion Reference
Dihydroorotate dehydrogenase inhibit 295

Pictogram Signal Statements Precautionary Statement Codes
Warning

Aggregated GHS information provided by 48 companies from 6 notifications to the ECHA C&L Inventory.


Reported as not meeting GHS hazard criteria by 1 of 48 companies. For more detailed information, please visit ECHA C&L website


Of the 5 notification(s) provided by 47 of 48 companies with hazard statement code(s):


H302 (95.74%): Harmful if swallowed [Warning Acute toxicity, oral]


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.


 P264, P270, P301+P312, P330, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
rat LD50 oral 4438mg/kg (4438mg/kg) Oyo Yakuri. Pharmacometrics. Vol. 39, Pg. 95, 1990.
rat LD50 intraperitoneal 705mg/kg (705mg/kg) Oyo Yakuri. Pharmacometrics. Vol. 39, Pg. 95, 1990.
mouse LD50 oral 3gm/kg (3000mg/kg) Oyo Yakuri. Pharmacometrics. Vol. 39, Pg. 95, 1990.
dog LD50 oral > 5gm/kg (5000mg/kg) Oyo Yakuri. Pharmacometrics. Vol. 39, Pg. 95, 1990.
mouse LD50 subcutaneous 1009mg/kg (1009mg/kg) behavioral: muscle contraction or spasticity) Oyo Yakuri. Pharmacometrics. Vol. 39, Pg. 95, 1990.
women LDLo oral 108mg/kg/77W- (108mg/kg) Australian and New Zealand Journal of Medicine. Vol. 25, Pg. 745, 1995.
rat LD50 subcutaneous 672mg/kg (672mg/kg) behavioral: muscle contraction or spasticity) Oyo Yakuri. Pharmacometrics. Vol. 39, Pg. 95, 1990.
mouse LD50 intraperitoneal 798mg/kg (798mg/kg) Oyo Yakuri. Pharmacometrics. Vol. 39, Pg. 95, 1990.
women TDLo oral 2800ug/kg/7D- (2.8mg/kg) Medical Journal of Australia. Vol. 155, Pg. 61, 1991.


  • (2Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide (Teriflunomide) (2Z)-2-[hydroxy-[4-(trifluoromethyl)anilino]methylidene]-3-oxobutanenitrile (2Z)-3-oxidanylidene-2-[oxidanyl-[[4-(trifluoromethyl)phenyl]amino]methylidene]butanenitrile
    (2z)-2-Cyano-3-Hydroxy-N-[4-(Trifluoromethyl)phenyl]but-2-Enamide (Z)-2-Cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)but-2-enamide (Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
    (Z)-2-Cyano-alpha'alpha'alpha-trifluoro-3-hydroxy-p-crotonotoluidide (Z)-2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide (Z)-2-cyano-alpha,alpha,alpha-trifluoro-3-hydroxy-p-crotonotoluidide
    108605-62-5 1185240-22-5 163451-81-8
    163451-81-8 (Z Isomer) , 108605-62-5 (E/Z Mixture) 1C058IKG3B 2-Butenamide, 2-cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)-
    2-Butenamide, 2-cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)-, (Z)- 2-Butenamide, 2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]- 2-Butenamide, 2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-, (2Z)-
    2-Cyano-3-OH-N-(4-trifluoromethylphenyl)croton amide 2-Cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)-2-butenamide 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-beuteamide
    2-cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)but-2-enamide 2-cyano-3-hydroxy-n-[4-(trifluoromethyl)phenyl]-2-butenamide 2-hydroxyethylidene-cyanoacetic acid-4-trifluoromethyl anilide
    A 1726 A 77-1726 A 77-1726;A771726;HMR1726;CAS# 108605-62-5
    A 771726 A-771726 A26
    A77 1726 A77-1726 A771726
    A801897 AB01565775_02 AC-26446
    AKOS015994773 API0000341 Active metabolite of leflunomide
    Aubagio Aubagio (TN) BDBM50018011
    C-16971 CC-10329 CHEBI:68540
    Cyano Keto leflunomide impurity D10172 DB08880
    DTXSID80893457 EN300-189832 Flucyamide
    GTPL6844 HMR 1726 HMR-1726
    HMR1726 J-010046 LE-0275
    LS-46899 Leflunomide EP Impurity B Leflunomide Related Compound B, United States Pharmacopeia (USP) Reference Standard
    Leflunomide USP RC B Leflunomide-d4 Metabolite (Teriflunomide-d4) Malononitrilamide
    N-(4-Trifluoromethylphenyl)-2-cyano-2-hydroxycrotonamide N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
    N-[4-(Trifluoromethyl)phenyl]-2-cyano-3-hydroxycrotonamide Q3077133 RS 61980
    RS-61980 RT-011141 SB16822
    SC-90977 SCHEMBL22661 ST24036515
    SU 20 SU-0020 SW219377-1
    Teriflunamide Teriflunomide Teriflunomide
    Teriflunomide (USAN) Teriflunomide [INN] Teriflunomide [USAN:INN]
    Teriflunomide(A-771726) Teriflunomide(Random Configuration) Teriflunomide, A77 1726
    UNII-1C058IKG3B UTNUDOFZCWSZMS-YFHOEESVSA-N ZINC13512456
    s4169 teriflunomida teriflunomidum

    DrugBank Name Teriflunomide
    DrugBank DB08880
    CAS Number 108605-62-5, 1185240-22-5, 163451-81-8, 79902-63-9
    PubChem Compound 54684141
    KEGG Drug D10172
    PubChem.Substance 347827807
    ChEBI 68540
    ChemSpider 16737143
    BindingDB 50018011.0
    Wikipedia Teriflunomide
    HET A26
    DPD 22169