Search References Drug Actions/Targets About Access data Feedback
Sign In
mitontu@gmail.com
2021 MitoTox | (CC BY-NC 4.0)
Drug

D1138 | triclabendazole

Molecular Formula C14H9Cl3N2OS
Molecular Weight 359.7
Structure
State solid
Volume of distribution The apparent volume of distribution (Vd) of the sulfoxide metabolite in fed patients is about 1 L/kg.[FDA label]
Route of elimination No data regarding excretion is available in humans. In animals, triclabendazole is primarily excreted by the biliary tract in the feces (90%), together with the sulfoxide and sulfone metabolite. Less than 10% of an oral dose is found excreted in the urine.[FDA label]
Protein binding Protein-binding of triclabendazole, sulfoxide metabolite and sulfone metabolite in human plasma was 96.7%, 98.4% and 98.8% respectively.[FDA label]
Half life The plasma elimination half-life (t1/2) of triclabendazole, the sulfoxide and sulfone metabolites in human is about 8, 14, and 11 hours, respectively.[FDA label]
Absorption After a single oral dose of 10 mg/kg triclabendazole with a 560-kcal meal to patients diagnosed with fascioliasis, mean peak plasma concentrations (Cmax) for triclabendazole, the sulfoxide, and sulfone metabolites were 1.16, 38.6, and 2.29 μmol/L, respectively. The area under the curve (AUC) for triclabendazole, the sulfoxide and sulfone metabolites were 5.72, 386, and 30.5 μmol∙h/L, respectively.[FDA label] After the oral administration of a single dose of triclabendazole at 10 mg/kg with a 560 calorie meal to patients with fascioliasis, the median Tmax for the parent compound as well as the active sulfoxide metabolite was 3 to 4 hours.[FDA label] **Effect of Food** Cmax and AUC of triclabendazole and sulfoxide metabolite increased about 2-3 times when triclabendazole was administered as a single dose at 10 mg/kg with a meal containing approximately 560 calories. Additionally, the sulfoxide metabolite Tmax increased from 2 hours in fasting subjects to 4 hours in fed subjects [FDA label].

P

P02BX04 Triclabendazole


[P02BX] Other antitrematodal agents


[P02B] ANTITREMATODALS


[P02] ANTHELMINTICS


[P] Antiparasitic products, insecticides and repellents

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 1.84±0.15 human qHTS-HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 5.48 human HepG2 MMP assay decrease IC50 163
MEMBRANE POTENTIAL 15.55±2.52 rat hepatocytes MMP assay decrease IC50 163

Pictogram Signal Statements Precautionary Statement Codes
Warning

Aggregated GHS information provided by 79 companies from 6 notifications to the ECHA C&L Inventory.


Reported as not meeting GHS hazard criteria by 41 of 79 companies. For more detailed information, please visit ECHA C&L website


Of the 4 notification(s) provided by 38 of 79 companies with hazard statement code(s):


H373 (92.11%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]


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.


 P260, P314, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)


  • 1H-BENZIMIDAZOLE, 5-CHLORO-6-(2,3-DICHLOROPHENOXY)-2-(METHYLTHIO)- 1H-Benzimidazole, 6-chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)- 4784C8E03O
    5-Chloro-6-(2,3-dichlorophenoxy)-2-(methylsulfanyl)-1H-benzimidazole 5-Chloro-6-(2,3-dichlorophenoxy)-2-(methylthio)-1H-benzimidazole 5-Chloro-6-(2,3-dichlorophenoxy)-2-(methylthio)benzimidazole
    5-[2,3-bis(chloranyl)phenoxy]-6-chloranyl-2-methylsulfanyl-1H-benzimidazole 5-chloro-6-(2,3-dichlorophenoxy)-2-(methylthio)-1H-benzo[d]imidazole 5-chloro-6-(2,3-dichlorophenoxy)-2-methylsulfanyl-1H-benzimidazole
    6-CHLORO-5-(2,3-DICHLOROPHENOXY)-2-METHYLTHIO-BENZ 6-Chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)-1H-benzo[d]imidazole 6-Chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)benzimidazole
    6-Chloro-5-(2,3-dichlorophenoxy)-2-methylthio-benzimidazole 6-chloro-5-(2,3-dichlorophenoxy)-2-(methylsulfanyl)-1H-1,3-benzodiazole 6-chloro-5-(2,3-dichlorophenoxy)-2-(methylsulfanyl)-1H-benzimidazole
    6-chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)-1H-benzimidazole 6-chloro-5-(2,3-dichlorophenoxy)-2-methylsulfanyl-1H-benzimidazole 6-chloro-5-(2,3-dichlorophenoxy)-2-methylthiobenzimidazole
    68786-66-3 786T663 A836250
    AB0013427 AB00639964-10 AB00639964_12
    AB00639964_13 AB1004580 AC-7627
    AK-68238 AKOS005439340 AKOS015950804
    ANW-42745 API0004496 AX8034628
    BDBM58491 BEN631 BR-68238
    BRD-K81916719-001-05-5 C14H9Cl3N2OS CAS-68786-66-3
    CCG-100881 CCRIS 8988 CGA 89317
    CGA-89317 CGA89317 CHEBI:94759
    CHEMBL1086440 CPD000466357 CS-2859
    CTK5C8452 D07364 DB12245
    DSSTox_CID_23952 DSSTox_GSID_43952 DSSTox_RID_80094
    DTXSID7043952 EGA230B Egaten
    Egaten (TN) FT-0602564 Fasinex
    Fasinex (TN) HMS2051E16 HMS2232D14
    HMS3370H02 HMS3393E16 HMS3652M16
    HMS3715P16 HMS3744I09 HY-B0621
    I018 KS-00000KPE KS-5329
    KUC103451N LS-32758 MCULE-8131756770
    MLS000759473 MLS000876812 MLS001424101
    MP-0274 NC00131 NCGC00164610-01
    NCGC00164610-02 NQPDXQQQCQDHHW-UHFFFAOYSA-N NSC-759250
    NSC759250 NVP-EGA230 Oprea1_236106
    Pharmakon1600-01505786 Q419739 SAM001246681
    SB17173 SBI-0207022.P001 SC-17720
    SCHEMBL165712 SMR000466357 SR-01000759363
    SR-01000759363-4 ST2418930 STK332284
    SW197511-2 TR-022940 Tox21_112231
    Triclabendazol Triclabendazol [INN-Spanish] Triclabendazole
    Triclabendazole (USAN/INN) Triclabendazole [BAN:INN] Triclabendazole [USAN:INN:BAN]
    Triclabendazole for system suitability, EuropePharmacopoeia (EP) Reference Standard; Triclabendazole, 98% Triclabendazole, EuropePharmacopoeia (EP) Reference Standard
    Triclabendazole, VETRANAL(TM), analytical standard Triclabendazolum Triclabendazolum [INN-Latin]
    UNII-4784C8E03O ZINC1444556 cid_50248
    s4114

    DrugBank DB12245
    CAS Number 68786-66-3
    PubChem Compound 50248
    KEGG Drug D07364
    ChEBI 94759