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triclabendazole

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Triclabendazole is a synthetic benzimidazole anthelmintic that is effective against a broad spectrum of helminths, including liver flukes, lungworms, and gastrointestinal nematodes. It is used in both human and veterinary medicine. Triclabendazole has a unique mode of action, inhibiting tubulin polymerization, which is essential for the formation of microtubules in helminths. This disruption leads to paralysis and eventual death of the parasites. The synthesis of triclabendazole involves multiple steps, including the condensation of 2-aminobenzimidazole with a substituted benzoyl chloride, followed by cyclization and reduction. Triclabendazole is widely studied due to its effectiveness against drug-resistant parasites, its potential for use in controlling zoonotic infections, and its importance in animal health and food security. The drug has been shown to be effective in treating fascioliasis, a parasitic disease caused by the liver fluke Fasciola hepatica, in both humans and livestock. Triclabendazole has also been found to be effective against other important parasites, such as Dicrocoelium dendriticum, Paramphistomum cervi, and Haemonchus contortus. '

Cross-References

ID SourceID
PubMed CID50248
CHEMBL ID1086440
CHEBI ID94759
SCHEMBL ID165712
MeSH IDM0117690

Synonyms (113)

Synonym
AKOS005439340
HMS3393E16
5-chloro-6-(2,3-dichlorophenoxy)-2-(methylthio)-1h-benzimidazole
triclabendazolum [inn-latin]
triclabendazol [inn-spanish]
ccris 8988
6-chloro-5-(2,3-dichlorophenoxy)-2-methylthio-benzimidazole
5-chloro-6-(2,3-dichlorophenoxy)-2-(methylthio)benzimidazole
1h-benzimidazole, 5-chloro-6-(2,3-dichlorophenoxy)-2-(methylthio)-
cga 89317
6-chloro-5-(2,3-dichlorophenoxy)-2-methylthiobenzimidazole
egaten (tn)
D07364
fasinex (tn)
triclabendazole (usan/inn)
68786-66-3
OPREA1_236106
triclabendazole ,
fasinex
egaten
cga-89317
MLS001424101 ,
MLS000759473
smr000466357
cpd000466357 ,
NCGC00164610-01
MLS000876812
STK332284
6-chloro-5-(2,3-dichlorophenoxy)-2-(methylsulfanyl)-1h-benzimidazole
AC-7627
HMS2051E16
KUC103451N
ega230b
CHEMBL1086440 ,
nvp-ega230
nsc-759250
6-chloro-5-(2,3-dichlorophenoxy)-2-methylsulfanyl-1h-benzimidazole
6-chloro-5-(2,3-dichlorophenoxy)-2-methylsulfanyl-1h-benzimidazole;triclabendazole
A836250
NCGC00164610-02
T2826
6-chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)benzimidazole
1h-benzimidazole, 6-chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)-
triclabendazole [usan:inn:ban]
triclabendazolum
unii-4784c8e03o
4784c8e03o ,
triclabendazol
nsc 759250
dtxsid7043952 ,
dtxcid5023952
tox21_112231
cas-68786-66-3
nsc759250
pharmakon1600-01505786
AKOS015950804
HMS2232D14
S4114
CCG-100881
6-chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)-1h-benzo[d]imidazole
FT-0602564
HMS3370H02
triclabendazole [orange book]
triclabendazole [usan]
triclabendazole [mi]
triclabendazole [inn]
triclabendazole [who-dd]
triclabendazole [mart.]
HY-B0621
AB00639964-10
NC00131
SCHEMBL165712
KS-5329
NQPDXQQQCQDHHW-UHFFFAOYSA-N
6-chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)-1h-benzimidazole
5-[2,3-bis(chloranyl)phenoxy]-6-chloranyl-2-methylsulfanyl-1h-benzimidazole
bdbm58491
cid_50248
AB00639964_12
AB00639964_13
5-chloro-6-(2',3'-dichlorophenoxy)-2-(methylthio)benzimidazole
mfcd00864519
cga89317
SR-01000759363-4
sr-01000759363
6-chloro-5-(2,3-dichlorophenoxy)-2-(methylsulfanyl)-1h-1,3-benzodiazole
triclabendazole, vetranal(tm), analytical standard
CHEBI:94759
HMS3652M16
triclabendazole for system suitability, europepharmacopoeia (ep) reference standard
triclabendazole, europepharmacopoeia (ep) reference standard
SBI-0207022.P001
HMS3715P16
SW197511-2
DB12245
5-chloro-6-(2,3-dichlorophenoxy)-2-(methylthio)-1h-benzo[d]imidazole
Q419739
triclabendazole 100 microg/ml in acetonitrile
5-chloro-6-(2,3-dichlorophenoxy)-2-(methylsulfanyl)-1h-1,3-benzodiazole
BRD-K81916719-001-05-5
SB17173
HMS3744I09
CCG-268150
AT10531
6-[2,3-bis(chloranyl)phenoxy]-5-chloranyl-2-methylsulfanyl-1h-benzimidazole
JA9 ,
Z3069281092
triclabendazole (mart.)
triclabendazol (inn-spanish)
triclabendazole micronized
triclabendazolum (inn-latin)
p02bx04
6-chloro-2-(methylsulfanyl)-1h-1,3-benzimidazol-5-yl (2,3-dichlorophenyl) ether

Research Excerpts

Overview

Triclabendazole (TCBZ) is a benzimidazole used to treat fasciolosis in adults and children. It is a poorly-water soluble (0.24 μg/mL) compound classified into the Class II/IV of the Biopharmaceutical Classification System.

ExcerptReferenceRelevance
"Triclabendazole (TCBZ) is a benzimidazole used to treat fasciolosis in adults and children."(
Borges, BS; Bueno, GP; Figueiredo, FB; Soares Medeiros, LC; Tomiotto-Pellissier, F, 2022
)
1.44
"Triclabendazole is an effective and well-tolerated treatment for human fascioliasis. "( Effects of triclabendazole and its metabolite exposure on the heart-rate-corrected QT intervals: A randomized, placebo- and positive-controlled thorough QT study in healthy individuals.
Gray, C; Iyer, GR; Lecot, J; Prince, WT; Shakeri-Nejad, K; Taylor, A; Venishetty, VK; Zack, J, 2023
)
2.74
"Triclabendazole is a poorly-water soluble (0.24 μg/mL) compound classified into the Class II/IV of the Biopharmaceutical Classification System. "( Chitosan-based nanodelivery systems applied to the development of novel triclabendazole formulations.
Goycoolea, FM; Hoffmann, S; Leonardi, D; Real, D; Salomon, C, 2018
)
2.16
"Triclabendazole is a flukicide used in the treatment of liver fluke in cattle. "( Investigation of the persistence of triclabendazole residues in bovine milk following lactating-cow and dry-cow treatments.
Bloemhoff, Y; Danaher, M; Furey, A; Jordan, K; O'Brien, B; Power, C; Sayers, R; Whelan, M, 2013
)
2.11
"Triclabendazole (TCB) is a flukicide used in the treatment of liver fluke in cattle; however, its use is currently prohibited in lactating dairy cows. "( Investigation of the migration of triclabendazole residues to milk products manufactured from bovine milk, and stability therein, following lactating cow treatment.
Clancy, C; Danaher, M; Furey, A; Jordan, K; O'Brien, B; Power, C; Sayers, R, 2013
)
2.11
"Triclabendazole (TCBZ) is an efficient fasciolicide that affects both juvenile and adult worms. "( Detoxifying and anti-oxidant enzymes of Fasciola gigantica worms under triclabendazole sulphoxide (TCBZ-SX): an in vitro study.
Ebeid, SM; El-Samak, MY; Hussein, NM; Shehab, AY, 2009
)
2.03
"Triclabendazole (TCBZ) is a flukicidal halogenated benzimidazole compound extensively used in veterinary medicine. "( Residual concentrations of the flukicidal compound triclabendazole in dairy cows' milk and cheese.
Alvarez, L; Cabrera, M; Farias, C; Iezzi, S; Imperiale, F; Lanusse, C; Ortiz, P; Pérez, J; Sallovitz, JM, 2011
)
2.06
"Triclabendazole is an intriguing case in which tautomeric and conformational variations co-exist in the polymorphs."( Triclabendazole: an intriguing case of co-existence of conformational and tautomeric polymorphism.
Bhogala, BR; Desiraju, GR; Gorantla, AR; Jetti, RK; Thakur, TS; Tothadi, S, 2012
)
2.54
"Triclabendazole is an halogenated benzimidazole anthelmintic with potent flukicidal activity."( Measurement of triclabendazole and its metabolites in liver flukes: method development and full validation.
Alvarez, L; Lanusse, C; Moreno, L; Mottier, L; Virkel, G, 2004
)
1.4
"Triclabendazole (TCBZ) is an halogenated trematodicidal benzimidazole compound extensively used in veterinary medicine. "( Triclabendazole biotransformation and comparative diffusion of the parent drug and its oxidized metabolites into Fasciola hepatica.
Alvarez, L; Lanusse, C; Mottier, L; Salles, J; Solana, H; Virkel, G,
)
3.02
"Triclabendazole (TCBZ) is a halogenated benzimidazole compound that possesses high activity against immature and adult stages of the liver fluke, Fasciola hepatica. "( Altered drug influx/efflux and enhanced metabolic activity in triclabendazole-resistant liver flukes.
Alvarez, LI; Fairweather, I; Lanusse, CE; Mottier, ML; Solana, HD; Virkel, GL, 2005
)
2.01
"Triclabendazole (TCBZ) is an halogenated benzimidazole (BZD) compound worldwide used to control immature and adult stages of the liver fluke Fasciola hepatica. "( Assessment of the main metabolism pathways for the flukicidal compound triclabendazole in sheep.
Lanusse, C; Lifschitz, A; Pis, A; Sallovitz, J; Virkel, G, 2006
)
2.01
"Triclabendazole 20 mg/kg is an effective therapy for the treatment of F."( The efficacy and tolerability of triclabendazole in Cuban patients with latent and chronic Fasciola hepatica infection.
Freise, S; Millán, JC; Mull, R; Richter, J,
)
1.13

Effects

Triclabendazole (TCBZ) has been used for decades as a broad spectrum anthelmintic to control this perilous disease. emergence of resistance in flukes against TCBZ has prompted researchers across the world to explore for new drugs and antigenic targets.

ExcerptReferenceRelevance
"Triclabendazole (TBD) has been widely used in the treatment of helminthic infection. "( Inhibition of Staphylococcus aureus and biofilm formation by the anthelminthic drug, triclabendazole.
Chen, C; Cheng, H; Deng, Q; Guo, J; Li, D; Wang, Z; Wen, Z; Yu, Z; Zhang, Y, 2022
)
2.39
"The triclabendazole (TCBZ) has been used for decades as a broad spectrum anthelmintic to control this perilous disease but the emergence of resistance in flukes against TCBZ has prompted researchers across the world to explore for new drugs and antigenic targets."( Characterization of Monoamine Oxidase-A in tropical liver fluke, Fasciola gigantica.
Abidi, SMA; Beg, MA; Farhat, F; Rehman, A; Rehman, L; Ullah, R; Wasim, S, 2023
)
1.39
"Triclabendazole has the anthelmintic effect on the adults as well as eggs of Fasciola gigantica."( [Comparison between albendazole and triclabendazole against Fasciola gigantica in human].
Chen, F; Fang, W; Liu, HK; Yang, L; Yang, Q, 2014
)
1.4
"Triclabendazole has marked therapeutic effect on paragonimiasis skrjabini. "( [A clinical trial of triclabendazole in the treatment of human paragonimiasis skrjabini].
Hu, P; Liu, YH, 2001
)
2.07
"Triclabendazole (TCBZ) has been the drug of choice to treat liver fluke infections in livestock for >20 years, due to its high activity against both adult and juvenile flukes. "( Understanding triclabendazole resistance.
Alvarez, L; Brennan, GP; Brophy, PM; Fairweather, I; Hoey, E; Lanusse, C; McConville, M; McFerran, N; Meaney, M; Mottier, L; Robinson, M; Ryan, L; Solana, H; Trudgett, A; Virkel, G, 2007
)
2.14

Treatment

The treatment with Triclabendazole (Egaten(®) for two days with a total dosage of 2000 mg was followed by a remarkable recovery of the patient's symptoms and decrease of eosinophilia in the blood count. Treatment with triclab endazole is effective, but resistance is emerging in livestock and may pose a threat for patients.

ExcerptReferenceRelevance
"The treatment with Triclabendazole (Egaten(®)) for two days with a total dosage of 2000 mg was followed by a remarkable recovery of the patient's symptoms and decrease of eosinophilia in the blood count just one month after treatment and normalization after four months."( [Multiple liver lesions accompanied by eosinophilia - a case report of fascioliosis].
Auer, H; Haller, J; Klaushofer, K; Mikosch, P; Osterreicher, C; Spenger, J; Trifina, E; Zandieh, S, 2011
)
0.69
"Treatment with triclabendazole is effective, but resistance is emerging in livestock and may pose a threat for patients."( New developments in epidemiology, diagnosis, and treatment of fascioliasis.
Cabada, MM; White, AC, 2012
)
0.72
"Treatment with triclabendazole, by eliminating most of these flukes, largely reduced haematological alterations."( Triclabendazole treatment in experimental goat fasciolosis: anthelmintic efficacy and influence in antibody response and pathophysiology of the disease.
Becerra, C; Hernández, S; Jiménez, V; Martínez-Cruz, MS; Martínez-Moreno, A; Martínez-Moreno, FJ, 1997
)
2.08

Toxicity

ExcerptReferenceRelevance
" Interviews to assess the occurrence of adverse events were conducted on treatment day, one week later, and one month after treatment."( Administration of triclabendazole is safe and effective in controlling fascioliasis in an endemic community of the Bolivian Altiplano.
Angles, R; Ault, SK; Barrientos, R; Barrios, G; Engels, D; Gabrielli, AF; Grueninger, H; Hamed, K; Mas-Coma, S; Montresor, A; Valero, MA; Villegas, F, 2012
)
0.71
" Adverse events were infrequent and mild."( Administration of triclabendazole is safe and effective in controlling fascioliasis in an endemic community of the Bolivian Altiplano.
Angles, R; Ault, SK; Barrientos, R; Barrios, G; Engels, D; Gabrielli, AF; Grueninger, H; Hamed, K; Mas-Coma, S; Montresor, A; Valero, MA; Villegas, F, 2012
)
0.71
"Administration of triclabendazole is a feasible, safe and efficacious public health intervention in an endemic community in the Bolivian Altiplano, suggesting that preventive chemotherapy can be applied to control of fascioliasis."( Administration of triclabendazole is safe and effective in controlling fascioliasis in an endemic community of the Bolivian Altiplano.
Angles, R; Ault, SK; Barrientos, R; Barrios, G; Engels, D; Gabrielli, AF; Grueninger, H; Hamed, K; Mas-Coma, S; Montresor, A; Valero, MA; Villegas, F, 2012
)
1.05

Pharmacokinetics

A comparative pharmacokinetic study was conducted to determine the order and the rate of absorption of triclabendazole (TCBZ) in cattle and sheep.

ExcerptReferenceRelevance
" The pharmacokinetic behaviour of triclabendazole was not altered in animals with fascioliasis."( Pharmacokinetics and efficacy of triclabendazole in goats with induced fascioliasis.
Bogan, JA; Kinabo, LD, 1988
)
0.84
" Pharmacokinetic profiles of triclabendazole (TCBZ) following intravenous (i."( Pharmacokinetics of triclabendazole in rabbits.
Alvarez-Bujidos, ML; Cubría, JC; Negro, A; Ordóñez, D; Ortiz, AI, 1993
)
0.9
"Fasioliasis as an infective condition widely spread in Egypt has no significant effect on the pharmacokinetic parameters of the orally administered TCBZ and at the same time it is very effective against the parasite which strongly and safely suggests the use of this medication for the treatment of this infection."( Effect of Fascioliasis on the pharmacokinetic parameters of triclabendazole in human subjects.
El-Tantawy, WH; Mohammed Safwat, NA; Salem, HF, 2007
)
0.58
"A comparative pharmacokinetic study was conducted to determine the order and the rate of absorption of triclabendazole (TCBZ) in cattle and sheep."( Pharmacokinetic disposition of triclabendazole in cattle and sheep; discrimination of the order and the rate of the absorption process of its active metabolite triclabendazole sulfoxide.
Errecalde, JO; Fernandez, C; Formentini, EA; Hernández, EM; Lucas, MF; Mestorino, N; Modamio, P, 2008
)
0.85
" Only the Test I formulation did not differ from the RF for all pharmacokinetic parameters measured for either metabolite (p>0."( Pharmacokinetic evaluation of different generic triclabendazole formulations in heifers.
Alvarez, L; Cabrera, M; Castope, N; Farias, C; Lanusse, C; Ortiz, P; Suarez, G, 2014
)
0.66

Compound-Compound Interactions

The aim of the present study was to investigate the effect of triclabendazole (CAS 68786-66-3) therapy alone or in combination with ascorbic acid (vitamin C, CAS 50-81-7) and tocofersolan (Vitamin E, CAS 30999-06-5) in Fasciola hepatica patients.

ExcerptReferenceRelevance
"The aim of the present study was to investigate the effect of triclabendazole (CAS 68786-66-3) therapy alone or in combination with ascorbic acid (vitamin C, CAS 50-81-7) and tocofersolan (vitamin E, CAS 30999-06-5), in Fasciola hepatica patients, on Lipo-peroxidation (LPO) and blood antioxidant capacity."( Antioxidant capacity in Fasciola hepatica patients before and after treatment with triclabendazole alone or in combination with ascorbic acid (vitamin C) and tocofersolan (vitamin E).
el-Toukhy, MA; Fouad, HN; Hishmat, M; Rawash, NA; Rehim, WM; Sharaf, IA, 2003
)
0.78
"The use of polypharmacy in the present day clinical therapy has made the identification of clinical drug-drug interaction risk an important aspect of drug development process."( In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone.
Giri, P; Giri, S; Gupta, L; Joshi, V; Naidu, S; Patel, N; Srinivas, NR, 2018
)
0.7
"In vitro drug-drug interaction potential of test compounds was investigated in two stages; 1) assessment of CYP450 inhibition potential of test compounds using human liver microsomes (HLM); and 2) assessment of test compounds as substrate of Phase I enzymes; including CYP450, FMO, AO and MAO using HLM, recombinant human CYP enzymes (rhCYP), Human Liver Cytosol (HLC) and Human Liver Mitochondrial (HLMit)."( In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone.
Giri, P; Giri, S; Gupta, L; Joshi, V; Naidu, S; Patel, N; Srinivas, NR, 2018
)
0.7
", perpetrator and/or victim drug) to overcome any imminent risk of potential clinical drug-drug interaction when sulfoxide/sulfone metabolite(s) generating drugs are coadministered in therapy."( In Vitro Drug-Drug Interaction Potential of Sulfoxide and/or Sulfone Metabolites of Albendazole, Triclabendazole , Aldicarb, Methiocarb, Montelukast and Ziprasidone.
Giri, P; Giri, S; Gupta, L; Joshi, V; Naidu, S; Patel, N; Srinivas, NR, 2018
)
0.7

Bioavailability

Triclabendazole (TCBZ) was more in buffaloes with mature flukes than with immature flukes.

ExcerptReferenceRelevance
" Bioavailability of triclabendazole was more in buffaloes with mature flukes than with immature flukes."( Efficacy and pharmacokinetics of triclabendazole in buffalo with induced fasciolosis.
Gupta, SC; Sanyal, PK, 1996
)
0.9
"A comparative pharmacokinetic study was conducted to determine the order and the rate of absorption of triclabendazole (TCBZ) in cattle and sheep."( Pharmacokinetic disposition of triclabendazole in cattle and sheep; discrimination of the order and the rate of the absorption process of its active metabolite triclabendazole sulfoxide.
Errecalde, JO; Fernandez, C; Formentini, EA; Hernández, EM; Lucas, MF; Mestorino, N; Modamio, P, 2008
)
0.85
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Triclabendazole belongs to the class II/IV of the Biopharmaceuticals Classification System. Its low aqueous solubility represents a major drawback during the development of effective dosage forms. Triclab endazole was effective only at the screening dosage (40 g per kg of feed for 10 d)

ExcerptRelevanceReference
" Triclabendazole was administered to cows in a dosage of approximately 12 mg kg-1."( [Triclabendazole (Fasinex) residue in milk: determination and excretion kinetics].
Counotte, GH; Hasselt, H; Redder, B; Reimink, A, 1990
)
2.1
"A restricted programme of strategic dosing with triclabendazole was used to treat a sheep flock with severe clinical fascioliasis."( A study of a restricted programme of strategic dosing against Fasciola hepatica with triclabendazole.
Fawcett, AR, 1990
)
0.76
" Ten deer were given a 5% suspension of triclabendazole orally at a dosage of 10 mg/kg body weight and 10 deer were given a placebo."( Efficacy of triclabendazole against fascioloidiasis (Fascioloides magna) in naturally infected white-tailed deer (Odocoileus virginianus).
Craig, TM; Davis, DS; Drawe, DL; Qureshi, T, 1989
)
0.92
" Calves given triclabendazole (either dosage level) had a 100% reduction in F hepatica burden as compared with the untreated controls."( Efficacy of triclabendazole against Fasciola hepatica and Fascioloides magna in naturally infected calves.
Craig, TM; Huey, RL, 1984
)
1.01
"Groups of parasite-free lambs which were either housed and fed hay and concentrates or were grazing on pasture were dosed with the oral flukicides rafoxanide and triclabendazole and subsequent plasma concentrations monitored."( Effects of dietary variations on plasma concentrations of oral flukicides in sheep.
Blanchflower, J; Hewitt, SA; Kennedy, DG; Mallon, TR; Taylor, SM, 1993
)
0.48
"This study examined the effectiveness of a strategic dosing scheme in lowering the incidence of fasciolosis on a mixed dry-stock farm and in maintaining the reduced incidence following a reduction in dosing intensity."( A strategic dosing scheme for the control of fasciolosis in cattle and sheep in Ireland.
Gray, JS; Parr, SL, 2000
)
0.31
" One month and two months after infection, the infected rats were treated with triclabendazole at the total dosage of 300 mg/kg over 2 days, 450 mg/kg over 3 days and 600 mg/kg over 3 days, respectively."( [Experimental therapy of Pagumogonimus skrjabini infection in rats with triclabendazole].
Gao, J; Liu, C; Liu, Y; Su, Q; Wang, X; Yu, D, 1999
)
0.76
"Four patients were treated with triclabendazole at dosage of 10 mg/kg bid for 3 days and were followed up for 6-10 months."( [A clinical trial of triclabendazole in the treatment of human paragonimiasis skrjabini].
Hu, P; Liu, YH, 2001
)
0.91
" One and two months after infection, they were treated with triclabendazole at the dosage of 300 mg."( Triclabendazole in the treatment of Paragonimiasis skrjabini.
Gao, J; Hu, P; Liu, Y; Wang, X, 2003
)
2
" For the in vivo experiment, rats were dosed with TCBZ (6."( Fasciola hepatica: morphological effects of a combination of triclabendazole and clorsulon against mature fluke.
Allister, J; Brennan, GP; Fairweather, I; Forbes, AB; McKinstry, B; McLaughlin, K; Meaney, M, 2006
)
0.58
" Anthelmintic dosing occurred at 4 weeks post-infection with 10 mg/kg triclabendazole."( Tegumental surface changes in juvenile Fasciola hepatica in response to treatment in vivo with triclabendazole.
Brennan, GP; Edgar, HW; Fairweather, I; Halferty, L; Hanna, RE; Hoey, L; McConville, M; Meaney, MM; Trudgett, A, 2008
)
0.8
" hepatica, dosed orally with artemether at a concentration of 200 mg/kg and flukes recovered at 24, 48 and 72 h post-treatment (p."( Adult triclabendazole-resistant Fasciola hepatica: morphological changes in the tegument and gut following in vivo treatment with artemether in the rat model.
Brennan, GP; Fairweather, I; Halferty, L; Johnston, RC; Keiser, J; O'Neill, JF, 2009
)
0.83
" At 12 weeks post-infection, sheep were dosed with 10mg/kg triclabendazole."( Tegumental surface changes in adult Fasciola hepatica in response to treatment in vivo with triclabendazole in the sheep host.
Brennan, GP; Edgar, HW; Fairweather, I; Hanna, RE; Toner, E, 2010
)
0.82
" Negative binomial regressions of worm and egg counts were used to analyze dose-response relationships and whether the effects of drug combinations were synergistic or antagonistic."( In vivo and in vitro sensitivity of Fasciola hepatica to triclabendazole combined with artesunate, artemether, or OZ78.
Duthaler, U; Keiser, J; Smith, TA, 2010
)
0.61
" At 12 weeks post-infection, sheep were dosed with 10mg/kg triclabendazole."( Time-dependent changes to the tegumental system and gastrodermis of adult Fasciola hepatica following treatment in vivo with triclabendazole in the sheep host.
Brennan, GP; Edgar, HW; Fairweather, I; Hanna, RE; Toner, E, 2010
)
0.81
" The first group was dosed orally with TCBZ at a dosage of 10mg/kg and KTZ at a dosage of 10mg/kg."( Enhancement of triclabendazole action in vivo against a triclabendazole-resistant isolate of Fasciola hepatica by co-treatment with ketoconazole.
Alvarez, LI; Brennan, GP; Devine, C; Fairweather, I; Hoey, E; Lanusse, CE; Trudgett, A, 2011
)
0.72
" hepatica, dosed orally with triclabendazole at a dosage of 10mg/kg live weight and ketoconazole at a dosage of 10mg/kg live weight."( Potentiation of triclabendazole action in vivo against a triclabendazole-resistant isolate of Fasciola hepatica following its co-administration with the metabolic inhibitor, ketoconazole.
Alvarez, LI; Brennan, GP; Devine, C; Fairweather, I; Hoey, E; Lanusse, CE; Trudgett, A, 2012
)
1.02
"Lambs infected with the Cullompton triclabendazole (TCBZ)-susceptible isolate of Fasciola hepatica were treated with TCBZ at a dosage of 10mg/kg at 16 weeks post-infection."( Early onset of changes to the reproductive system of Fasciola hepatica following in vivo treatment with triclabendazole.
Fairweather, I; Hanna, RE; McConnell, S; Scarcella, S; Solana, H, 2012
)
0.87
" The treatment with Triclabendazole (Egaten(®)) for two days with a total dosage of 2000 mg was followed by a remarkable recovery of the patient's symptoms and decrease of eosinophilia in the blood count just one month after treatment and normalization after four months."( [Multiple liver lesions accompanied by eosinophilia - a case report of fascioliosis].
Auer, H; Haller, J; Klaushofer, K; Mikosch, P; Osterreicher, C; Spenger, J; Trifina, E; Zandieh, S, 2011
)
0.69
" TCBZ treatment failure was noted on both farms, despite accurate weighing of animals and dosing of treatment products."( On farm evaluation of the coproantigen ELISA and coproantigen reduction test in Scottish sheep naturally infected with Fasciola hepatica.
Gordon, DK; Sargison, ND; Skuce, PJ; Stevenson, H; Zadoks, RN, 2012
)
0.38
" Ovicidal activity of ABZ against Fasciola eggs in isolates from both farms and one additional bovine isolate were tested by FEHT to exclude the presence of juvenile flukes and other factors such as dosing failure and poor quality of drug product."( Assessment of flukicide efficacy against Fasciola hepatica in sheep in Sweden in the absence of a standardised test.
Amaya Solis, N; Höglund, J; Novobilský, A; Skarin, M, 2016
)
0.43
"Triclabendazole belongs to the class II/IV of the Biopharmaceuticals Classification System, and its low aqueous solubility represents a major drawback during the development of effective dosage forms."( Improving the Dissolution of Triclabendazole from Stable Crystalline Solid Dispersions Formulated for Oral Delivery.
Leonardi, D; Orzan, L; Real, D; Salomon, CJ, 2019
)
2.25
" As currently TBZ is prescribed on a weight-based dosage regimen, it is imperative to develop a dose-customizable fast dissolving pediatric formulation."( Development of a safe pediatric liquisolid self-nanoemulsifying system of triclabendazole for the treatment of fascioliasis.
Daware, S; Palekar, S; Patel, K; Patki, M; Saraswat, A, 2022
)
0.95
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (47)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.81140.140911.194039.8107AID2451
LuciferasePhotinus pyralis (common eastern firefly)Potency37.93300.007215.758889.3584AID588342
glp-1 receptor, partialHomo sapiens (human)Potency11.22020.01846.806014.1254AID624417
phosphopantetheinyl transferaseBacillus subtilisPotency50.11870.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency50.11870.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency24.75580.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency14.21910.180013.557439.8107AID1460; AID1468
AR proteinHomo sapiens (human)Potency25.84250.000221.22318,912.5098AID743035; AID743054; AID743063
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
PINK1Homo sapiens (human)Potency50.11872.818418.895944.6684AID624263
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency14.31790.000214.376460.0339AID720691; AID720692; AID720719
pregnane X nuclear receptorHomo sapiens (human)Potency15.84890.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency23.57860.000229.305416,493.5996AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091
ParkinHomo sapiens (human)Potency50.11870.819914.830644.6684AID624263
hepatitis C virus polyproteinPotency88.69910.444510.437124.9988AID720575
alpha-galactosidaseHomo sapiens (human)Potency50.11874.466818.391635.4813AID1467
IDH1Homo sapiens (human)Potency9.20000.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.32180.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency23.86750.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency23.71010.001723.839378.1014AID743083
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency18.35640.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency39.81073.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency31.62280.01789.637444.6684AID588834
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency35.48130.794321.275750.1187AID624246
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.62190.000323.4451159.6830AID743065; AID743067
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency20.04090.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency11.26800.004611.374133.4983AID624296
VprHuman immunodeficiency virus 1Potency12.58931.584919.626463.0957AID651644
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.12540.005612.367736.1254AID624032
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.58930.015812.3113615.5000AID1461
Cellular tumor antigen p53Homo sapiens (human)Potency17.85300.002319.595674.0614AID651631; AID720552
Alpha-synucleinHomo sapiens (human)Potency1.99530.56239.398525.1189AID652106
Guanine nucleotide-binding protein GHomo sapiens (human)Potency50.11871.995325.532750.1187AID624288
TAR DNA-binding protein 43Homo sapiens (human)Potency2.23871.778316.208135.4813AID652104
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency56.23413.981146.7448112.2020AID720708
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency18.83360.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency18.83360.011912.222168.7989AID651632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TransthyretinHomo sapiens (human)IC50 (µMol)3.50000.16004.292110.0000AID1774080
CruzipainTrypanosoma cruziIC50 (µMol)107.50000.00022.04508.0000AID484274; AID484275
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)3.81000.06008.9128130.5170AID1902; AID1914
Estrogen receptorRattus norvegicus (Norway rat)EC50 (µMol)4.69500.006022.3670130.5170AID1914
Estrogen receptor betaRattus norvegicus (Norway rat)EC50 (µMol)4.69500.006022.3670130.5170AID1914
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)AC504.24700.19503.667918.6960AID540270
heat shock protein 90, putativePlasmodium falciparum 3D7AC506.41300.19504.992098.5000AID540268
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (241)

Processvia Protein(s)Taxonomy
signal transductionTransthyretinHomo sapiens (human)
purine nucleobase metabolic processTransthyretinHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (72)

Processvia Protein(s)Taxonomy
hormone activityTransthyretinHomo sapiens (human)
protein bindingTransthyretinHomo sapiens (human)
identical protein bindingTransthyretinHomo sapiens (human)
thyroid hormone bindingTransthyretinHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (48)

Processvia Protein(s)Taxonomy
extracellular regionTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
azurophil granule lumenTransthyretinHomo sapiens (human)
extracellular exosomeTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (62)

Assay IDTitleYearJournalArticle
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1774085Stabilization of TTR V142I mutant (unknown origin) expressed in Escherichia coli assessed as reduction in trypsin-induced aggregation incubated for 3 to 4 days by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1173747Antiparasitic activity against Fasciola hepatica assessed as mortality at 50 mg/L after 72 hrs relative to untreated control2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID490824Antitrichinellosis activity against adult phase of Trichinella spiralis ML infected in mouse assessed as reduction of parasites level at 75 mg/kg administered 3 days after postinfection measured after 6 days relative to control2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological activity of 2-(trifluoromethyl)-1H-benzimidazole derivatives against some protozoa and Trichinella spiralis.
AID1173748Antiparasitic activity against Fasciola hepatica assessed as mortality at 10 mg/L after 72 hrs relative to untreated control2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID1173743Antiparasitic activity against Fasciola hepatica assessed as mortality at 50 mg/L after 24 hrs relative to untreated control2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1774080Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1774076Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1173744Antiparasitic activity against Fasciola hepatica assessed as mortality at 10 mg/L after 24 hrs relative to untreated control2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID1774083Stabilization of wild type TTR (unknown origin) expressed in Escherichia coli assessed as reduction in methanol-induced aggregation at 50 uM incubated for 60 min by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID484275Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-1002010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1173742Aqueous stability of the compound assessed as time duration showing >95% compound stability at pH 7 and room temperature by UV-HPLC2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID490823Antitrichinellosis activity against adult phase of Trichinella spiralis ML infected in mouse assessed as reduction of parasites level at 50 mg/kg administered 3 days after postinfection measured after 6 days relative to control2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological activity of 2-(trifluoromethyl)-1H-benzimidazole derivatives against some protozoa and Trichinella spiralis.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1774078Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1173746Antiparasitic activity against Fasciola hepatica assessed as mortality at 10 mg/L after 48 hrs relative to untreated control2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID1774082Stabilization of TTR V3OM mutant (unknown origin) assessed as suppression of TTR tetramer dissociation at 3 uM incubated for 9 days by glutaraldehyde cross-linking assay based SDS-PAGE analysis relative to control2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1774075Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID484276Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1173741Aqueous solubility of the compound at pH 7 and 25 degC2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID484383Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 10 uM by dynamic light scattering assay in presence of 1% DMSO2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID490825Antitrichinellosis activity against muscle larvae pahse of Trichinella spiralis ML larvae infected in mouse assessed as reduction of parasites level at 75 mg/kg administered for 7 consecutive days from day 28 postinfection measured on day 7 relative to co2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Synthesis and biological activity of 2-(trifluoromethyl)-1H-benzimidazole derivatives against some protozoa and Trichinella spiralis.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1173745Antiparasitic activity against Fasciola hepatica assessed as mortality at 50 mg/L after 48 hrs relative to untreated control2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1774081Stabilization of TTR V3OM mutant (unknown origin) assessed as suppression of TTR tetramer dissociation at 1 to 10 uM incubated for 9 days by glutaraldehyde cross-linking assay based SDS-PAGE analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1774079Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID484274Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-1002010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Colloid formation by drugs in simulated intestinal fluid.
AID1774087Tmax in human2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (466)

TimeframeStudies, This Drug (%)All Drugs %
pre-199032 (6.87)18.7374
1990's78 (16.74)18.2507
2000's115 (24.68)29.6817
2010's193 (41.42)24.3611
2020's48 (10.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 61.17

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index61.17 (24.57)
Research Supply Index6.30 (2.92)
Research Growth Index4.94 (4.65)
Search Engine Demand Index105.66 (26.88)
Search Engine Supply Index2.04 (0.95)

This Compound (61.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials44 (8.85%)5.53%
Reviews24 (4.83%)6.00%
Case Studies103 (20.72%)4.05%
Observational1 (0.20%)0.25%
Other325 (65.39%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase IV, Multi-center, Open-label Study to Determine the Safety, Tolerability and Clinical Outcomes Following Oral Administration of EGATEN™ (Triclabendazole) in Patients (6 Years of Age or Older) With Fascioliasis. [NCT04230148]Phase 4300 participants (Anticipated)Interventional2022-02-11Recruiting
"Compassionate Use of Triclabendazole for the Treatment of Parasites (Prior to FDA Approval; Expanded Access Program)" [NCT01931085]0 participants Expanded AccessNo longer available
[information is prepared from clinicaltrials.gov, extracted Sep-2024]