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. '
ID Source | ID |
---|---|
PubMed CID | 50248 |
CHEMBL ID | 1086440 |
CHEBI ID | 94759 |
SCHEMBL ID | 165712 |
MeSH ID | M0117690 |
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 |
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.
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.
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
A comparative pharmacokinetic study was conducted to determine the order and the rate of absorption of triclabendazole (TCBZ) in cattle and sheep.
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Triclabendazole (TCBZ) was more in buffaloes with mature flukes than with immature flukes.
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)
Class | Description |
---|---|
aromatic ether | Any 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 15.8114 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 37.9330 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 11.2202 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 50.1187 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
USP1 protein, partial | Homo sapiens (human) | Potency | 50.1187 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
TDP1 protein | Homo sapiens (human) | Potency | 24.7558 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 14.2191 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
AR protein | Homo sapiens (human) | Potency | 25.8425 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743054; AID743063 |
Smad3 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
PINK1 | Homo sapiens (human) | Potency | 50.1187 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 14.3179 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 15.8489 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 23.5786 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091 |
Parkin | Homo sapiens (human) | Potency | 50.1187 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
hepatitis C virus polyprotein | Potency | 88.6991 | 0.4445 | 10.4371 | 24.9988 | AID720575 | |
alpha-galactosidase | Homo sapiens (human) | Potency | 50.1187 | 4.4668 | 18.3916 | 35.4813 | AID1467 |
IDH1 | Homo sapiens (human) | Potency | 9.2000 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 19.3218 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 23.8675 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 23.7101 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 18.3564 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 39.8107 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 31.6228 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 35.4813 | 0.7943 | 21.2757 | 50.1187 | AID624246 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 10.6219 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
plasminogen precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 7.0795 | 0.1585 | 5.2879 | 12.5893 | AID540303 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 20.0409 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
geminin | Homo sapiens (human) | Potency | 11.2680 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
Vpr | Human immunodeficiency virus 1 | Potency | 12.5893 | 1.5849 | 19.6264 | 63.0957 | AID651644 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 36.1254 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 12.5893 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 17.8530 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
Alpha-synuclein | Homo sapiens (human) | Potency | 1.9953 | 0.5623 | 9.3985 | 25.1189 | AID652106 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 50.1187 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 2.2387 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 56.2341 | 3.9811 | 46.7448 | 112.2020 | AID720708 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 18.8336 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
Ataxin-2 | Homo sapiens (human) | Potency | 18.8336 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Transthyretin | Homo sapiens (human) | IC50 (µMol) | 3.5000 | 0.1600 | 4.2921 | 10.0000 | AID1774080 |
Cruzipain | Trypanosoma cruzi | IC50 (µMol) | 107.5000 | 0.0002 | 2.0450 | 8.0000 | AID484274; AID484275 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 (µMol) | 3.8100 | 0.0600 | 8.9128 | 130.5170 | AID1902; AID1914 |
Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 4.6950 | 0.0060 | 22.3670 | 130.5170 | AID1914 |
Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 (µMol) | 4.6950 | 0.0060 | 22.3670 | 130.5170 | AID1914 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
heat shock protein HSP 90-alpha isoform 2 | Homo sapiens (human) | AC50 | 4.2470 | 0.1950 | 3.6679 | 18.6960 | AID540270 |
heat shock protein 90, putative | Plasmodium falciparum 3D7 | AC50 | 6.4130 | 0.1950 | 4.9920 | 98.5000 | AID540268 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1774085 | Stabilization 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 method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1173747 | Antiparasitic activity against Fasciola hepatica assessed as mortality at 50 mg/L after 72 hrs relative to untreated control | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID490824 | Antitrichinellosis 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 control | 2010 | European 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. |
AID1173748 | Antiparasitic activity against Fasciola hepatica assessed as mortality at 10 mg/L after 72 hrs relative to untreated control | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID1173743 | Antiparasitic activity against Fasciola hepatica assessed as mortality at 50 mg/L after 24 hrs relative to untreated control | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1079935 | Cytolytic 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] | |||
AID1774080 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1774076 | Inhibition 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%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1173744 | Antiparasitic activity against Fasciola hepatica assessed as mortality at 10 mg/L after 24 hrs relative to untreated control | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID1774083 | Stabilization 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 method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID484275 | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Colloid formation by drugs in simulated intestinal fluid. |
AID1173742 | Aqueous stability of the compound assessed as time duration showing >95% compound stability at pH 7 and room temperature by UV-HPLC | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID490823 | Antitrichinellosis 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 control | 2010 | European 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. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1774078 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1173746 | Antiparasitic activity against Fasciola hepatica assessed as mortality at 10 mg/L after 48 hrs relative to untreated control | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID1774082 | Stabilization 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 control | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1774075 | Inhibition 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%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID484276 | Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 1% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Colloid formation by drugs in simulated intestinal fluid. |
AID1173741 | Aqueous solubility of the compound at pH 7 and 25 degC | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1079938 | Chronic 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] | |||
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID484383 | Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 10 uM by dynamic light scattering assay in presence of 1% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Colloid formation by drugs in simulated intestinal fluid. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID490825 | Antitrichinellosis 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 co | 2010 | European 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. |
AID1079931 | Moderate 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] | |||
AID1079936 | Choleostatic 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] | |||
AID1079933 | Acute 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 | |||
AID1173745 | Antiparasitic activity against Fasciola hepatica assessed as mortality at 50 mg/L after 48 hrs relative to untreated control | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | A highly water soluble benzimidazole derivative useful for the treatment of fasciolosis. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID1774081 | Stabilization 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 analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1774079 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID484274 | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Colloid formation by drugs in simulated intestinal fluid. |
AID1774087 | Tmax in human | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 32 (6.87) | 18.7374 |
1990's | 78 (16.74) | 18.2507 |
2000's | 115 (24.68) | 29.6817 |
2010's | 193 (41.42) | 24.3611 |
2020's | 48 (10.30) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (61.17) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 44 (8.85%) | 5.53% |
Reviews | 24 (4.83%) | 6.00% |
Case Studies | 103 (20.72%) | 4.05% |
Observational | 1 (0.20%) | 0.25% |
Other | 325 (65.39%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
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 4 | 300 participants (Anticipated) | Interventional | 2022-02-11 | Recruiting | ||
"Compassionate Use of Triclabendazole for the Treatment of Parasites (Prior to FDA Approval; Expanded Access Program)" [NCT01931085] | 0 participants | Expanded Access | No longer available | ||||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |