Page last updated: 2024-11-06

flubendazole

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Description

Flubendazole is a benzimidazole anthelmintic drug that was first synthesized in 1973. It acts by inhibiting the polymerization of tubulin, a protein that is essential for the formation of microtubules. Microtubules are involved in a variety of cellular processes, including cell division, migration, and intracellular transport. By inhibiting tubulin polymerization, flubendazole prevents the formation of microtubules, which disrupts these cellular processes and ultimately leads to the death of the parasite. Flubendazole is used to treat a variety of parasitic infections, including infections caused by roundworms, tapeworms, and flukes. It is also used to treat some types of cancer. Flubendazole is generally well-tolerated, but it can cause side effects such as nausea, vomiting, and diarrhea. Research on flubendazole continues to focus on its potential to treat a wider range of parasitic infections, as well as its potential to treat cancer. '

flubendazole: the p-fluoro analog of mebendazole [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

flubendazole : A member of the class of mebendazole in which the benzoyl group is replaced by a p-fluorobenzoyl group. A broad-spectrum anthelmintic, it is used, particularly in veterinary medicine, for the treatment of nematodal infections. [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]

Cross-References

ID SourceID
PubMed CID35802
CHEMBL ID1454946
CHEBI ID77095
SCHEMBL ID167185
MeSH IDM0070980

Synonyms (115)

Synonym
methyl [5-(4-fluorobenzoyl)-1h-benzimidazol-2-yl]carbamate
HMS3393A18
AB00639981-08
methyl n-[5-(4-fluorobenzoyl)-1h-benzimidazol-2-yl]carbamate
n-{5-[(4-fluorophenyl)carbonyl]benzimidazol-2-yl}methyloxymethanamide
flicum
methyl {6-[(4-fluorophenyl)carbonyl]-1h-benzimidazol-2-yl}carbamate
flubenol
nsc-313680
r 17899
fluvermal
flubendazole
r 17,889
methyl 5-(p-fluorobenzoyl)-2-benzimidazolecarbamate
31430-15-6
nsc313680
c16h12fn3o3
ccris 4480
fluoromebendazole
methyl n-(5-(p-fluorobenzoyl)-2-benzimidazolyl)carbamate
(5-(4-fluorobenzoyl)-1h-benzimidazole-2-yl)carbamic acid methyl ester
2-benzimidazolecarbamic acid, 5-(p-fluorobenzoyl)-, methyl ester
carbamic acid, (5-(4-fluorobenzoyl)-1h-benzimidazol-2-yl)-, methyl ester
nsc 313680
flumoxal
flubendazolum [inn-latin]
einecs 250-624-4
flubendazol [inn-spanish]
flumoxane
r-17,889
r-17889
flubendazole (usan/inn)
D04200
MLS001424042
MLS000759477
smr000466360
cpd000466360
HMS2051A18
HMS2090I16
methyl n-[6-(4-fluorobenzoyl)-1h-benzimidazol-2-yl]carbamate
NCGC00246966-01
A820846
n-[6-[(4-fluorophenyl)-oxomethyl]-1h-benzimidazol-2-yl]carbamic acid methyl ester
methyl (5-(4-fluorobenzoyl)-1h-benzo[d]imidazol-2-yl)carbamate
methyl [5-(4-fluorobenzoyl)benzimidazol-2-yl]carbamate
F0825
[5-(4-fluorobenzoyl)benzimidazol-2-yl]carbamic acid methyl ester
AKOS015960439
CCG-100887
flubendazol
flubendazolum
r8m46911lr ,
flubendazole [usan:inn:ban]
unii-r8m46911lr
CHEMBL1454946
chebi:77095 ,
FT-0626436
NCGC00246966-03
S1837
AKOS015894917
HY-B0294
AB00639981-06
MLS006010905
NC00137
SCHEMBL167185
flubendazole [usan]
flubendazole [mart.]
flubendazole [mi]
flubendazole [ep monograph]
flubendazole [who-dd]
flubendazole [inn]
CPEUVMUXAHMANV-UHFFFAOYSA-N
Q-201119
flubendazole, antibiotic for culture media use only
AB00639981_09
mfcd00871999
DTXSID8023058 ,
DB08974
flubendazole d3
flumoxanal
sr-01000759412
SR-01000759412-4
SR-01000759412-5
AC-8716
methyl (6-(4-fluorobenzoyl)-1h-benzo[d]imidazol-2-yl)carbamate
flubendazol, vetranal(tm), analytical standard
flubendazol, european pharmacopoeia (ep) reference standard
flubendazole for system suitability, european pharmacopoeia (ep) reference standard
NCGC00246966-12
HMS3714D06
Z2037280409
flubendazole (flutelmium)
methyl n-{5-[(4-fluorophenyl)carbonyl]-1h-1,3-benzodiazol-2-yl}carbamate
methyl 5-(4-fluorobenzoyl)-1h-benzo[d]imidazol-2-ylcarbamate
Q241992
AS-12271
nsc 313680; nsc313680; nsc-313680; r 17899; r17899; r-17899
BCP34258
CCG-267614
D70276
methyl (5-(4-fluorobenzoyl)-1h-benzo-[d]imidazol-2-yl)carbamate
flubendazole for system suitability
carbamicacid, [5-(4-fluorobenzoyl)-1h-benzimidazol-2-yl]-methylester
carbamic acid, n-[5-(4-fluorobenzoyl)-1h-benzimidazol-2-yl]-, methyl ester
flubendazol (inn-spanish)
p02ca05
dtxcid003058
flubendazole (mart.)
zelcom
methyl(5-(4-fluorobenzoyl)-1h-benzimidazol-2-yl)carbamate
flubendazole (ep monograph)
methyl (5-(4-fluorobenzoyl)-1h-benzimidazol-2-yl)carbamate
flubendazolum (inn-latin)
EN300-7361973
methyl n-[5-(4-fluorobenzoyl)-1h-1,3-benzodiazol-2-yl]carbamate

Research Excerpts

Overview

Flubendazole is a well-known anti-malarial drug that is recently reported to be a potential anti-tumor agent in various types of human cancer cells. Flub endazole (FLBZ) is a broad-spectrum benzimidazole anthelmintic compound used in pigs, poultry and humans.

ExcerptReferenceRelevance
"Flubendazole (FBZ) is a poorly water-soluble drug, and different methodologies have been proposed to improve its oral bioavailability. "( Describing the Influence of Ball-milling on the Amorphization of Flubendazole Using the PDF and RMC Methods with X-ray Powder Diffraction Data.
Bezzon, VDN; de Araújo, GLB; de Lima, JC; Ferreira, FF; Pinto, RDS, 2022
)
2.4
"Flubendazole (FLU) is an anthelmintic that has been used to treat worm infections in humans and animals for decades."( Flubendazole inhibits PD-1 and suppresses melanoma growth in immunocompetent mice.
Corley, S; Hossain, MJ; Khachigian, LM; Li, Y; O'Meara, C; Quagliata, L; Wilkins, MR; Wu, B, 2023
)
3.07
"Flubendazole is an anthelmintic and categorized in benzimidazole. "( [Flubendazole Inhibits the Proliferation of A549 and H460 Cells and Promotes Autophagy].
Dong, T; Li, J; Liu, Y; Lu, Z; Wen, J, 2020
)
2.91
"Flubendazole is a well-known anti-malarial drug that is recently reported to be a potential anti-tumor agent in various types of human cancer cells."( Flubendazole, FDA-approved anthelmintic, elicits valid antitumor effects by targeting P53 and promoting ferroptosis in castration-resistant prostate cancer.
Cen, S; Chen, W; Li, C; Luo, J; Mao, X; Shu, F; Tan, X; Wu, K; Yang, T; Yang, Y; Zhou, X; Zou, L, 2021
)
2.79
"Flubendazole is a widely used anthelmintic drug belonging to benzimidazole group. "( Anthelmintic Flubendazole and Its Potential Use in Anticancer Therapy.
Čáňová, K; Rozkydalová, L; Rudolf, E,
)
1.94
"Flubendazole (FLU) is a widely used anthelmintic drug belonging to benzimidazole group. "( Flubendazole induces mitotic catastrophe and apoptosis in melanoma cells.
Čáňová, K; Rozkydalová, L; Rudolf, E; Vokurková, D, 2018
)
3.37
"Flubendazole (FLBZ) is a potent and efficacious macrofilaricide after parenteral administration. "( Potential Role for Flubendazole in Limiting Filariasis Transmission: Observations of Microfilarial Sensitivity.
Burkman, E; Dzimianski, M; Geary, TG; Kengne-Ouafo, JA; Mackenzie, CD; Moorhead, A; Ndongmo, PC; Njouendou, JA; O'Neill, M; Wanji, S, 2018
)
2.25
"Flubendazole (FLBZ) is a broad-spectrum benzimidazole anthelmintic used in pigs, poultry, and humans. "( Species differences in hepatic biotransformation of the anthelmintic drug flubendazole.
Geary, T; Lanusse, C; Mackenzie, C; Maté, ML; Virkel, G, 2017
)
2.13
"Flubendazole (FLBZ) is a broad-spectrum benzimidazole anthelmintic compound used in pigs, poultry and humans. "( Hepatic and extra-hepatic metabolic pathways involved in flubendazole biotransformation in sheep.
Ballent, M; Lanusse, C; Lifschitz, A; Maté, L; Virkel, G, 2008
)
2.03
"Flubendazole (FLU) is a widely administered benzimidazole anthelmintic indicated for the control of parasitic diseases in farm animals including pigs and pheasants. "( Modulation of porcine (Sus scrofa domestica) and pheasant (Phasianus colchicus) carbonyl reducing enzymes by anthelmintic therapy with flubendazole.
Krízová, V; Lamka, J; Nobilis, M; Savlík, M; Skálová, L; Szotáková, B, 2008
)
1.99
"Flubendazole (FLBZ) is a poor water solubility broad-spectrum BZD methylcarbamate anthelmintic compound. "( Exploring flubendazole formulations for use in sheep. Pharmacokinetic evaluation of a cyclodextrin-based solution.
Alvarez, L; Ceballos, L; Lanusse, C; Moreno, L; Torrado, JJ, 2012
)
2.22
"Flubendazole (FLBZ) is a broad-spectrum benzimidazole anthelmintic compound. "( Nematodicidal activity of flubendazole and its reduced metabolite on a murine model of Trichinella spiralis infection.
Confalonieri, A; Ignacio Alvarez, L; Lanusse, C; Sánchez Bruni, S; Urbizu, L, 2012
)
2.12
"Flubendazole (FLBZ) is a broad spectrum benzimidazole methylcarbamate anthelmintic widely used in poultry and swine. "( Integrated pharmacological assessment of flubendazole potential for use in sheep: disposition kinetics, liver metabolism and parasite diffusion ability.
Alvarez, L; Bruni, SS; Lanusse, C; Moreno, L; Mottier, L; Virkel, G, 2004
)
2.03
"Flubendazole is a prochiral drug, hence a racemic mixture is formed during non-stereoselective reductions at the carbonyl group."( Achiral and chiral high-performance liquid chromatographic determination of flubendazole and its metabolites in biomatrices using UV photodiode-array and mass spectrometric detection.
Holcapek, M; Jira, T; Lamka, J; Lísa, M; Nobilis, M; Skálová, L; Szotáková, B, 2007
)
1.29
"Flubendazole is an effective anthelmintic against both Trichuris trichiura and Ascaris lumbricoides. "( The anthelmintic effects of flubendazole on Trichuris trichiura and Ascaris lumbricoides.
Kan, SP, 1983
)
2

Effects

Flubendazole has been given orally before surgery for a 10 days mean period. It is given at a daily dosage of 50 mg/kg for 16 months to 10 patients with hepatic alveolar echinococcosis.

ExcerptReferenceRelevance
"Flubendazole has shown poor in vivo efficacy against CE in humans and mice."( Flubendazole in cystic echinococcosis therapy: pharmaco-parasitological evaluation in mice.
Alvarez, L; Bruni, SS; Ceballos, L; Denegri, G; Elissondo, M; Lanusse, C, 2009
)
2.52
"Flubendazole has been given orally before surgery for a 10 days mean period, at 4 g daily in adults and 1 g daily in children."( [Flubendazole in human Echinococcus granulosus hydatidosis. Preoperative care: parasit-pharmacologic study].
Excler, JL; Garin, JP; Maisonneuve, H; Paillard, B; Piens, MA,
)
1.76
"Flubendazole has been given at a daily dosage of 50 mg/kg for 16 months (extremes 10 and 24 months) to 10 patients with hepatic alveolar echinococcosis. "( [Treatment of human alveolar echinococcosis with flubendazole. Clinical, morphological and immunological study].
Barale, T; Estavoyer, JM; Gillet, M; Lassègue, A; Miguet, JP; Minazzi, H; Vuitton, D, 1984
)
1.96

Actions

Flubendazole did not cause erratic migration of Ascaris in mixed infections at any of the dosages used.

ExcerptReferenceRelevance
"Flubendazole may inhibit the proliferation of A549 and H460 cells and promote autophagy."( [Flubendazole Inhibits the Proliferation of A549 and H460 Cells and Promotes Autophagy].
Dong, T; Li, J; Liu, Y; Lu, Z; Wen, J, 2020
)
2.91
"Flubendazole did not cause erratic migration of Ascaris in mixed infections at any of the dosages used."( The anthelmintic effects of flubendazole on Trichuris trichiura and Ascaris lumbricoides.
Kan, SP, 1983
)
1.28

Treatment

Treatment with Flubendazole (R17889-Janssen) 200 mg twice daily for 30 days resulted in clinical and parasitological cure.

ExcerptReferenceRelevance
"Treatment with flubendazole twice during fattening prevented A."( Effect of Ascaris suum infection on performance of fattening pigs.
Alban, L; Boes, J; Christiansen, S; Havn, KT; Jacobs, J; Kanora, A; Vestergaard-Nielsen, K, 2010
)
0.7
"A treatment by flubendazole 4 g/day is started on February 1982."( [Hydatic cyst of the pelvis. Failure of treatment with flubendazole].
Dumon, H; Gallais, H; Quilici, M; Raoult, D; Xeridat, B, 1983
)
0.85
"Treatment with Flubendazole (R17889-Janssen) 200 mg twice daily for 30 days resulted in clinical and parasitological cure."( Intestinal capillariasis in Egypt: a case report.
Mansour, NS; Mikhail, EM; Youssef, FG, 1989
)
0.62

Toxicity

ExcerptReferenceRelevance
" These studies have shown that monthly topical administration of selamectin is safe and highly effective in the treatment of naturally acquired ascarid and hookworm infections in cats."( Efficacy and safety of selamectin against gastrointestinal nematodes in cats presented as veterinary patients.
Benchaoui, HA; Boy, MG; Clemence, RG; Jernigan, AD; Rowan, TG; Six, RH; Smith, DG; Sture, GH; Thomas, CA; Watson, P, 2000
)
0.31
" In rats, the No Observed Adverse Effect Level (NOAEL) was 5 mg (as base)/kg body weight/day (mg eq."( Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients.
Bailey, G; Engelen, M; Lachau-Durand, S; Lammens, L; Lampo, A; van der Leede, BJ; Van Gompel, J, 2019
)
0.75
"Based on these results, in combination with previously described genotoxicity and reproductive toxicity data and the outcome of the preclinical efficacy studies, it was concluded that no flubendazole treatment regimen can be selected that would provide efficacy in humans at safe exposure."( Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients.
Bailey, G; Engelen, M; Lachau-Durand, S; Lammens, L; Lampo, A; van der Leede, BJ; Van Gompel, J, 2019
)
0.94

Pharmacokinetics

A pharmacokinetic study of flubendazole was carried out, using a radioimmunological method, in patients with hydatid disease about to undergo surgery. There was no evidence of drug penetration into the walls or contents of the cysts. Flub endazole up to high peak plasma concentrations does not induce Cmax related effects in CNS or cardiovascular system.

ExcerptReferenceRelevance
"A sensitive and specific radioimmunoassay procedure was developed for mebendazole and flubendazole enabling a more thorough study of the systemic absorption and pharmacokinetic behaviour of the drugs."( The pharmacokinetics of mebendazole and flubendazole in animals and man.
Hendriks, R; Heykants, J; Michiels, M; van den Bossche, H, 1982
)
0.76
"A pharmacokinetic study of flubendazole was carried out, using a radioimmunological method, in patients with hydatid disease about to undergo surgery; there was no evidence of drug penetration into the walls or contents of the cysts."( [Pharmacokinetic study of flubendazole in human hydatid disease caused by Echinococcus granulosus. Preliminary results (author's transl)].
Coulaud, JP; Hay, JM; Manuel, C; Meulemans, A; Mohler, J; Saimot, AG, 1981
)
0.86
" Oral absorption is rapid compared with IM dosing; the absorption half-life (K01-HL) for the IM treatment is approximately 14 hr compared with 1 and 2 hr for the PO regimen of salt and free base forms, respectively."( Pharmacokinetics of UMF-078, a candidate antifilarial drug, in infected dogs.
Dzimianski, MT; Fleckenstein, L; McCall, JW; Theplertboon, R, 2000
)
0.31
" For in vivo pharmacokinetic studies, further improvement and optimization of bioanalytical HPLC method in terms of sensitivity and selectivity was necessary."( Sensitive chiral high-performance liquid chromatographic determination of anthelmintic flubendazole and its phase I metabolites in blood plasma using UV photodiode-array and fluorescence detection Application to pharmacokinetic studies in sheep.
Krízová, V; Kubícek, V; Lamka, J; Nobilis, M; Skálová, L; Soukupová, M; Szotáková, B; Vybíralová, Z, 2008
)
0.57
" The information on FLU's pharmacokinetic behavior in animal species with forestomach (ruminants) has been limited although the use of FLU in these species could be beneficial."( Pharmacokinetics of flubendazole and its metabolites in lambs and adult sheep (Ovis aries).
Chládek, J; Cvilink, V; Krízová, V; Lamka, J; Nobilis, M; Prusková, L; Skálová, L; Szotáková, B, 2009
)
0.68
" Additionally, the comparative pharmacokinetic behaviour of FLBZ (and its metabolites) administered by the intraruminal (i."( Exploring flubendazole formulations for use in sheep. Pharmacokinetic evaluation of a cyclodextrin-based solution.
Alvarez, L; Ceballos, L; Lanusse, C; Moreno, L; Torrado, JJ, 2012
)
0.78
" However, oppositely to what was expected, the absorption-related pharmacokinetic parameters did not show any marked formulation-dependant effect."( Exploring flubendazole formulations for use in sheep. Pharmacokinetic evaluation of a cyclodextrin-based solution.
Alvarez, L; Ceballos, L; Lanusse, C; Moreno, L; Torrado, JJ, 2012
)
0.78
" Pharmacokinetic study: Balb/C mice received FLBZ (5 mg/kg) orally either alone or co-administered with NTZ (100 mg/kg)."( Combined flubendazole-nitazoxanide treatment of cystic echinococcosis: Pharmacokinetic and efficacy assessment in mice.
Carlos, L; Celina, E; Guillermo, D; Laura, C; Luis, A; Sergio, SB, 2015
)
0.83
" The goal of the current experimental work was to compare the pharmacokinetic plasma behavior of FLBZ, and its metabolites, formulated as either an aqueous hydroxypropyl- β -cyclodextrin-solution (HPBCD), an aqueous carboxymethyl cellulose-suspension (CMC) or a Tween 80-based formulation, in pigs."( Pharmacokinetic comparison of different flubendazole formulations in pigs: A further contribution to its development as a macrofilaricide molecule.
Alvarez, L; Ceballos, L; Geary, T; Lanusse, C; Mackenzie, C, 2015
)
0.68
" As this formulation results in improved systemic absorption, the pharmacokinetic and toxicological profile of the flubendazole ASD formulation have been assessed to ensure human safety before clinical trials could be initiated."( Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients.
Bailey, G; Engelen, M; Lachau-Durand, S; Lammens, L; Lampo, A; van der Leede, BJ; Van Gompel, J, 2019
)
0.96
" Flubendazole, up to high peak plasma concentrations, does not induce Cmax related effects in CNS or cardiovascular system."( Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients.
Bailey, G; Engelen, M; Lachau-Durand, S; Lammens, L; Lampo, A; van der Leede, BJ; Van Gompel, J, 2019
)
1.66

Bioavailability

The bioavailability of the anthelminthic flubendazole was remarkably enhanced in comparison with the pure crystalline drug by developing completely amorphous electrospun nanofibres. In animals, flub endazole has good oral bioavailability from an ASD formulation ranging from 15% in dogs, 27% in rats to more than 100% in jirds.

ExcerptReferenceRelevance
" These observations demonstrate the inefficacy of FZ in this series of 10 patients with alveolar echinococcosis, possibly related to the extremely poor bioavailability of FZ."( [Treatment of human alveolar echinococcosis with flubendazole. Clinical, morphological and immunological study].
Barale, T; Estavoyer, JM; Gillet, M; Lassègue, A; Miguet, JP; Minazzi, H; Vuitton, D, 1984
)
0.52
" However, a new formulation that provided sufficient bioavailability following oral administration could render FLBZ an effective treatment for onchocerciasis and LF."( In vitro flubendazole-induced damage to vital tissues in adult females of the filarial nematode Brugia malayi.
Agnew, DW; Geary, JF; Geary, TG; Mackenzie, CD; O'Neill, M, 2015
)
0.83
"This study investigates 3 amorphous technologies to improve the dissolution rate and oral bioavailability of flubendazole (FLU)."( Evaluation of Three Amorphous Drug Delivery Technologies to Improve the Oral Absorption of Flubendazole.
Backx, K; Boeykens, P; Bone, S; Brewster, ME; Ceulemans, J; Hillewaert, V; Jager, C; Kesselaers, E; Lachau-Durand, S; Mackie, C; Meurs, G; Novoa de Armas, H; Psathas, P; Smulders, S; Van Geel, K; Van Hove, B; Van Speybroeck, M; Verheyen, L; Verreck, G; Vialpando, M; Vodak, D; Voets, M; Weuts, I, 2016
)
0.87
" Unfortunately, the marketed formulation of FLBZ provides very limited oral bioavailability and parenteral administration is required for macrofilaricidal efficacy."( An In Vitro/In Vivo Model to Analyze the Effects of Flubendazole Exposure on Adult Female Brugia malayi.
DiCosty, U; Dzimianski, M; Geary, J; Geary, TG; Mackenzie, CD; Mansour, A; McCall, JW; McCall, SD; O'Neill, M, 2016
)
0.68
"The bioavailability of the anthelminthic flubendazole was remarkably enhanced in comparison with the pure crystalline drug by developing completely amorphous electrospun nanofibres with a matrix consisting of hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone."( Oral bioavailability enhancement of flubendazole by developing nanofibrous solid dosage forms.
Balogh, A; Boeykens, P; Borbás, E; Démuth, B; Galata, DL; Mackie, C; Marosi, G; Nagy, ZK; Pataki, H; Psathas, P; Van Assche, I; Van Hove, B; Verreck, G; Vialpando, M; Vigh, T, 2017
)
1
" For this purpose, an orally bioavailable amorphous solid dispersion (ASD) formulation of flubendazole was developed."( Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients.
Bailey, G; Engelen, M; Lachau-Durand, S; Lammens, L; Lampo, A; van der Leede, BJ; Van Gompel, J, 2019
)
0.97
" In animals, flubendazole has good oral bioavailability from an ASD formulation ranging from 15% in dogs, 27% in rats to more than 100% in jirds."( Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients.
Bailey, G; Engelen, M; Lachau-Durand, S; Lammens, L; Lampo, A; van der Leede, BJ; Van Gompel, J, 2019
)
1.12
" As part of an effort to stimulate the discovery and development of new macrofilaricides, particularly for onchocerciasis, research has recently been devoted to the development of new formulations that would afford high oral bioavailability of FBZ, paving the way for potential clinical development of this repurposed drug for the treatment of human filariases."( Flubendazole as a macrofilaricide: History and background.
Geary, TG; Mackenzie, CD; Silber, SA, 2019
)
1.96
"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
" Flubendazole's potential use in clinical oncology will require further understanding of its mechanistic roles, range of inhibition of cancer types, capacity for adjunctive therapy and possible reformulation for enhanced solubility, bioavailability and potency."( Emerging insights on functions of the anthelmintic flubendazole as a repurposed anticancer agent.
Khachigian, LM, 2021
)
1.78
"In this work, an important step is taken towards the bioavailability improvement of poorly water-soluble drugs, such as flubendazole (Flu), posing a challenge in the current development of many novel oral-administrable therapeutics."( Stable amorphous solid dispersion of flubendazole with high loading via electrospinning.
Becelaere, J; Borgmans, S; Creemers, K; De Clerck, K; Hoogenboom, R; Schoolaert, E; Van Den Broeck, E; Van Guyse, JFR; Van Speybroeck, V; Vanhoorne, V; Vergaelen, M; Vervaet, C, 2022
)
1.2
" However, currently, a simple and efficient in vitro test to investigate critical factors that may impact the drug release and bioavailability at the development stage of a drug-loaded nanoemulsion (NE) is lacking."( Biphasic dissolution combined with modified cylinder method-A new promising method for dissolution test in drug-loaded nanoemulsions.
Bou-Chacra, NA; de Araujo, GLB; Henostroza, MAB; Löbenberg, R; Park, C; Yousef, M; Yukuyama, MN; Zuo, J, 2023
)
0.91

Dosage Studied

The same grade of damage was reached when incubating for a longer period at a low dosage or for a shorter period in medium containing a high amount (10 or 100 micro g/ml) Flubendazole has been given at a daily dosage of 50 mg/kg for 16 months (extremes 10 and 24 months) to 10 patients.

ExcerptRelevanceReference
" Faecal examination for 5 months, the period from medication to dissection of rats, showed that L1 release ceased in all the rats of medicated groups by about 1 week after the termination of dosing and resumed 1-2 months later in 86% of the rats which were dissected at the end of experiments with the recovery of adult worms of both sexes."( Effect of flubendazole on the number of first-stage larvae of Angiostrongylus cantonensis released in the faeces of treated rats.
Maki, J; Yanagisawa, T, 1990
)
0.68
"A precise and accurate differential pulse polarographic method was developed for the determination of flubendazole in dosage forms without any prior extraction procedure of interference from the other stated ingredients."( Determination of flubendazole in pharmaceutical dosage forms by differential pulse polarography and UV spectroscopy.
Gratteri, P; La Porta, E; Mura, P; Papeschi, G; Pinzauti, S; Santoni, G, 1990
)
0.83
" The drugs exhibited better anthelmintic efficacy in a divided dosing regimen than in a single dosing regimen."( Studies on anthelmintic effects of flubendazole and mebendazole on the rat lungworm Angiostrongylus cantonensis in mice and rats.
Maki, J; Yanagisawa, T, 1986
)
0.55
" nana were eliminated from mice by bithionol and mebendazole respectively, at the same dosage regimen."( Anthelmintic effects of bithionol, paromomycin sulphate, flubendazole and mebendazole on mature and immature Hymenolepis nana in mice.
Maki, J; Yanagisawa, T, 1985
)
0.51
"4% past formulation was given at a dosage of 22 mg/kg of body weight once a day for 2 or 3 consecutive days."( Anthelmintic efficacy of flubendazole paste against nematodes and cestodes in dogs and cats.
Hermans, L; Van der Flaes, L; Vanparijs, O, 1985
)
0.57
"Flubendazole has been given at a daily dosage of 50 mg/kg for 16 months (extremes 10 and 24 months) to 10 patients with hepatic alveolar echinococcosis."( [Treatment of human alveolar echinococcosis with flubendazole. Clinical, morphological and immunological study].
Barale, T; Estavoyer, JM; Gillet, M; Lassègue, A; Miguet, JP; Minazzi, H; Vuitton, D, 1984
)
1.96
" This dosage level indicated 100% efficacy against mature Ascaris suum, Oesophagostomum dentatum, Trichuris suis, and Metastrongylus apri."( Flubendazole: dose range and efficacy studies against common internal parasites of swine.
Becker, HN; Bradley, RE; Guerrero, J; Michael, BF; Newcomb, K, 1983
)
1.71
" The increase in the dosage allowed higher levels, as opposed to previous assertions."( [Treatment of alveolar echinococcosis with flubendazole. Pharmacological study (author's transl)].
Canton, P; Dureux, JB; Gérard, A; Roche, G, 1982
)
0.53
" The game were extremely willing to ingest the drug applied with feed, the dosing schedule being confirmed."( [Effect of flubendazole on Muellerius capillaris in mouflon].
Klecá ková, J; Lamka, J; Vondrejc, M, 1996
)
0.68
" The eggs from the lowest dosed group (3 mg kg-1 feed) did contain residues, but most of them were only slightly higher than the LOD."( Flubendazole residues in eggs after oral administration to laying hens: determination with reversed phase liquid chromatography.
Kan, CA; Keukens, HJ; Tomassen, MJ, 1998
)
1.74
" In contrast to oral administration, IM dosing of UMF-078 provides sustained, relatively low plasma drug levels, with good tolerance and efficacy."( Pharmacokinetics of UMF-078, a candidate antifilarial drug, in infected dogs.
Dzimianski, MT; Fleckenstein, L; McCall, JW; Theplertboon, R, 2000
)
0.31
" Unit doses of selamectin (providing a minimum dosage of 6mgkg(-1)) were administered topically to the skin in a single spot at monthly intervals."( Efficacy and safety of selamectin against gastrointestinal nematodes in cats presented as veterinary patients.
Benchaoui, HA; Boy, MG; Clemence, RG; Jernigan, AD; Rowan, TG; Six, RH; Smith, DG; Sture, GH; Thomas, CA; Watson, P, 2000
)
0.31
" It is nearly insoluble in water and it influences not only the selection of the dosage form, but also its biological availability."( [Effect of temperature on drug solubility in complex formation of flubendazole and 2-hydroxypropyl-beta-cyclodextrin].
Rabisková, M; Sucman, E; Vetchý, D, 2000
)
0.54
"), when treated with a dosage of 20 mg/kg for 5 consecutive days (99."( Efficacy of flubendazole and albendazole against Trichinella spiralis in mice.
Cho, SW; Chung, MS; Joo, KH; Kwon, HS; Quan, FS, 2001
)
0.69
" the same grade of damage was reached when incubating for a longer period at a low dosage or for a shorter period in medium containing a high amount (10 or 100 micro g/ml) of flubendazole."( In vitro studies on the effects of flubendazole against Toxocara canis and Ascaris suum.
Hanser, E; Hoeben, D; Mehlhorn, H; Vlaminck, K, 2003
)
0.79
") (4% suspension) administrations at the same dosage (5 mg/kg) with a 21-day washout period between treatments."( Integrated pharmacological assessment of flubendazole potential for use in sheep: disposition kinetics, liver metabolism and parasite diffusion ability.
Alvarez, L; Bruni, SS; Lanusse, C; Moreno, L; Mottier, L; Virkel, G, 2004
)
0.59
" Subcellular fractions were prepared from liver and intestinal mucosa 24 h after the final dosage was administered."( Activities of biotransformation enzymes and flubendazole metabolism in lambs (Ovis aries): effect of gender and flubendazole therapy.
Bártíková, H; Krízová, V; Kubícek, V; Lamka, J; Skálová, L; Stepnicková, M; Szotáková, B,
)
0.39
" Combined surgery and continuous administration of albendazole at high dosage may allow alveolar echinococcosis patients to survive more than 30 years after diagnosis despite multi-organ involvement."( 30-yr course and favorable outcome of alveolar echinococcosis despite multiple metastatic organ involvement in a non-immune suppressed patient.
Bardonnet, K; Blagosklonov, O; Bresson-Hadni, S; Delabrousse, E; Grenouillet, F; Mantion, GA; Miguet, JP; Vuitton, DA, 2013
)
0.39
" Healthy animals of both species were allocated into four experimental groups of 44 animals each: FLBZ-CD oral and FLBZ-CDsc, treated with the FLBZ-CD formulation by the oral or subcutaneous routes, respectively; FLBZ-TWEENsc, dosed subcutaneously with the FLBZ-TWEEN formulation; and FLBZ-CMC oral, treated orally with the FLBZ suspension."( Exploring the potential of flubendazole in filariasis control: evaluation of the systemic exposure for different pharmaceutical preparations.
Alvarez, L; Ceballos, L; Geary, T; Lanusse, C; Mackenzie, C, 2014
)
0.7
" Analysis of dose-response curves from the in vitro tests, using recently developed point of departure approaches, demonstrate that the aneugenic potency of flubendazole is very similar to related anti-parasitic benzimidazoles, including albendazole, which is used in mass drug administration programmes to combat endemic filarial diseases."( Genotoxicity of flubendazole and its metabolites in vitro and the impact of a new formulation on in vivo aneugenicity.
Evans, DB; Johnson, GE; Scandale, I; Tweats, DJ; Whitwell, J, 2016
)
0.98
" All formulations were dosed to rats at 20 mg/kg in suspension."( Evaluation of Three Amorphous Drug Delivery Technologies to Improve the Oral Absorption of Flubendazole.
Backx, K; Boeykens, P; Bone, S; Brewster, ME; Ceulemans, J; Hillewaert, V; Jager, C; Kesselaers, E; Lachau-Durand, S; Mackie, C; Meurs, G; Novoa de Armas, H; Psathas, P; Smulders, S; Van Geel, K; Van Hove, B; Van Speybroeck, M; Verheyen, L; Verreck, G; Vialpando, M; Vodak, D; Voets, M; Weuts, I, 2016
)
0.65
" Systemic exposures of FBZ/FBZ metabolites achieved following dosing were measured by pharmacokinetic (PK) bioanalysis."( Short-course, oral flubendazole does not mediate significant efficacy against Onchocerca adult male worms or Brugia microfilariae in murine infection models.
Akumtoh, DN; Aljayyoussi, G; Baeten, B; Chounna, PWN; Chunda, VC; Engelen, M; Fombad, FF; Gandjui, NVT; Lachaud, S; Metuge, HM; Ndzeshang, BL; Njouendou, AJ; Pionnier, N; Quirynen, L; Sjoberg, HT; Steven, A; Taylor, MJ; Tayong, DB; Tekle, F; Turner, JD; Wanji, S; Ward, SA, 2019
)
0.84
" In summary, oral doses of ASD formulated FBZ did not significantly reduce total worm burden but longer treatments, extended takedown times or a second dosing regimen, may decrease female fecundity and the number of mf shed by female worms."( Efficacy of subcutaneous doses and a new oral amorphous solid dispersion formulation of flubendazole on male jirds (Meriones unguiculatus) infected with the filarial nematode Brugia pahangi.
Baeten, B; Beerntsen, B; Bulman, CA; Engelen, M; Fischer, C; Gut, J; Ibiricu Urriza, I; Lachau-Durand, S; Lim, KC; Lustigman, S; Quirynen, L; Sakanari, J; Tekle, F, 2019
)
0.74
"Dissolution testing is important in assessing the in vitro drug release performance for oral administration dosage forms."( Biphasic dissolution combined with modified cylinder method-A new promising method for dissolution test in drug-loaded nanoemulsions.
Bou-Chacra, NA; de Araujo, GLB; Henostroza, MAB; Löbenberg, R; Park, C; Yousef, M; Yukuyama, MN; Zuo, J, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antinematodal drugA substance used in the treatment or control of nematode infestations.
teratogenic agentA role played by a chemical compound in biological systems with adverse consequences in embryo developments, leading to birth defects, embryo death or altered development, growth retardation and functional defect.
[role 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]

Drug Classes (4)

ClassDescription
benzimidazolesAn organic heterocyclic compound containing a benzene ring fused to an imidazole ring.
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency0.74270.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency1.47400.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency0.70650.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency0.74270.00308.794948.0869AID1347053
mitogen-activated protein kinase 1Homo sapiens (human)Potency10.00000.039816.784239.8107AID1454
relaxin receptor 1 isoform 1Homo sapiens (human)Potency25.11890.038814.350143.6206AID2676
Interferon betaHomo sapiens (human)Potency1.47400.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (98)

Assay IDTitleYearJournalArticle
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.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347135qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347141qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347137qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347136qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347140qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347139qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347138qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' 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]
AID1403130Selectivity ratio of EC50 for cytotoxicity against human PC3M cells to EC50 for cytotoxicity against human PC3MLN4 cells2018European journal of medicinal chemistry, Jan-20, Volume: 144Synthesis and anticancer activity of novel water soluble benzimidazole carbamates.
AID1192806Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as viral DNA replication after 9 days by real-time PCR analysis (Rvb = 6.12 +/- 1.46 AU)2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy.
AID1470755Inhibition of Trypanosoma cruzi trans-sialidase at 1 mM using N-acetyllactosamine as substrate in presence of 3'-sialyllactose measured after 15 mins by HPAEC-PAD relative to control2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
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]
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]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1192803Selectivity index, ratio of CC50 for human HepG2.2.15 cells to IC50 for decrease in hepatitis B viral surface antigen HBsAg secretion in human HepG2.2.15 cells2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1470763Solubility of the compound in water2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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]
AID1403129Cytotoxicity against human PC3M cells assessed as reduction in cell viability after 48 hrs by cyquant reagent based fluorescence spectrometric assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Synthesis and anticancer activity of novel water soluble benzimidazole carbamates.
AID1470754Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood after 24 hrs by optical microscopic method2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1470752Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood after 24 hrs by optical microscopic method2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1192808Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as viral HBcAg level after 9 days by ELISA (Rvb = 14.16 +/- 1.92 ng/ml)2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1403128Cytotoxicity against human PC3MLN4 cells assessed as reduction in cell viability after 48 hrs by cyquant reagent based fluorescence spectrometric assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Synthesis and anticancer activity of novel water soluble benzimidazole carbamates.
AID1470751Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood assessed as parasite lysis at 50 ug/ml after 24 hrs by optical microscopic method relative to control2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1512699Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 750 nM after 24 hrs by MTT assay relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.
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
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]
AID1192807Antiviral activity against hepatitis B viral in human HepG2.2.15 cells assessed as viral surface antigen HBsAg level after 9 days by ELISA (Rvb = 721 +/- 32 pg/ml)2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy.
AID1470753Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood assessed as parasite lysis at 50 ug/ml after 24 hrs by optical microscopic method relative to control2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1192805Selectivity index, ratio of CC50 for human HepG2.2.15 cells to IC50 for decrease in hepatitis B viral HBeAg secretion in human HepG2.2.15 cells2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease 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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (242)

TimeframeStudies, This Drug (%)All Drugs %
pre-199068 (28.10)18.7374
1990's18 (7.44)18.2507
2000's40 (16.53)29.6817
2010's79 (32.64)24.3611
2020's37 (15.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.50

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index46.50 (24.57)
Research Supply Index5.63 (2.92)
Research Growth Index4.84 (4.65)
Search Engine Demand Index107.96 (26.88)
Search Engine Supply Index2.96 (0.95)

This Compound (46.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials20 (7.78%)5.53%
Reviews10 (3.89%)6.00%
Case Studies13 (5.06%)4.05%
Observational0 (0.00%)0.25%
Other214 (83.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]