Page last updated: 2024-12-06

halofuginone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID62894
CHEMBL ID1197091
CHEBI ID184758
SCHEMBL ID1937106
MeSH IDM0055492
PubMed CID456390
CHEMBL ID1199540
SCHEMBL ID9541147
MeSH IDM0055492

Synonyms (70)

Synonym
halofuginone [inn:ban]
ht-100
halofuginone
c16h17brcln3o3
halofuginon
55837-20-2
7-bromo-6-chloro-3-[3-(3-hydroxypiperidin-2-yl)-2-oxopropyl]quinazolin-4-one
CHEBI:184758
7-bromo-6-chloro-3-[3-(3-hydroxypiperidin-2-yl)-2-oxopropyl]-3,4-dihydroquinazolin-4-one
AKOS015962039
halofuginona
halofuginonum
CHEMBL1197091
SCHEMBL1937106
7-bromo-6-chloro-3-[3-(3-hydroxy-2-piperidyl)-acetonyl]-4(3h)-quinazolinone
LVASCWIMLIKXLA-UHFFFAOYSA-N
AC-29749
7-bromo-6-chloro-3-[3-(3-hydroxypiperidin-2-yl)-2-oxopropyl]quinazolin-4(3h)-one
7-bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3h)-quinazolinone
7-bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3h)-quinazolinone, 9ci
7-bromo-6-chloro-3-(3-(3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3h)-one
tempostatin;ru-19110;ru 19110;ru19110
BCP07016
gtpl10153
SB19686
TQP0820
64544-01-0
A901326
DTXSID80860689
4(3h)-quinazolinone, 7-bromo-6-chloro-3-(3-((2r,3s)-3-hydroxy-2-piperidinyl)-2-oxopropyl)-, rel-
4(3h)-quinazolinone, 7-bromo-6-chloro-3-(3-(3-hydroxy-2-piperidinyl)-2-oxopropyl)-, trans-(+-)-
halofuginonum [inn-latin]
trans-7-bromo-6-chloro-3-(3-(3-hydroxy-2-piperidinyl)-2-oxopropyl)-4(3h)-quinazolinone
4(3h)-quinazolinone, 7-bromo-6-chloro-3-(3-(3-hydroxy-2-piperidinyl)-2-oxopropyl)-, trans-
halofuginona [inn-spanish]
(+/-)-trans-7-bromo-6-chloro-3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3h)-quinazolinone hydrobromide
halocurtm
7-bromo-6-chloro-3-[3-[(2r,3s)-3-hydroxy-2-piperidyl]-2-oxo-propyl]quinazolin-4-one
halofunginone
halofuginone, (+)-
6-chloro-7-bromo-(+)-febrifugine
7-bromo-6-chloro-3-(3-((2r,3s)-3-hydroxy-2-piperidinyl)-2-oxopropyl)-4(3h)-quinazolinone
(+)-halofuginone
CHEMBL1199540
(+-)-trans-7-bromo-6-chloro-3-(3-(3-hydroxy-2-piperidyl)acetonyl-4(3h)-quinazolinone
l31mm1385e ,
(+-)-trans-7-brom-6-chlor-3-(3-(3-hydroxy-2-piperidyl)acetonyl-4(3h)-chinazolinon
(+/-)-trans-7-bromo-6-chloro-3-(3-(3-hydroxy-2-piperidyl)-acetonyl)-4(3h)-quinazolinone
unii-l31mm1385e
4(3h4(3h)-quinazolinone, 7-bromo-6-chloro-3-(3-(3-hydroxy-2-piperidinyl)-2-oxopropyl)-, trans-(+/-)-
7-bromo-6-chloro-3-{3-[(2r,3s)-3-hydroxypiperidin-2-yl]-2-oxopropyl}quinazolin-4(3h)-one
HFG ,
S8144
halofuginone [inn]
halofuginone [mi]
DB04866
halofuginone [ema epar veterinary]
4(3h)-quinazolinone, 7-bromo-6-chloro-3-(3-(3-hydroxy-2-piperidinyl)-2-oxopropyl)-, trans-(+/-)-
AKOS022185424
SCHEMBL9541147
7-bromo-6-chloro-3-{3-[(2r,3s)-3-hydroxypiperidin-2-yl]-2-oxopropyl}-3,4-dihydroquinazolin-4-one
rel-7-bromo-6-chloro-3-[3-[(2r,3s)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-4(3h)-quinazolinone
Q4132745
rel-7-bromo-6-chloro-3-(3-((2r,3s)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3h)-one
868851-54-1
H84E4Y7HC9 ,
4(3h)-quinazolinone, 7-bromo-6-chloro-3-(3-((2r,3s)-3-hydroxy-2-piperidinyl)-2-oxopropyl)-
CCG-268823
unii-h84e4y7hc9
DTXSID301339439

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Both rapamycin (RAPA) and cyclosporin A (CsA) are commonly used for immunosuppression, however their adverse side effects limit their application."( Halofuginone Synergistically Enhances Anti-Proliferation of Rapamycin in T Cells and Reduces Cytotoxicity of Cyclosporine in Cultured Renal Tubular Epithelial Cells.
Chu, TL; Du, C; Guan, Q; Nguan, CY, 2015
)
0.42
" LC-MS/MS analysis revealed that the reduction in the magnitude of adverse effects was the result of the ability to release HF from the HFm core in a slow and sustained manner."( Halofuginone micelle nanoparticles eradicate Nrf2-activated lung adenocarcinoma without systemic toxicity.
Baird, L; Miyata, K; Naito, M; Panda, H; Saito, R; Suzuki, M; Uruno, A; Wen, H; Yamamoto, M, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" The apparent terminal elimination half-life ranged from 24."( Pharmacokinetics of halofuginone in cattle.
Kinabo, LD; McKellar, QA,
)
0.13
" For pharmacokinetic analysis plasma sampling was performed during the first and second course and assayed using a validated high-performance liquid chromatographic assay with mass spectrometric detection."( Phase I and pharmacokinetic study of halofuginone, an oral quinazolinone derivative in patients with advanced solid tumours.
de Jonge, MJ; Dumez, H; Lacombe, D; Marréaud, S; Punt, CJ; Snyder, D; van Oosterom, A; Verweij, J; Yamaguchi, T; Yarkoni, S, 2006
)
0.33
" Diclazuril and halofuginone resulted in a significant short distribution half-life (t(½α)) (7."( Pharmacokinetic and tissue distribution of doxycycline in broiler chickens pretreated with either: diclazuril or halofuginone.
Amer, AM; Atef, M; El-Gendi, AY; Kamel, GM, 2010
)
0.36

Bioavailability

ExcerptReferenceRelevance
" The ability of halofuginone to interfere with key events in neovascularization, together with its oral bioavailability and safe use as an anti-parasitic agent, make it a promising drug for further evaluation in the treatment of a wide range of diseases associated with pathological angiogenesis."( Halofuginone: a potent inhibitor of critical steps in angiogenesis progression.
Aingorn, E; Dou, HL; Elkin, M; Hemo, I; Miao, HQ; Nagler, A; Pines, M; Reich, R; Vlodavsky, I, 2000
)
0.31
" Systemic bioavailability was 22."( Pharmacokinetic and tissue distribution of doxycycline in broiler chickens pretreated with either: diclazuril or halofuginone.
Amer, AM; Atef, M; El-Gendi, AY; Kamel, GM, 2010
)
0.36

Dosage Studied

ExcerptRelevanceReference
"Halofuginone lactate, given once orally at a dosage rate of 1,2 mg/kg body mass on the 1st, 3rd or 5th days of fever, resulted in the recovery of only 1 out of 5 splenectomized cattle."( Chemotherapy of Theileria parva lawrencei infections in cattle with halofuginone.
De Vos, AJ; Roos, JA, 1983
)
0.27
" Faecal samples were collected on the first day of dosing and four, seven, 14 and 21 days later, and Cryptosporidium parvum oocysts were counted and faecal indices for diarrhoea were determined after a clinical examination."( Efficacy of halofuginone lactate in the prevention of cryptosporidiosis in suckling calves.
Chermette, R; Lefay, D; Naciri, M; Poirier, P, 2001
)
0.31
" dosing and 15-16% and 16% of the administered dose within 24 and 48 h, respectively, after oral dosing."( Pharmacokinetics and tissue distribution of halofuginone (NSC 713205) in CD2F1 mice and Fischer 344 rats.
Covey, JM; Egorin, MJ; Eiseman, JL; Hamburger, DR; Parise, RA; Stecklair, KP, 2001
)
0.31
" Following oral dosing the tested drug absorbed with t(½ab) of 41."( Pharmacokinetic and tissue distribution of doxycycline in broiler chickens pretreated with either: diclazuril or halofuginone.
Amer, AM; Atef, M; El-Gendi, AY; Kamel, GM, 2010
)
0.36
"7 % high dose), while both TGF-β3 dosage groups showed no significant change (65."( Preliminary results of antiscarring therapy in the prevention of postendoscopic esophageal mucosectomy strictures.
Chak, A; Cipriano, C; Lash, RH; Marks, JM; Ponsky, JL; Schomisch, SJ; Wu, Y, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinazolinesAny organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
[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]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1604670Antibacterial activity against Salmonella enterica 87 by visual method
AID1896830Inhibition of Escherichia coil ProRS expressed in Escherichia coli assessed as change in melting temperature in presence of AMPPNP at 0.5 mM by fluorescence-based thermal shift assay
AID1706142Binding affinity to Salmonella enterica Threonyl-tRNA synthetase assessed as change in melting temperature at 0.5 mM incubated for 10 mins by SYPRO orange dye-based thermal shift assay
AID1896831Inhibition of Salmonella typhi ProRS expressed in Escherichia coli assessed as change in melting temperature in presence of AMPPNP at 0.5 mM by fluorescence-based thermal shift assay
AID748224Inhibition of heme crystallization to hemozoin2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
AID1896836Binding affinity to methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as dissociation constant in presence of 0.05 nM ATP by microscale thermophoresis assay
AID1706155Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as reduction in bacterial growth incubated for 18 hrs by CLSI based broth microdilution assay
AID1896833Inhibition of human ProRS expressed in Escherichia coli assessed as change in melting temperature in presence of AMPPNP at 0.5 mM by fluorescence-based thermal shift assay
AID1896844Antibacterial activity against Salmonella typhi CMCC50094 assessed as prevention of visible growth by broth microdilution method
AID1896849Cytotoxicity against human HepG2 cells
AID1604671Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by visual method
AID1706143Inhibition of Salmonella enterica Threonyl-tRNA synthetase assessed as reduction in aminoacylation activity at 100 uM using L-threonine as substrate incubated for 3 hrs by Kinase-glo luminescence assay relative to control
AID1896840Binding affinity to methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as dissociation constant in presence of 1 nM ATP by microscale thermophoresis assay
AID1896838Binding affinity to methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as dissociation constant in presence of 0.2 nM ATP by microscale thermophoresis assay
AID1896843Antibacterial activity against Shigella flexneri CMCC51572 assessed as prevention of visible growth by broth microdilution method
AID1604321Antiparasitic activity against Toxoplasma gondii2019European journal of medicinal chemistry, Dec-01, Volume: 183Recent progress on anti-Toxoplasma drugs discovery: Design, synthesis and screening.
AID1604664Inhibition of Salmonella enterica Threonyl-tRNA synthetase assessed as reduction in aminoacylation activity using L-threonine as substrate in presence of incubated for 3 hrs by Kinase-glo luminescence assay
AID1706144Inhibition of Salmonella enterica Threonyl-tRNA synthetase assessed as reduction in aminoacylation activity using L-threonine as substrate incubated for 3 hrs by Kinase-glo luminescence assay
AID1896827Inhibition of methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as generation of inorganic monophosphate by pre-transfer editing-based experiment
AID1896825Inhibition of Escherichia coli ProRS expressed in Escherichia coli assessed as generation of inorganic monophosphate by pre-transfer editing-based experiment
AID1706152Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as reduction in bacterial growth incubated for 18 hrs by CLSI based broth microdilution assay
AID1896829Inhibition of Saccharomyces cerevisiae ProRS expressed in Escherichia coli assessed as generation of inorganic monophosphate at 0 to 100 uM by pre-transfer editing-based experiment
AID1604668Antibacterial activity against Enterococcus faecalis ATCC 29212 by visual method
AID748225Binding affinity to hematin (unknown origin) by UV-visible titration analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
AID1604669Antibacterial activity against Escherichia coli ATCC 25922 by visual method
AID1896828Inhibition of human ProRS expressed in Escherichia coli assessed as generation of inorganic monophosphate by pre-transfer editing-based experiment
AID1896835Binding affinity to methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as dissociation constant by microscale thermophoresis assay
AID1896845Antibacterial activity against methicillin-resistant Staphylococcus aureus 252 assessed as prevention of visible growth by broth microdilution method
AID748227Antiplasmodial activity against ring stage Plasmodium falciparum W2 infected in human RBC after 48 hrs by FACS analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
AID1896832Inhibition of methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as change in melting temperature in presence of AMPPNP at 0.5 mM by fluorescence-based thermal shift assay
AID1604663Inhibition of Salmonella enterica Threonyl-tRNA synthetase assessed as reduction in aminoacylation activity at 100 uM using L-threonine as substrate incubated for 3 hrs by Kinase-glo luminescence assay relative to control
AID1896841Binding affinity to methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as dissociation constant in presence of 2 nM ATP by microscale thermophoresis assay
AID1604666Antibacterial activity against Staphylococcus aureus ATCC 29213 by visual method
AID1896842Antibacterial activity against Escherichia coli ATCC25922 assessed as prevention of visible growth by broth microdilution method
AID748228Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
AID1706150Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 18 hrs by CLSI based broth microdilution assay
AID1896848Antibacterial activity against Staphylococcus aureus ATCC25923 assessed as prevention of visible growth by broth microdilution method
AID1896839Binding affinity to methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as dissociation constant in presence of 0.5 nM ATP by microscale thermophoresis assay
AID1706153Antibacterial activity against Escherichia coli ATCC 25922 assessed as reduction in bacterial growth incubated for 18 hrs by CLSI based broth microdilution assay
AID1896846Antibacterial activity against methicillin-resistant Staphylococcus aureus R3708 assessed as prevention of visible growth by broth microdilution method
AID1896834Inhibition of Saccharomyces cerevisiae ProRS expressed in Escherichia coli assessed as change in melting temperature in presence of AMPPNP at 0.5 mM by fluorescence-based thermal shift assay
AID1706151Antibacterial activity against methicillin-resistant Staphylococcus aureus R3708 assessed as reduction in bacterial growth incubated for 18 hrs by CLSI based broth microdilution assay
AID1896847Antibacterial activity against Staphylococcus aureus ATCC29213 assessed as prevention of visible growth by broth microdilution method
AID748223Cytotoxicity against human HepG2 cells after 48 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
AID1896837Binding affinity to methicillin-resistant Staphylococcus aureus ProRS expressed in Escherichia coli assessed as dissociation constant in presence of 0.1 nM ATP by microscale thermophoresis assay
AID1706154Antibacterial activity against Salmonella enterica 87 assessed as reduction in bacterial growth incubated for 18 hrs by CLSI based broth microdilution assay
AID1896826Inhibition of Salmonella typhi ProRS expressed in Escherichia coli assessed as generation of inorganic monophosphate by pre-transfer editing-based experiment
AID1604662Binding affinity to Salmonella enterica Threonyl-tRNA synthetase assessed as change in melting temperature at 0.5 mM incubated for 10 mins by SYPRO orange dye-based thermal shift assay
AID1604667Antibacterial activity against methicillin-resistant Staphylococcus aureus R3708 by visual method
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (319)

TimeframeStudies, This Drug (%)All Drugs %
pre-199044 (13.79)18.7374
1990's43 (13.48)18.2507
2000's77 (24.14)29.6817
2010's121 (37.93)24.3611
2020's34 (10.66)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (4.91%)5.53%
Trials0 (0.00%)5.53%
Reviews20 (6.13%)6.00%
Reviews1 (20.00%)6.00%
Case Studies1 (0.31%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other289 (88.65%)84.16%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
HT-100 Long-term Safety and Pharmacodynamics in Patients With DMD Who Have Completed Protocols HALO-DMD-01 and HALO-DMD-02 [NCT02525302]Phase 210 participants (Actual)Interventional2015-05-31Terminated(stopped due to Dosing stopped)
A Phase 1b Open Label, Single and Multiple Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of HT-100 in Patients With Duchenne Muscular Dystrophy [NCT01847573]Phase 1/Phase 217 participants (Actual)Interventional2013-05-31Terminated(stopped due to Dosing stopped)
A Phase II Trial of Topical Halofuginone in Patients With HIV Related Kaposi's Sarcoma [NCT00064142]Phase 230 participants (Actual)Interventional2003-05-31Completed
An Open Label Extension Study of HT-100 in Patients With Duchenne Muscular Dystrophy Who Have Completed Protocol HALO-DMD-01 [NCT01978366]Phase 217 participants (Actual)Interventional2013-10-31Terminated(stopped due to Dosing stopped)
Phase I Study To Determine The Safety Of Halofuginone In Patients With A Solid Progressive Tumor [NCT00027677]Phase 125 participants (Actual)Interventional2001-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]