Compounds > ponazuril
Page last updated: 2024-11-10

ponazuril

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

Description

ponazuril: a major metabolite of toltrazuril [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3050408
CHEMBL ID2104856
SCHEMBL ID203030
MeSH IDM0371914

Synonyms (46)

Synonym
1-methyl-3-(4-(p-((trifluoromethyl)sulfonyl)phenoxy)-m-tolyl)-s-triazine-2,4,6(1h,3h,5h)-trione.
unii-jpw84as66u
bay-vi 9143
1-methyl-3-(4-(p-((trifluoromethyl)sulfonyl)phenoxy)-m-tolyl)-s-triazine-2,4,6(1h,3h,5h)-trione
marquis
jpw84as66u ,
ponazuril [inn]
toltrazuril (sulfone)
HY-17008
ponazuril
1-methyl-3-[3-methyl-4-[4-(trifluoromethylsulfonyl)phenoxy]phenyl]-1,3,5-triazinane-2,4,6-trione
69004-04-2
A836307
1-methyl-3-[3-methyl-4-[4-(trifluoromethylsulfonyl)phenoxy]phenyl]-1,3,5-triazinane-2,4,6-trione;toltrazuril sulfone
NCGC00182044-01
toltrazuril sulfone
dtxsid7048958 ,
cas-69004-04-2
tox21_113390
dtxcid4028884
CHEMBL2104856
FT-0673975
1-methyl-3-{3-methyl-4-[4-(trifluoromethylsulfonyl)phenoxy]phenyl}-1,3,5-triazine-2,4,6(1h,3h,5h)-trione
CS-0615
ponazuril [green book]
ponazuril [mi]
SCHEMBL203030
AC-28364
AKOS025312522
toltrazuril sulfone, vetranal(tm), analytical standard
AS-74844
1-methyl-3-[3-methyl-4-(4-trifluoromethanesulfonylphenoxy)phenyl]-1,3,5-triazinane-2,4,6-trione
1-methyl-3-(3-methyl-4-(4-((trifluoromethyl)sulfonyl)phenoxy)phenyl)-1,3,5-triazinane-2,4,6-trione
DB11452
BCP14930
Q7227567
NCGC00182044-02
D95987
vbunoixrznjnad-uhfffaoysa-n
gtpl12223
acd-855
marquis (vet use only)
acd855
ponazurilo
ponazurilum
marquis antiprotozoal oral paste

Research Excerpts

Overview

Ponazuril is a triazine anticoccidial recently approved for use in horses in the United States.

ExcerptReferenceRelevance
"Ponazuril is a triazine anticoccidial recently approved for use in horses in the United States."( Mode of action of ponazuril against Toxoplasma gondii tachyzoites in cell culture.
Davis, WL; Lindsay, DS; Mitchell, SM; Zajac, AM, 2003)		1.37
"Ponazuril is a triazine anticoccidial recently approved for use in horses in the United States."( Efficacy of ponazuril in vitro and in preventing and treating Toxoplasma gondii infections in mice.
Davis, WL; Lindsay, DS; Mitchell, SM; Zajac, AM, 2004)		1.42

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameters were derived by use of a standard noncompartmental pharmacokinetic analysis."( Pharmacokinetics of ponazuril after oral administration to healthy llamas (Lama glama).
Boileau, MJ; Martin-Jimenez, T; Meibohm, B; Prado, ME; Ryman, JT, 2011)		0.69
"0 mg/L, and the elimination half-life was 135."( Pharmacokinetics of ponazuril after oral administration to healthy llamas (Lama glama).
Boileau, MJ; Martin-Jimenez, T; Meibohm, B; Prado, ME; Ryman, JT, 2011)		0.69
" Pharmacokinetic parameters were derived by use of a standard noncompartmental pharmacokinetic analysis."( Detection, quantifications, and pharmacokinetics of ponazuril in healthy swine.
Guo, G; Zhang, Q; Zhao, Y; Zou, M, 2014)		0.65
"8 μg/mL after 168 h with an average elimination half-life of 129 ± 72 h post drug administration."( Pharmacokinetics of single-dose oral ponazuril in weanling goats.
Fajt, V; Gibbons, P; Jones, M; Love, D, 2016)		0.71

Bioavailability

Ponazuril is relatively well absorbed after a single oral dose in goats. This makes it likely to be effective in swine.

ExcerptReferenceRelevance
" This study shows that toltrazuril sulfone is relatively well absorbed after oral dose in cattle."( Detection, quantifications and pharmacokinetics of toltrazuril sulfone (Ponazuril) in cattle.
Chakkath, T; Dirikolu, L; Ferguson, DC; Garrett, EF; Yohn, R, 2009)		0.59
" In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses."( Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse.
Dirikolu, L; Karpiesiuk, W; Lehner, AF; Tobin, T, 2012)		0.38
" The results indicate that ponazuril was relatively well absorbed following a single dose, which makes ponazuril likely to be effective in swine."( Detection, quantifications, and pharmacokinetics of ponazuril in healthy swine.
Guo, G; Zhang, Q; Zhao, Y; Zou, M, 2014)		0.95
" This study shows that ponazuril is relatively well absorbed after a single oral dose in goats."( Pharmacokinetics of single-dose oral ponazuril in weanling goats.
Fajt, V; Gibbons, P; Jones, M; Love, D, 2016)		1.02
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

Ponazuril 15% oral paste was administered to 24 horses at 0, 10, or 30 mg/kg body weight for either 28 or 56 days. Analysis of serum levels indicated that therapeutic levels could be achieved at a dosage of 5mg/kg p.

ExcerptRelevanceReference
" Ponazuril 15% oral paste was administered to 24 horses at 0, 10, or 30 mg/kg body weight for either 28 or 56 days, representing zero, two, and six times the proposed dosage rate and one and two times the recommended duration of treatment, respectively."( Safety of ponazuril 15% oral paste in horses.
Campbell, J; Kennedy, T; Selzer, V, 2001)		1.62
" Cerebrospinal fluid concentration did not vary during the 28 days of dosing and concentrations declined rapidly after cessation of administration on Day 28."( Cerebrospinal fluid and serum concentrations of ponazuril in horses.
Furr, M; Kennedy, T, 2001)		0.57
" The aim of this study was to determine the efficacy of ponazuril paste at each of three dosages (dosage 1, 50mg/kg q24 h for 3 days, dogs n=14, cats n=16; dosage 2, 50mg/kg as a single dose, dogs n=13, cats n=25; or dosage 3, 20mg/kg as a single dose, dogs n=16, cats n=23) in shelter-housed dogs (n=43) and cats (n=64) with confirmed coccidiosis."( Use of ponazuril paste to treat coccidiosis in shelter-housed cats and dogs.
Camp, J; Hall, K; Litster, AL; Mohamed, AS; Nichols, J, 2014)		1.1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency21.69880.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency22.65990.000221.22318,912.5098AID743035; AID743042; AID743053; AID743054; AID743063
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency11.98560.000214.376460.0339AID720691
estrogen nuclear receptor alphaHomo sapiens (human)Potency20.43120.000229.305416,493.5996AID743069; AID743075; AID743078; AID743079; AID743080; AID743091
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency15.99800.001019.414170.9645AID743094; AID743140
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency23.17800.000323.4451159.6830AID743065; AID743066; AID743067
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.44810.009610.525035.4813AID1479145; AID1479148
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (9.30)18.7374
1990's0 (0.00)18.2507
2000's17 (39.53)29.6817
2010's14 (32.56)24.3611
2020's8 (18.60)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.59

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 Index39.59 (24.57)
Research Supply Index3.95 (2.92)
Research Growth Index5.81 (4.65)
Search Engine Demand Index107.37 (26.88)
Search Engine Supply Index3.98 (0.95)

This Compound (39.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (8.51%)5.53%
Reviews1 (2.13%)6.00%
Case Studies5 (10.64%)4.05%
Observational0 (0.00%)0.25%
Other37 (78.72%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
amprolium
Amprolium: A veterinary coccidiostat that interferes with THIAMINE metabolism.. amprolium : An organic chloride salt having 1-[(4-amino-2-propylpyrimidin-5-yl)methyl]-2-methylpyridin-1-ium as the counterion. Used for prevention of coccidiosis in poultry and cattle.. amprolium(1+) : A pyridinium ion that is the cationic portion of amprolium, a veterinary drug which is used for prevention of coccidiosis in poultry and cattle.		7.1310pyridinium ioncoccidiostat
clazuril
[no description available]		3.2710
toltrazuril
toltrazuril: structure in first source		4.460aromatic ether
cortisone
[no description available]		2.021011-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		human metabolite;
mouse metabolite
diclazuril
[no description available]		3.2710nitrile
2-(3-methyl-4-(4-nitrophenoxy)phenyl)-1,2,4-triazine-3,5(2h,4h)-dione
2-(3-methyl-4-(4-nitrophenoxy)phenyl)-1,2,4-triazine-3,5(2H,4H)-dione: a coccidiostat		3.2710
ConditionIndicatedRelationship StrengthStudiesTrials
Besnoitiasis
[description not available]		04.7100
Cat Diseases
Diseases of the domestic cat (Felis catus or F. domesticus). This term does not include diseases of the so-called big cats such as CHEETAHS; LIONS; tigers, cougars, panthers, leopards, and other Felidae for which the heading CARNIVORA is used.		02.5820
Cognitive Decline
[description not available]		02.3110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.9640
Cognitive Dysfunction
Diminished or impaired mental and/or intellectual function.		02.3110
Protozoan Infections, Animal
Infections with unicellular organisms formerly members of the subkingdom Protozoa. The infections may be experimental or veterinary.		03.0910
Encephalitis, Equine
[description not available]		03.0910
Toxoplasmosis, Animal
Acquired infection of non-human animals by organisms of the genus TOXOPLASMA.		03.3820
Encephalomyelitis, Inflammatory
[description not available]		05.3672
Equine Diseases
[description not available]		05.7173
Sarcocystosis
Infection of the striated muscle of mammals by parasites of the genus SARCOCYSTIS. Disease symptoms such as vomiting, diarrhea, muscle weakness, and paralysis are produced by sarcocystin, a toxin produced by the organism.		05.3672
Encephalomyelitis
A general term indicating inflammation of the BRAIN and SPINAL CORD, often used to indicate an infectious process, but also applicable to a variety of autoimmune and toxic-metabolic conditions. There is significant overlap regarding the usage of this term and ENCEPHALITIS in the literature.		05.3672
Canine Diseases
[description not available]		02.110
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.4620
Caprine Diseases
[description not available]		02.1310
Eye Disorders
[description not available]		02.0510
Anterior Horn Cell Disease
[description not available]		02.0510
Eye Diseases
Diseases affecting the eye.		02.0510
Motor Neuron Disease
Diseases characterized by a selective degeneration of the motor neurons of the spinal cord, brainstem, or motor cortex. Clinical subtypes are distinguished by the major site of degeneration. In AMYOTROPHIC LATERAL SCLEROSIS there is involvement of upper, lower, and brainstem motor neurons. In progressive muscular atrophy and related syndromes (see MUSCULAR ATROPHY, SPINAL) the motor neurons in the spinal cord are primarily affected. With progressive bulbar palsy (BULBAR PALSY, PROGRESSIVE), the initial degeneration occurs in the brainstem. In primary lateral sclerosis, the cortical neurons are affected in isolation. (Adams et al., Principles of Neurology, 6th ed, p1089)		02.0510
Acute Disease
Disease having a short and relatively severe course.		02.0210
Central Nervous System Toxoplasmosis
[description not available]		02.0310
Toxoplasmosis, Cerebral
Infections of the BRAIN caused by the protozoan TOXOPLASMA gondii that primarily arise in individuals with IMMUNOLOGIC DEFICIENCY SYNDROMES (see also AIDS-RELATED OPPORTUNISTIC INFECTIONS). The infection may involve the brain diffusely or form discrete abscesses. Clinical manifestations include SEIZURES, altered mentation, headache, focal neurologic deficits, and INTRACRANIAL HYPERTENSION. (From Joynt, Clinical Neurology, 1998, Ch27, pp41-3)		02.0310