Page last updated: 2024-11-05

triflusal

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Description

Triflusal is a non-steroidal anti-inflammatory drug (NSAID) with antiplatelet activity. It is used to prevent blood clots in people who have had a heart attack, stroke, or other circulatory problems. Triflusal is a prodrug that is converted to its active metabolite, salicylic acid, in the body. Triflusal inhibits platelet aggregation by irreversibly acetylating the platelet cyclooxygenase enzyme. This inhibition of cyclooxygenase prevents the formation of thromboxane A2, a potent platelet aggregator. Triflusal has been shown to reduce the risk of cardiovascular events, such as stroke and myocardial infarction, in patients with a history of cardiovascular disease. Triflusal is also being studied for its potential use in the prevention of Alzheimer's disease. Triflusal is generally well-tolerated, but it can cause gastrointestinal side effects such as heartburn, nausea, and ulcers. It can also increase the risk of bleeding. Triflusal should be used with caution in patients with a history of gastrointestinal bleeding, kidney disease, or liver disease.'

triflusal: inhibits platelet aggregation similarly to aspirin; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9458
CHEMBL ID1332032
CHEBI ID94721
SCHEMBL ID136423
MeSH IDM0065977

Synonyms (87)

Synonym
AC-1829
PRESTWICK3_000528
triflux
disgren
ur-1501
tecnosal
BPBIO1_000567
BSPBIO_000515
einecs 206-297-5
2,4-cresotic acid, alpha,alpha,alpha-trifluoro-, acetate
3-acetoxy-alpha,alpha,alpha-trifluoro-p-toluic acid
c10h7f3o4
2-(acetyloxy)-4-(trifluoromethyl)benzoic acid
benzoic acid, 2-(acetyloxy)-4-(trifluoromethyl)-
brn 2945374
4-trifluoromethylsalicylic acid acetate
alpha,alpha,alpha-trifluoro-2,4-creosotic acid acetate
triflusalum [inn-latin]
2-acetoxy-4-trifluoromethylbenzoic acid
triflusal [inn]
alpha,alpha,alpha-trifluoro-2,4-cresotic acid acetate
ur 1501
triflusal
322-79-2
PRESTWICK_851
NCGC00016431-01
cas-322-79-2
triflusal (inn)
D07142
PRESTWICK2_000528
SPBIO_002436
PRESTWICK1_000528
PRESTWICK0_000528
NCGC00016431-02
2-acetyloxy-4-(trifluoromethyl)benzoic acid
HMS1569J17
A5797
2-acetoxy-4-trifluoromethyl-benzoic acid
HMS2096J17
triflusal [inn:ban]
grendis
unii-1z0yfi05oo
triflusalum
aflen
4-10-00-00619 (beilstein handbook reference)
1z0yfi05oo ,
dtxcid6025305
dtxsid8045305 ,
tox21_110436
S3200
FT-0601555
AKOS015890393
CHEMBL1332032
BRD-K71696703-001-01-2
2-acetoxy-4-(trifluoromethyl)benzoic acid
CCG-222319
CCG-220528
HY-B0531
SCHEMBL136423
MB01536
triflusal [mi]
triflusal [ep monograph]
triflusal [mart.]
triflusal [who-dd]
NCGC00016431-04
W-106849
drisgen
ur1501
SR-01000872666-1
sr-01000872666
CHEBI:94721
HMS3652M11
AS-63983
triflusal; 2-(acetyloxy)-4-(trifluoromethyl)benzoic acid
HMS3713J17
SW196982-3
DB08814
mfcd00866793
2-acetoxy-4-trifluoromethyl benzoic acid
T3601
acetyl-4-(trifluoromethyl)salicylic acid
BCP10024
Q1758668
NCGC00016431-11
HMS3885I13
T72290
EN300-18567716

Research Excerpts

Overview

Triflusal is a 4-fluoromethyl derivative of salicylic acid used for secondary prevention of ischemic stroke. It exhibits different pharmacological and pharmacokinetic properties from aspirin. TrifLusal is an antiplatelet agent that has shown clinical advantages when compared with aspirin.

ExcerptReferenceRelevance
"Triflusal is a drug that inhibits platelet aggregation. "( Population pharmacokinetic and pharmacodynamic modeling of transformed binary effect data of triflusal in healthy Korean male volunteers: a randomized, open-label, multiple dose, crossover study.
Gwon, MR; Han, S; Kwon, KI; Lee, HW; Lee, J; Lim, MS; Park, JG; Park, SM; Seong, SJ; Yang, DH; Yoon, YR, 2014
)
2.06
"Triflusal is a 4-fluoromethyl derivative of salicylic acid used for secondary prevention of ischemic stroke. "( Triflusal and aspirin have different effects on inflammatory biomarkers measured in patients with acute ischemic stroke.
Alvarez-Sabín, J; García-Bonilla, L; Krupinski, J; Montaner, J; Penalba, A; Quintana, M, 2009
)
3.24
"Triflusal is a derivative of acetylsalicylic acid but it exhibits different pharmacological and pharmacokinetic properties. "( Comparison of triple antiplatelet therapy including triflusal and conventional dual therapy in patients who underwent drug-eluting stent implantation.
Kang, HJ; Kim, HS; Kim, SY; Kim, YS; Koo, BK; Park, JS; Suh, JW, 2009
)
2.05
"Triflusal is an antiplatelet agent that irreversibly acetylates cyclooxygenase isoform 1 (COX-1) and therefore inhibits thromboxane biosynthesis. "( Gastrointestinal safety of triflusal solution in healthy volunteers: a proof of concept endoscopic study.
Antonijoan, RM; Azaro, A; Balanzó, J; Barbanoj, MJ; Blanch, I; Borja, J; Donado, E; Gich, I; Izquierdo, I; Sainz, S, 2011
)
2.11
"Triflusal is an antiplatelet salicylate derivative with anti-inflammatory effects."( Comparative effects of triflusal, S-adenosylmethionine, and dextromethorphan over intestinal ischemia/reperfusion injury.
Alarcón-Galván, G; Cámara-Lemarroy, CR; Cordero-Pérez, P; Fernández-Garza, NE; Guzmán-de la Garza, FJ; Muñoz-Espinosa, LE; Torres-Gonzalez, L, 2011
)
1.4
"Triflusal is an antiplatelet agent that has shown clinical advantages when compared with aspirin in the secondary prevention of vascular events. "( Triflusal vs aspirin for prevention of cerebral infarction: a randomized stroke study.
Abiusi, G; Bauso-Tosselli, L; Culebras, A; Domínguez, R; Famulari, A; Ferrari, J; Gori, H; Reich, E; Rey, R; Rotta-Escalante, R; Vila, J, 2004
)
3.21
"Triflusal is a fluorinated derivative of acetylsalicylic acid (ASA) with demonstrated antithrombotic activity. "( Protective effect of triflusal and its main metabolite HTB in an in vitro model of anoxia-reoxygenation in rat brain slices: comparison with acetylsalicylic and salicylic acids.
Arrebola, MM; De La Cruz, JP; González-Correa, JA; Guerrero, A; Muñoz-Marín, J; Ruiz-Villafranca, D; Sánchez de la Cuesta, F; Ureña, IM, 2005
)
2.09
"Triflusal is an antiplatelet drug related to aspirin, with different pharmacological properties and a lower haemorrhagic risk. "( Inhibition of thromboxane biosynthesis by triflusal in type 2 diabetes mellitus.
Avellone, G; Ballone, E; Ciabattoni, G; Davì, G; Di Febbo, C; Di Nicola, M; Falco, A; Pinto, A; Salvati, F; Vitacolonna, E, 2005
)
2.04
"Triflusal is a derivative of salicylic acid with a well-established platelet aggregation inhibitory profile. "( Triflusal: an antiplatelet drug with a neuroprotective effect?
De La Cruz, JP; González-Correa, JA, 2006
)
3.22
"Triflusal is a preferential COX-2 inhibitor antiplatelet agent that is as effective as aspirin in the prevention of serious vascular events."( Safety of triflusal (antiplatelet drug) in patients with aspirin-exacerbated respiratory diseases.
Borja, J; Fraj, J; Izquierdo, I; Pérez, I; Picado, C; Valero, A; Vives, R, 2008
)
1.47
"Triflusal is an antiplatelet agent structurally related to the salicylate group of compounds, but it is not derived from aspirin (acetylsalicylic acid). "( Triflusal.
Goa, KL; McNeely, W, 1998
)
3.19
"Triflusal is a fluorinated aspirin derivative with antiplatelet properties, which is used in Spain for the management and prevention of thromboembolic disease."( Photosensitivity associated with treatment with triflusal.
Aliaga, A; Nagore, E; Pérez-Ferriols, A; Sánchez-Motilla, JM; Serrano, G, 2000
)
2.01
"Triflusal is a platelet antiaggregant drug with photoallergic side effects. "( Photochemistry of 2-hydroxy-4-trifluoromethylbenzoic acid, major metabolite of the photosensitizing platelet antiaggregant drug triflusal.
Boscá, F; Cuquerella, MC; Marín, ML; Miranda, MA, 2001
)
1.96
"Triflusal is an irreversible inhibitor of platelet cyclooxygenase. "( Compliance of geriatric patients subjected to antiplatelet agents with Triflusal in peripheral arteriopathy. Preliminary data.
Apostolou, D; Comelli, S; Maselli, M; Moniaci, D; Ortensio, M; Scovazzi, P; Varetto, G; Zan, S, 2002
)
1.99
"Triflusal is a new antithrombotic agent, structurally similar to acetylsalicylic acid (ASA), which has been shown to possess a different pharmacological profile, suggesting a different mechanism of action for both compounds. "( Comparison of the inhibitory effects of acetylsalicylic acid and trifusal on enzymes related to thrombosis.
Garcia Rafanell, J; Planas, JM; Puig-Parellada, P, 1979
)
1.7
"1. Triflusal is a salicylic derivative that inhibits platelet aggregation in human whole blood with a minimal inhibition of prostacyclin production. "( Triflusal vs aspirin on the inhibition of human platelet and vascular cyclooxygenase.
de la Cruz, JP; Mata, JM; Sanchez de la Cuesta, F, 1992
)
2.35
"Triflusal (TR) is a new salicylic acid derivative used clinically as an antiplatelet drug. "( Effects and interaction studies of triflusal and other salicylic derivatives on cyclooxygenase in rats.
Albors, M; De Castellarnau, C; Rutllant, ML; Sancho, MJ; Vila, L, 1988
)
1.99

Effects

Triflusal has demonstrated an efficacy similar to aspirin in the prevention of vascular events in patients with acute myocardial infarction (ΜΙ) and ischaemic stroke. It downregulates molecules considered responsible for the development of Alzheimer's disease.

ExcerptReferenceRelevance
"Triflusal has demonstrated an efficacy similar to aspirin in the prevention of vascular events in patients with acute myocardial infarction (ΜΙ) and ischaemic stroke but with less bleeding events."( Comparison of Triflusal with Aspirin in the Secondary Prevention of Atherothrombotic Events; Α Randomised Clinical Trial.
Adamopoulos, D; Asimakopoulos, C; Bourdakis, A; Chantzichristos, VG; Darmanis, P; Dimitriadou, A; Gkiokas, S; Goudevenos, JA; Ipeirotis, K; Kalantzi, KI; Kitikidou, K; Klonaris, I; Kostaki, A; Logothetis, D; Mainas, K; Mais, T; Maragiannis, A; Martiadou, K; Mavronasos, K; Michelongonas, I; Mitropoulos, D; Ntalas, IV; Panagiotakos, DB; Papadimitriou, G; Papadopoulos, A; Papaioakeim, M; Sofillas, K; Stabola, S; Stefanakis, E; Stergiou, D; Thoma, M; Tselepis, AD; Tsoumani, ME; Zenetos, A; Zisekas, S, 2019
)
2.32
"Triflusal has been shown to exert neuroprotective effects by downregulating molecules considered responsible for the development of Alzheimer's disease (AD). "( Access of HTB, main metabolite of triflusal, to cerebrospinal fluid in healthy volunteers.
Barbanoj, MJ; Brunner, M; Donner, A; Eichler, HG; Herranz, U; Izquierdo, I; Klein, N; Müller, M; Valle, M, 2005
)
2.05

Actions

ExcerptReferenceRelevance
"Triflusal displays a Cmax of 11.6 +/- 1.7 micrograms/ml and a tmax of 0.88 +/- 0.26 h."( Pharmacokinetics of triflusal and its main metabolite HTB in healthy subjects following a single oral dose.
Forn, J; Gorina, E; Jané, F; Mis, R; Ramis, J; Torrent, J,
)
1.18

Treatment

Triflusal treatment did not alter the total brain Abeta accumulation but significantly reduced dense-cored plaque load and associated glial cell proliferation. Posttreatment diminishes glial NF-kappaB, downregulates the glial response and improves the lesion outcome.

ExcerptReferenceRelevance
"Triflusal treatment did not alter the total brain Abeta accumulation but significantly reduced dense-cored plaque load and associated glial cell proliferation, proinflammatory cytokine levels and abnormal axonal curvature, and rescued cognitive deficits in Tg2576 mice."( Triflusal reduces dense-core plaque load, associated axonal alterations and inflammatory changes, and rescues cognition in a transgenic mouse model of Alzheimer's disease.
Agulló, J; Bacskai, BJ; Borrelli, LA; Clarimón, J; Coma, M; Da Rocha-Souto, B; España, J; Garcia-Alloza, M; Gómez-Isla, T; Guardia-Laguarta, C; Hyman, BT; Lleó, A; Rodríguez, M; Sánchez, MB; Saura, CA; Scotton, TC; Serenó, L, 2010
)
2.52
"Triflusal posttreatment diminishes glial NF-kappaB, downregulates the glial response, and improves the lesion outcome, suggesting a neuroprotective role of this compound against excitotoxic injury in the immature brain."( Triflusal posttreatment inhibits glial nuclear factor-kappaB, downregulates the glial response, and is neuroprotective in an excitotoxic injury model in postnatal brain.
Acarin, L; Castellano, B; González, B, 2001
)
3.2

Toxicity

ExcerptReferenceRelevance
"Low-dose aspirin (acetylsalicylic acid) has been shown to be as effective as high-dose aspirin in the prevention of stroke, with fewer adverse bleeding events."( Adverse effects and drug interactions of antithrombotic agents used in prevention of ischaemic stroke.
Weinberger, J, 2005
)
0.33
"An enteric-coated formulation of triflusal (triflusal EC), an antiplatelet agent, was developed to reduce the high incidence of gastrointestinal adverse events (AEs)."( A phase I study to characterize the multiple-dose pharmacokinetics, pharmacodynamics and safety of new enteric-coated triflusal formulations in healthy male volunteers.
Baek, IH; Kwon, KI; Lee, HW; Lee, J; Lim, MS; Park, J; Seo, JJ; Seong, SJ; Yoon, YR; Yun, HY, 2011
)
0.86
" Safety was assessed by adverse events, ECG, laboratory testing, and vital signs."( Pharmacokinetics, safety and tolerability of triflusal and its main active metabolite HTB in healthy Chinese subjects.
Hua, W; Huang, M; Wang, M; Zhang, Q; Zhou, W; Zong, S, 2014
)
0.66

Pharmacokinetics

The pharmacokinetic profile of triflusal (2-acetoxy-4-trifluoromethyl benzoic acid) and its main metabolite HTB has been studied in 8 healthy subjects (4 males and 4 females), after a single oral dose of 900 mg. The mean Cmax of tr iflusal and HTB were 13.

ExcerptReferenceRelevance
" In the present study, we have developed a new analytical technique based on HPLC that enabled us to carry out a pharmacokinetic study of the drug and its metabolite in animals."( Pharmacokinetics of triflusal and its main metabolite in rats and dogs.
Forn, J; Mis, R; Ramis, J,
)
0.45
"The pharmacokinetic profile of triflusal (2-acetoxy-4-trifluoromethyl benzoic acid) and its main metabolite HTB (2-hydroxy-4-trifluoromethyl benzoic acid) has been studied in 8 healthy subjects (4 males and 4 females), after a single oral dose of 900 mg of triflusal."( Pharmacokinetics of triflusal and its main metabolite HTB in healthy subjects following a single oral dose.
Forn, J; Gorina, E; Jané, F; Mis, R; Ramis, J; Torrent, J,
)
0.74
" No significant differences were observed between the elimination half-life obtained after the single dose and after the two repeated dose regimens studied."( Pharmacokinetics of triflusal after single and repeated doses in man.
Barbanoj, MJ; Conte, L; Forn, J; Jané, J; Mis, R; Ramis, J; Torrent, J, 1990
)
0.6
"The pharmacokinetic and pharmacodynamic profiles of the two triflusal formulations met the requirements for bioequivalence and non-inferiority, respectively."( A phase I study to characterize the multiple-dose pharmacokinetics, pharmacodynamics and safety of new enteric-coated triflusal formulations in healthy male volunteers.
Baek, IH; Kwon, KI; Lee, HW; Lee, J; Lim, MS; Park, J; Seo, JJ; Seong, SJ; Yoon, YR; Yun, HY, 2011
)
0.82
" In this study we investigated the dose-exposure-response relationship of a triflusal formulation by population pharmacokinetic (PK) and pharmacodynamic (PD) modeling of its main active metabolite, hydroxy-4-(trifluoromethyl) benzoic acid (HTB)."( Population pharmacokinetic and pharmacodynamic modeling of transformed binary effect data of triflusal in healthy Korean male volunteers: a randomized, open-label, multiple dose, crossover study.
Gwon, MR; Han, S; Kwon, KI; Lee, HW; Lee, J; Lim, MS; Park, JG; Park, SM; Seong, SJ; Yang, DH; Yoon, YR, 2014
)
0.85
"The objective of this study was to evaluate the pharmacokinetic parameters of triflusal and its major active metabolite, 2-hydroxy-4-trifluoromethyl benzoic acid (HTB), following a single oral dose of 900 mg in healthy subjects under fed and fasting conditions."( Effect of food on the pharmacokinetics of triflusal and its major active metabolite, 2-hydroxy-4-trifluoromethyl benzoic acid, in healthy subjects.
Ding, LK; Ding, Y; Ge, J; Jia, YY; Lu, CT; Song, W; Song, Y; Wen, AD; Yang, J, 2015
)
0.91
"The mean Cmax of triflusal and HTB were 13."( Effect of food on the pharmacokinetics of triflusal and its major active metabolite, 2-hydroxy-4-trifluoromethyl benzoic acid, in healthy subjects.
Ding, LK; Ding, Y; Ge, J; Jia, YY; Lu, CT; Song, W; Song, Y; Wen, AD; Yang, J, 2015
)
1.02

Bioavailability

The purpose of this clinical trial was to study the relative bioavailability of the new oral solution of triflusal versus the capsules formulation. Both were administered as a single dose.

ExcerptReferenceRelevance
" The bioavailability of triflusal in rats was only 10."( Pharmacokinetics of triflusal and its main metabolite in rats and dogs.
Forn, J; Mis, R; Ramis, J,
)
0.76
" The purpose of this clinical trial was to study the relative bioavailability of the new oral solution of triflusal versus the capsules formulation, both administered as a single dose."( Comparative bioavailability study of triflusal oral solution vs. triflusal capsules in healthy subjects. A single, randomized, two-way cross-over, open-label phase I study.
Borja, J; Cebrecos, J; García-Rafanell, J; Izquierdo, I; Pelagio, P; Rovira, S; Torres, F, 2010
)
0.85
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Triflusal pharmacokinetics were evaluated in 8 healthy subjects after a single 300 mg dose and after repeated doses of 300 mg every 8 h and 600 mg every 24 h during 13 days.

ExcerptRelevanceReference
"ss) during the multiple dosage regimen of 300 mg every 8 h, and 131 micrograms."( Binding of a metabolite of triflusal (2-hydroxy-4-trifluoromethylbenzoic acid) to serum proteins in rat and man.
Conte, L; Forn, J; Mis, R; Ramis, J, 1992
)
0.58
"Triflusal pharmacokinetics were evaluated in 8 healthy subjects after a single 300 mg dose and after repeated doses of 300 mg every 8 h and 600 mg every 24 h during 13 days, with the aim of establishing a relationship between plasma levels and dosage patterns."( Pharmacokinetics of triflusal after single and repeated doses in man.
Barbanoj, MJ; Conte, L; Forn, J; Jané, J; Mis, R; Ramis, J; Torrent, J, 1990
)
2.05
"Following oral dosing under fasting condition, triflusal is promptly absorbed and rapidly depleted from the systemic circulation."( Pharmacokinetics, safety and tolerability of triflusal and its main active metabolite HTB in healthy Chinese subjects.
Hua, W; Huang, M; Wang, M; Zhang, Q; Zhou, W; Zong, S, 2014
)
0.92
"The time-concentration profile of HTB over the entire dosing period was described by a one-compartment model with a first-order formation rate constant for HTB."( Population pharmacokinetic and pharmacodynamic modeling of transformed binary effect data of triflusal in healthy Korean male volunteers: a randomized, open-label, multiple dose, crossover study.
Gwon, MR; Han, S; Kwon, KI; Lee, HW; Lee, J; Lim, MS; Park, JG; Park, SM; Seong, SJ; Yang, DH; Yoon, YR, 2014
)
0.62
" Following oral dosing in rats for 7 days, salbutamol and triflusal, but not dimethadione or trazodone, significantly elevated FGF20 levels in the nigrostriatal tract."( Targeted repositioning identifies drugs that increase fibroblast growth factor 20 production and protect against 6-hydroxydopamine-induced nigral cell loss in rats.
Doherty, P; Duty, S; Fletcher, EJR; Jamieson, AD; Williams, G, 2019
)
0.76
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

ClassDescription
salicylatesAny salt or ester arising from reaction of the carboxy group of salicylic acid, or any ester resulting from the condensation of the phenolic hydroxy group of salicylic acid with an organic acid.
carboxylic esterAn ester of a carboxylic acid, R(1)C(=O)OR(2), where R(1) = H or organyl and R(2) = organyl.
benzoic acidsAny aromatic carboxylic acid that consists of benzene in which at least a single hydrogen has been substituted by a carboxy group.
[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 (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency12.58930.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency12.58930.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency15.84890.177814.390939.8107AID2147
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency15.84890.011212.4002100.0000AID1030
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.52210.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency21.31740.01238.964839.8107AID1645842
cytochrome P450 2C19 precursorHomo sapiens (human)Potency3.98110.00255.840031.6228AID899
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency14.12540.001815.663839.8107AID894
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency5.01190.65619.452025.1189AID927
Interferon betaHomo sapiens (human)Potency21.31740.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency5.01191.584913.004325.1189AID927
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (82)

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)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

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)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (29)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1136196Antiinflammatory activity against carrageenan-induced foot edema in rat administered via gastric gavage1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Novel analgesic-antiinflammatory salicylates.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (147)

TimeframeStudies, This Drug (%)All Drugs %
pre-199024 (16.33)18.7374
1990's25 (17.01)18.2507
2000's55 (37.41)29.6817
2010's37 (25.17)24.3611
2020's6 (4.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.41

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

MetricThis Compound (vs All)
Research Demand Index56.41 (24.57)
Research Supply Index5.32 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index91.89 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials39 (23.78%)5.53%
Reviews11 (6.71%)6.00%
Case Studies9 (5.49%)4.05%
Observational1 (0.61%)0.25%
Other104 (63.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Randomized Placebo Controlled Phase II Cross Over Study on the Influence of Triflusal on Cognitive Functions in Healthy Participants [NCT02321852]Phase 240 participants (Actual)Interventional2015-01-31Completed
Comparison of Triflusal and Clopidogrel Effect in Secondary Prevention of Stroke Based on the Cytochrome P450 2C19 Genotyping [NCT01174693]Phase 4795 participants (Actual)Interventional2010-03-31Completed
Comparison of Triflusal With Aspirin in the Secondary Prevention of Atherothrombotic Events [NCT02616497]Phase 41,220 participants (Actual)Interventional2015-09-30Completed
Randomized Placebo Controlled Phase II Cross Over Study on the Influence of Triflusal on Cognitive Functions in Subjects Under Chronic Stress [NCT02904109]Phase 241 participants (Actual)Interventional2016-09-13Completed
Phase IIa Study of Triflusal in the Attenuation of Insulin Resistance in Men and Woman With Obesity [NCT00162799]Phase 230 participants Interventional2002-07-31Completed
The Effect of Triflusal on Peripheral Microcirculation Dysfunction: A Double-Blind, Randomized, Controlled, Crossover Study. [NCT01612273]Phase 492 participants (Actual)Interventional2011-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]