Delving into the Latest Updates on Triflusal with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Aflen, Disgren, Tecnosal

+ [4]

Target

COX-1

Action

inhibitors

Mechanism

COX-1 inhibitors(Cyclooxygenase-1 inhibitors), Platelet aggregation inhibitors

Therapeutic Areas

Cardiovascular DiseasesNervous System Diseases

Active Indication

ThromboembolismThrombosisBrain Infarction+ [1]

Inactive Indication

Blood Platelet DisordersInsulin Resistance

Originator Organization

Noucor Health SA

Active Organization

Noucor Health SA

Xi'an Xintong Pharmaceutical Research Co., Ltd.

Zhengzhou Tongtai Pharmaceutical Technology Co., Ltd.

+ [1]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Spain (01 Jan 1981),

ThromboembolismThrombosis

Regulation-

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Structure/Sequence

Molecular FormulaC10H7F3O4

InChIKeyRMWVZGDJPAKBDE-UHFFFAOYSA-N

CAS Registry322-79-2

Quality deterioration due to undesirable discolorations in crude pine oleoresin during storage is a major problem limiting its subsequent processing applications.To reveal the essence of color changes, the browning phenomenon and comprehensive mechanism of crude pine oleoresin during storage were investigated in depth using an approach based on high-resolution mass spectrometry metabolomics.Crude pine oleoresin was stored with sterile, deionized, tap, and pond water for 30, 60, 90, 120, 150, and 180 days, resp.The changes in browning substrate were detected by tracking anal. protein, reducing sugar, ascorbic acid, and total phenol content, browning was evaluated through colorimeter measurement.The metabolism of crude pine oleoresin in different storage times was uncovered that total color difference (ΔE) increased with storage time, and the browning of crude pine oleoresin soaked in tap water was greatest while soaked in deionized water exhibited the mildest.The content of reducing sugars, proteins, and total phenols increased with storage time, whereas the ascorbic acid content tended to increase and then decrease.Furthermore, the metabolomics analyses showed that 1,194 and 979 differentially metabolized compounds were found between days 120 and days 150, and days 120 and days 180.The metabolite profiles in the water samples changed as crude pine oleoresin storage time increased.Most carbohydrate content decreased, and the phenols and organic acids content increased.Metabolic network mapping linking differentially metabolized compounds by mapping different biosynthetic pathways proved that caffeoylquinic acid and catechin play a key role in the browning of crude pine oleoresin during storage: caffeoylquinic acid forms black iron complexes with iron, and catechin is oxidized to catechol quinone, which eventually produces a yellow dimer.This study will provide a scientific basis for developing or choosing more effective methods for controlling the discoloration of crude pine oleoresin and other similar products during storage.

21 Sep 2024·International journal of molecular sciences

Differential Effect of Omega-3 Fatty Acids on Platelet Inhibition by Antiplatelet Drugs In Vitro.

Article

Author: Tsouka, Aikaterini N ; Tselepis, Alexandros D ; Pantazi, Despoina ; Argyropoulou, Ourania ; Tellis, Constantinos C ; Koutsaliaris, Ioannis K

The omega-3 polyunsaturated fatty acids (PUFAs) Docosahexaenoic acid (DHA) and Eicosapentaenoic acid (EPA) exert multiple cardioprotective effects, influencing inflammation, platelet activation, endothelial function and lipid metabolism, besides their well-established triglyceride lowering properties. It is not uncommon for omega-3 PUFAs to be prescribed for hypertriglyceridemia, alongside antiplatelet therapy in cardiovascular disease (CVD) patients. In this regard, we studied the effect of EPA and DHA, in combination with antiplatelet drugs, in platelet aggregation and P-selectin and α_IIbβ₃ membrane expression. The antiplatelet drugs aspirin and triflusal, inhibitors of cyclooxygenase-1 (COX-1); ticagrelor, an inhibitor of the receptor P2Y₁₂; vorapaxar, an inhibitor of the PAR-1 receptor, were combined with DHA or EPA and evaluated against in vitro platelet aggregation induced by agonists arachidonic acid (AA), adenosine diphosphate (ADP) and TRAP-6. We further investigated procaspase-activating compound 1 (PAC-1) binding and P-selectin membrane expression in platelets stimulated with ADP and TRAP-6. Both DHA and EPA displayed a dose-dependent inhibitory effect on platelet aggregation induced by AA, ADP and TRAP-6. In platelet aggregation induced by AA, DHA significantly improved acetylsalicylic acid (ASA) and triflusal's inhibitory activity, while EPA enhanced the inhibitory effect of ASA. In combination with EPA, ASA and ticagrelor expressed an increased inhibitory effect towards ADP-induced platelet activation. Both fatty acids could not improve the inhibitory effect of vorapaxar on AA- and ADP-induced platelet aggregation. In the presence of EPA, all antiplatelet drugs displayed a stronger inhibitory effect towards TRAP-6-induced platelet activation. Both omega-3 PUFAs inhibited the membrane expression of α_IIbβ₃, though they had no effect on P-selectin expression induced by ADP or TRAP-6. The antiplatelet drugs exhibited heterogeneity regarding their effect on P-selectin and α_IIbβ₃ membrane expression, while both omega-3 PUFAs inhibited the membrane expression of α_IIbβ₃, though had no effect on P-selectin expression induced by ADP or TRAP-6. The combinatory effect of DHA and EPA with the antiplatelet drugs did not result in enhanced inhibitory activity compared to the sum of the individual effects of each component.

01 Jul 2024·Revista Española de Cardiología (English Edition)

Impact of prior use of antiplatelets on COVID-19 susceptibility, progression, and severity: a population-based study

Article

Author: Salgado-Barreira, Ángel ; Prieto-Campo, Ángela ; Zapata-Cachafeiro, Maruxa ; Piñeiro-Lamas, María ; Figueiras, Adolfo ; Portela-Romero, Manuel

INTRODUCTION AND OBJECTIVESHypercoagulability and thromboembolism are processes that arise from severe acute respiratory syndrome coronavirus 2 infection and are responsible for a high degree of coronavirus disease 2019 (COVID-19)-related morbidity and mortality. This study sought to assess the effect of antiplatelet drugs on COVID-19 severity (risk of hospitalization and mortality), susceptibility to severe acute respiratory syndrome coronavirus 2 infection, and progression to severe COVID-19.METHODSWe conducted a population-based case-control study in a northwestern region of Spain in 2020. The study involved 3060 participants with a positive polymerase chain reaction test who were hospitalized, 26 757 participants with a positive polymerase chain reaction test who were not hospitalized, and 56 785 healthy controls.RESULTSTriflusal seemed to be associated with a significant increase in risk of hospitalization (aOR, 1.97; 95%CI, 1.27-3.04) and susceptibility to infection (OR, 1.45; 95%CI, 1.07-1.96). It also appeared to lead to a nonsignificant increase in the risk of mortality (OR, 2.23; 95%CI, 0.89-5.55) and/or progression to more severe disease stages (OR, 1.42; 95%CI, 0.8-2.51). Aspirin seemed to be associated with a statistically significant decrease in susceptibility to severe acute respiratory syndrome coronavirus 2 infection (OR, 0.92; 95%CI, 0.86-0.98).CONCLUSIONSTriflusal use appears to increase the risk of susceptibility to COVID-19 infection and an even higher risk of hospitalization, whereas the other antiplatelets could be associated with a reduction in the risk of the various outcomes or have no effect on risk. These findings could support reconsideration of triflusal prescription in COVID-19 pandemic situations.

100 Deals associated with Triflusal

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External Link

KEGG	Wiki	ATC	Drug Bank
D07142	Triflusal	B01AC18	DB08814

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Thromboembolism	Spain	Noucor Health SA	01 Jan 1981
Thrombosis	Spain	Noucor Health SA	01 Jan 1981

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Brain Infarction	Phase 3	China	Xi'an Xintong Pharmaceutical Research Co., Ltd.	04 Nov 2015
Arterial embolism	Phase 1	China	Furen Medicines Group Co., Ltd.	15 Nov 2013
Thrombosis	Phase 1	China	Xi'an Xintong Pharmaceutical Research Co., Ltd.	15 Jan 2013
Blood Platelet Disorders	Discovery	China	Zhengzhou Tongtai Pharmaceutical Technology Co., Ltd.	19 Nov 2014
Thromboembolism	Discovery	China	Furen Medicines Group Co., Ltd.	15 Nov 2013
Insulin Resistance	Discovery	Spain	Noucor Health SA	01 Jul 2002

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02616497 (ASTERIAS, Pubmed \| Curr Vasc Pharmacol)	Phase 4	-	1,220	Triflusal 300 mg twice or 600 mg once daily	dophfrsiei(lcmdibtuco) = ereytwhuwk tkfbowtzwz (btsqcfgwfp, -1.1 to 3.5)	Positive	01 Jan 2019
NCT01174693 (ISC2017)	Phase 4	Stroke cytochrome P450 2C19 (CYP2C19) genotype	784	Triflusal 300 mg	iidrwmuvzh(vamzqmjmmi) = qyjcjiaumi hldccleurl (zrgkkoqyxu )	Negative	01 Feb 2017
NCT01174693 (ISC2017)	Phase 4	Stroke cytochrome P450 2C19 (CYP2C19) genotype	784	Clopidogrel 75 mg	iidrwmuvzh(vamzqmjmmi) = axgsvgghzk hldccleurl (zrgkkoqyxu )	Negative	01 Feb 2017
SFN2001	Not Applicable	Brain Injuries	-	Triflusal (30mg/kg)	cuthtkpric(rtjjepinxk) = vuexeykwck htyjgfcxfs (ztvbtrkpkf )	-	14 Nov 2001