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

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

ES (01 Jan 1981),

ThromboembolismThrombosis

Regulation-

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Structure

Molecular FormulaC10H7F3O4

InChIKeyRMWVZGDJPAKBDE-UHFFFAOYSA-N

CAS Registry322-79-2

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 ; Portela-Romero, Manuel ; Figueiras, Adolfo

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.

01 Mar 2024·Microbes and Infection

Unravelling the potential of Triflusal as an anti-TB repurposed drug by targeting replication protein DciA

Article

Author: Agarwal, Meetu ; Jamal, Salma ; Gangwar, Rishabh ; Ahmed, Faraz ; Grover, Sonam ; Prakash Dwivedi, Ved ; Pahuja, Isha ; Sharma, Rahul ; Ali, Waseem

The increasing prevalence of drug-resistant Tuberculosis (TB) is imposing extreme difficulties in controlling the TB infection rate globally, making treatment critically challenging. To combat the prevailing situation, it is crucial to explore new anti-TB drugs with a novel mechanism of action and high efficacy. The Mycobacterium tuberculosis (M.tb)DciA is an essential protein involved in bacterial replication and regulates its growth. DciA interacts with DNA and provides critical help in binding other replication machinery proteins to the DNA. Moreover, the lack of any structural homology of M.tb DciA with human proteins makes it an appropriate target for drug development. In this study, FDA-approved drugs were virtually screened against M.tb DciA to identify potential inhibitors. Four drugs namely Lanreotide, Risedronate, Triflusal, and Zoledronic acid showed higher molecular docking scores. Further, molecular dynamics simulations analysis of DciA-drugs complexes reported stable interaction, more compactness, and reduced atomic motion. The anti-TB activity of drugs was further evaluated under in vitro and ex vivo conditions where Triflusal was observed to have the best possible activity with the MIC of 25 μg/ml. Our findings present novel DciA inhibitors and anti-TB activity of Triflusal. Further investigations on the use of Triflusal may lead to the discovery of a new anti-TB drug.

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	ES	Noucor Health SA	01 Jan 1981
Thrombosis	ES	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	CN	Xi'an Xintong Pharmaceutical Research Co., Ltd.	04 Nov 2015
Thromboembolism	Phase 2	CN	Furen Medicines Group Co., Ltd.	15 Nov 2013
Insulin Resistance	Phase 2	ES	Noucor Health SA	01 Jul 2002
Blood Platelet Disorders	Phase 1	CN	Zhengzhou Tongtai Pharmaceutical Technology Co., Ltd.	19 Nov 2014
Arterial embolism	Phase 1	CN	Furen Medicines Group Co., Ltd.	15 Nov 2013
Thrombosis	Phase 1	CN	Xi'an Xintong Pharmaceutical Research Co., Ltd.	15 Jan 2013

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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	ylmfswrgiw(vlijyuwbqz) = nswvguxvzu yfiqzmqqnt (ropmiqkuna, -1.1 to 3.5)	Positive	01 Jan 2019