三氟柳(Triflusal) - 药物靶点：COX-1_在研适应症：血栓栓塞，血栓形成，脑梗塞_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Aflen、Disgren、Tecnosal

+ [4]

靶点

COX-1

作用机制

COX-1抑制剂(环氧化酶-1抑制剂)、血小板聚集抑制剂

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

+ [1]

非在研机构-

最高研发阶段批准上市

首次获批日期

西班牙 (1981-01-01),

血栓栓塞血栓形成

最高研发阶段(中国)临床3期

特殊审评-

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结构/序列

分子式C10H7F3O4

InChIKeyRMWVZGDJPAKBDE-UHFFFAOYSA-N

CAS号322-79-2

关联

14

项与三氟柳相关的临床试验

NCT02904109

/ Completed临床2期

Randomized Placebo Controlled Phase II Cross Over Study on the Influence of Triflusal on Cognitive Functions in Subjects Under Chronic Stress

The purpose of this study is to investigate the effects of the eNOS activating agent triflusal on episodic memory and cognitive functions in participants under chronic stress.

开始日期2016-09-13

申办/合作机构

University of Basel

NCT02616497

/ Completed临床4期

Comparison of Triflusal With Aspirin in the Secondary Prevention of Atherothrombotic Events

Investigation of the efficacy and safety of triflusal in comparison with aspirin in patients with stable coronary artery disease (CAD) and in those with a history of an acute non-cardioembolic ischemic stroke.

开始日期2015-09-01

申办/合作机构

University of Ioannina

NCT02321852

/ Completed临床2期

Randomized Placebo Controlled Phase II Cross Over Study on the Influence of Triflusal on Cognitive Functions in Healthy Participants

The purpose of this study is to investigate the effects of the eNOS activating agent triflusal on episodic memory and cognitive functions in healthy participants.

开始日期2015-01-01

申办/合作机构

University of Basel

100 项与三氟柳相关的临床结果

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100 项与三氟柳相关的转化医学

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100 项与三氟柳相关的专利（医药）

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186

项与三氟柳相关的文献（医药）

2024-09-21·International journal of molecular sciences

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

Article

作者: 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.

2024-07-01·Revista Española de Cardiología (English Edition)

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

Article

作者: 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.

2024-03-01·Microbes and Infection

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

Article

作者: 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 项与三氟柳相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D07142	三氟柳	B01AC18	DB08814

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
血栓栓塞	西班牙	Noucor Health SA	1981-01-01
血栓形成	西班牙	Noucor Health SA	1981-01-01

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
脑梗塞	临床3期	中国	西安新通药物研究股份有限公司	2015-11-04
动脉栓塞	临床1期	中国	辅仁药业集团有限公司	2013-11-15
血栓形成	临床1期	中国	西安新通药物研究股份有限公司	2013-01-15
血小板疾病	药物发现	中国	郑州通泰医药科技有限公司	2014-11-19
血栓栓塞	药物发现	中国	辅仁药业集团有限公司	2013-11-15
胰岛素抵抗	药物发现	西班牙	Noucor Health SA	2002-07-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02616497 (ASTERIAS, Pubmed \| Curr Vasc Pharmacol)	临床4期	-	1,220	Triflusal 300 mg twice or 600 mg once daily	餘顧網襯網鑰簾鹹鏇網(憲鹹醖網簾願壓鑰網窪) = 築選壓蓋鹹齋鹽鹽積積憲齋襯襯壓膚膚壓觸選 (繭築餘窪鏇積夢網構鹽, -1.1 ~ 3.5)	积极	2019-01-01
NCT01174693 (ISC2017)	临床4期	脑卒中 cytochrome P450 2C19 (CYP2C19) genotype	784	Triflusal 300 mg	觸網艱鬱鹹鬱鏇築鹽膚(衊膚壓範簾鑰選淵餘繭) = 衊鑰窪憲醖淵淵觸醖網繭膚淵鏇遞廠糧夢鹽艱 (廠網醖築淵壓衊廠艱醖 )	不佳	2017-02-01
NCT01174693 (ISC2017)	临床4期	脑卒中 cytochrome P450 2C19 (CYP2C19) genotype	784	Clopidogrel 75 mg	觸網艱鬱鹹鬱鏇築鹽膚(衊膚壓範簾鑰選淵餘繭) = 鑰範積範構壓網遞餘醖繭膚淵鏇遞廠糧夢鹽艱 (廠網醖築淵壓衊廠艱醖 )	不佳	2017-02-01
SFN2001	N/A	脑损伤	-	Triflusal (30mg/kg)	鏇糧窪夢鑰蓋遞鬱鏇鑰(壓蓋網簾觸醖網繭淵艱) = 壓廠鹹鹽範夢醖範網膚夢製膚選範鏇鏇鹽顧鹹 (鑰壓夢齋簾獵蓋鹽衊簾 )	-	2001-11-14