醋硝香豆素(Acenocoumarol) - 药物靶点：NQO1 x VKOR_在研适应症：血栓栓塞_专利_临床

概要

基本信息

药物类型

小分子化药

别名

3-(alpha-(4'-Nitrophenyl)-beta-acetylethyl)-4-hydroxycoumarin、3-(alpha-(p-Nitrophenol)-beta-acetylethyl)-4-hydroxycoumarin、3-(alpha-Acetonyl-4-nitrobenzyl)-4-hydroxycoumarin

+ [21]

靶点

NQO1 x VKOR

作用方式

抑制剂、拮抗剂

作用机制

NQO1抑制剂(苯醌还原酶-1抑制剂)、VKOR抑制剂(维生素K环氧化物还原酶复合体1抑制剂)、维生素K拮抗剂

治疗领域

心血管疾病

在研适应症

血栓栓塞

非在研适应症-

原研机构-

在研机构-

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C19H15NO6

InChIKeyVABCILAOYCMVPS-UHFFFAOYSA-N

CAS号152-72-7

关联

14

项与醋硝香豆素相关的临床试验

NCT03153150

/ Completed临床3期IIT

Start or STop Anticoagulants Randomised Trial (SoSTART) After Spontaneous Intracranial Haemorrhage

Primary research question: For adults surviving spontaneous (non-traumatic) symptomatic intracranial haemorrhage with persistent/paroxysmal atrial fibrillation/flutter (AF), does starting full treatment dose oral anticoagulation (OAC) result in a beneficial net reduction of all serious vascular events compared with not starting OAC?
Trial design: Investigator-led, multicentre, randomised, open, assessor-masked, parallel group, clinical trial of investigational medicinal product (CTIMP) prescribing strategies. Investigators plan for a pilot phase, followed by a safety phase.

开始日期2018-03-28

申办/合作机构

The University of Edinburgh

[+1]

NCT03154489

/ CompletedN/AIIT

Effectiveness of a Multidisciplinary Medication Review With Follow-up for Patients Treated With Coumarin Anticoagulants in Primary Care

The interdisciplinary collaboration between doctors, nurses and pharmacists, can facilitate the control of patients under treatment with coumarin anticoagulants, increasing their safety and effectiveness. On the other hand, the clinical utility of tools such as pharmacogenetics and the SAME-TT2R2 is unexplored. Based on the foregoing, it seems necessary to study the impact of the Program of medication review with follow-up in collaboration with doctors and nurses in primary care improves the degree of control of the patients under treatment with coumarin anticoagulants. Method: a randomized, controlled study for the main objective. Population and scope of study: Patients on treatment with coumarin anticoagulants with time in therapeutic range (TTR) according to the method of Rosendaal less than 70% in follow-up from primary care in a health area of the Arrabal Health Center (Zaragoza, Spain). Each patient will be followed by a period of 6 months. After this period, patients in the control group (CG) will receive the service of medication review with follow-up for a period of time equivalent (6 months). Intervention: Program of pharmacotherapy follow-up. Variables result: Stability of the INR, drug adherence, intake of vitamin K, knowledge of the patient on the use of acenocoumarol, associated costs, avoided costs, quality of life, satisfaction of patients and professionals involved. Statistical analysis and sample size: 204 patients. Multivariate analysis will be used and cost-effectiveness..

开始日期2017-05-22

申办/合作机构

Roche Diagnostics Corp.

EUCTR2016-003086-25-NL

/ Unknown status临床3期

More precise dosing of acenocoumarol in patients aged 80 and above, a pilot study - Eighty and a half

开始日期2017-04-19

申办/合作机构

University Medical Center Groningen

100 项与醋硝香豆素相关的临床结果

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100 项与醋硝香豆素相关的转化医学

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100 项与醋硝香豆素相关的专利（医药）

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1,770

项与醋硝香豆素相关的文献（医药）

2025-10-01·Talanta

Chiral separation of pharmaceuticals and agrochemicals using capillary electrophoresis: Migration order, modeling and chiral recognition mechanism

Article

作者: Ali, Imran ; Hefnawy, Mohamed ; Giunashvili, Lasha ; Chankvetadze, Lali ; Tatunashvili, Elene ; Gogolashvili, Ann

Chiral separation of pharmaceuticals (acenocoumarin, coumatetralyl, and warfarin) and agrochemicals (mecoprop and dichloroprop) was achieved utilizing native cyclodextrins (α-, β-, and γ-CDs) as chiral selectors in capillary electrophoresis (CE); with a particular focus on enantiomer reversal order migration of mecoprop and dichloroprop. This is the first study to demonstrate the reversal migration order for these agrochemical compounds, which provides new insights into the chiral recognition mechanisms of native CDs. The best chiral separation was achieved on γ-CD with selectivity coefficient (α) ranging from 1.018 to 1.066, resolution factor from 1.40 to 2.06, and the number of theoretical plates from 10.597 to 95.890 (R-enantiomers) and 7.352 to 90.777 (S-enantiomers). The fused silica and polyvinyl alcohol-coated capillaries gave the best results with 200 mM MESS buffer [2-(N-morpholino)ethanesulfonic acid] buffer containing 0.1 % hydroxymethylcellulose (pH 3.0 and 4.5). The best resolution was of coumatetralyl, dichloroprop, and mecoprop with β-CD. Chiral recognition mechanisms were determined by modeling and NMR studies by considering acenocoumarin as an example. R-enantiomer of acenocoumarin migrated first with a -3.4 kcal/mol binding affinity and three hydrogen bonds with γ-CD, compared to the S-enantiomer, which exhibited a -3.6 kcal/mol binding affinity and four hydrogen bonds. This study provides valuable insights for the enantioselective analysis of the reported compounds and demonstrates the potential of CE for resolving unknown chiral samples. The reversal order of migration served as a key tool in determining the chiral separation mechanism.

2025-06-01·Annales de Cardiologie et d'Angéiologie

Management of Acenocoumarol in Tunisian elderly population : Risk factors of overdose and bleeding

Article

作者: Cherif, Eya ; Hamdi, Mohamed Salah ; Tekaya, Asma ; Kechaou, Ines ; Taouay, Amira ; Hassine, Lamia Ben

INTRODUCTIONAnticoagulant therapy, often required in the elderly, is not without risk. This study aims to investigate the particularities of the use of anticoagulants in the elderly during hospital stay, along with the factors associated with bleeding and overdose.RESULTSThere were 55 women and 45 men (sex ratio: 0.81), with a mean age of 75.7 ± 6.9 years. The indications for anticoagulant treatment were venous thromboembolism (VTE) (92%) and atrial fibrillation (AF) (8%). The average duration of treatment with acenocoumarol was 17.22 days ± 7.9. The dose of acenocoumarol initiation was 1 mg in 85% of patients and 2 mg in 15%. INR < 2 was observed in 15% of patients. INR in the target area was obtained in 47% of patients with a mean dose of 2.33 mg of acenocoumarol. An overdose of acenocoumarol was noted in 38% of patients: average INR at 4.7. Seven patients had bleeding events. An overdose was reported in 4 of them. Fever, infection, inflammatory syndrome, hypoalbuminemia, hypoprotidemia, and malnutrition were associated with a greater risk of overdose in our patients. Gastroduodenal ulcer disease, past medical history of gastrointestinal bleeding and renal failure were risk factors for bleeding in our patients.CONCLUSIONThe use of anticoagulants in the elderly requires a comprehensive assessment, including comorbidities, geriatric settings, and social environment.

2025-05-01·Journal of Pharmaceutical and Biomedical Analysis

Simultaneous quantification of eighteen therapeutic oral anticoagulants, rodenticides, and antiplatelet agents by LC-MS/MS and its application in post-mortem forensic cases

Article

作者: Delavenne, Xavier ; Bidat, Carolyne ; Escal, Jean ; Hodin, Sophie ; Duband, Sébastien ; Drague, Angélique ; Dellinger, Sandrine ; Feliu, Catherine

Anticoagulants and antiplatelet agents, which interfere with blood coagulation, can lead to fatal bleeding. Moreover, their widespread use as drugs or rodenticides poses a high risk of accidental or intentional poisoning. Therefore, quantifying these substances is essential in forensic investigations. This research aimed to develop and validate a liquid chromatography-tandem mass spectrometry method capable of quantifying eighteen anticoagulant or antiplatelet compounds (apixaban, rivaroxaban, dabigatran, warfarin, acenocoumarol, fluindione, brodifacoum, bromadiolone, difenacoum, difethialone, chlorophacinone, coumatetralyl, flocoumafen, acetylsalicylic acid, clopidogrel, dipyridamole, ticagrelor, and ticlopidine) in a single run with simple sample preparation. The method was validated according to the FDA recommendations for all compounds, with an eight-min run time in human whole blood, the gold standard in toxicological forensic investigation. The method was also validated for therapeutic compounds and most rodenticides in bile and vitreous humor. Following validation, the method was applied to seven forensic cases with a known history of anticoagulant or antiplatelet agent use to prove the validity of the method. This method provides a valuable tool for legal contexts where precise determination of anticoagulant compound presence and concentration is required.

100 项与醋硝香豆素相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D07064	醋硝香豆素	B01AA07	DB01418

研发状态

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	-	-	-

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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


NCT02696226 (CTgov)	N/A	血栓形成 \| 主动脉瓣疾病	3	SAVR Warfarin (SAVR Warfarin Arm)	鏇鑰鬱鹹艱願範齋鹹鑰(遞願繭製艱膚糧蓋膚齋) = 鏇構醖積範衊鬱襯簾衊鹹製鏇範膚築繭衊鹽鑰 (壓鏇積鑰選網齋獵獵襯, 壓餘選糧築鬱鹽蓋壓獵 ~ 鹽醖鹹廠襯網衊淵膚遞) 更多	-	2017-11-08
				Warfarin+clopidogrel (TAVR Warfarin and Clopidogrel Arm)	鏇鑰鬱鹹艱願範齋鹹鑰(遞願繭製艱膚糧蓋膚齋) = 夢鏇醖範鑰構淵壓鏇積鹹製鏇範膚築繭衊鹽鑰 (壓鏇積鑰選網齋獵獵襯, 觸鏇壓醖鏇簾壓簾艱襯 ~ 構鹹糧選夢觸範繭憲廠) 更多