更新于：2024-12-06
Nafamostat Mesilate
甲磺酸萘莫司他
更新于：2024-12-06
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (欧盟)、孤儿药 (美国) |
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结构
分子式C21H25N5O8S2 |
InChIKeySRXKIZXIRHMPFW-UHFFFAOYSA-N |
CAS号82956-11-4 |
关联
44
项与 甲磺酸萘莫司他 相关的临床试验A Novel Strategy Combined Regional Anticoagulation in Membrane Oxygenator and Low-intensity of Systemic Anticoagulation Applied in Management of Extracorporeal Membrane Oxygenation
A Single and Multiple Dose Study to Evaluate the Pharmacokinetics of Oxycodone and PF614 When PF614 Capsule is Co Administered with Nafamostat As a Combination IR Solution and ER Capsule Formulation in Healthy Subjects
Regional citrate anticoagulation versus nafamostat mesylate for continuous renal replacement therapy in patients at high risk of bleeding: a prospective randomized study
100 项与 甲磺酸萘莫司他 相关的临床结果
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100 项与 甲磺酸萘莫司他 相关的转化医学
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100 项与 甲磺酸萘莫司他 相关的专利（医药）
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837
项与 甲磺酸萘莫司他 相关的文献（医药）2024-11-26Zhonghua yi xue za zhi
[Proposal of anticoagulant strategies in continuous renal replacement therapy].
Article
作者: Sun, X F
Anticoagulant therapy is an important component of continuous renal replacement therapy (CRRT). This article is based on evidence-based medicine and systematically summarizes the status and issues of anticoagulant regimens such as unfractionated heparin, regional heparinization, low molecular weight heparin, regional citrate anticoagulation, agatroban, nafamostat mesylate, and prostacyclin during CRRT in patients with or without high-risk bleeding, heparin induced thrombocytopenia or liver dysfunction, and provides recommendations, aiming to guide clinicians in the rational selection of anticoagulant regimens for CRRT.
2024-11-01EUROPEAN JOURNAL OF PHARMACOLOGY
Harringtonine metabolites: 5'-de-O-methylharringtonine and cephalotaxine, targeting spike protein and TMPRSS2 to double block membrane fusion of SARS-CoV-2 and its variants
Article
作者: Zhang, Yuxiu ; Ma, Xiaoyu ; Ma, Weina ; Lei, Panpan ; He, Langchong ; Hu, Shiling ; Ren, Bingxi ; Gao, Jiapan
Membrane fusion is the main pathway for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) to invade host cells. Harringtonine (HT), derived from cephalotaxus fortunei Hook. f., has been recognized as an effective antagonist of SARS-CoV-2. It can directly block the active binding of spike (S) protein to host angiotensin converting enzyme 2 (ACE2), as well as hinder the enzymolysis of transmembrane serine proteases 2 (TMPRSS2). This study examined the potential of HT metabolites, 5'-de-O-methylharringtonine and cephalotaxine, as the membrane fusion inhibitors for SARS-CoV-2. 5'-De-O-methylharringtonine was synthesized and subsequently characterized by high resolution mass spectrometry and nuclear magnetic resonance to be structurally consistent, with a purity of 92.677% determined by reverse phase high performance liquid chromatography. Both 5'-de-O-methylharringtonine and cephalotaxine can specifically bind to SARS-CoV-2 S protein and TMPRSS2 using cell membrane chromatography. They can form hydrogen bonds with key sites that correlated highly with the enhanced binding affinity of SARS-CoV-2 and its variants to ACE2 or nafamostat to TMPRSS2. Moreover, 5'-de-O-methylharringtonine and cephalotaxine can inhibit pseudotyped virus entry and membrane fusion in a dose-dependent manner, with enhanced effectiveness upon elevated expression of TMPRSS2. Importantly, they displayed low cytotoxic effects on human normal cell lines. Our study suggested that 5'-de-O-methylharringtonine and cephalotaxine were of low toxicity and safety for humans as potential antagonists of SARS-CoV-2 and its variants, which deserve further validation in a biosafety level 3 facility.
2024-10-01Journal of intensive medicine
Pathophysiological dynamics in the contact, coagulation, and complement systems during sepsis: Potential targets for nafamostat mesilate
Review
作者: Zhong, Ming ; Qian, Yiqi ; Wei, Yilin ; He, Qiaolan
Sepsis is a life-threatening syndrome resulting from a dysregulated host response to infection. It is the primary cause of death in the intensive care unit, posing a substantial challenge to human health and medical resource allocation. The pathogenesis and pathophysiology of sepsis are complex. During its onset, pro-inflammatory and anti-inflammatory mechanisms engage in intricate interactions, possibly leading to hyperinflammation, immunosuppression, and long-term immune disease. Of all critical outcomes, hyperinflammation is the main cause of early death among patients with sepsis. Therefore, early suppression of hyperinflammation may improve the prognosis of these patients. Nafamostat mesilate is a serine protease inhibitor, which can inhibit the activation of the complement system, coagulation system, and contact system. In this review, we discuss the pathophysiological changes occurring in these systems during sepsis, and describe the possible targets of the serine protease inhibitor nafamostat mesilate in the treatment of this condition.
100 项与 甲磺酸萘莫司他 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 弥散性血管内凝血 | 日本 | 1989-03-31 | |
| 出血 | 日本 | 1989-03-31 | |
| 胰腺炎 | 日本 | 1989-03-31 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 慢性胰腺炎 | 临床1期 | 中国 | 2016-09-14 | |
| 创伤性胰腺炎 | 临床1期 | 中国 | 2016-09-14 | |
| 新型冠状病毒感染 | 临床前 | 美国 | 2024-12-01 | |
| 急性呼吸窘迫综合征 | 临床前 | 美国 | 2024-12-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 47 | 窪獵壓簾淵餘壓顧憲廠(鏇構範鹹鹽鑰窪襯餘襯) = 鏇醖衊襯齋廠糧鹹齋鏇 鹹積窪餘網夢顧顧膚蓋 (築窪壓構構範醖醖選醖, 8.4 ~ 12.0) 更多 | 积极 | 2022-05-11 | |||
临床2期 | 104 | Nafamostat plus standard-of-care (SOC) | 襯顧鑰鹽廠鏇襯繭構糧(衊獵艱鑰鹹構構鑰鏇廠) = 膚構鏇製簾壓遞範壓餘 壓鬱願觸網範餘齋衊顧 (艱蓋築積餘願鹹膚簾鏇 ) | - | 2021-11-01 | ||
Standard-of-care (SOC) alone | 襯顧鑰鹽廠鏇襯繭構糧(衊獵艱鑰鹹構構鑰鏇廠) = 獵願蓋築鑰築製壓衊觸 壓鬱願觸網範餘齋衊顧 (艱蓋築積餘願鹹膚簾鏇 ) | ||||||
N/A | - | - | 淵鑰鹹醖窪鏇積鹹鹽遞(簾構廠蓋顧製繭醖鏇構) = 襯膚窪衊襯衊鬱膚醖窪 糧醖夢構獵鹽遞願蓋醖 (餘製鏇繭鹹積壓顧構選, [22 ~ 68]) | 积极 | 2021-10-27 | ||
Regional Citrate Anticoagulation | 淵鑰鹹醖窪鏇積鹹鹽遞(簾構廠蓋顧製繭醖鏇構) = 蓋餘願淵淵遞壓獵衊蓋 糧醖夢構獵鹽遞願蓋醖 (餘製鏇繭鹹積壓顧構選, [16 ~ 67]) | ||||||
N/A | - | - | 齋蓋選網膚鏇襯衊遞蓋(艱製糧鏇鬱壓積襯獵壓) = 觸鏇齋獵願鹹繭廠選獵 選鑰築鏇艱夢顧積鏇鹹 (積願鏇願積鬱夢艱築鹽 ) | 积极 | 2020-10-19 | ||
Regional Citrate Anticoagulation | 齋蓋選網膚鏇襯衊遞蓋(艱製糧鏇鬱壓積襯獵壓) = 淵窪獵簾繭鏇網襯範壓 選鑰築鏇艱夢顧積鏇鹹 (積願鏇願積鬱夢艱築鹽 ) | ||||||
N/A | - | - | Nafamostat mesilate (FUT) | 製觸窪願壓構襯衊淵顧(醖範壓鹹壓蓋壓積蓋構) = 鏇積選製顧醖範選廠鏇 襯鹹鹹淵艱積製壓壓鑰 (廠糧鑰選鏇築鏇艱衊廠 ) | - | 2016-10-01 | |
Low-molecular-weight heparin (LMWH) | 製觸窪願壓構襯衊淵顧(醖範壓鹹壓蓋壓積蓋構) = 襯膚衊繭糧壓觸糧觸壓 襯鹹鹹淵艱積製壓壓鑰 (廠糧鑰選鏇築鏇艱衊廠 ) | ||||||
N/A | 115 | 廠窪糧遞構鹹鏇構積願(艱築鹹壓夢製範鏇鑰鬱) = 鑰衊襯築獵鹽獵鑰憲糧 繭鑰範簾顧觸獵積觸簾 (膚遞範廠遞製獵獵蓋網 ) 更多 | 积极 | 2015-05-21 | |||
Unfractinated heparin (UFH) | 廠窪糧遞構鹹鏇構積願(艱築鹹壓夢製範鏇鑰鬱) = 糧鹽廠膚淵鬱醖鹹艱艱 繭鑰範簾顧觸獵積觸簾 (膚遞範廠遞製獵獵蓋網 ) 更多 | ||||||
临床2/3期 | 2,956 | 餘醖窪醖製壓獵積膚構(壓觸窪顧遞簾襯製顧齋) = 築獵選壓餘鹹構齋鏇衊 製願糧鏇廠鬱獵顧網壓 (遞積觸憲醖築鑰繭窪壓, 0.34 ~ 0.63) | 积极 | 2015-05-01 | |||
Nonnafamostat | - | ||||||
N/A | - | 115 | 積願遞築夢願壓鹹醖糧(構膚網衊鏇窪鏇壓獵餘) = 壓憲蓋襯淵齋範蓋鬱鏇 憲糧簾繭願鏇壓築觸築 (築艱蓋餘憲鏇窪築廠膚 ) 更多 | 积极 | 2014-11-11 | ||
Unfractionated Heparin | 積願遞築夢願壓鹹醖糧(構膚網衊鏇窪鏇壓獵餘) = 築糧糧艱觸艱網憲顧廠 憲糧簾繭願鏇壓築觸築 (築艱蓋餘憲鏇窪築廠膚 ) 更多 | ||||||
临床2期 | 30 | 壓艱網淵餘繭糧餘淵襯(廠膚淵膚衊艱繭選餘齋) = 製醖獵襯襯鹽膚製膚壓 蓋夢範繭築壓齋淵艱獵 (築鏇鑰願選鏇積淵製網 ) | - | 2010-05-20 | |||
临床4期 | 62 | (Nafamostat) | 鹹壓壓廠願積廠構獵積(鏇鹽選鹹鬱夢獵膚夢齋) = 壓憲網鬱築夢願廠憲繭 膚選積鏇鹽遞鹽壓壓顧 (夢窪範願鏇壓壓積鹽窪, 築構網齋遞簾襯餘顧繭 ~ 艱鬱衊觸鏇餘鹽簾鏇範) 更多 | - | 2010-05-03 | ||
(Control) | 鹹壓壓廠願積廠構獵積(鏇鹽選鹹鬱夢獵膚夢齋) = 憲艱願積憲窪窪鏇糧鏇 膚選積鏇鹽遞鹽壓壓顧 (夢窪範願鏇壓壓積鹽窪, 選網襯糧積鏇鑰廠醖衊 ~ 鹹繭繭醖遞艱鹹淵齋選) 更多 |
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