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更新于：2025-02-25
Nafamostat Mesilate
甲磺酸萘莫司他
更新于：2025-02-25
概要
基本信息
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 (美国)、孤儿药 (欧盟) |
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结构/序列
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NCT06500793
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
NCT06676085
A Novel Strategy Combined Regional Anticoagulation in Membrane Oxygenator and Low-intensity of Systemic Anticoagulation Applied in Management of Extracorporeal Membrane Oxygenation
ChiCTR2400083973
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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1,267
项与 甲磺酸萘莫司他 相关的文献（医药）2025-03-24Journal of biomolecular structure & dynamics
Inhibition of respiratory syncytial virus by Daclatasvir and its derivatives: synthesis of computational derivatives as a new drug development
Article
作者: Mitra, Debanjan ; Abdalla, Mohnad ; Afreen, Shagufta ; Das Mohapatra, Pradeep K.
The most common cause of respiratory tract illness in newborns and young children is the respiratory syncytial virus (RSV). There is no approved vaccination or specific antiviral medication for RSV infections. Here, an attempt has been made to explore the potential of currently marketed drugs as well as their probable derivatives to improve the possibility of developing stronger medications against RSV. From the 100 synthetic drug compounds library, the best drug molecule was identified through drug-likeness properties, toxicity, molecular docking and molecular dynamics simulations. Molecular Mechanics Generalized Born Surface Area (MM-GBSA) was also a method that was applied in this study. Daclatasvir showed the highest binding energy and appeared as the best drug to inhibit matrix protein and a fusion protein of RSV. Based on Daclatasvir, 40 computational derivatives were made. D28, D34 and D40 showed far better results than the actual drug. Changes in lipophilicity character increase the binding energy of derivatives. Molecular dynamic simulations showed their non-deviated, non-fluctuated and stable complex formation with target proteins. The high number of amino acid contacts throughout the trajectory increases the stability and effectiveness of derivatives. The key to producing a novel medicine to eradicate RSV is provided by derivatives. Daclatasvir will be employed as a potential RSV inhibitor up until that point.Communicated by Ramaswamy H. Sarma.
2025-02-01ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
The identification of insect specific iAANAT inhibitors
Article
作者: Sabbagh, Christian ; Henry, Gabrielle ; Radulovic, Peter W ; Merkler, David J ; Suarez, Gabriela ; Hawley, Aidan J ; Holets, Tyler ; Scearbo, Matthew ; Bhandari, Suzeeta ; Borisova, Natalia
An important aspect of food security is the development of innovative insecticides, particularly ones that specifically target insect pests and exhibit minimal toxicity to mammals. The insect arylalkylamine N-acyltransferases (iAANATs) could serve as targets for novel insecticides that satisfy these criteria. There exists a wealth of structural and biochemical information for the iAANATs and iAANAT knockdown experiments show that these enzymes are critical to insect health. Herein, we have expressed, purified, and characterized two new iAANATs, one from Apis mellifera (honey bee, AmNAT1) and another from Diaphorina citri (Asian citrus psyllid, DcNAT). We discovered that diminazene, a compound used to treat livestock for trypanosomiasis and babesiosis, inhibits AmNAT1, DcNAT, and D. melanogaster DmAgmNAT with modest affinity, Ki values ranging from 0.8 μM to 200 μM. We found a series of guanidines, amidines, and a hydroxamate, structurally related to diminazene, also inhibit the iAANATs, including camostat, gabexate, nafamostate, and panobinostat. Significantly, we found DmAgmNAT is far more susceptible to inhibition by four of these five of these compounds. In particular, camostat, nafamostat, and gabexate inhibit DmAgmNAT with Ki values of 0.2-30 μM, but no inhibition of AmNAT1 and DcNAT was observed at 500 μM for any of the three. These results show that a species-specific inhibitor targeted against an iAANAT is a real possibility. Also, we report that adipoyl-CoA is a substrate for AmNAT1 and DcNAT and that succinoyl-CoA is a substrate for DcNAT. These results contribute to a growing body of data suggesting that N-dicarboxyacyl-amines are metabolites in insects and other organisms.
2025-01-31JOURNAL OF VIROLOGY
The respective roles of TMPRSS2 and cathepsins for SARS-CoV-2 infection in human respiratory organoids
Article
作者: Katoh, Hiroshi ; Takeda, Makoto ; Ryo, Akihide ; Kakizaki, Masatoshi ; Nagata, Noriyo ; Kitai, Yuki ; Shirato, Kazuya ; Takayama, Kazuo ; Hashimoto, Rina ; Okura, Takashi ; Akahori, Yukiko ; Yamamoto, Takuya
ABSTRACT:
A critical aspect of the mechanism of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection is the protease-mediated activation of the viral spike (S) protein. The type II transmembrane serine protease TMPRSS2 is crucial for SARS-CoV-2 infection in lung epithelial Calu-3 cells and murine airways. However, the importance of TMPRSS2 needs to be re-examined because the ability to utilize TMPRSS2 is significantly reduced in the Omicron variants that spread globally. For this purpose, replication profiles of SARS-CoV-2 were analyzed in human respiratory organoids. All tested viruses, including Omicron variants, replicated efficiently in these organoids. Notably, all SARS-CoV-2 strains retained replication ability in TMPRSS2-gene knockout (KO) respiratory organoids, suggesting that TMPRSS2 is not essential for SARS-CoV-2 infection in human respiratory tissues. However, TMPRSS2-gene knockout significantly reduces the inhibitory effect of nafamostat, indicating the advantage of TMPRSS2-utilizing ability for the SARS-CoV-2 infection in these organoids. Interestingly, Omicron variants regained the TMPRSS2-utilizing ability in recent subvariants. The basal infectivity would be supported mainly by cathepsins because the cathepsin inhibitor, EST, showed a significant inhibitory effect on infection with any SARS-CoV-2 strains, mainly when used with nafamostat. A supplementary contribution of other serine proteases was also suggested because the infection of the Delta variant was still inhibited partially by nafamostat in TMPRSS2 KO organoids. Thus, various proteases, including TMPRSS2, other serine proteases, and cathepsins, co-operatively contribute to SARS-CoV-2 infection significantly in the respiratory organoids. Thus, SARS-CoV-2 infection in the human respiratory tissues would be more complex than observed in cell lines or mice.
IMPORTANCE:
We explored how the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus infects human respiratory organoids, which are a cultured cell model made to mimic the physiological conditions of the human airways. We focused on understanding the role of different proteases of host cells in activating the virus spike proteins. Specifically, we looked at TMPRSS2, a transmembrane serine protease, and cathepsin L, a lysosomal enzyme, which helps the virus enter cells by cutting the viral spike protein. We discovered that while TMPRSS2 is crucial for the virus in certain cells and animal models, other proteases, including cathepsins and various serine proteases, also play significant roles in the SARS-CoV-2 infection of human respiratory organoids. We suggest that SARS-CoV-2 uses a more complex mechanism involving multiple proteases to infect human airways, differing from what we see in conventional cell lines or animal models. This complexity might help explain how different variants can spread and infect people effectively.
76
项与 甲磺酸萘莫司他 相关的新闻（医药）2025-02-24
·药筛
临床3期临床成功上市批准申请上市抗体药物偶联物
2025-02-23
·信狐药迅
疫苗信使RNA申请上市临床申请
2025-02-12
·信狐药迅
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 | 襯獵壓觸壓製遞廠艱繭(鹹鑰鑰範衊淵襯淵願齋) = 顧糧鏇廠遞構窪願鬱襯 網鑰夢齋範齋壓觸繭襯 (繭憲鹽醖壓衊衊選鑰醖, 8.4 ~ 12.0) 更多 | 积极 | 2022-05-11 | |||
临床2期 | 104 | Nafamostat plus standard-of-care (SOC) | 網選鹽鏇顧餘鑰遞鬱構(簾膚觸齋遞夢積鑰範鹹) = 廠繭製獵積膚製願夢簾 選鏇糧鹹襯鹹觸鹹壓觸 (積鏇憲鏇鬱淵淵鑰繭餘 ) | - | 2021-11-01 | ||
Standard-of-care (SOC) alone | 網選鹽鏇顧餘鑰遞鬱構(簾膚觸齋遞夢積鑰範鹹) = 構願齋遞顧鏇觸製願選 選鏇糧鹹襯鹹觸鹹壓觸 (積鏇憲鏇鬱淵淵鑰繭餘 ) | ||||||
N/A | - | - | 夢範築網襯壓壓淵襯衊(夢齋糧夢範襯觸觸壓艱) = 網壓範壓廠製選襯憲夢 膚蓋廠鹽鏇遞獵選積簾 (襯窪積繭餘鹽遞糧鏇鹽, [22 ~ 68]) | 积极 | 2021-10-27 | ||
Regional Citrate Anticoagulation | 夢範築網襯壓壓淵襯衊(夢齋糧夢範襯觸觸壓艱) = 艱餘憲襯蓋襯鏇製膚襯 膚蓋廠鹽鏇遞獵選積簾 (襯窪積繭餘鹽遞糧鏇鹽, [16 ~ 67]) | ||||||
N/A | - | - | 製鏇遞網膚簾觸築獵繭(齋壓壓積襯願鬱蓋窪築) = 顧積鬱鑰製衊選醖簾觸 選積膚襯壓鬱鹽蓋顧醖 (廠遞壓選膚遞餘構構遞 ) | 积极 | 2020-10-19 | ||
Regional Citrate Anticoagulation | 製鏇遞網膚簾觸築獵繭(齋壓壓積襯願鬱蓋窪築) = 壓鹹齋淵網鹹膚願糧壓 選積膚襯壓鬱鹽蓋顧醖 (廠遞壓選膚遞餘構構遞 ) | ||||||
N/A | - | - | Nafamostat mesilate (FUT) | 繭醖窪憲繭廠製鹹淵繭(觸艱遞願鏇壓襯艱觸淵) = 鑰襯膚願構襯壓製選願 範選選艱窪廠膚憲衊糧 (壓鏇壓積簾蓋顧襯壓繭 ) | - | 2016-10-01 | |
Low-molecular-weight heparin (LMWH) | 繭醖窪憲繭廠製鹹淵繭(觸艱遞願鏇壓襯艱觸淵) = 鏇齋醖窪淵製鹽艱糧積 範選選艱窪廠膚憲衊糧 (壓鏇壓積簾蓋顧襯壓繭 ) | ||||||
N/A | 115 | 繭夢膚繭鬱蓋窪製積齋(獵遞夢憲醖築壓築艱積) = 餘鏇醖夢衊獵範廠醖願 憲構餘觸簾窪鏇網製範 (鹹襯衊夢選鏇膚簾蓋遞 ) 更多 | 积极 | 2015-05-21 | |||
Unfractinated heparin (UFH) | 繭夢膚繭鬱蓋窪製積齋(獵遞夢憲醖築壓築艱積) = 淵鏇鹽繭鬱網築廠願夢 憲構餘觸簾窪鏇網製範 (鹹襯衊夢選鏇膚簾蓋遞 ) 更多 | ||||||
临床2/3期 | 2,956 | 醖遞鹹鹹繭網鹹夢廠衊(簾網襯艱製糧窪廠獵窪) = 觸築夢製積餘壓窪鑰鹽 壓獵遞獵築鏇膚鹽艱蓋 (蓋餘選鏇鬱衊廠繭餘蓋, 0.34 ~ 0.63) | 积极 | 2015-05-01 | |||
Nonnafamostat | - | ||||||
N/A | - | 115 | 鹹鏇鑰範醖積廠醖鹹範(餘醖網遞鏇選獵齋艱鏇) = 積選繭構積壓構繭製淵 構糧齋製簾顧膚鬱餘鑰 (築鹽襯憲壓獵壓網壓網 ) 更多 | 积极 | 2014-11-11 | ||
Unfractionated Heparin | 鹹鏇鑰範醖積廠醖鹹範(餘醖網遞鏇選獵齋艱鏇) = 簾衊簾餘範壓繭鑰夢鹹 構糧齋製簾顧膚鬱餘鑰 (築鹽襯憲壓獵壓網壓網 ) 更多 | ||||||
临床2期 | 30 | 顧簾鬱鹽簾鹹顧襯夢繭(齋顧範鹽醖壓夢繭鑰鏇) = 簾襯襯艱製網簾觸簾鑰 憲襯膚鏇鑰鬱獵襯築糧 (簾簾艱鑰醖壓遞鏇簾窪 ) | - | 2010-05-20 | |||
临床4期 | 62 | (Nafamostat) | 襯艱壓壓窪鏇選觸廠鏇(鬱糧醖獵構艱繭憲繭窪) = 構憲衊襯網簾鑰鑰製蓋 鏇夢鬱淵觸夢獵鹹願鏇 (構艱範願淵餘顧齋獵糧, 簾醖顧衊鹽夢鹹鏇膚獵 ~ 顧願願觸願願醖顧鹽憲) 更多 | - | 2010-05-03 | ||
(Control) | 襯艱壓壓窪鏇選觸廠鏇(鬱糧醖獵構艱繭憲繭窪) = 簾願鹹遞鹹網構範願觸 鏇夢鬱淵觸夢獵鹹願鏇 (構艱範願淵餘顧齋獵糧, 範觸觸餘鬱襯繭簾獵襯 ~ 繭糧襯夢顧淵襯鏇壓窪) 更多 |
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