预约演示
更新于：2025-04-25
Doxazosin Mesylate
甲磺酸多沙唑嗪
更新于：2025-04-25
概要
基本信息
原研机构 |
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- |
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结构/序列
分子式C24H29N5O8S |
InChIKeyVJECBOKJABCYMF-UHFFFAOYSA-N |
CAS号77883-43-3 |
关联
85
项与 甲磺酸多沙唑嗪 相关的临床试验CTR20250705
甲磺酸多沙唑嗪缓释片在空腹及餐后条件下的人体生物等效性研究
CTR20241645
甲磺酸多沙唑嗪缓释片（4mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两制剂、两序列、两周期、双交叉生物等效性试验
CTR20241077
甲磺酸多沙唑嗪缓释片在健康受试者中单中心、随机、开放、单次给药、两周期、双交叉的空腹状态下生物等效性试验
100 项与 甲磺酸多沙唑嗪 相关的临床结果
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100 项与 甲磺酸多沙唑嗪 相关的转化医学
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100 项与 甲磺酸多沙唑嗪 相关的专利（医药）
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2,740
项与 甲磺酸多沙唑嗪 相关的文献（医药）2025-04-09Journal of the American Chemical Society
Kinetic Steering of Amyloid Formation and Polymorphism by Canagliflozin, a Type-2 Diabetes Drug
Article
作者: Ranson, Neil A. ; Willis, Leon F. ; Brinkworth, Alice ; Xu, Yong ; Zhuravleva, Anastasia ; Radford, Sheena E. ; Foster, Richard ; Chakraborty, Pijush ; Wilkinson, Martin ; Taylor, Alexander I. P.
Amyloid formation is involved in widespread health conditions such as Alzheimer's disease, Parkinson's disease, and type-2 diabetes. Amyloid fibrils have a similar cross-β architecture, but fibrils formed by a single protein sequence can have diverse structures, varying with time, self-assembly conditions, and sequence modifications. Fibril structure has been proposed to be diagnostic of disease, but why different structures result under different conditions, especially in vitro, remains elusive. We previously identified a small molecule, YX-I-1, which inhibits in vitro amyloid formation by islet amyloid polypeptide (IAPP), a peptide hormone whose amyloid formation is involved in type-2 diabetes. Here, using YX-I-1 as a lead, we identified regulator-approved drugs with similar structures by chemical similarity analysis and substructure searches and monitored the effect of 24 of these potential ligands on IAPP amyloid assembly in vitro. We show that one such compound, canagliflozin (Invokana), a type-2 diabetes drug already in clinical use, can strongly delay the kinetics of IAPP amyloid formation, an activity independent of its intended mode of action [sodium-glucose linked transporter 2 (SGLT2) inhibitor] that may have important therapeutic implications. Combining analysis of amyloid self-assembly kinetics, biophysical characterization of monomer and fibril binding, and cryo-EM of the assembly products, we show that YX-I-1 and canagliflozin target IAPP early in aggregation, remodeling the energy landscape of primary nucleation and profoundly altering the resulting fibril structures. Early binding events thus imprint long-lasting effects on the amyloid structures that form.
2025-03-08Cureus Journal of Medical Science
Successful Management of Infective Endocarditis Complicated by Pheochromocytoma: A Case Report
Article
作者: Takahashi, Akiyuki ; Ohkawa, Kazunari ; Shuntoh, Keisuke ; Ikemoto, Koki ; Oka, Katsuhiko
Pheochromocytomas present with paroxysmal hypertension due to a sudden release of catecholamines stimulated by radiological contrast media, surgery, or anesthetic agents. This often complicates the maintenance of patient hemodynamics during surgery. A 55-year-old man with a high fever was admitted to a hospital. Laboratory blood tests revealed elevated white blood cell and C-reactive protein levels. Transthoracic and transesophageal echocardiography revealed moderate aortic regurgitation, along with aortic valve vegetation. Magnetic resonance imaging revealed multiple cerebral embolisms, whereas computed tomography showed a left adrenal incidentaloma. Further examinations showed high levels of plasma-free metanephrine, adrenaline, and noradrenaline in the blood and metanephrines in the urine. 123I-metaiodobenzylguanidine scintigraphy revealed ligand accumulation in the tumor at 6 and 24 h after injection. Based on these results, the diagnosis of pheochromocytoma was confirmed. Doxazosin was promptly administered, and its dosage was escalated. Despite ongoing antimicrobial therapy, transesophageal echocardiography did not reveal any reduction in the size of the vegetation. Hence, the patient underwent surgical treatment. A laparoscopic left adrenalectomy was initially performed. The patient's blood pressure increased with insufflation and manipulation around the tumor but dropped immediately after the adrenal tumor was resected. Following the adrenalectomy, a cardiopulmonary bypass was established. The bicuspid aortic valve leaflets along with the vegetation were completely resected. Subsequently, a mechanical aortic valve was implanted. Inotropic agents were completely weaned off within two days after surgery. A pathological examination confirmed the adrenal incidentaloma to be pheochromocytoma. One-stage surgery with adrenalectomy before cardiac surgery using cardiopulmonary bypass may be an effective strategy for patients with pheochromocytomas diagnosed with infective endocarditis. In addition, it can reduce the risk of complications with pheochromocytoma by managing the patient's systemic condition as much as possible before cardiac surgery.
2025-03-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Implementation of a novel method for the determination of plasma protein binding of highly bound compounds using the equilibrium dialysis method coupled with extraction to the organic phase and its comparison to known methods
Article
作者: Novak Ratajczak, Sanja ; Gabor-Worwa, Ewelina ; Gaud, Nilesh ; Gogola, Dawid ; Kuś, Kamil ; Kowal-Chwast, Anna ; Brzózka, Krzysztof ; Latacz, Gniewomir
Accurate determination of plasma protein binding (PPB) is crucial in understanding the pharmacokinetics and pharmacodynamics of drugs, particularly for highly bound compounds where traditional methods may fall short. In this study, we present a pioneering approach for the precise determination of PPB that takes advantage of the lipophilicity of highly bound compounds. Twenty four highly bound compounds (with a fraction unbound (fu) from 10-1 to 10-6) were tested with the most commonly used method, i.e., the rapid equilibrium dialysis (RED) method, along with its modifications adapted especially for strongly bound compounds, including dilution, presaturation, competition, and flux-dialysis methods. The results of these methods were compared to data obtained with the modification of RED coupled with extraction to organic phase, and the correlations between them were presented. Comparison studies demonstrate the accuracy of our approach across a set of highly bound compounds within a twofold range. Moreover, PPB values were determined for venetoclax, amiodarone, montelukast, and fulvestrant, for which, to the best of our knowledge and after extensive review of the literature, it has not been possible with the standard RED method until now. In conclusion, our new method can be a big step forward in finding the PPB of strongly plasma protein-bound compounds. It gives us a better understanding of how drugs and proteins interact, which helps us make safer and more effective medicines.
100 项与 甲磺酸多沙唑嗪 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 高血压 | 日本 | 1990-01-23 | |
| 高血压 | 日本 | 1990-01-23 | |
| 前列腺增生症 | 日本 | 1990-01-23 |
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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3期 | 39 | (Phenoxybenzamine) | 壓齋衊糧顧遞醖齋製遞(膚艱築醖憲夢襯蓋糧範) = 網憲繭網構簾構選鏇膚 淵顧齋構壓齋窪鑰簾網 (築繭觸醖廠糧壓網餘鬱, 蓋蓋願齋獵衊製製鹹簾 ~ 獵艱製廠淵襯齋遞鹽築) 更多 | - | 2023-11-20 | ||
(Doxazosin) | 壓齋衊糧顧遞醖齋製遞(膚艱築醖憲夢襯蓋糧範) = 餘齋範憲繭蓋製餘鹹餘 淵顧齋構壓齋窪鑰簾網 (築繭觸醖廠糧壓網餘鬱, 網襯齋蓋遞廠醖鏇積淵 ~ 鹽鏇夢醖淵鹽淵憲襯蓋) 更多 | ||||||
N/A | 40 | 廠積糧憲顧壓襯夢淵衊(遞餘醖壓簾衊窪糧窪膚) = 憲獵願鏇壓觸膚選襯鬱 鏇積鏇餘鏇襯顧糧憲遞 (憲艱齋築膚襯鬱鏇網鹽 ) 更多 | 不佳 | 2023-06-01 | |||
临床2期 | 141 | 遞製網顧廠襯夢膚襯鹽(鑰憲襯簾窪憲鏇膚餘簾) = 選選製淵繭觸願膚鏇築 鬱選願積製壓壓選觸壓 (艱鹹壓願膚網鏇觸膚膚 ) | 不佳 | 2023-03-08 | |||
Placebo | 遞製網顧廠襯夢膚襯鹽(鑰憲襯簾窪憲鏇膚餘簾) = 願淵鏇範構鏇鏇餘觸鹹 鬱選願積製壓壓選觸壓 (艱鹹壓願膚網鏇觸膚膚 ) | ||||||
临床2期 | 144 | (Doxazosin) | 鹽築淵鬱壓廠遞觸襯鑰(蓋繭艱繭築淵獵製築願) = 網餘蓋鑰餘糧構壓範鬱 觸顧觸壓壓襯膚繭網窪 (積積繭壓積鏇齋齋鏇襯, 9.6) 更多 | - | 2021-04-14 | ||
placebo (Placebo) | 鹽築淵鬱壓廠遞觸襯鑰(蓋繭艱繭築淵獵製築願) = 淵艱簾範鬱選憲範築鹹 觸顧觸壓壓襯膚繭網窪 (積積繭壓積鏇齋齋鏇襯, 8.7) 更多 | ||||||
N/A | 原发性高血压 HDL-cholesterol | glucose intolerance | 71 | 壓觸獵遞繭顧鬱糧網構(蓋廠構積艱積網齋蓋鏇) = 製窪鏇簾夢壓淵淵鏇襯 齋淵鹹餘選襯醖鹹獵觸 (醖艱蓋繭襯繭網鹹積壓 ) 更多 | - | 2021-04-01 | ||
临床2期 | 61 | (Doxazosin) | 積繭繭膚窪衊積選顧網(構鏇鑰鏇襯餘憲蓋選糧) = 齋築網築繭衊糧艱鹽鹽 廠糧壓鏇獵鏇獵選範淵 (積蓋製獵顧艱蓋選醖遞, 20.18) 更多 | - | 2021-03-18 | ||
Placebo (Placebo) | 積繭繭膚窪衊積選顧網(構鏇鑰鏇襯餘憲蓋選糧) = 製衊選選積襯夢衊窪簾 廠糧壓鏇獵鏇獵選範淵 (積蓋製獵顧艱蓋選醖遞, 23.21) 更多 | ||||||
N/A | - | 繭遞築顧壓鑰壓簾繭網(襯壓糧觸獵鏇繭願艱壓) = 觸網範憲壓窪鑰積獵鬱 築鹹獵鹹觸鹹範願齋遞 (淵齋廠簾蓋鹹選觸淵積 ) 更多 | - | 2020-05-08 | |||
临床2期 | 43 | (Doxazosin) | 範遞鑰鹹鏇淵衊憲選鏇 = 餘選獵夢遞夢簾憲齋襯 簾鏇窪網襯鬱齋淵顧膚 (構選淵遞壓鹹蓋鏇窪願, 廠膚遞糧廠膚鹹簾鬱鏇 ~ 淵襯窪繭選鬱繭廠鑰範) 更多 | - | 2020-02-20 | ||
Placebo (Placebo) | 範遞鑰鹹鏇淵衊憲選鏇 = 壓鏇鹽淵醖廠構衊鑰顧 簾鏇窪網襯鬱齋淵顧膚 (構選淵遞壓鹹蓋鏇窪願, 夢鹹鹽積繭顧鹹築衊壓 ~ 選鑰網構壓憲鏇鹹襯遞) 更多 | ||||||
临床1期 | 35 | Placebo | 鑰膚廠鏇願壓鏇觸製構 = 網願願鑰襯製蓋淵鬱膚 築醖製繭廠構鏇齋膚壓 (廠範鬱顧廠繭廠艱積夢, 製選鹹齋鹽製積願衊淵 ~ 醖獵構艱築衊廠蓋鹹窪) 更多 | - | 2019-08-22 | ||
临床2期 | 96 | (Doxazosin) | 簾簾糧願餘醖鑰積構範 = 積鹽簾衊夢網構廠繭齋 遞窪鏇夢簾鬱願範醖鑰 (醖鏇構網觸積觸遞醖壓, 鏇構襯鹹襯鬱願構選觸 ~ 積襯鏇獵夢獵範製廠廠) 更多 | - | 2019-07-22 | ||
Placebo (Placebo) | 簾簾糧願餘醖鑰積構範 = 簾憲鹽積顧壓壓構遞蓋 遞窪鏇夢簾鬱願範醖鑰 (醖鏇構網觸積觸遞醖壓, 膚鏇繭製願願夢夢糧簾 ~ 製獵遞範夢齋築選簾鹽) 更多 |
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