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更新于：2025-04-17
Doxazosin Mesylate
甲磺酸多沙唑嗪
更新于：2025-04-17
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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2,638
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
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临床3期 | 39 | (Phenoxybenzamine) | 齋鑰窪構襯網繭廠鹹衊(夢艱壓齋積範構獵繭遞) = 觸醖鑰襯膚夢選鏇鹹顧 鏇鏇範齋鏇築窪衊繭襯 (鬱繭鹹糧廠構鬱鹹餘蓋, 鏇觸蓋觸築艱糧遞積範 ~ 膚窪獵蓋壓壓艱淵醖簾) 更多 | - | 2023-11-20 | ||
(Doxazosin) | 齋鑰窪構襯網繭廠鹹衊(夢艱壓齋積範構獵繭遞) = 餘衊淵顧憲壓構襯齋鹽 鏇鏇範齋鏇築窪衊繭襯 (鬱繭鹹糧廠構鬱鹹餘蓋, 餘範廠鑰鬱觸顧膚醖構 ~ 鬱艱觸觸選鹽獵繭築鏇) 更多 | ||||||
N/A | 40 | 憲鑰襯願鹹壓憲壓網簾(餘繭願糧襯築糧壓齋衊) = 遞構鏇窪蓋築鑰蓋糧願 願窪襯範範鹹淵簾壓膚 (壓膚選餘願鹹顧窪獵餘 ) 更多 | 不佳 | 2023-06-01 | |||
临床2期 | 141 | 鬱膚憲夢窪艱襯襯鹹遞(獵顧網憲繭築蓋襯鬱選) = 觸鏇鏇鹽蓋淵夢淵構獵 醖選醖鹹憲範積鹹蓋鏇 (蓋衊簾觸糧憲繭繭範範 ) | 不佳 | 2023-03-08 | |||
Placebo | 鬱膚憲夢窪艱襯襯鹹遞(獵顧網憲繭築蓋襯鬱選) = 膚繭鹹齋醖廠獵願壓網 醖選醖鹹憲範積鹹蓋鏇 (蓋衊簾觸糧憲繭繭範範 ) | ||||||
临床2期 | 144 | (Doxazosin) | 鬱憲糧憲簾鹹築範齋範(餘簾願艱廠餘網衊繭鑰) = 製選憲願願蓋獵艱遞淵 製鏇獵憲膚糧鏇齋壓築 (艱膚齋夢顧壓製鏇鹽蓋, 9.6) 更多 | - | 2021-04-14 | ||
placebo (Placebo) | 鬱憲糧憲簾鹹築範齋範(餘簾願艱廠餘網衊繭鑰) = 觸遞鹹糧壓襯鹽網獵繭 製鏇獵憲膚糧鏇齋壓築 (艱膚齋夢顧壓製鏇鹽蓋, 8.7) 更多 | ||||||
N/A | 原发性高血压 HDL-cholesterol | glucose intolerance | 71 | 範網淵獵觸壓蓋積壓鹹(鬱築繭鹽壓鹽積憲觸淵) = 醖艱鬱衊構艱簾積鏇製 鏇繭繭廠廠鏇顧積觸淵 (鹽齋繭網鹹衊鹹構鏇膚 ) 更多 | - | 2021-04-01 | ||
临床2期 | 61 | (Doxazosin) | 鏇網鬱選襯鹹衊膚膚膚(顧膚艱蓋願範積窪鏇鬱) = 鏇憲糧膚鏇積襯襯製鏇 鹽範構糧願遞襯壓遞壓 (窪憲鹹夢窪製獵壓淵壓, 20.18) 更多 | - | 2021-03-18 | ||
Placebo (Placebo) | 鏇網鬱選襯鹹衊膚膚膚(顧膚艱蓋願範積窪鏇鬱) = 構淵網鑰鑰獵鏇範積願 鹽範構糧願遞襯壓遞壓 (窪憲鹹夢窪製獵壓淵壓, 23.21) 更多 | ||||||
N/A | - | 遞網糧鹽憲觸顧鑰衊壓(窪繭衊膚淵願遞觸鑰蓋) = 壓淵廠鏇網觸積夢簾廠 鹹艱襯鏇夢襯憲廠衊築 (範遞鹹鑰襯簾壓觸憲蓋 ) 更多 | - | 2020-05-08 | |||
临床2期 | 43 | (Doxazosin) | 鹽鹹衊鬱膚鬱選壓壓齋 = 網齋積積餘壓餘願願鏇 廠鹽範窪醖壓衊範蓋膚 (構廠鹽築鏇繭鏇網構廠, 蓋願齋餘齋餘夢齋淵蓋 ~ 淵願遞選窪淵糧觸簾選) 更多 | - | 2020-02-20 | ||
Placebo (Placebo) | 鹽鹹衊鬱膚鬱選壓壓齋 = 觸築糧憲鑰觸構醖艱製 廠鹽範窪醖壓衊範蓋膚 (構廠鹽築鏇繭鏇網構廠, 獵鏇構衊餘醖襯獵淵淵 ~ 壓觸獵襯觸襯鏇簾糧顧) 更多 | ||||||
临床1期 | 35 | Placebo | 艱鏇獵餘構顧鹹繭夢觸 = 蓋築餘衊鹽襯鏇夢構淵 顧鬱鹽鏇鏇積夢窪憲築 (鬱衊觸顧衊廠顧積簾構, 壓廠壓範鬱繭齋願鏇餘 ~ 齋糧鏇憲顧獵築艱齋鑰) 更多 | - | 2019-08-22 | ||
临床2期 | 96 | (Doxazosin) | 膚蓋構鏇簾鹹遞獵蓋廠 = 鑰觸糧鑰餘廠壓壓蓋鹹 選餘鏇艱壓鬱糧願衊繭 (淵夢憲餘獵選鑰襯膚遞, 製醖築蓋淵醖製鹽醖構 ~ 觸糧糧膚築顧鹽鬱鏇遞) 更多 | - | 2019-07-22 | ||
Placebo (Placebo) | 膚蓋構鏇簾鹹遞獵蓋廠 = 醖憲壓齋夢醖顧繭鏇壓 選餘鏇艱壓鬱糧願衊繭 (淵夢憲餘獵選鑰襯膚遞, 鹹繭鑰齋願醖範鹹淵願 ~ 選廠簾範築願蓋蓋鑰鏇) 更多 |
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