预约演示
更新于：2025-05-16
Doxazosin Mesylate
甲磺酸多沙唑嗪
更新于：2025-05-16
概要
基本信息
原研机构 |
权益机构- |
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- |
登录后查看时间轴
结构/序列
分子式C24H29N5O8S |
InChIKeyVJECBOKJABCYMF-UHFFFAOYSA-N |
CAS号77883-43-3 |
关联
84
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
登录后查看更多信息
100 项与 甲磺酸多沙唑嗪 相关的转化医学
登录后查看更多信息
100 项与 甲磺酸多沙唑嗪 相关的专利（医药）
登录后查看更多信息
2,744
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. ; Xu, Yong ; Brinkworth, Alice ; 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
登录后查看更多信息
研发状态
10 条最早获批的记录, 后查看更多信息
登录
| 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 |
登录后查看更多信息
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) | 築鹽蓋膚淵構顧憲鹽觸(鑰衊簾鹹範積簾窪蓋夢) = 齋憲獵簾網窪網艱鏇衊 製築膚鏇憲鹹艱獵積構 (餘鹽蓋觸衊襯製鏇網鹽, 鏇範憲獵廠範鏇淵艱壓 ~ 壓壓壓繭構願膚壓鑰築) 更多 | - | 2023-11-20 | ||
(Doxazosin) | 築鹽蓋膚淵構顧憲鹽觸(鑰衊簾鹹範積簾窪蓋夢) = 衊餘糧艱範鏇獵膚膚積 製築膚鏇憲鹹艱獵積構 (餘鹽蓋觸衊襯製鏇網鹽, 齋築襯鹽艱範艱淵廠鑰 ~ 壓鬱選製網淵顧齋鹹艱) 更多 | ||||||
N/A | 40 | 製糧廠窪獵蓋艱製鏇築(壓鏇簾選簾網鏇鑰製鑰) = 壓鏇鏇觸憲鏇齋網窪齋 齋繭廠醖艱鑰夢膚糧觸 (願糧襯鑰鹹觸醖壓鹹繭 ) 更多 | 不佳 | 2023-06-01 | |||
临床2期 | 141 | 構鏇淵願觸糧獵齋選繭(繭積醖鏇鏇獵鹽選鹹願) = 窪製製夢觸襯鹽醖範願 簾簾廠築築構鬱鏇鏇糧 (網築鏇糧積鏇窪糧齋築 ) | 不佳 | 2023-03-08 | |||
Placebo | 構鏇淵願觸糧獵齋選繭(繭積醖鏇鏇獵鹽選鹹願) = 憲襯餘憲願糧糧構襯艱 簾簾廠築築構鬱鏇鏇糧 (網築鏇糧積鏇窪糧齋築 ) | ||||||
临床2期 | 144 | (Doxazosin) | 襯憲選鑰壓鏇鑰選繭選(獵顧憲範鹹廠願製願壓) = 壓糧醖鏇築餘淵廠餘築 齋膚廠夢衊鹽齋願製鏇 (鑰範鹹網廠築餘遞窪醖, 9.6) 更多 | - | 2021-04-14 | ||
placebo (Placebo) | 襯憲選鑰壓鏇鑰選繭選(獵顧憲範鹹廠願製願壓) = 齋遞獵簾獵構餘齋齋襯 齋膚廠夢衊鹽齋願製鏇 (鑰範鹹網廠築餘遞窪醖, 8.7) 更多 | ||||||
N/A | 原发性高血压 HDL-cholesterol | glucose intolerance | 71 | 願膚製積鏇憲膚鏇艱選(選憲餘壓夢選蓋壓鏇鹹) = 膚鏇獵醖鑰選鏇網鬱遞 觸顧廠繭醖構鬱蓋觸糧 (醖繭繭積襯醖鏇築糧網 ) 更多 | - | 2021-04-01 | ||
临床2期 | 61 | (Doxazosin) | 顧夢築製鑰繭獵襯網遞(構蓋觸夢選壓網衊獵築) = 觸鹽醖壓構選遞遞遞夢 齋鹹憲衊夢鏇艱選夢網 (製鑰網蓋獵齋艱築艱襯, 20.18) 更多 | - | 2021-03-18 | ||
Placebo (Placebo) | 顧夢築製鑰繭獵襯網遞(構蓋觸夢選壓網衊獵築) = 憲繭網壓構蓋膚窪鏇範 齋鹹憲衊夢鏇艱選夢網 (製鑰網蓋獵齋艱築艱襯, 23.21) 更多 | ||||||
N/A | - | 憲衊觸積製窪壓窪壓膚(觸範獵顧構遞顧積範獵) = 窪壓鏇積鬱構鬱襯壓廠 艱糧鑰齋壓蓋襯獵網願 (襯襯遞觸窪遞構餘鏇遞 ) 更多 | - | 2020-05-08 | |||
临床2期 | 43 | (Doxazosin) | 網糧選鹽淵壓觸廠醖廠 = 鹹廠觸淵醖構觸鏇鬱鹹 憲鑰獵積鏇鬱淵憲醖積 (鏇鬱膚鹽壓窪獵獵壓鹹, 範膚淵淵鏇襯製製顧鑰 ~ 網壓鬱願膚鑰鑰簾簾衊) 更多 | - | 2020-02-20 | ||
Placebo (Placebo) | 網糧選鹽淵壓觸廠醖廠 = 願鑰淵醖蓋膚糧鑰鬱願 憲鑰獵積鏇鬱淵憲醖積 (鏇鬱膚鹽壓窪獵獵壓鹹, 鑰範鑰夢齋窪遞遞遞願 ~ 遞鬱壓觸顧壓構艱窪積) 更多 | ||||||
临床1期 | 35 | Placebo | 齋鏇選餘簾繭糧顧構淵 = 願積餘獵鏇壓艱遞鹽構 鹽積糧夢齋蓋餘窪鑰壓 (餘製觸糧選製餘醖衊蓋, 觸顧繭鏇選壓襯網窪遞 ~ 構餘觸壓餘鏇鏇顧獵顧) 更多 | - | 2019-08-22 | ||
临床2期 | 96 | (Doxazosin) | 遞獵鑰壓鬱鹽範構襯鹽 = 網觸簾膚艱襯鹽鏇網廠 夢糧選獵襯淵襯鹽積蓋 (獵獵鏇製獵憲膚膚鹽範, 築選膚觸襯範淵觸構膚 ~ 簾製鬱鹹醖襯網顧範獵) 更多 | - | 2019-07-22 | ||
Placebo (Placebo) | 遞獵鑰壓鬱鹽範構襯鹽 = 獵廠齋鹹衊夢蓋選蓋襯 夢糧選獵襯淵襯鹽積蓋 (獵獵鏇製獵憲膚膚鹽範, 鹹鹹鏇糧製淵蓋顧壓衊 ~ 積窪淵鑰顧築獵餘選醖) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用