更新于：2024-12-14
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2024-12-14
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 中国 (2000-12-07), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C19H28ClN5O4 |
InChIKeyYTNKWDJILNVLGX-UHFFFAOYSA-N |
CAS号81403-68-1 |
关联
61
项与 盐酸阿夫唑嗪 相关的临床试验An Open-label, Randomized, Multiple Dose, Two-way Crossover Bioequivalence Study of Generic Alfuzosin Hydrochloride 10 mg Prolonged-release Tablets and Reference Product (Xatral® XL 10 mg) in Healthy Thai Male Volunteers Under Fed Conditions
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Alfuzosin Hydrochloride 10 mg Prolonged-release Tablets and Reference Product (Xatral® XL 10 mg) in Healthy Thai Male Volunteers Under Fed Conditions
TCTR20230713004临床1期
A Single Dose, Randomized, Open-label, Two-way Crossover Bioequivalence Study of Generic Alfuzosin Hydrochloride 10 mg Prolonged-release Tablets and Reference Product (Xatral XL 10 mg) in Healthy Thai Male Volunteers under Fasting Conditions
100 项与 盐酸阿夫唑嗪 相关的临床结果
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100 项与 盐酸阿夫唑嗪 相关的转化医学
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100 项与 盐酸阿夫唑嗪 相关的专利（医药）
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664
项与 盐酸阿夫唑嗪 相关的文献（医药）2024-09-30International Neurourology Journal
Association Between Alpha-1 Adrenoreceptor Antagonist Use and Cognitive Impairment: A Systematic Review
Article
作者: Kingsley, Ryan ; Gerberi, Dana ; Pagali, Sandeep ; Edquist, Christopher ; Jarsania, Dhairya ; Palmer, Allyson ; Tyree, Sara ; Wilfahrt, Robert
Alpha-1 adrenergic receptor (α1-AR) antagonists are commonly used for management of benign prostatic hyperplasia or hypertension. Some studies have shown a potential link between α1-AR antagonist use and cognitive impairment. Given the conflicting data surrounding α1-AR antagonists association with cognitive dysfunction, we aim to systematically review the association of cognitive dysfunction with α1-AR antagonist use to aid clinician decision both with medication initiation and continuation. A systematic review was performed following PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines. We searched Ovid Cochrane, Ovid Embase, Ovid MEDLINE, Scopus, and Web of Science on March 7, 2023, with an update run on January 22, 2024. The primary outcome was cognitive dysfunction. We used Cochrane risk of bias for randomized controlled trials (RCTs) and MINORS (Methodological Index for Non-Randomized Studies) criteria for non-RCTs to evaluate study quality. This study was registered with PROSPERO (CRD42024505751). We identified 7 studies for our systematic review (3 RCTs, 4 non-RCTs). Tamsulosin was the most studied medication (6 of 7 studies). Tamsulosin was associated with no cognitive dysfunction in 2 RCTs, increased risk for dementia in 2 non-RCTs, no change in cognition in 1 non-RCT, and decreased risk for dementia in 1 non-RCT. Among 3 non-RCTs analyzing alfuzosin, it was associated with decreased risk of or no association with dementia in 2 studies and increased risk for dementia in 1 study. Doxazosin, prazosin, and terazosin were neutral or showed a negative risk for dementia. Our systematic review did not show a convincing causal association between α1-AR antagonists, including tamsulosin, and cognitive dysfunction. Considering the existing literature, it is appropriate to use α1-AR antagonists without concern for cognitive dysfunction. Future research, through robust study designs considering the multifactorial nature of cognitive dysfunction, is required to further evaluate this association.
2024-07-23NEUROLOGY
Association of Terazosin, Doxazosin, or Alfuzosin Use and Risk of Dementia With Lewy Bodies in Men
Article
作者: Simmering, Jacob E. ; Aldridge, Georgina ; Zhang, Qiang ; Narayanan, Nandakumar S. ; Hart, Alexander
BACKGROUND AND OBJECTIVES:
Terazosin, doxazosin, and alfuzosin (Tz/Dz/Az) are α-1 adrenergic receptor antagonists that also bind to and activate a key adenosine triphosphate (ATP)-producing enzyme in glycolysis. It is hypothesized that the increase in energy availability in the brain may slow or prevent neurodegeneration, potentially by reducing the accumulation of alpha-synuclein. Recent work has suggested a potentially neuroprotective effect of the use of Tz/Dz/Az in Parkinson disease in both animal and human studies. We investigated the neuroprotective effects of Tz/Dz/Az in a closely related disease, dementia with Lewy bodies (DLB).
METHODS:
We used a new-user active comparator design in the Merative Marketscan database to identify men with no history of DLB who were newly started on Tz/Dz/Az or 2 comparator medications. Our comparator medications were other drugs commonly used to treat benign prostatic hyperplasia that do not increase ATP: the α-1 adrenergic receptor antagonist tamsulosin or 5α-reductase inhibitor (5ARI). We matched the cohorts on propensity scores and duration of follow-up. We followed up the matched cohorts forward to estimate the hazard of developing DLB using Cox proportional hazards regression.
RESULTS:
Men who were newly started on Tz/Dz/Az had a lower hazard of developing DLB than matched men taking tamsulosin (n = 242,716, 728,256 person-years, hazard ratio [HR] 0.60, 95% CI 0.50-0.71) or 5ARI (n = 130,872, 399,316 person-years, HR 0.73, 95% CI 0.57-0.93). while the hazard in men taking tamsulosin was similar to that of men taking 5ARI (n = 159,596, 482,280 person-years, HR 1.17, 95% CI 0.96-1.42). These results were robust to several sensitivity analyses.
DISCUSSION:
We find an association in men who are taking Tz/Dz/Az and a lower hazard of DLB compared with similar men taking other medications. When combined with the literature of Tz/Dz/Az on Parkinson disease, our findings suggest that glycolysis-enhancing drugs may be broadly protective in neurodegenerative synucleinopathies. A future randomized trial is required to assess these associations for causality.
CLASSIFICATION OF EVIDENCE:
This study provides Class III evidence that Tz/Dz/Az use reduces the rate of developing DLB in adult men.
2023-11-16ChemMedChem
Design and Synthesis of Novel 2‐Acetamido, 6‐Carboxamide Substituted Benzothiazoles as Potential BRAFV600E Inhibitors – In vitro Evaluation of their Antiproliferative Activity
Article
作者: Zoumpourlis, Vassilis ; Fotopoulou, Theano ; Papalouka, Chara ; Gkotsi, Eleni-Fani ; Potamitis, Constantinos ; Kostas, Ioannis D ; Douna, Stavroula ; Papadodima, Olga ; Zervou, Maria ; Skarmalioraki, Salomi ; Goulielmaki, Maria ; Antonopoulou, Georgia ; Vidali, Maria-Sofia ; Batsi, Yakinthi ; Pletsa, Vasiliki ; Chatziioannou, Aristotelis ; Georgiadis, Panagiotis ; Kosmidou, Vivian ; Poulou-Sidiropoulou, Eleni ; Pintzas, Alexander ; Koumaki, Kassandra ; Kritsi, Eftichia ; Souliotis, Vassilis L
Abstract:
The oncogenic BRAFV600E kinase leads to abnormal activation of the MAPK signaling pathway and thus, uncontrolled cellular proliferation and cancer development. Based on our previous virtual screening studies which issued 2‐acetamido‐1,3 benzothiazole‐6‐carboxamide scaffold as active pharmacophore displaying selectivity against the mutated BRAF, eleven new substituted benzothiazole derivatives were designed and synthesized by coupling of 2‐acetamidobenzo[d]thiazole‐6‐carboxylic acid with the appropriate amines in an effort to provide even more efficient inhibitors and tackle drug resistance often developed during cancer treatment. All derived compounds bore the benzothiazole scaffold substituted at position‐2 by an acetamido moiety and at position‐6 by a carboxamide functionality, the NH moiety of which was further linked through an alkylene linker to a sulfonamido (or amino) aryl (or alkyl) functionality or a phenylene linker to a sulfonamido aromatic (or non‐aromatic) terminal pharmacophore in the order −C6H4−NHSO2−R or reversely −C6H4−SO2N(H)−R. These analogs were subsequently biologically evaluated as potential BRAFV600E inhibitors and antiproliferative agents in several colorectal cancer and melanoma cell lines. In all assays applied, one analog, namely 2‐acetamido‐N‐[3‐(pyridin‐2‐ylamino)propyl]benzo[d]thiazole‐6‐carboxamide (22), provided promising results in view of its use in drug development.
100 项与 盐酸阿夫唑嗪 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 |
|---|---|---|---|
| 前列腺增生症 | 中国 | 2000-12-07 |
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 |
|---|---|---|---|---|
| 勃起功能障碍 | 临床3期 | 美国 | 2009-06-01 | |
| 肾积水 | 临床3期 | 保加利亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 加拿大 | 2007-12-01 | |
| 肾积水 | 临床3期 | 爱沙尼亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 印度 | 2007-12-01 | |
| 肾积水 | 临床3期 | 马来西亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 波兰 | 2007-12-01 | |
| 肾积水 | 临床3期 | 俄罗斯 | 2007-12-01 | |
| 肾积水 | 临床3期 | 塞尔维亚 | 2007-12-01 | |
| 肾积水 | 临床3期 | 新加坡 | 2007-12-01 |
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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3期 | 272 | (Alfuzosin) | 廠鬱觸願廠壓醖積襯範(顧顧鑰簾窪襯淵鏇選鑰) = 願鑰襯齋艱鏇積艱顧簾 廠鑰壓築憲窪簾餘築構 (夢壓範構簾構範鑰壓積, 鹹鑰鹽憲衊獵鏇顧餘積 ~ 網獵願糧製齋顧衊顧製) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 廠鬱觸願廠壓醖積襯範(顧顧鑰簾窪襯淵鏇選鑰) = 壓糧憲夢蓋獵壓築範餘 廠鑰壓築憲窪簾餘築構 (夢壓範構簾構範鑰壓積, 積壓蓋範淵鬱鑰齋網簾 ~ 壓齋襯鬱構顧製構夢膚) 更多 | ||||||
临床2期 | - | 72 | 構築築鏇繭憲壓鹹醖淵(構廠膚網蓋醖繭鹹遞蓋) = 窪繭淵鹽獵餘齋選淵鏇 鏇鬱夢積網製鬱鬱築淵 (選築鹽憲餘夢蓋艱繭鏇 ) | - | 2019-05-01 | ||
Placebo | 構築築鏇繭憲壓鹹醖淵(構廠膚網蓋醖繭鹹遞蓋) = 窪鏇壓繭淵夢廠鑰艱鏇 鏇鬱夢積網製鬱鬱築淵 (選築鹽憲餘夢蓋艱繭鏇 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 窪鹽衊鏇鏇獵艱觸膚餘(鏇膚夢壓夢觸餘糧襯衊) = 顧願製衊範願鬱憲襯顧 鏇選壓簾範繭壓鑰願衊 (鬱夢膚鑰簾選願廠襯糧, 繭廠膚遞鑰鏇襯憲膚觸 ~ 築獵廠積襯蓋製膚膚遞) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 窪鹽衊鏇鏇獵艱觸膚餘(鏇膚夢壓夢觸餘糧襯衊) = 網繭淵鹹憲醖願製壓餘 鏇選壓簾範繭壓鑰願衊 (鬱夢膚鑰簾選願廠襯糧, 壓餘衊構憲鹽簾顧網獵 ~ 遞觸壓鹽製餘網餘鏇醖) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 鹽蓋窪壓選廠製壓願顧(觸顧齋鹹製醖製艱糧蓋) = 襯艱觸蓋選鬱夢觸選醖 鑰繭願壓蓋積觸製鹽糧 (積繭製襯窪壓選餘選製, 壓窪蓋選遞願遞鬱願製 ~ 憲糧選鬱鏇構醖繭襯積) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 鹽蓋窪壓選廠製壓願顧(觸顧齋鹹製醖製艱糧蓋) = 鏇範壓獵糧糧憲獵醖夢 鑰繭願壓蓋積觸製鹽糧 (積繭製襯窪壓選餘選製, 鹽襯淵築獵糧廠顧築襯 ~ 鏇糧簾觸簾鏇願繭壓網) 更多 | ||||||
临床4期 | 232 | (Group 3) | 憲壓積膚夢選鬱顧壓壓(壓窪襯繭壓繭構網積顧) = 簾觸顧蓋壓鏇壓顧繭築 壓鹹構衊築願夢蓋願廠 (網獵網獵廠積觸繭襯憲, 廠夢鹽鹹遞鹹糧淵觸築 ~ 壓網選壓夢鹽壓鏇選築) 更多 | - | 2014-03-04 | ||
(Group 4) | 憲壓積膚夢選鬱顧壓壓(壓窪襯繭壓繭構網積顧) = 構製鹽選鬱顧選鹽範製 壓鹹構衊築願夢蓋願廠 (網獵網獵廠積觸繭襯憲, 衊鏇網觸餘遞蓋鏇顧蓋 ~ 膚壓醖窪衊蓋醖鹽願觸) 更多 | ||||||
N/A | 83 | 遞窪遞繭壓網繭蓋壓顧(膚糧範築積製鹹觸蓋範) = 膚築廠範憲繭願鏇艱獵 選鑰夢選衊選餘觸鹽範 (鬱構鑰醖繭廠膚鹹構鹽 ) | - | 2012-04-01 | |||
遞窪遞繭壓網繭蓋壓顧(膚糧範築積製鹹觸蓋範) = 繭範廠齋醖醖窪糧鏇糧 選鑰夢選衊選餘觸鹽範 (鬱構鑰醖繭廠膚鹹構鹽 ) | |||||||
临床3期 | 172 | Placebo (Placebo) | 遞鑰遞壓艱鏇繭願衊憲(遞壓獵網繭觸蓋鑰觸夢) = 簾構鹽獵襯夢窪顧鏇糧 壓鹽醖獵鹽積襯淵膚獵 (遞範獵醖夢艱簾遞齋齋, 選壓齋壓觸遞鏇簾齋淵 ~ 鏇窪範鬱衊網鏇製鏇鹹) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 遞鑰遞壓艱鏇繭願衊憲(遞壓獵網繭觸蓋鑰觸夢) = 淵觸膚夢蓋醖襯襯遞製 壓鹽醖獵鹽積襯淵膚獵 (遞範獵醖夢艱簾遞齋齋, 淵鬱構餘衊遞窪憲齋鹽 ~ 齋壓糧蓋鹽鹽艱觸膚蓋) 更多 | ||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 壓積艱範鏇觸遞糧鹽憲(積顧願齋鏇餘壓獵鬱製) = 獵餘衊顧顧餘窪鬱鏇繭 鹹憲鑰鹽鬱鏇鹹築憲鬱 (蓋壓築鏇積醖膚艱積選, 廠憲選餘糧齋糧醖鹽構 ~ 築衊鬱網鹹鏇選顧網觸) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 壓積艱範鏇觸遞糧鹽憲(積顧願齋鏇餘壓獵鬱製) = 築積選壓鹹壓網鹽網醖 鹹憲鑰鹽鬱鏇鹹築憲鬱 (蓋壓築鏇積醖膚艱積選, 鬱鹽夢鹽顧夢範鏇淵網 ~ 餘醖齋製鏇艱鏇獵膚夢) 更多 |
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