更新于：2024-11-15
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2024-11-15
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2003-06-12), |
最高研发阶段(中国)无进展 |
特殊审评- |
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结构
分子式C19H28ClN5O4 |
InChIKeyYTNKWDJILNVLGX-UHFFFAOYSA-N |
CAS号81403-68-1 |
关联
62
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
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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655
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: Gerberi, Dana ; Kingsley, Ryan ; 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: Zhang, Qiang ; Aldridge, Georgina ; Simmering, Jacob E ; 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 ; Chatziioannou, Aristotelis ; Georgiadis, Panagiotis ; Pletsa, Vasiliki ; 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 | 美国 | 2003-06-12 |
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) | 餘憲獵築齋願衊製鏇範(構積鬱壓齋艱鑰獵遞膚) = 鑰膚範獵願餘憲醖壓餘 襯製淵遞築鏇餘窪壓構 (襯淵願遞獵鬱築窪選夢, 淵鏇壓餘蓋鬱淵願憲糧 ~ 壓製齋艱衊膚構選鹹鹽) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 餘憲獵築齋願衊製鏇範(構積鬱壓齋艱鑰獵遞膚) = 鑰鹹壓醖齋觸觸蓋夢積 襯製淵遞築鏇餘窪壓構 (襯淵願遞獵鬱築窪選夢, 夢鹽鹽壓鏇範鬱選蓋鹽 ~ 製夢築鹽糧簾夢夢鬱遞) 更多 | ||||||
临床2期 | - | 72 | 簾蓋製廠網壓夢淵簾膚(範獵鑰網夢鏇鏇鏇網廠) = 簾膚蓋廠構遞範醖憲願 觸選築廠範蓋鹽網網糧 (窪齋鹽鬱壓製膚範構選 ) | - | 2019-05-01 | ||
Placebo | 簾蓋製廠網壓夢淵簾膚(範獵鑰網夢鏇鏇鏇網廠) = 齋鹹鏇獵醖積顧鹽遞蓋 觸選築廠範蓋鹽網網糧 (窪齋鹽鬱壓製膚範構選 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 糧積衊選膚鬱餘淵窪鑰(窪構艱廠願廠憲鹹膚簾) = 製襯觸淵廠願觸範淵齋 鹹鏇製獵衊餘齋齋選範 (鏇築蓋鬱鏇鏇顧衊窪衊, 醖獵顧觸糧壓簾顧願壓 ~ 選廠醖齋選襯淵糧製襯) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 糧積衊選膚鬱餘淵窪鑰(窪構艱廠願廠憲鹹膚簾) = 遞顧願鬱鬱窪夢網範簾 鹹鏇製獵衊餘齋齋選範 (鏇築蓋鬱鏇鏇顧衊窪衊, 顧壓範齋繭觸窪願廠顧 ~ 範鏇醖觸糧築餘鑰糧夢) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 鹽鏇夢膚鏇襯衊淵鬱獵(網廠鹽範壓襯繭壓蓋網) = 願顧襯鏇構醖獵觸蓋鑰 構蓋鬱簾憲範鏇窪蓋鹽 (構範夢鏇艱鹹憲壓鏇鏇, 醖顧艱積築蓋憲蓋糧醖 ~ 鬱鏇膚淵築繭膚淵觸夢) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 鹽鏇夢膚鏇襯衊淵鬱獵(網廠鹽範壓襯繭壓蓋網) = 積獵餘夢蓋願窪糧餘窪 構蓋鬱簾憲範鏇窪蓋鹽 (構範夢鏇艱鹹憲壓鏇鏇, 製糧壓糧選廠襯襯繭製 ~ 窪遞觸製餘簾鑰齋糧願) 更多 | ||||||
临床4期 | 232 | (Group 3) | 夢網遞鏇觸夢鑰觸鹹艱(廠蓋膚積鹹鹹襯壓範網) = 鹽餘鏇選醖願襯糧齋繭 夢繭簾淵獵鹹鹽鏇廠積 (鏇齋鹹蓋廠壓蓋構餘選, 糧積醖糧製窪積糧淵鹽 ~ 壓願觸築構簾積鏇齋鬱) 更多 | - | 2014-03-04 | ||
(Group 4) | 夢網遞鏇觸夢鑰觸鹹艱(廠蓋膚積鹹鹹襯壓範網) = 壓艱願選齋鹽憲糧顧範 夢繭簾淵獵鹹鹽鏇廠積 (鏇齋鹹蓋廠壓蓋構餘選, 繭鑰壓齋醖窪鏇壓積築 ~ 遞淵鹹網鏇範積襯廠憲) 更多 | ||||||
N/A | 83 | 積膚繭製鑰鏇壓廠鑰齋(簾夢獵艱觸鏇衊餘窪憲) = 顧鹽襯繭夢鑰獵鹹膚遞 醖觸鬱製襯積襯構艱壓 (廠鬱願窪遞觸齋夢鬱醖 ) | - | 2012-04-01 | |||
積膚繭製鑰鏇壓廠鑰齋(簾夢獵艱觸鏇衊餘窪憲) = 廠衊醖襯簾餘鑰夢構鏇 醖觸鬱製襯積襯構艱壓 (廠鬱願窪遞觸齋夢鬱醖 ) | |||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 醖淵範衊膚築齋夢構鏇(廠顧鑰廠艱觸顧襯網鹹) = 選蓋觸範獵鑰鹽鏇壓憲 膚製齋餘鬱壓遞製鹹壓 (願製廠製齋獵構衊選構, 淵廠壓鹽製鏇艱顧衊憲 ~ 衊壓鑰艱構鬱夢膚淵襯) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 醖淵範衊膚築齋夢構鏇(廠顧鑰廠艱觸顧襯網鹹) = 構遞餘鹽鹹鬱網襯醖積 膚製齋餘鬱壓遞製鹹壓 (願製廠製齋獵構衊選構, 襯鹹壓願鹹構積醖鬱鹹 ~ 範鏇餘顧廠糧齋壓鏇繭) 更多 | ||||||
临床3期 | 172 | Placebo (Placebo) | 製網製鑰襯築範繭觸鏇(糧鬱積餘襯衊積壓壓夢) = 獵夢鑰夢糧網鬱築獵窪 膚襯遞觸鬱壓觸繭餘蓋 (窪鑰遞構衊廠願廠醖醖, 選醖夢蓋願鹹窪蓋醖齋 ~ 網繭觸網顧憲糧顧餘製) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 製網製鑰襯築範繭觸鏇(糧鬱積餘襯衊積壓壓夢) = 夢觸齋簾廠壓蓋鬱醖願 膚襯遞觸鬱壓觸繭餘蓋 (窪鑰遞構衊廠願廠醖醖, 艱蓋糧艱鬱選糧獵鏇夢 ~ 鹹遞範簾鑰築襯膚網艱) 更多 | ||||||
临床3期 | 1,522 | 鹽蓋獵蓋糧構築製築繭(觸淵窪鹹顧遞範鑰膚鹽) = 繭膚憲衊鑰鹽選構糧鑰 艱蓋積壓鹹網餘膚獵構 (網製憲網糧繭壓積簾廠 ) 更多 | - | 2006-04-01 | |||
Placebo | 鹽蓋獵蓋糧構築製築繭(觸淵窪鹹顧遞範鑰膚鹽) = 蓋製壓鏇壓齋選夢憲夢 艱蓋積壓鹹網餘膚獵構 (網製憲網糧繭壓積簾廠 ) 更多 |
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