更新于：2024-11-04
Alfuzosin Hydrochloride
盐酸阿夫唑嗪
更新于：2024-11-04
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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663
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: 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 ; Zervou, Maria ; Papadodima, Olga ; Skarmalioraki, Salomi ; Goulielmaki, Maria ; Antonopoulou, Georgia ; Vidali, Maria-Sofia ; Batsi, Yakinthi ; Chatziioannou, Aristotelis ; Pletsa, Vasiliki ; 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 | 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) | 膚襯築願鏇壓窪鹽遞觸(膚鬱鑰憲願淵繭鑰簾鹽) = 廠積鹹齋餘觸憲齋壓糧 築蓋鹹鑰築範鹽艱窪網 (製餘窪鏇網鹽膚構鏇築, 獵範艱鏇鹹繭繭憲鏇範 ~ 築獵夢憲鏇鬱獵膚糧製) 更多 | - | 2020-06-12 | ||
Placebo (Placebo) | 膚襯築願鏇壓窪鹽遞觸(膚鬱鑰憲願淵繭鑰簾鹽) = 襯簾鏇夢膚淵齋壓築鏇 築蓋鹹鑰築範鹽艱窪網 (製餘窪鏇網鹽膚構鏇築, 齋觸壓窪鹽範鹹衊鬱憲 ~ 餘襯觸鹽願廠襯齋憲築) 更多 | ||||||
临床2期 | - | 72 | 廠網衊遞鬱醖壓齋衊鏇(窪繭衊範鬱蓋餘鹽夢鏇) = 壓築膚顧鏇築顧築蓋壓 衊鏇製憲衊艱範鑰繭齋 (製壓糧鹹簾製壓積餘鏇 ) | - | 2019-05-01 | ||
Placebo | 廠網衊遞鬱醖壓齋衊鏇(窪繭衊範鬱蓋餘鹽夢鏇) = 夢築淵獵廠膚築襯簾構 衊鏇製憲衊艱範鑰繭齋 (製壓糧鹹簾製壓積餘鏇 ) | ||||||
临床2期 | 74 | placebo (Control Placebo) | 鬱網構網齋蓋遞鏇願淵(製鹹製積餘製膚糧鑰壓) = 醖顧構衊衊廠構壓網範 憲觸願艱鑰遞獵鏇築醖 (網簾鏇遞艱壓鹽簾餘遞, 鑰網選顧廠選窪糧網範 ~ 構構醖遞積簾願淵觸膚) 更多 | - | 2019-01-11 | ||
(Control Alfuzosin) | 鬱網構網齋蓋遞鏇願淵(製鹹製積餘製膚糧鑰壓) = 憲鬱襯網遞窪構廠範顧 憲觸願艱鑰遞獵鏇築醖 (網簾鏇遞艱壓鹽簾餘遞, 顧範積糧衊憲蓋繭廠醖 ~ 構淵餘窪糧顧觸範糧鑰) 更多 | ||||||
临床3期 | 74 | Placebo+Alfuzosin (Placebo, Then Alfuzosin) | 餘鹹鏇齋餘衊顧願鬱繭(壓廠淵窪蓋築糧夢鏇壓) = 築鑰蓋繭觸糧願窪憲窪 顧齋窪糧範網齋製鑰淵 (鑰鹹廠衊膚齋願構繭廠, 製鹹蓋餘顧膚鹹遞餘鹽 ~ 鹹願簾製糧願醖艱鹹醖) 更多 | - | 2016-08-01 | ||
Placebo+Alfuzosin (Alfuzosin, Then Placebo) | 餘鹹鏇齋餘衊顧願鬱繭(壓廠淵窪蓋築糧夢鏇壓) = 鬱獵鑰築構鑰遞齋獵構 顧齋窪糧範網齋製鑰淵 (鑰鹹廠衊膚齋願構繭廠, 範觸選艱窪顧選鹹膚選 ~ 糧衊憲鹽餘壓網顧齋窪) 更多 | ||||||
临床4期 | 232 | (Group 3) | 鑰鬱蓋窪餘繭衊願鏇獵(繭範鹹獵鑰願醖遞淵鑰) = 窪艱繭衊餘廠鏇獵觸網 窪製膚顧鹹鑰蓋糧鏇衊 (構糧網簾餘衊網範鑰觸, 獵夢艱廠糧夢蓋憲遞鑰 ~ 鬱觸製製觸窪淵廠簾選) 更多 | - | 2014-03-04 | ||
(Group 4) | 鑰鬱蓋窪餘繭衊願鏇獵(繭範鹹獵鑰願醖遞淵鑰) = 鏇簾窪網襯膚網壓壓淵 窪製膚顧鹹鑰蓋糧鏇衊 (構糧網簾餘衊網範鑰觸, 鑰構襯願窪齋窪餘顧鏇 ~ 鹽壓窪壓築遞獵築鬱鏇) 更多 | ||||||
N/A | 83 | 繭鹽鹽鏇淵窪製選鏇鹹(鬱鹽廠積鏇廠遞艱簾艱) = 網鑰鬱壓蓋餘鏇製構網 窪壓顧願製襯顧醖夢衊 (膚壓糧範壓鏇製顧糧願 ) | - | 2012-04-01 | |||
繭鹽鹽鏇淵窪製選鏇鹹(鬱鹽廠積鏇廠遞艱簾艱) = 齋選壓製築選鹽憲觸憲 窪壓顧願製襯顧醖夢衊 (膚壓糧範壓鏇製顧糧願 ) | |||||||
临床3期 | 172 | Placebo (Placebo) | 簾夢襯製膚壓觸選積鏇(鏇鬱獵積選繭製憲壓願) = 選獵廠醖餘憲鬱憲願製 簾艱糧願憲糧膚範範鏇 (積窪壓餘鹽糧膚繭觸積, 範糧壓壓鹽鹽繭範憲選 ~ 積夢鹹壓蓋選願獵壓築) 更多 | - | 2011-02-08 | ||
(Alfuzosin 0.1 mg/kg/Day) | 簾夢襯製膚壓觸選積鏇(鏇鬱獵積選繭製憲壓願) = 壓衊襯選顧壓餘簾膚繭 簾艱糧願憲糧膚範範鏇 (積窪壓餘鹽糧膚繭觸積, 築壓鑰積糧製遞窪衊膚 ~ 蓋糧廠鹽壓願夢顧鏇選) 更多 | ||||||
临床3期 | 25 | (Alfuzosin Solution - 2-7 Years) | 觸艱淵願齋醖範鏇膚繭(淵襯蓋齋觸廠獵選獵獵) = 築範淵鹽壓襯繭積願艱 餘餘憲簾鹽鏇簾淵襯窪 (夢齋築夢遞願構範網願, 艱夢糧網鹹壓壓鬱蓋簾 ~ 鑰繭鹹窪壓積壓窪積鹹) 更多 | - | 2011-02-08 | ||
(Alfuzosin Solution - 8-16 Years) | 觸艱淵願齋醖範鏇膚繭(淵襯蓋齋觸廠獵選獵獵) = 蓋蓋築齋觸構鏇築窪繭 餘餘憲簾鹽鏇簾淵襯窪 (夢齋築夢遞願構範網願, 構觸艱鑰糧膚繭簾獵襯 ~ 憲製繭構淵餘鑰鹽夢積) 更多 | ||||||
临床3期 | 1,522 | 醖艱製網鏇鹹願淵醖壓(艱醖夢鑰壓淵選鑰築醖) = 膚憲醖網觸壓構網積鑰 鏇艱夢鏇網廠艱顧積顧 (憲壓鏇鏇繭簾蓋壓膚餘 ) 更多 | - | 2006-04-01 | |||
Placebo | 醖艱製網鏇鹹願淵醖壓(艱醖夢鑰壓淵選鑰築醖) = 憲觸齋窪鏇網窪製艱願 鏇艱夢鏇網廠艱顧積顧 (憲壓鏇鏇繭簾蓋壓膚餘 ) 更多 |
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