萘哌地尔(Naftopidil) - 药物靶点：ADRA1_在研适应症：排尿困难，前列腺增生症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Avishot、Eapidil、Naftopidil (JP17/INN)

+ [14]

靶点

ADRA1

作用机制

ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)

治疗领域

泌尿生殖系统疾病其他疾病

在研适应症

排尿困难前列腺增生症

非在研适应症

术后疼痛神经性膀胱功能障碍泌尿结石

原研机构

F. Hoffmann-La Roche Ltd.

在研机构

Dong-A ST Co., Ltd.贵州一康药业有限公司

非在研机构

Asahi Kasei Corp.

最高研发阶段批准上市

首次获批日期

日本 (1998-12-25),

排尿困难前列腺增生症

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C24H28N2O3

InChIKeyHRRBJVNMSRJFHQ-UHFFFAOYSA-N

CAS号57149-07-2

关联

20

项与萘哌地尔相关的临床试验

JPRN-jRCTs031180176 / Not yet recruiting临床3期

A prospective randomized controlled study on Suppression of Prostate cancer by Naftopidil - SNAP study

开始日期2017-02-22

申办/合作机构-

CTR20160675 / Completed

评估KT-611片和那妥于空腹和餐后状态下中国健康男性的随机、开放、单剂量、两阶段、两序列、交叉生物等效性研究

评估日本旭化成制药株式会社生产的KT-611片25mg和中国南京美瑞制药有限公司生产的“那妥”片25mg作用于空腹和餐后状态下中国健康男性受试者的生物等效性。

开始日期2016-12-03

申办/合作机构

Asahi Kasei Pharma Corp.

[+1]

CTR20160671 / Completed

评估KT-611片和司坦迪于空腹和餐后状态下中国健康男性的随机、开放、单剂量、两阶段、两序列、交叉生物等效性研究

评估日本旭化成制药株式会社生产的KT-611片25mg和中国北京双鹭药业股份有限公司生产的“司坦迪”片25mg作用于空腹和餐后状态下中国健康男性受试者的生物等效性。

开始日期2016-11-05

申办/合作机构

Asahi Kasei Pharma Corp.

[+1]

100 项与萘哌地尔相关的临床结果

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100 项与萘哌地尔相关的转化医学

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100 项与萘哌地尔相关的专利（医药）

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300

项与萘哌地尔相关的文献（医药）

2024-05-01·Basic & Clinical Pharmacology & Toxicology

Characteristics of α₁‐adrenoceptor antagonists‐induced ejaculatory dysfunction on spontaneous seminal emission in rats

Article

作者: Watanabe, Chizuko ; Sakurada, Shinobu ; Yonezawa, Akihiko ; Mizoguchi, Hirokazu ; Yoshizumi, Masaru ; Ise, Shin-Nosuke

AbstractAlthough α1‐adrenoceptor (α1‐AR) antagonists used to treat benign prostatic hyperplasia can cause ejaculation disorders, the aetiology of this adverse event is still controversial. Therefore, we investigated the effects of antagonists with different affinities for α1‐AR subtypes on ejaculatory function and their mechanisms of action in normal rats. In the spontaneous seminal emission (SSE) test, systemically administered prazosin, terazosin, tamsulosin and naftopidil decreased the weight of ejaculated seminal material in a dose‐dependent manner; the potency order was as follows: tamsulosin > terazosin > prazosin > naftopidil. The selective α1D‐AR antagonist BMY7378 had no effect on SSE. Intrathecal tamsulosin and naftopidil did not inhibit SSE. Tamsulosin, the most potent, was ineffective as a single dose and significantly increased seminal vesicle fluid in rats treated for 2 weeks but did not significantly change retrograde ejaculation. These results indicated that the difference in inhibitory potency of the five α1‐AR antagonists against SSE was due to the involvement of α1A‐AR subtypes. Our results further suggested that α1‐AR antagonist‐induced ejaculatory dysfunction at the peripheral level was mainly due to the loss of seminal emission, although some retrograde ejaculation may also be involved.

2024-02-26·JACS Au

Ligated Pd-Catalyzed Aminations of Aryl/Heteroaryl Halides with Aliphatic Amines under Sustainable Aqueous Micellar Conditions

Article

作者: Iyer, Karthik S. ; Yirak, Jordan R. ; Lammert, Robert M. ; Kavthe, Rahul D. ; Lipshutz, Bruce H.

Sustainable technology for constructing Pd-catalyzed C-N bonds involving aliphatic amines is reported. A catalytic system that relies on low levels of recyclable precious metal, a known and commercially available ligand, and a recyclable aqueous medium are combined, leading to a newly developed procedure. This new technology can be used in ocean water with equal effectiveness. Applications involving highly challenging reaction partners constituting late-stage functionalization are documented, as is a short but efficient synthesis of the drug naftopidil. Comparisons with existing aminations highlight the many advances being offered.

2023-10-01·International journal of clinical pharmacy

Association of silodosin, tamsulosin, and naftopidil with delirium: analysis of the pharmacovigilance database in Japan.

Article

作者: Noritake, Yumi ; Kawakami, Yasuhiro ; Kotake, Kazumasa

BACKGROUNDAn association between adrenergic alpha-1 receptor antagonists and delirium has been suggested, but the details are unclear.AIMThis study investigated the association between adrenergic alpha-1 receptor antagonists and delirium in patients with benign prostatic hyperplasia using the Japanese Adverse Drug Event Report database.METHODFirst, disproportionality analysis compared the frequency of delirium in the adrenergic alpha-1 receptor antagonists silodosin, tamsulosin, and naftopidil. Next, multivariate logistic analysis was performed to examine the association between delirium and adrenergic alpha-1 receptor antagonists where disproportionality was detected.RESULTSA disproportionality in delirium was observed in patients receiving tamsulosin (reporting odds ratio [ROR] 1.85, 95% confidence interval [CI] 1.38-2.44, P < 0.01) compared with those who did not, and also in patients receiving naftopidil (ROR 2.23, 95% CI 1.45-3.28, P < 0.01) compared with those who did not. Multivariate logistic analysis revealed that in addition to previously reported risk factors for delirium, delirium in patients receiving tamsulosin was significantly increased with concomitant use of anticholinergics (odds ratio 2.73, 95% CI 1.41-5.29, P < 0.01) and delirium in patients receiving naftopidil was significantly increased with concomitant use of beta3-adrenergic receptor agonists (odds ratio 4.19, 95% CI 1.66-10.6, P < 0.01).CONCLUSIONAnticholinergics or beta3-adrenergic receptor agonists to treat overactive bladder in patients receiving tamsulosin and naftopidil was strongly associated with delirium. Confirming the medical history and concomitant medications of patients receiving tamsulosin or naftopidil may contribute to preventing delirium in patients with benign prostatic hyperplasia and to improving their outcomes.

1

项与萘哌地尔相关的新闻（医药）

2023-07-20

·蒲公英Ouryao

监督检查→有3家不符合GMP

来源：山东药监局整理：wangxinglai2004 近日，山东药监局发布了2023年药品生产监督检查结果通告，共计51家次药品生产单位进行了现场检查，其中23家药品生产单位符合要求、23家药品生产单位基本符合要求、3家药品生产单位不符合要求。重点内容01 蓬莱金创药业有限公司检查时间：2023年4月13日至15日生产企业：蓬莱金创药业有限公司检查结论：不符合GMP要求检查范围：萘哌地尔分散片：口服固体制剂车间片剂生产线；脑心舒口服液、生脉饮、补中益气合剂：口服液体制剂车间合剂、口服液生产线；中药提取车间：中药前处理、中药提取生产线；特殊药品使用。02 山东万福堂中药饮片有限公司检查时间：2023年5月13日至14日生产企业：山东万福堂中药饮片有限公司检查结论：不符合GMP要求检查范围：中药饮片03 石药（山东）中药饮片有限公司检查时间：2023年5月11日生产企业：石药（山东）中药饮片有限公司检查结论：不符合GMP要求检查范围：中药饮片根据《药品管理法》《疫苗管理法》《药品生产监督管理办法》《药品生产质量管理规范》等法律法规规章规定，按照2023年药品生产监督检查工作计划，近期组织对51家次药品生产单位进行了现场检查。其中23家药品生产单位符合要求；23家药品生产单位基本符合要求要求；3家药品生产单位不符合要求；1家药品生产单位不具备生产条件，处于长期停产状态；1家药品生产单位许可证已过期，提出延期换证申请，不具备生产条件具体名单如下：根据检查情况，由相关检查分局督促有关单位严格落实企业主体责任，认真做好缺陷项目的监督整改和日常监管，并依法依规做好后处置工作。

疫苗

100 项与萘哌地尔相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01674	萘哌地尔	G04CA	DB12092

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
排尿困难	日本	-	1998-12-25
前列腺增生症	日本	-	1998-12-25

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
术后疼痛	临床2期	韩国	Dong-A ST Co., Ltd.	2013-10-25
神经性膀胱功能障碍	临床2期	日本	Asahi Kasei Corp.	-
泌尿结石	临床2期	韩国	Dong-A ST Co., Ltd.	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


AUA2011	N/A	脊髓损伤	-	Naftopidil	積醖夢鏇糧鑰蓋淵膚壓(窪鑰觸鹽蓋壓廠網願艱) = 簾壓鏇範觸鑰網窪壓憲醖窪鏇構醖蓋襯鬱範膚 (鬱壓夢製築艱鑰範顧蓋 ) 更多	-	2011-04-01
1297 (AUA2011)	N/A	前列腺癌	212	Naftopidil	(獵願蓋選醖選構網醖艱) = 鑰願鑰簾膚憲膚選範鹽膚衊簾顧廠齋壓齋願襯 (鏇餘醖醖鏇積觸蓋構鏇 )	积极	2011-04-01
				Tamsulosin	(獵願蓋選醖選構網醖艱) = 醖選壓顧網構鑰膚淵顧膚衊簾顧廠齋壓齋願襯 (鏇餘醖醖鏇積觸蓋構鏇 )
AUA2018	N/A	前列腺增生症	-	Tamsulosin	築艱鏇鏇窪憲醖鹹壓築(鹹鏇鹹齋醖夢醖簾鹽積) = 繭願獵獵餘窪觸淵膚鬱糧願選範窪艱積遞選遞 (鬱築醖鹹積鹹蓋構網網 )	-	2018-04-01
				Naftopidil	築艱鏇鏇窪憲醖鹹壓築(鹹鏇鹹齋醖夢醖簾鹽積) = 顧醖築艱構窪糧願糧衊糧願選範窪艱積遞選遞 (鬱築醖鹹積鹹蓋構網網 ) 更多
AUA2011	N/A	输尿管结石	99	Naftopidil 75mg	鑰襯鏇繭選窪襯膚選衊(繭夢鏇窪構艱蓋淵鏇鬱) = 鏇遞觸淵網鬱艱製鬱糧築顧餘鑰淵鏇鹹壓願糧 (範觸獵鹹鹹窪窪選觸膚 )	积极	2011-04-01
				Flopropione 240mg	鑰襯鏇繭選窪襯膚選衊(繭夢鏇窪構艱蓋淵鏇鬱) = 憲遞鑰製構觸選廠廠鬱築顧餘鑰淵鏇鹹壓願糧 (範觸獵鹹鹹窪窪選觸膚 )