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)

+ [15]

靶点

ADRA1

作用方式

拮抗剂

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

医疗器械不适术后疼痛输尿管结石病+ [1]

原研机构

F. Hoffmann-La Roche Ltd.

在研机构

非在研机构

权益机构

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/序列

分子式C24H28N2O3

InChIKeyHRRBJVNMSRJFHQ-UHFFFAOYSA-N

CAS号57149-07-2

关联

19

项与萘哌地尔相关的临床试验

JPRN-jRCTs031180176

/ Not yet recruiting临床3期IIT

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

/ CompletedN/A

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

/ CompletedN/A

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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530

项与萘哌地尔相关的文献（医药）

2025-01-01·Crystal Growth & Design

Organic Crystals: Comprehensive Understanding of Proton States of Naftopidil Salts via XPS

作者: Tothadi, Srinu ; Addala, Uma Mahesh ; Dandela, Rambabu

In this study, 18 Naftopidil (NFPD) binary salts were synthesized and then analyzed via XPS.Among these salts, nine known binary salts were initially investigated via SCXRD, where in every binary complex, the carboxylic acid (-COOH) proton is transferred to N of naftopidil.Afterward, these nine naftopidil salts were examined via XPS, where N 1s binding energies of salts showed a significant binding energy shift (2.1 to 2.6 eV) compared to neutral N 1s binding energies of naftopidil.Later, nine novel complexes were synthesized and explored via XPS.Interestingly, these new crystalline materials also manifest considerable N 1s binding energy shifts (1.9 to 2.4 eV) compared to the neutral N 1s binding energies of naftopidil.After a detailed evaluation of XPS exptl. results, new complexes were predicted as naftopidil salts, and SCXRD studies further confirmed these results.Moreover, all these crystalline materials were also characterized by Powder X-ray diffraction (PXRD) and Fourier Transform IR Spectroscopy (FT-IR).Intermol. interactions are further studied by Hirshfeld Surface Anal. (HSA).

2024-12-01·International Journal of Urology

Trends in drug treatment of benign prostatic hyperplasia in Japan based on the National Database Open Data

Article

作者: Sasaki, Kenichi ; Suzuki, Motofumi ; Takahashi, Satoru ; Kume, Haruki ; Nishino, Yoshinori ; Nakamura, Masaki

ObjectiveThis study examined prescription trends for benign prostatic hyperplasia (BPH) drug therapy in Japan over the past decade, focusing on drugs rated as grade A according to Japanese clinical guidelines.MethodsUsing the National Database Open Data, this study analyzed prescription data from the fiscal years of 2014 to 2021, tracking α1‐blockers, 5α‐reductase inhibitors, and phosphodiesterase type 5 inhibitors. We adjusted for demographics and calculated medication costs to determine prescribing patterns and changes in drug utilization.ResultsPrescriptions for α1‐blockers increased from 9898 per 1000 males in 2014 to 12 613 in 2021. Prescriptions for 5α‐reductase inhibitors rose from 1441 per 1000 males in 2014 to 2310 in 2021. Tadalafil prescriptions saw a significant increase, from 900 in 2015 to 2520 in 2021. Despite these increases, the overall market size for BPH drugs decreased from 664 million dollars in 2014 to 279 million dollars in 2021, indicating a shift toward generic medications driven by healthcare policies.ConclusionsAlthough BPH medication prescriptions are increasing, driven by Japan's aging population and clinical guidelines, market dynamics are shifting owing to generic and government price adjustments. This analysis underscores the changing BPH treatment landscape in Japan, highlighting the importance of continuous evaluation of treatment efficacy and cost‐effectiveness in evolving healthcare policies and demographics.

2024-11-15·The Journal of Organic Chemistry

Molybdenum Complex-Catalyzed N-Alkylation of Bulky Primary and Secondary Amines

Article

作者: Khan, Ajmal ; Zhang, Junjie ; Khan, Shahid ; Wang, Lingyun ; Perveen, Shahida

Aliphatic allylic amines are present in a large number of complex and pharmaceutically relevant molecules. The direct amination of allylic electrophiles serves as the most common method toward the preparation of these motifs. However, the use of feedstock reaction components (allyl alcohol and aliphatic amine) in these transformations remains a great challenge. Such a challenge primarily stems from the high Lewis basicity and large steric hindrance of aliphatic amines, in addition to the low reactivity of allylic alcohols. Herein, we report a general solution to these challenges. The developed protocol allows an efficient allylic amination of allyl alcohols with sterically bulky aliphatic amines in the presence of an inexpensive earth-abundant molybdenum complex. This simple and economic protocol also enables regioselective branched amination; the practicality of the reaction was shown in an efficient, scaled-up synthesis of several drugs.

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
神经性膀胱功能障碍	临床前	日本	Asahi Kasei Corp.	-
医疗器械不适	药物发现	韩国	Dong-A ST Co., Ltd.	2014-05-01
输尿管结石病	药物发现	韩国	Dong-A ST Co., Ltd.	2014-05-01
术后疼痛	药物发现	韩国	Dong-A ST Co., Ltd.	2013-10-25

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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	输尿管结石	99	Naftopidil 75mg	鹽憲淵餘簾壓構積繭觸(餘窪膚廠獵鬱艱鹽憲鏇) = 觸壓膚築顧壓構獵醖廠糧網獵餘醖廠製積醖網 (遞觸遞積範積艱艱築襯 )	积极	2011-04-01
				Flopropione 240mg	鹽憲淵餘簾壓構積繭觸(餘窪膚廠獵鬱艱鹽憲鏇) = 衊窪鹽鬱願夢鹽襯艱獵糧網獵餘醖廠製積醖網 (遞觸遞積範積艱艱築襯 )
1297 (AUA2011)	N/A	前列腺癌	212	Naftopidil	(餘鬱齋夢顧願製艱壓獵) = 繭鹽醖鏇膚齋醖範觸壓夢願選鑰鬱範鏇鹽遞壓 (艱餘鏇範齋製觸壓簾蓋 )	积极	2011-04-01
				Tamsulosin	(餘鬱齋夢顧願製艱壓獵) = 淵齋願獵構鏇窪範製簾夢願選鑰鬱範鏇鹽遞壓 (艱餘鏇範齋製觸壓簾蓋 )