阿折地平(Azelnidipine) - 药物靶点：L-type calcium channel_在研适应症：高血压_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Azelnidipine (JP17/INN)

+ [5]

靶点

L-type calcium channel

作用机制

L-type calcium channel阻滞剂(L-型电压门控性钙通道家族阻滞剂)

治疗领域

心血管疾病

在研适应症

高血压

非在研适应症-

原研机构

Daiichi Sankyo Co., Ltd.

在研机构

Daiichi Sankyo Co., Ltd.

连云港润众制药有限公司

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (2003-01-31),

高血压

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C33H34N4O6

InChIKeyZKFQEACEUNWPMT-UHFFFAOYSA-N

CAS号123524-52-7

关联

34

项与阿折地平相关的临床试验

CTRI/2024/08/072999

/ RecruitingN/AIIT

Comparison of the Efficacy of 24 Hour BP Control of Azelnidipine, Amlodipine and Cilnidipine in Mild to Moderate Essential Hypertension – a Prospective Multi-centric Parallel Arm Real-world Study (AMCILAZ-EH Study) - AMCILAZ-EH Study

开始日期2024-09-04

申办/合作机构-

CTRI/2024/08/071803

/ Not yet recruitingN/AIIT

Post-approval, case control analyses to assess clinical safety and effectiveness of Azelnidipine and Cilnidipine as initial -addon therapy in management of T2DM with HTN - HYDIAZ

开始日期2024-08-13

申办/合作机构-

CTRI/2024/07/071061

/ Not yet recruitingN/A

Post-approval, observational study to assess clinical safety and effectiveness of Azelnidipine and Telmisartan in management of Diabetic HTN - TELAZ

开始日期2024-08-02

申办/合作机构

Torrent Pharmaceuticals Ltd.

100 项与阿折地平相关的临床结果

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100 项与阿折地平相关的转化医学

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100 项与阿折地平相关的专利（医药）

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254

项与阿折地平相关的文献（医药）

2024-05-01·Luminescence

Selective detection of azelnidipine in pharmaceuticals via carbon dot mediated spectrofluorimetric method: A green approach

Article

作者: Shah, Shailesh A ; Patil, Pravin O ; Joshi, Shrikant V ; Patel, Paresh N ; Patel, Hetal P ; Kalyankar, Gajanan G ; Maulvi, Furqan A ; Shah, Dinesh R ; Pillai, Arya J ; Merchant, Jesika G ; Lodha, Sandesh R ; Gore, Anil H

AbstractA spectrofluorimetric method using fluorescent carbon dots (CDs) was developed for the selective detection of azelnidipine (AZEL) pharmaceutical in the presence of other drugs. In this study, N‐doped CDs (N‐CDs) were synthesized through a single‐step hydrothermal process, using citric acid and urea as precursor materials. The prepared N‐CDs showed a highly intense blue fluorescence emission at 447 nm, with a photoluminescence quantum yield of ~21.15% and a fluorescence lifetime of 0.47 ns. The N‐CDs showed selective fluorescence quenching in the presence of all three antihypertensive drugs, which was used as a successful detection platform for the analysis of AZEL. The photophysical properties, UV–vis light absorbance, fluorescence emission, and lifetime measurements support the interaction between N‐CDs and AZEL, leading to fluorescence quenching of N‐CDs as a result of ground‐state complex formation followed by a static fluorescence quenching phenomenon. The detection platform showed linearity in the range 10–200 μg/ml (R2 = 0.9837). The developed method was effectively utilized for the quantitative analysis of AZEL in commercially available pharmaceutical tablets, yielding results that closely align with those obtained from the standard method (UV spectroscopy). With a score of 0.76 on the ‘Analytical GREEnness (AGREE)’ scale, the developed analytical method, incorporating 12 distinct green analytical chemistry components, stands out as an important technique for estimating AZEL.

2024-04-01·Drug Metabolism and Pharmacokinetics

Physiologically based pharmacokinetic modeling to predict the clinical effect of azole antifungal agents as CYP3A inhibitors on azelnidipine pharmacokinetics

Article

作者: Watanabe, Akiko ; Kotsuma, Masakatsu

In this study, a physiologically based pharmacokinetic (PBPK) model of the cytochrome P450 3A (CYP3A) substrate azelnidipine was developed using in vitro and clinical data to predict the effects of azole antifungals on azelnidipine pharmacokinetics. Modeling and simulations were conducted using the Simcyp™ PBPK simulator. The azelnidipine model consisted of a full PBPK model and a first-order absorption model. CYP3A was assumed as the only azelnidipine elimination route, and CYP3A clearance was optimized using the pharmacokinetic profile of single-dose 5-mg azelnidipine in healthy participants. The model reproduced the results of a clinical drug-drug interaction study and met validation criteria. PBPK model simulations using azole antifungals (itraconazole, voriconazole, posaconazole, fluconazole, fosfluconazole) and azelnidipine or midazolam (CYP3A index substrate) were performed. Increases in the simulated area under the plasma concentration-time curve from time zero extrapolated to infinity with inhibitors were comparable between azelnidipine (range, 2.11-6.47) and midazolam (range, 2.26-9.22), demonstrating that azelnidipine is a sensitive CYP3A substrate. Increased azelnidipine plasma concentrations are expected when co-administered with azole antifungals, potentially affecting azelnidipine safety. These findings support the avoidance of azole antifungals in patients taking azelnidipine and demonstrate the utility of PBPK modeling to inform appropriate drug use.

2024-04-01·BMJ Case Reports

Acute quadruple extremity compartment syndrome due to angio-oedema after polypharmacy overdose including olmesartan medoxomil, telmisartan and vildagliptin

Article

作者: Kono, Yumi ; Fujii, Motoki ; Hayashi, Yoshiro ; Takimoto, Kohei

This case report describes a rare manifestation of acute compartment syndrome (ACS) involving all four extremities, precipitated by angio-oedema in a middle-aged woman who consumed an overdose of multiple medications: nifedipine, azelnidipine, amlodipine besylate, olmesartan medoxomil, telmisartan, esaxerenone and vildagliptin. She presented with haemodynamic instability, necessitating intubation. Despite stabilising haemodynamic parameters within 24 hours, she manifested escalating extremity oedema. At 52 hours after ingestion, mottled skin was observed, along with necrotic alterations in the swollen hands and compartment pressures exceeding 30 mm Hg in all extremities. ACS was diagnosed, leading to fasciotomies. The aetiology is postulated to be drug-induced angio-oedema, possibly intensified by the concurrent overdose of olmesartan medoxomil, telmisartan and vildagliptin, each of which has a risk of angio-oedema even at standard dosages. This scenario is a very rare case caused by drug-induced angio-oedema, which underscores the importance of vigilant monitoring to detect ACS in patients with progressing limb oedema.

100 项与阿折地平相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01145	阿折地平	C08CA	DB09230

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
高血压	日本	Daiichi Sankyo Co., Ltd.	2003-01-31

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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


GUARD study (ESH2012)	N/A	-	-	Olmesartan + Azelnidipine	(憲構製網窪壓糧鹹顧憲) = 艱壓憲獵製積鏇鹽襯積淵構顧壓獵鏇鬱鹽餘選 (鑰衊餘選積鏇積窪鏇網 )	积极	2012-09-01
				Olmesartan + Trichlormethiazide	(憲構製網窪壓糧鹹顧憲) = 淵餘壓艱醖鏇衊鏇夢構淵構顧壓獵鏇鬱鹽餘選 (鑰衊餘選積鏇積窪鏇網 )
555 (ESH2012)	N/A	高血压	-	Amlodipine	(鹽淵蓋鏇壓淵艱蓋網構) = 窪夢淵網壓願構廠壓簾顧齋鬱遞糧積網願淵鬱 (憲製構範鏇顧鑰觸顧壓 ) 更多	积极	2012-09-01
				Azelnidipine	(鹽淵蓋鏇壓淵艱蓋網構) = 範獵遞艱壓鹽觸鑰廠鬱顧齋鬱遞糧積網願淵鬱 (憲製構範鏇顧鑰觸顧壓 ) 更多
201 (ESH2012)	N/A	高血压	-	Azelnidipine	(範網鑰積夢願鏇顧襯構) = 齋衊獵觸網鹹淵壓遞構艱壓襯餘窪願憲築艱襯 (膚憲鏇憲鹽壓襯範廠蓋 ) 更多	积极	2012-09-01
				Amlodipine	(範網鑰積夢願鏇顧襯構) = 艱範膚壓餘製製膚鹽鹹艱壓襯餘窪願憲築艱襯 (膚憲鏇憲鹽壓襯範廠蓋 ) 更多
PP.1.32 (ESH2010)	N/A	功能障碍	-	Azelnidipine 0.3 mg/kg	醖鹹顧艱鏇襯簾願窪鏇(範齋觸鬱觸選繭憲蓋築) = 糧顧製範觸糧憲蓋鹽鑰鹹積壓願選餘願廠鏇觸 (遞鑰鹹網顧鹽製膚窪壓, 5) 更多	积极	2010-06-01
				Labetalol 3 mg/kg	醖鹹顧艱鏇襯簾願窪鏇(範齋觸鬱觸選繭憲蓋築) = 夢鹽鹽願襯齋構製網窪鹹積壓願選餘願廠鏇觸 (遞鑰鹹網顧鹽製膚窪壓, 4) 更多