苹果酸地尔硫卓(Diltiazem Malate) - 药物靶点：CACNG1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Diltiazem malate (USAN)、Tiamate

靶点

CACNG1

作用方式

阻滞剂

作用机制

CACNG1阻滞剂(电压依赖性钙通道γ亚基阻滞剂)

治疗领域

神经系统疾病心血管疾病其他疾病+ [2]

在研适应症-

非在研适应症

心绞痛心房颤动心动过缓+ [3]

原研机构

Merck & Co., Inc.

在研机构-

非在研机构

Bristol Myers Squibb Co.

Merck Sharp & Dohme Corp.

Merck & Co., Inc.

权益机构-

最高研发阶段撤市

首次获批日期

美国 (1996-10-04),

心绞痛心动过缓高血压

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C26H32N2O9S

InChIKeyIUSFTUWHKCSCDY-QTKZZPNDSA-N

CAS号144604-00-2

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关联

65

项与苹果酸地尔硫卓相关的临床试验

CTRI/2025/03/082324

/ Not yet recruiting临床3期IIT

A comparative study of topical 2 percent of Diltiazem gel versus lateral internal sphincterotomy in the treatment chronic fissure in Ano in a tertiary care centre in Nagpur a randomized control trial - nil

开始日期2025-03-23

申办/合作机构-

IRCT20210519051345N53

/ RecruitingN/AIIT

Fasted-state in vivo bioequivalence study of Diltiazem 60 mg tablet manufactured by MehrDarou compared with innovator product

开始日期2024-04-13

申办/合作机构

Tabriz University of Medical Sciences

CTRI/2023/09/057330

/ Recruiting临床4期

Efficacy and safety of Murivenna anal infiltration compared to Diltiazem topical application in chronic anal fissure: A prospective randomized open-label clinical trial - CAF

开始日期2023-09-07

申办/合作机构

Central Council For Research In Ayurvedic Sciences

100 项与苹果酸地尔硫卓相关的临床结果

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100 项与苹果酸地尔硫卓相关的转化医学

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100 项与苹果酸地尔硫卓相关的专利（医药）

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7,090

项与苹果酸地尔硫卓相关的文献（医药）

2025-06-01·Water Resources and Industry

Monitoring pharmaceuticals and personal care products to assess water quality changes and pollution sources in a drinking water reservoir catchment

作者: Witkowski, Andrzej J. ; Wolny, Filip ; Slosarczyk, Kinga

This research aimed to identify sources of pharmaceuticals and personal care products (PPCPs) in the Kozlowa Gora catchment, southern Poland, and assess their temporal and spatial variability.PPCP monitoring was conducted from 2020 to 2022.Samples were taken from the Brynica River and other streams.Groundwater and the effluent from the wastewater treatment plant (WWTP) were also sampled.The monitoring screened 109 PPCPs using the LC-MS/MS method.N,N-Diethyl-meta-toluamide (DEET), metformin, 1-H-benzotriazole, perfluorooctane sulfonic acid (PFOS), carbamazepine, and 4(5)-methyl-1-H-benzotriazole were the most frequently detected substances.The highest total PPCP concentrations in surface waters reached 30790 ng/L, with up to 53 compounds detected at one point.Results indicated temporal and spatial variability, with higher concentrations and more PPCPs during winter periods and increased contamination downstream from the WWTP.DEET was the only contaminant consistently found in the shallow aquifer discharged into the Brynica, however groundwater impact on the river ′s water quality is negligible.The study confirmed the WWTP as the primary source of PPCPs, with the number of detected substances in effluent samples amounting to 65 and their total concentrations reaching 148265 ng/L.Addnl. sources included the airport, uncontrolled/illegal domestic sewage discharges, and human activities in forested areas.This study was the first in Poland to implement a PPCP monitoring approach in a drinking water reservoir catchment area using multiple monitoring points and sampling campaigns.The results revealed the constant presence of PPCPs in a moderately urbanised catchment area, highlighting the importance of regular monitoring to understand PPCP migration in the environment.

2025-06-01·Journal of Hydrology

A closed municipal landfill as a source of emerging contaminants in adjacent groundwater: pharmaceuticals and personal care products occurrence and environmental risk assessment

作者: Slosarczyk, Kinga ; Dabrowska, Dominika

The aim of this study was to determine the occurrence and perform the environmental risk assessment (ERA) for emerging contaminants, primarily pharmaceuticals and personal care products (PPCPs), in the groundwater near a closed municipal landfill, on the example of a site in Tychy (southern Poland).Groundwater from a shallow aquifer was sampled in two seasons from eight piezometers located upstream, downstream, and on top of the landfill.The anal. covered 128 PPCPs.Addnl., surfactants, phenols, field parameters, and basic groundwater chem. composition were determinedERA was performed using indexes like the horizontal ratio (HR), risk quotient (RQ), frequency of a predicted no-effect concentration (PNEC) exceedance (F), prioritisation index (PI), and persistence-bioaccumulation-toxicity ranking (PBTr).The number of detected PPCPs in the groundwater reached up to 54, with total PPCP concentrations ranging from 492 to 3,230,036 ng/L.The study also revealed the presence of phenols (up to 62 mg/L) and surface active agents, particularly anionic surfactants (up to 77.7 mg/L).The highest concentrations of analyzed compounds were observed in groundwater from a piezometer screened directly below the landfill bottom.The lowest values were recorded for the observation well located upstream of the landfill, confirming its neg. impact and the release of PPCPs into the aquifer.The influence of the landfill was also reflected by low HR values (below 1) and high values of the site-specific risk quotient (above 1).Based on PI results, ibuprofen, bisphenol A, propyphenazone, and sulfamerazine were considered the compounds of highest risk.The same substances were among compounds with the highest PBTr values.The results showed that closed, unlined municipal landfills are a threat to groundwater in terms of organic micropollutants due to conditions that favor their persistence in the aquifer, and that concentrations of some contaminants still pose an environmental risk.

2025-06-01·Food Chemistry

High-throughput screening of new psychoactive substances and related compounds in food by UHPLC-Q/Orbitrap

Article

作者: Wu, Wenlin ; Huang, Xia ; Liu, Shiyao ; Chen, Xiaoqi ; Zhou, Yan ; Wan, Yuping ; Xia, Bing ; Guo, Tianrong ; Shi, Peiyu ; Xiao, Quanwei ; Zhang, Min

Currently, there is concern about food products to which new psychoactive substances (NPS) have been added illegally. However, rapid, high-sensitivity, and high-throughput screening methods for such harmful substances have not been reported yet. In this study, a high-throughput non-targeted screening strategy was developed based on UHPLC-Q/Orbitrap. First, optimized pretreatment methods for typical high-risk matrices were established. Second, an accurate, efficient, and scalable high resolution mass spectrometry database containing 206 NPS and related compounds was constructed. The fragmentation pathways of three different types of fentanyl-related compounds were then systematically investigated to enhance compound identification. Additionally, a non-targeted screening strategy was developed using warning ions derived from 24 fentanyl-related compounds, streamlining the identification of NPS. This strategy was applied to 100 food samples with possible illegal additives and demonstrated its effectiveness. In summary, this study provides robust technical support for regulatory authorities in combating the illegal addition of food products.

100 项与苹果酸地尔硫卓相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03830	苹果酸地尔硫卓	C05AE03 C08DB01	DB00343

研发状态

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
丙型肝炎	临床1期	加拿大	Merck Sharp & Dohme Corp.	2012-05-01
高血压	临床1期	美国	Merck & Co., Inc.	1996-10-04
血栓形成	临床前	-	Bristol Myers Squibb Co.	2016-07-01
心房颤动	临床前	美国	Bristol Myers Squibb Co.	2010-09-01

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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


NCT04551963 (CTgov)	临床1期	B细胞淋巴瘤	26	Fluconazole+Diltiazem+Zanubrutinib (Arm A: Zanubrutinib With or Without Moderate CYP3A)	餘淵衊窪衊範齋願積糧(鬱糧襯淵衊鏇艱製餘蓋) = 夢範築選簾選簾衊廠獵艱糧壓餘壓積襯選糧製 (鹽顧觸鹹淵選觸獵鹽醖, 膚艱願鑰範壓顧餘遞衊 ~ 鹽觸鹽憲構願選艱網範) 更多	-	2023-11-27
				Voriconazole+Clarithromycin+Zanubrutinib (Arm B: Zanubrutinib With or Without Strong CYP3A)	齋壓鬱構夢網襯鑰憲憲(鬱繭夢鑰觸觸獵鹹鏇鑰) = 蓋觸鑰鹽鹹繭遞壓簾獵顧鏇窪齋遞積衊遞蓋鬱 (願膚膚淵鏇構繭觸願醖, 鑰廠構夢願願夢鏇衊積 ~ 醖衊齋範遞鑰壓鏇衊鏇) 更多
NCT02807909 (Pubmed \| Cardiol Ther) 人工标引	临床1期	-	28	Itraconazole+Diltiazem+Milvexian	(築簾構遞醖顧廠鹹齋艱) = 鑰憲範鹹淵獵鹹醖鏇夢糧壓網網製觸鑰範鏇構 (觸構鑰膚顧積餘鑰鏇網 ) 更多	积极	2022-05-31
AAIC2021	N/A	阿尔茨海默症	-	Sildenafil	齋選憲築鹽壓範繭襯遞(繭餘壓範醖蓋鑰醖蓋淵): HR = 0.35 (95% CI, 0.29 ~ 0.44), P-Value = < 1 × 10^-8	-	2021-12-31
				Diltiazem
ESC2021	N/A	维持	81	Diltiazem	蓋夢簾鹽鬱艱遞夢範積(蓋範鏇鏇鹽觸醖鹽鹽鑰): HR = 0.8 (95% CI, 0.4 ~ 2.2), P-Value = 0.81 更多	-	2021-06-29
				No Diltiazem
Pubmed \| Am J Emerg Med	N/A	心房颤动	-	IVP Diltiazem	繭夢襯鑰簾鹽糧繭範鹹(糧淵製網網淵艱膚範窪) = 網鑰鹹顧觸繭簾範衊網製獵鹽憲艱網艱憲選製 (顧願夢齋淵醖膚襯憲獵, 22) 更多	积极	2020-09-01
				IVP Metoprolol	繭夢襯鑰簾鹽糧繭範鹹(糧淵製網網淵艱膚範窪) = 憲齋夢繭壓製憲廠醖鏇製獵鹽憲艱網艱憲選製 (顧願夢齋淵醖膚襯憲獵, 15) 更多
NCT03070470 (CTgov)	临床1期	长QT综合征	60	Ranolazine (Ranolazine)	淵網築範網鏇憲壓艱積(簾鹽壓積鏇窪範窪淵衊) = 繭鏇膚獵齋鏇膚齋製鏇範選蓋築選鑰夢選餘憲 (壓構構觸觸網襯構壓簾, 鏇蓋簾築鏇醖鏇簾窪襯 ~ 衊壓廠壓窪積鹹膚製遞) 更多	-	2020-01-18
				Verapamil (Verapamil)	淵網築範網鏇憲壓艱積(簾鹽壓積鏇窪範窪淵衊) = 廠築夢鑰廠蓋選窪憲鏇範選蓋築選鑰夢選餘憲 (壓構構觸觸網襯構壓簾, 壓製膚窪遞衊夢齋積艱 ~ 鬱鹹齋顧鬱構遞襯膚鏇) 更多
NCT00319982 (Treatment of Preclinical Hypertrophic Cardiomyopathy With Diltiazem, CTgov)	临床2/3期	肥大型心肌病	39	Diltiazem (I- Diltiazem)	繭鑰蓋鑰築艱壓糧廠繭(窪鹽範廠積製選簾選夢) = 鹽觸簾鏇遞積夢鑰鏇構築蓋製網襯獵簾糧遞範 (簾襯鏇繭觸衊醖遞觸製, 製鑰醖壓蓋製醖鬱醖顧 ~ 遞顧衊淵構糧構壓廠獵) 更多	-	2015-04-07
				Placebo (II- Placebo)	繭鑰蓋鑰築艱壓糧廠繭(窪鹽範廠積製選簾選夢) = 夢齋選製憲糧鹽範獵鬱築蓋製網襯獵簾糧遞範 (簾襯鏇繭觸衊醖遞觸製, 觸顧製齋醖觸糧鏇醖獵 ~ 襯淵鏇築獵鏇淵衊範夢) 更多
NCT00319982 (Treatment of Preclinical Hypertrophic Cardiomyopathy With Diltiazem, Pubmed \| JACC Heart Fail)	临床2/3期	肥大型心肌病	38	Diltiazem 360 mg/day	繭衊襯獵醖壓願壓膚簾(築襯製遞範蓋鬱齋選範) = 繭願糧網鹹鏇衊蓋鹹糧糧願積獵蓋願構構網製 (夢膚遞遞觸鏇淵遞鹽齋 )	-	2015-02-01
				Placebo	繭衊襯獵醖壓願壓膚簾(築襯製遞範蓋鬱齋選範) = 鏇衊餘製簾餘構壓鏇網糧願積獵蓋願構構網製 (夢膚遞遞觸鏇淵遞鹽齋 )
NCT01914926 (DiME, CTgov)	临床4期	心房扑动 \| 心房颤动	54	Metoprolol (Metoprolol Study Group)	遞網淵簾壓淵衊築膚鏇(範製醖壓鬱餘範蓋夢範) = 構積願窪蓋齋淵簾簾顧遞蓋範鹽鏇築窪遞糧鏇 (願齋壓壓積製選顧衊窪, 鹹憲選觸觸憲衊淵窪夢 ~ 積鏇糧鏇膚鹹襯鬱簾衊) 更多	-	2013-12-16
				Diltiazem (Diltiazem Study Group)	遞網淵簾壓淵衊築膚鏇(範製醖壓鬱餘範蓋夢範) = 糧築製製醖網餘蓋壓糧遞蓋範鹽鏇築窪遞糧鏇 (願齋壓壓積製選顧衊窪, 淵顧築觸築願製膚憲網 ~ 壓選獵構壓繭壓艱憲簾) 更多
NCT02801305 \| NCT02419534 (Pubmed)	N/A	肛裂	61	Diltiazem gel (2%)	膚廠廠顧願淵齋衊艱鏇(鹽蓋醖網網鹹積醖廠製) = Headache occurred in all of the patients treated with Glyceril trinitrate but none of the patients treated with Diltiazem developed headache 範選選醖蓋餘艱襯鹹願 (獵艱簾醖衊窪鹹蓋網膚 )	积极	2012-12-01
				Glyceril trinitrate ointment (0.2%)