佐芬普利钙(Zofenopril Calcium) - 药物靶点：ACE_在研适应症：高血压，心肌梗塞，原发性高血压_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Bifril、Zantipress、Zofenil

+ [12]

靶点

ACE

作用方式

抑制剂

作用机制

ACE抑制剂(血管紧张素转化酶抑制剂)

治疗领域

心血管疾病

在研适应症

高血压心肌梗塞原发性高血压

非在研适应症

心脏衰竭

原研机构

Menarini International Operations Luxembourg SA

在研机构

上海医药工业研究院有限公司Menarini International Operations Luxembourg SA

江苏康缘药业股份有限公司

非在研机构

A. Menarini Industrie Farmaceutiche Riunite Srl

Bristol Myers Squibb Co.

BioSyent, Inc.

权益机构-

最高研发阶段批准上市

首次获批日期

英国 (2008-07-05),

高血压心肌梗塞

最高研发阶段(中国)临床2期

特殊审评-

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结构/序列

分子式C44H46CaN2O8S4

InChIKeyHSCMHYHMIZMAQI-LETVYOFWSA-N

CAS号81938-43-4

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关联

7

项与佐芬普利钙相关的临床试验

NCT05279807

/ Completed临床4期

Interventional Clinical Trial to Assess Efficacy and Safety of the Extemporaneous Combination of Zofenopril Calcium and Amlodipine in Grade 1-2 Hypertensive Patients Versus Each Monotherapy - (MASOLINO Study)

Study to assess the anti-hypertensive efficacy and safety of the extemporaneous combination of Zofenopril 30 mg in combination with Amlodipine 5 mg or AML 10 mg in lowering the sitting diastolic BP after 8 weeks of treatment in patients with uncontrolled BP previously treated with Zofenopril or Amlodipine (5 mg) monotherapies for at least 4 weeks.

开始日期2021-10-15

申办/合作机构

Menarini International Operations Luxembourg SA

NCT05257148

/ Completed临床4期

Open-label, Multicenter, Multinational, Interventional Clinical Trial to Assess Effectiveness and SAfety of the Extemporaneous Combination of Nebivolol and Zofenopril Calcium in Grade 1 to 2 Hypertensive patIents Versus Each mOnotherapy

Open-label, interventional clinical trial to assess effectiveness and safety of the extemporaneous combination of nebivolol and zofenopril calcium in grade 1 to 2 hypertensive patients versus each monotherapy

开始日期2021-05-26

申办/合作机构

Menarini International Operations Luxembourg SA

DRKS00020911

/ Completed临床1期

Bioequivalence of Zofenopril and Nebivolol following their oral co-administration as fixed or extemporaneous combination in healthy volunteers. An open label, randomized, two periods, two sequences, cross-over study - ZOF-NEB-01

开始日期2020-06-18

申办/合作机构

Menarini Ricerche SpA

100 项与佐芬普利钙相关的临床结果

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100 项与佐芬普利钙相关的转化医学

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100 项与佐芬普利钙相关的专利（医药）

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330

项与佐芬普利钙相关的文献（医药）

2025-03-01·Biological Trace Element Research

Mercury Levels in Selected Medicines and Dietary Supplements in Poland

Article

作者: Ahnert, Bożena ; Brodziak-Dopierała, Barbara ; Fischer, Agnieszka

AbstractCurrent trends are promoting youth, beauty, health, and fitness. Individuals often seek out remedies, such as medicines or dietary supplements (DS), to achieve these goals. However, highly processed foods, chronic stress, and environmental pollution contribute to the development of civilization diseases. The aim of this study was to evaluate the mercury (Hg) content in medicines and DS that are available in Poland. A total of 139 preparations were tested (75 drugs, 64 DS). The medicines contained preparations belonging to antibacterial, antiviral, antifungal; analgesic, antipyretic, and anti-inflammatory; heart and blood vessel disease preventatives; respiratory tract infections treatment; diuretics; aiding digestion; supplements; antidiarrhoeals; anti-allergics; anti-rheumatics; antibiotics; and others. The tested dietary supplements had an effect on the following: improve the condition of skin, hair, and nails; vitamins; minerals; probiotics; weight loss; special for women; and others. The Hg content of the samples was determined using atomic absorption spectrometry (AAS). The Hg content of all the preparations varied widely (0.1–57.4 µg/kg), with a median Hg concentration of 1.2 µg/kg. The median Hg concentration for medicines was 0.8 µg/kg, prescription medicines having higher Hg concentrations (0.9 µg/kg) than over-the-counter (OTC) drugs (0.5 µg/kg). For DS, the Hg content was found to be higher than for drugs, at 2.0 µg/kg. The herbal preparations showed the highest Hg content among the individual DS groups (3.4 µg/kg). The Hg concentrations in the tested drug and DS samples did not exceed acceptable standards. However, if multiple pharmaceutical preparations are taken simultaneously over a long period of time, and there is existing environmental exposure, there is a possibility of Hg concentration accumulation and adverse health effects.

2024-11-28·Journal of Medicinal Chemistry

Proline Analogues in Drug Design: Current Trends and Future Prospects

Review

作者: Kubyshkin, Vladimir ; Mykhailiuk, Pavel K.

Proline analogues are versatile chemical building blocks that enable modular construction of small-molecule drugs and pharmaceutical peptides. Over the past 15 years, the FDA has approved over 15 drugs containing proline analogues in their structures, five in the last three years alone (daridorexant, trofinetide, nirmatrelvir, rezafungin, danicopan). This perspective offers an analysis of the most common types of proline analogues currently trending in drug design. We focus on examples of fluoroprolines, α-methylproline, bicyclic proline analogues, and aminoprolines, while also highlighting proline analogues that remain underrepresented. We supplement our analysis with physicochemical information regarding the specific molecular properties of these moieties. Additionally, we discuss several intriguing cases where nonproline residues were replaced with proline analogues as a strategy to eliminate unwanted hydrogen bond donor sites. In conclusion, we present some suggestions for the future exploration of this promising class of molecular entities in drug discovery.

2024-09-01·Hypertension Research

Risk of pneumonia-related hospitalization after initiating angiotensin-converting enzyme inhibitors compared with angiotensin II receptor blockers: a retrospective cohort study using LIFE Study data

Article

作者: Maeda, Megumi ; Fukuda, Haruhisa ; Murata, Fumiko ; Hieda, Michinari ; Uemura, Ryosuke

There is insufficient evidence that angiotensin-converting enzyme inhibitors (ACEIs) can reduce pneumonia by inducing a dry cough that confers a protective effect on the airway. To increase the evidence base on the clinical use of ACEIs for pneumonia prevention, this retrospective cohort study aimed to comparatively examine the risk of pneumonia-related hospitalization between ACEI initiators and angiotensin II receptor blocker (ARB) initiators using claims data from two Japanese municipalities. We identified persons who were newly prescribed any ACEI or ARB as their first antihypertensive agent between April 2016 and March 2020. The Fine-Gray method was applied to a Cox proportional hazards model to estimate the subdistribution hazard ratio (HR) of ACEI use (reference: ARB use) for pneumonia-related hospitalization, with death treated as a competing risk. Sex, age, comorbidities, medications, and pneumococcal immunization were included as covariates. The analysis was conducted on 1421 ACEI initiators and 9040 ARB initiators, and the adjusted subdistribution HR of ACEI use was estimated to be 1.21 (95% confidence interval: 0.89-1.65; P = 0.22). ACEI initiation did not demonstrate any significant preventive effect against pneumonia-related hospitalization relative to ARB initiation. There remains a lack of strong evidence on the protective effects of ACEIs, and further research is needed to ascertain the benefits of their use in preventing pneumonia. We conducted a large-scale retrospective cohort study using real-world healthcare data from a Japanese population. In this study, ACEI initiation did not indicate a significant preventive effect against pneumonia-related hospitalization.

100 项与佐芬普利钙相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03767	佐芬普利钙	C09AA15	DB13166

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
高血压	德国	Menarini International Operations Luxembourg SA	2008-07-05
高血压	法国	Menarini International Operations Luxembourg SA	2008-07-05
高血压	葡萄牙	Menarini International Operations Luxembourg SA	2008-07-05
高血压	爱尔兰	Menarini International Operations Luxembourg SA	2008-07-05
高血压	英国	Menarini International Operations Luxembourg SA	2008-07-05
高血压	荷兰	Menarini International Operations Luxembourg SA	2008-07-05
高血压	意大利	Menarini International Operations Luxembourg SA	2008-07-05
心肌梗塞	意大利	Menarini International Operations Luxembourg SA	2008-07-05
心肌梗塞	德国	Menarini International Operations Luxembourg SA	2008-07-05
心肌梗塞	荷兰	Menarini International Operations Luxembourg SA	2008-07-05
心肌梗塞	葡萄牙	Menarini International Operations Luxembourg SA	2008-07-05
心肌梗塞	爱尔兰	Menarini International Operations Luxembourg SA	2008-07-05
心肌梗塞	法国	Menarini International Operations Luxembourg SA	2008-07-05
心肌梗塞	英国	Menarini International Operations Luxembourg SA	2008-07-05

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
原发性高血压	临床2期	中国	江苏康缘药业股份有限公司	2013-08-30
原发性高血压	临床2期	中国	上海医药工业研究院有限公司	2013-08-30
心脏衰竭	临床2期	欧盟	A. Menarini Industrie Farmaceutiche Riunite Srl	-
高血压	临床2期	美国	Bristol Myers Squibb Co.	-

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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


SMILE (EULAR2017)	N/A	心肌梗塞 hyperuricemic	525	Zofenopril + XOI	(蓋選廠淵簾艱餘衊願壓) = 顧構製網壓醖襯構製醖築構鬱憲獵選壓鏇獵築 (範餘網膚廠衊鏇鹹壓膚 )	积极	2017-06-14
				Zofenopril (Placebo or other ACEIs + XOI)	(蓋選廠淵簾艱餘衊願壓) = 選壓構廠餘網鹹醖觸壓築構鬱憲獵選壓鏇獵築 (範餘網膚廠衊鏇鹹壓膚 )
[PP.35.26] (ESH2015)	N/A	高血压	30	Zofenopril 36.0 mg	網範簾膚觸膚憲遞夢製(蓋艱膚範願築襯廠鏇鑰) = 廠範繭願遞製襯窪觸膚鹽衊糧繭選糧範艱獵繭 (襯簾鹹蓋範衊蓋淵淵蓋 ) 更多	积极	2015-06-01
EUCTR2004-001150-88-IE (SMILE-4, ESH2015)	临床3期	急性心肌梗塞	265	Zofenopril + ASA	壓鏇糧築範艱壓糧壓衊(淵窪簾鏇餘鏇繭淵願願): OR = 0.61 (95% CI, 0.37 ~ 0.99), P-Value = 0.047 更多	积极	2015-06-01
				Ramipril + ASA
EUCTR2004-001150-88-IE (SMILE-4, EASD2012)	临床3期	左心室收缩功能障碍 diabetes mellitus	716	Zofenopril + ASA	淵餘壓齋遞鏇夢鑰構膚(遞鹹蓋網鏇觸鬱遞廠艱) = 範廠糧淵窪衊範網簾淵窪觸顧觸齋製獵衊積鏇 (壓獵齋築壓鏇襯蓋廠獵, 0.31 ~ 1.30)	积极	2012-10-04
				Ramipril + ASA	淵餘壓齋遞鏇夢鑰構膚(遞鹹蓋網鏇觸鬱遞廠艱) = 遞醖鏇膚衊膚願艱醖膚窪觸顧觸齋製獵衊積鏇 (壓獵齋築壓鏇襯蓋廠獵 )
SMILE-4 Study (ESH2012)	N/A	-	716	Zofenopril 60 mg plus ASA	醖鹹鏇鬱範窪窪範壓鹽(鏇網齋顧簾襯選繭鹹齋) = 構窪壓齋觸鏇衊獵範遞製選窪範鏇鹽簾鹹構觸 (蓋觸積製獵淵淵遞鹹襯 )	积极	2012-09-01
				Ramipril 10 mg plus ASA 100 mg	醖鹹鏇鬱範窪窪範壓鹽(鏇網齋顧簾襯選繭鹹齋) = 積淵夢鬱窪淵齋醖窪築製選窪範鏇鹽簾鹹構觸 (蓋觸積製獵淵淵遞鹹襯 )