更新于：2024-05-14
Sacubitril/Valsartan
沙库巴曲缬沙坦钠
更新于：2024-05-14
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2015-07-07), |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、优先审评 (中国) |
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结构
分子式C48H61N6NaO9 |
InChIKeyBHNNEXLQFVQGSE-LWRBNZNASA-N |
CAS号936623-90-4 |
关联
325
项与 沙库巴曲缬沙坦钠 相关的临床试验沙库巴曲缬沙坦钠片在中国成年健康受试者中的一项单中心、随机、开放、空腹和餐后单次给药、两制剂、两序列、四周期、完全重复交叉生物等效性研究
A Bioequivalence Study of Sacubitril 97 mg and Valsartan 103 mg Film-coated Tablets Relative to Entresto 97 mg/103 mg Film-coated Tablets in Healthy Thai Volunteers Under Fasting Condition
Effect of Sacubitril-Valsartan versus angiotensin-converting enzyme inhibitors (ACEI) and angiotensin receptor blocker (ARB) on left ventricular ejection fraction in patient with heart failure: a double-blind randomized clinical trial
100 项与 沙库巴曲缬沙坦钠 相关的临床结果
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100 项与 沙库巴曲缬沙坦钠 相关的转化医学
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100 项与 沙库巴曲缬沙坦钠 相关的专利（医药）
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425
项与 沙库巴曲缬沙坦钠 相关的文献（医药）2024-02-01Neuroscience Letters
The neuroprotective effect of LCZ696 on methamphetamine-induced cognitive impairment in mice
Article
作者: Liu, Yu ; Qian, Liyin ; Li, Xiaofang ; Shen, Yao ; Luo, Hu ; Si, Zizhen ; Yu, Zhaoying ; Lin, Shujun ; Ruan, Yuer ; Gong, Xinshuang
OBJECTIVE:
Methamphetamine (METH) exposure commonly causes cognitive impairment. An angiotensin II receptor/neprilysin inhibitor (ARNI), LCZ696 has been demonstrated to inhibit inflammation, oxidative stress and apoptosis. The present study was designed to examine the effect of LCZ696 on METH-induced cognitive impairment and the underlying mechanism.
METHODS:
Following daily treatment of either saline or METH (5 mg/kg) for 5 consecutive days, the cognitive function was tested using the Y-maze and the Novel Object Recognition (NOR) in Experiment 1. In Experiment 2, mice were initially treated with saline or LCZ696 (60 mg/kg) for 9 consecutive days, followed by LCZ696, METH or saline for 5 days. Cognitive testing was carried out as Experiment 1. In Experiment 3, SH-SY5Y cells were treated with either METH (2.5 Mm) or ddH2O for 12 h. The apoptosis and reactive oxygen species (ROS) level of SH-SY5Y were examined. In Experiment 4, SH-SY5Y cells were pretreated with either ddH2O or LCZ696 (70um) for 30 min, followed by ddH2O or METH treatment for 12 h. Nrf2 and HO-1 protein expression was examined in the ventral tegemental area (VTA) of all the animals and SH-SY5Y cells.
RESULTS:
LCZ696 significantly improved METH-induced cognitive impairment, in conjunction with decreased apoptosis and ROS levels in VTA of METH-treated mice and SH-SY5Y cells. METH significantly decreased Nrf2 and HO-1 protein expression in VTA of mice and SH-SY5Y cells, which was reversed by LCZ696 treatment.
CONCLUSION:
LCZ696 yields a neuroprotective effect against METH-induced cognitive dysfunction via the Nrf2/HO-1 signaling pathway.
2024-01-25Zhen ci yan jiu = Acupuncture research
Effect of electroacupuncture on ventricular structure and function in rats with myocardial ischemia-reperfusion injury.
Article
作者: Bai, Hua ; Zhang, Hong-Ru ; Xia, Ming-Hui ; Xu, Sen-Lei ; Wu, Shuang ; Gu, Yi-Huang ; Ding, Ya-Ping ; Liu, Qiong-Qiong ; Jiang, Wen
OBJECTIVES:
To observe the effect of electroacupuncture (EA) on changes of ventricular structure and function in rats with myocardial ischemia-reperfusion injury (MIRI), so as to explore its potential mechanisms underlying improvement of ventricular remodeling after MIRI.
METHODS:
Forty male SD rats were randomly divided into 4 groups：sham operation group, model group, EA group and medication (sacubactril valsartan, LCZ696) group, with 10 rats in each group. The MIRI model was established by ligation of the left anterior descending coronary artery and reperfusion. EA (2 Hz/100 Hz, 2 mA) was applied to bilateral "Neiguan" (PC6) for 20 min, once every other day for 21 d. Rats of the medication group received gavage of LCZ696 (60 mg·kg-1·d-1). After the intervention, echocardiography was used to detect the ejection fraction (EF) and fractional shortening (FS) of the left ventricle, and the contents of serum tumor necrosis factor-α(TNF-α), vascular cell adhesion molecule-1(VCAM-1) and intercellular cell adhesion molecule-1(ICAM-1) were assayed by enzyme-linked immunosorbent assay. The pathological changes of myocardial tissue were observed after HE staining. The Masson staining was used to evaluate the myocardial collagen deposition and myocardial fibrosis. The mRNA expression levels of collagen Ⅰ and Ⅲ and connective tissue growth factor (CTGF) in the myocardial tissue were detected by quantitative real-time PCR, and the expression levels of IL-1β and IL-18 were detected by Western blot.
RESULTS:
In contrast to the sham operation group, the EF and FS levels of the left ventricle were ob-viously decreased (P<0.001), while the contents of serum TNF-α, VCAM-1 and ICAM-1, the proportion of myocardial fibrosis area, the mRNA expression levels of myocardial collagen Ⅰ, collagen Ⅲ and CTGF, the expression levels of IL-1β and IL-18 were significantly increased (P<0.001, P<0.000 1, P<0.05, P<0.01) in the model group. Compared with the model group, the EF and FS levels were remarkably increased (P<0.01), whereas the contents of serum TNF-α, VCAM-1 and ICAM-1, the proportion of myocardial fibrosis area, the mRNA expression levels of myocardial collagen Ⅰ, collagen Ⅲ and CTGF, and the expression levels of IL-1β and IL-18 were significantly down-regulated (P<0.001, P<0.01, P<0.05) in both the medication and EA groups. No significant differences were found between the EA and medication groups in all the indexes mentioned above.
CONCLUSIONS:
EA can improve the left-ventricular fibrosis and function, delay or reverse ventricular remodeling in MIRI rats, which may be related to its functions in down-regulating myocardial inflammatory response and mRNA expression levels of myocardial collagen Ⅰ, collagen Ⅲ and CTGF.
2024-01-01European review for medical and pharmacological sciences
Knowledge domain and emerging trends in sacubitril/valsartan study from 2008 to 2023 - a visualized conclusive analysis based on novel scientometric tools.
Article
作者: Rong, J-C ; Zhao, X-C ; Huang, L ; Lu, B-H
OBJECTIVE:
This study aimed to determine the evolution of sacubitril-valsartan research and analyze the publications quantitatively and qualitatively.
MATERIALS AND METHODS:
We used the bibliometric method and a combination of CiteSpace_6.1.6 and VOSviewer_1.6.18 to identify top authors, countries, institutions, co-cited articles, co-cited journals, keywords, and trends. This study prioritized key aspects in the existing global research on Entresto (Sacubitril/Valsartan) to assess our depth of knowledge in this field and identify potential insights. The objective was to generate a reference for the utilization of the "angiotensin receptor-neprilysin inhibitor" (ARNI).
RESULTS:
From 2008 to 2022, citations of sacubitril-valsartan showed an upward trend. VOSviewer keyword analysis of 3,408 publications identified 624 keywords and divided them into seven different clusters. The clustered network was constructed based on 1,191 references cited by 3,408 publications that met the terms, where the clustered network of sacubitril-valsartan was presented. These publications can be regarded as fundamental to Entresto's research. Analysis of co-cited reference clusters showed that other than Entresto's novel application in other diseases, the new combination with other medication or mechanical assistance therapies against heart failure was Entresto's latest focus. Analysis of citation bursts showed that the rank of the top 25 keywords, according to the chronological sequence, marked Entresto's research entering a new era of exploring the extended application in other diseases and novel combinations with other diverse therapies.
CONCLUSIONS:
We found that emerging new mechanisms in sacubitril-valsartan therapy intended for more targets in the pathogenesis of specific diseases will be the focus of further studies.
100 项与 沙库巴曲缬沙坦钠 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 心脏衰竭 | 批准上市 | 加拿大 更多 | |
| 慢性心力衰竭 | 批准上市 | 冰岛 更多 | |
| 射血分数降低的心力衰竭 | 临床3期 | - | |
| 射血分数保留型心力衰竭 | 终止 | 日本 更多 | |
| 急性心肌梗塞 | 终止 | - |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 4,796 | 構顧鏇糧壓觸遞蓋範觸(築顧顧簾艱築齋衊憲範) = 選遞鏇淵廠顧齋鹹簾鹽 構製壓淵簾積簾餘觸選 (夢鏇憲壓鬱鹹憲範網衊 ) 更多 | 积极 | 2024-04-12 | |||
临床2/3期 | 375 | 艱簾壓窪構簾顧遞鬱廠(蓋範窪齋憲鹽鏇壓襯膚) = 鏇糧衊窪蓋鏇糧範糧觸 醖構顧憲願艱壓膚齋觸 (築艱鬱鏇鏇鏇選蓋餘糧 ) | 积极 | 2024-04-12 | |||
艱簾壓窪構簾顧遞鬱廠(蓋範窪齋憲鹽鏇壓襯膚) = 繭鹹遞廠糧繭願艱鬱夢 醖構顧憲願艱壓膚齋觸 (築艱鬱鏇鏇鏇選蓋餘糧 ) | |||||||
临床3期 | 8,399 | (chronic heart failure) | 遞鹽醖窪製範範積壓蓋(壓壓鹽憲獵選選簾鏇餘) = 築簾繭衊觸範鏇鏇簾壓 鹽壓蓋壓構築鏇窪醖繭 (夢製醖繭繭淵積壓鏇繭 ) 更多 | 积极 | 2024-04-12 | ||
临床3期 | - | 齋繭衊醖鹹範鬱窪廠壓(築選餘鏇膚廠夢夢廠衊) = Sacubitril/valsartan increased symptomatic hypotension (risk ratio: 1.35; 95% CI: 1.05-1.72) 窪觸鹹遞繭窪廠膚鹽糧 (壓憲繭獵遞襯窪糧遞齋 ) 更多 | - | 2024-03-26 | |||
Control therapy (Enalapril or Valsartan) | |||||||
临床3期 | - | 顧鹹鏇構鏇糧顧選襯鹹(醖繭網齋窪構遞鹽願選) = Of 4,796 patients in PARAGON-HF, 637 (13%) experienced hypotension, more frequently in the sacubitril/valsartan arm (p<0.001). Following documented hypotension, patients had higher risk of CV death and total HF hospitalizations (adjusted RR 1.63; CI 1.27-2.09; p<0.001) and all-cause death (adjusted HR 1.62; CI 1.28-2.05; p<0.001). LVEF modified the association between sacubitril/valsartan and risk of hypotension (Pinteraction=0.019) such that patients with LVEF≥60% experienced substantially higher treatment-related risks of hypotension. 窪鹽鏇憲齋艱壓觸顧範 (鑰簾憲鹽獵蓋齋遞構醖 ) | 不佳 | 2024-03-01 | |||
临床3期 | 27 | LCZ696 matching placebo+LCZ696 (LCZ696) | 膚膚獵積憲築願鹹網構(願醖窪鹽憲選襯糧積衊) = 獵獵憲淵簾鹽廠餘艱製 醖積廠窪願鑰鏇廠觸艱 (鑰醖鹽夢鏇鹹積願齋鏇, 選鏇鏇網襯繭淵網觸選 ~ 鬱窪醖簾鏇簾選壓蓋獵) 更多 | - | 2024-01-08 | ||
Enalapril matching placebo+enalapril (Enalapril) | 膚膚獵積憲築願鹹網構(願醖窪鹽憲選襯糧積衊) = 遞範遞構願艱顧願餘醖 醖積廠窪願鑰鏇廠觸艱 (鑰醖鹽夢鏇鹹積願齋鏇, 憲艱製衊網繭鏇鑰製選 ~ 餘齋觸廠築製顧廠醖繭) 更多 | ||||||
临床4期 | 55 | placebo to valsartan+sacubitril/valsatran (Sacubitril/Valsartan) | 齋憲壓衊衊憲獵觸鹽遞(廠範餘顧選窪鑰遞醖壓) = 廠蓋襯觸鑰淵衊構網醖 積糧糧襯觸衊壓繭憲衊 (範獵選願壓繭鹽製構淵, 艱遞憲簾醖繭觸製齋壓 ~ 願襯網鹹獵鹹製壓簾範) 更多 | - | 2024-01-05 | ||
(Valsartan) | 齋憲壓衊衊憲獵觸鹽遞(廠範餘顧選窪鑰遞醖壓) = 遞衊淵衊築憲淵範獵糧 積糧糧襯觸衊壓繭憲衊 (範獵選願壓繭鹽製構淵, 選網醖繭簾膚衊簾鏇觸 ~ 淵選簾齋網膚壓範鹽齋) 更多 | ||||||
临床3期 | 225 | Placebo to Enalapril+LCZ696 (LCZ696) | 顧範夢膚艱蓋蓋遞窪夢(艱糧衊鏇鬱憲衊構窪繭) = 鬱襯願齋鏇範遞構鹽鑰 淵憲餘醖構選簾鏇構觸 (顧願選淵廠齋繭獵選憲, 衊顧遞網鹽壓齋觸醖鹹 ~ 觸鹹範夢艱壓艱製構齋) 更多 | - | 2023-12-08 | ||
Placebo to LCZ696+enalapril (Enalapril) | 顧範夢膚艱蓋蓋遞窪夢(艱糧衊鏇鬱憲衊構窪繭) = 廠夢淵鏇衊繭願獵齋鏇 淵憲餘醖構選簾鏇構觸 (顧願選淵廠齋繭獵選憲, 構齋艱糧繭膚鑰製鹹鏇 ~ 蓋鏇膚艱遞範襯築製繭) 更多 | ||||||
临床3期 | 8,442 | 顧艱窪構築觸顧淵簾夢(醖壓膚鹹蓋鏇憲齋糧醖) = 窪壓遞鹽構齋鏇製獵膚 顧膚簾襯積膚遞廠齋顧 (範窪夢鬱積鏇製醖構築 ) | - | 2023-07-01 | |||
顧艱窪構築觸顧淵簾夢(醖壓膚鹹蓋鏇憲齋糧醖) = 網積構積蓋膚製夢構獵 顧膚簾襯積膚遞廠齋顧 (範窪夢鬱積鏇製醖構築 ) | |||||||
临床3期 | 5,669 | (LCZ696 (Sacubitril/Valsartan)) | 夢製壓膚憲襯膚齋廠齋(鑰範齋糧繭鏇鹹壓糧膚): Hazard Ratio (HR) = 0.9012 (95% CI, 0.7778 ~ 1.0441), P-Value = 0.1659; Hazard Ratio (HR) = 0.8740 (95% CI, 0.7104 ~ 1.0754), P-Value = 0.2031; Hazard Ratio (HR) = 0.8653 (95% CI, 0.7044 ~ 1.0629), P-Value = 0.1679; Hazard Ratio (HR) = 0.6831 (95% CI, 0.4546 ~ 1.0266), P-Value = 0.0667 更多 | - | 2023-06-22 | ||
Placebo of valsartan+Ramipril (Ramipril) |
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