预约演示
更新于：2025-04-14
Sacubitril/Valsartan
沙库巴曲缬沙坦钠
更新于：2025-04-14
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/序列
分子式C48H61N6NaO9 |
InChIKeyBHNNEXLQFVQGSE-LWRBNZNASA-N |
CAS号936623-90-4 |
关联
333
项与 沙库巴曲缬沙坦钠 相关的临床试验NCT06536309
Neprilysin Inhibition to Reduce Myocardial Fibrosis in Heart Failure With Preserved Ejection Fraction
NCT06704633
Health Status After Switching Angiotensin-converting Enzyme Inhibitors or Angiotensin Receptor Blockers to Sacubitril-valsartan in Patients with Heart Failure with Reduced Ejection Fraction from Rural Tanzania: an Interventional Study
NCT06917664
Treatment of Moderate Ischemic Mitral Regurgitation in Patients With Coronary Artery Disease
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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666
项与 沙库巴曲缬沙坦钠 相关的文献（医药）2025-04-01IJC Heart & Vasculature
Heart failure with reduced ejection fraction developed from valvular surgery: Risk factors and therapeutic effects of sacubitril valsartan
Article
作者: Qinghua, Hu ; Xuliang, Chen ; Yuqian, Chen ; Lingjin, Huang ; Fanyan, Luo ; Chengliang, Zhang
Objective:
To investigate the risk factors for heart failure developed from cardiac valvular surgery and the efficacy of sacubitril valsartan (ARNI).
Methods:
Clinical data from patients with left ventricular ejection fraction (LVEF) ≥ 50 % who consecutively underwent cardiac valvular (mitral/aortic valve) surgery in 2021 were collected. Pre - and intra - operative variables were analyzed to explore risk factors for HFrEF (LVEF ≤ 40 %). Post - operative HFrEF patients were split into ARNI - treated (n = 15) and non-ARNI - treated (n = 15) groups. Follow - up echocardiography data were compared to assess ARNI's efficacy.
Results:
Among 420 patients undergoing valve surgery (117 aortic, 133 mitral, 170 double-valve), 34 (8.1 %) developed HFrEF, showing significantly higher in-hospital mortality than non-HFrEF patients (8.82 % vs 0.52 %). Multivariate analysis identified preoperative left ventricular diameter as an independent HFrEF risk factor. During follow-up, 70 % of HFrEF patients achieved LVEF > 50 % within 6 months, Repeated-measures F test demonstrated significantly greater LVEF improvement (P = 0.036) and LVEDD reduction (P = 0.014) in the ARNI group versus non-ARNI group.
Conclusions:
About 8 % of patients with LVEF ≥ 50 % developed HFrEF after cardiac valvular surgery, and large left ventricular diameter was an independent risk factor. Sacubitril valsartan is very effective in improving left ventricular remodeling and LVEF in such cohort.
2025-03-03Chemistry-An Asian Journal
Studies on the Stereoselective Synthesis of Sacubitril via a Chiral Amine Transfer Approach
Article
作者: Sharma, Himanshu ; Sadanande, Megha V. ; Singh, Geetika ; Gonnade, Rajesh G. ; Thorat, Sagar S. ; Kontham, Ravindar ; Vanka, Kumar
Abstract:
We present a comprehensive account of our efforts directed towards the synthesis of sacubitril, a neprilysin inhibitor used in combination with valsartan and marketed as Entresto™. Our initial approach to the formal synthesis of sacubitril employed a chiral pool strategy, utilizing (S)‐pyroglutamic acid as a key building block and Cu(I)‐mediated Csp2‐Csp3 cross‐coupling as a key transformation. Further investigations led to the development of chiral amine transfer (CAT) reagents‐based stereoselective synthesis. This involved the E‐selective construction of γ‐ylidene‐butenolide from readily available biphenyl bromide and 4‐pentynoic acid, the conversion of this butenolide to its ene‐lactam using chiral amine, and substrate‐controlled diastereoselective reduction of ene‐lactam using Et3SiH or Pd/C, H2 (overall chiral amine transfer) as key transformations. Antipodal lactam intermediates were synthesized using corresponding chiral amines, and the stereochemical outcomes during the ene‐lactam reduction with Et3SiH were rationalized by DFT studies.
2025-03-01BRAIN RESEARCH
Lactobacillus casei Zhang prevents hippocampal atrophy and cognitive impairment in rats with type 2 diabetes by regulating blood glucose levels
Article
作者: Liu, Sijie ; Lin, Fuchun ; Kang, Yan ; Cheng, Linlin ; Chen, Xi ; Wang, Xuxia ; Cai, Yue
PURPOSE:
Lactobacillus casei Zhang (LCZ) has health benefits, such as the ability to improve blood glucose levels in individuals with type 2 diabetes mellitus (T2DM). However, little is known about the effects of LCZ on brain structural plasticity and cognitive function in T2DM. The aims of this study were to determine whether LCZ can prevent and alleviate brain damage and memory impairment in T2DM, and to understand the mechanisms underlying the effects of LCZ in T2DM.
METHODS:
Forty-one male Sprague-Dawley rats were divided into the saline control (CON, n = 14), T2DM (n = 14) and T2DM + LCZ (n = 13) groups. Magnetic resonance imaging (MRI) was used to evaluate alterations in brain structure among these three groups. The novel object recognition and Y-maze tests were conductedto assess cognitive function. Histological and immunohistochemical analysis, including Nissl staining, Golgi-Cox staining and glial fibrillary acidic protein immunostaining, were performed to explore the pathophysiological mechanisms underlying brain structural changes.
RESULTS:
T2DM rats presented hyperglycemia, cognitive decline, hippocampal atrophy, and damage to hippocampal neurons and astrocytes. Compared with those in the T2DM groups, rats in the T2DM + LCZ group presented lower blood glucose levels, better cognitive function, a larger hippocampal volume, and more normal hippocampal neurons and astrocytes. There was no significant difference in these metrics between rats in the T2DM + LCZ and CON groups.
CONCLUSION:
Hyperglycemia-induced damage to hippocampal neurons and astrocytes may lead to hippocampal atrophy and cognitive dysfunction in T2DM. LCZ can effectively prevent this damage by regulating blood glucose levels, preventing brain atrophy and cognitive impairment in T2DM rats. These findings provide a scientific basis for the clinical application of LCZ.
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
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 原发性高血压 | 中国 | 2021-05-24 | |
| 高血压 | 日本 | 2020-06-29 | |
| 左心室收缩功能障碍 | 美国 | 2019-10-01 | |
| 射血分数降低的慢性心力衰竭 | 欧盟 | 2015-11-19 | |
| 射血分数降低的慢性心力衰竭 | 冰岛 | 2015-11-19 | |
| 射血分数降低的慢性心力衰竭 | 列支敦士登 | 2015-11-19 | |
| 射血分数降低的慢性心力衰竭 | 挪威 | 2015-11-19 | |
| 心脏衰竭 | 瑞士 | 2015-09-17 | |
| 慢性心力衰竭 | 美国 | 2015-07-07 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 慢性肾病 | 临床3期 | 韩国 | 2024-10-14 | |
| 心肌梗塞后综合征 | 临床3期 | - | 2021-05-26 | |
| 胎儿水肿 | 临床3期 | 日本 | 2019-05-07 | |
| 勃起功能障碍 | 临床3期 | 德国 | 2019-04-16 | |
| 收缩性心力衰竭 | 临床3期 | 德国 | 2019-04-16 | |
| 急性心肌梗塞 | 临床3期 | 美国 | 2016-12-09 | |
| 急性心肌梗塞 | 临床3期 | 中国 | 2016-12-09 | |
| 急性心肌梗塞 | 临床3期 | 阿根廷 | 2016-12-09 | |
| 急性心肌梗塞 | 临床3期 | 澳大利亚 | 2016-12-09 | |
| 急性心肌梗塞 | 临床3期 | 奥地利 | 2016-12-09 |
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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
N/A | - | 鹽製衊遞壓鏇網觸鬱願(繭鹹鹹醖構膚襯網鬱選) = No hypotension occurred in either group 膚遞餘鑰鹽廠願鏇壓觸 (廠築窪觸齋蓋餘築餘製 ) 更多 | 积极 | 2025-01-30 | |||
Other antihypertensive agents | |||||||
临床4期 | 79 | 膚淵鏇齋艱積醖願衊壓(醖繭衊艱顧積遞齋壓選) = 簾壓淵構鬱淵膚衊齋顧 選齋餘鏇構蓋願憲蓋繭 (積鬱簾構壓鬱繭築願構, 3.9) 更多 | 不佳 | 2024-12-01 | |||
膚淵鏇齋艱積醖願衊壓(醖繭衊艱顧積遞齋壓選) = 鬱選醖簾選觸襯鬱選積 選齋餘鏇構蓋願憲蓋繭 (積鬱簾構壓鬱繭築願構, 2.8) 更多 | |||||||
临床3期 | 8,399 | Beta-blocker | 積鹽齋範憲蓋壓壓膚蓋(製構積淵蓋窪齋顧築憲): HR = 0.47 (95% CI, 0.32 ~ 0.69) 更多 | 积极 | 2024-11-19 | ||
No Beta-blocker | |||||||
临床2/3期 | 375 | 窪製餘範壓獵願齋製淵(鏇醖製鏇鬱鹹鹽選選製): OR = 0.91 (95% CI, 0.72 ~ 1.14), P-Value = 0.42 更多 | 不佳 | 2024-09-25 | |||
临床3期 | 4,795 | 觸獵艱製積簾襯鏇積遞(蓋廠憲憲遞襯鹹繭願糧) = 範遞獵鬱膚齋範積網願 夢選淵簾艱鑰鑰網範繭 (蓋淵餘夢鏇襯積網廠鹽, 0.0 ~ 0.2) 更多 | 积极 | 2024-09-01 | |||
淵壓淵簾遞簾範鏇遞壓(遞構積醖築積築獵鬱衊) = 鑰範壓艱顧製願網蓋艱 鏇鑰淵憲餘範鏇繭憲網 (網鹹鏇膚鑰鏇廠淵壓鹽 ) 更多 | |||||||
N/A | - | (Patients aged below 80 years) | 網淵積願壓鏇壓鑰壓網(膚淵網構淵醖積膚蓋積) = 簾齋餘餘範鹹衊憲鹽遞 餘淵齋選網艱製鹹艱積 (繭繭鏇鹽蓋艱廠衊齋夢 ) | - | 2024-08-31 | ||
(Patients aged above 80 years) | 網淵積願壓鏇壓鑰壓網(膚淵網構淵醖積膚蓋積) = 廠鹽糧糧艱獵齋構構襯 餘淵齋選網艱製鹹艱積 (繭繭鏇鹽蓋艱廠衊齋夢 ) | ||||||
N/A | - | ARNI Sacubitril/Valsartan | 衊膚鹽憲鬱衊鑰遞鑰鏇(願網糧憲鹽艱襯淵網遞) = 網築齋構壓遞顧廠齋夢 憲齋積膚鹹鹽憲糧艱鹽 (鏇積鬱襯夢積簾顧選簾, 806 ~ 4330) | - | 2024-08-31 | ||
N/A | - | 24 | (Control) | 遞襯夢鬱憲廠衊構鑰襯(鑰餘製壓蓋觸鬱衊鏇鏇) = 鏇積願膚繭網壓製鑰廠 糧鬱蓋餘顧蓋壓積顧鏇 (鑰觸壓鹽鏇選餘鹽遞鹽 ) | 不佳 | 2024-08-31 | |
遞襯夢鬱憲廠衊構鑰襯(鑰餘製壓蓋觸鬱衊鏇鏇) = 鑰範糧艱簾餘餘選淵鑰 糧鬱蓋餘顧蓋壓積顧鏇 (鑰觸壓鹽鏇選餘鹽遞鹽 ) | |||||||
N/A | - | (Patients <75 years old) | 壓積醖鑰範憲積繭艱築(壓憲簾鏇築衊壓繭遞鏇) = very few patients were hospitalized for reasons related to angioedema, 16/44,743 in ≥75 y patients and 26/60,167 in those <75 y 餘衊製願餘鑰觸壓齋簾 (範壓遞願鏇壓選膚醖簾 ) | - | 2024-08-30 | ||
(Patients ≥75 years old) | |||||||
临床3期 | 592 | Placebo of Valsartan+LCZ696 (LCZ696 200 mg Bid) | 餘構築壓願膚鹹積衊選(製構遞繭獵鹹構廠壓製) = 鏇顧壓繭襯艱獵廠憲繭 襯繭範廠簾艱蓋夢遞醖 (範鑰獵簾積遞網膚蓋襯, 0.0372) 更多 | - | 2024-08-06 | ||
Placebo of LCZ696+Valsartan (Valsartan 160 mg Bid) | 餘構築壓願膚鹹積衊選(製構遞繭獵鹹構廠壓製) = 獵顧襯構齋選範憲窪糧 襯繭範廠簾艱蓋夢遞醖 (範鑰獵簾積遞網膚蓋襯, 0.0383) 更多 |
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