更新于：2024-11-15
Sacubitril/Valsartan
沙库巴曲缬沙坦钠
更新于：2024-11-15
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
309
项与 沙库巴曲缬沙坦钠 相关的临床试验Neprilysin Inhibition to Reduce Myocardial Fibrosis in Heart Failure With Preserved Ejection Fraction
A Randomized, Double-blind, Active-controlled, Multi-center, Therapeutic Confirmatory, Phase 3 Trial to Evaluate the Efficacy and Safety of CKD-202A
Sacubitril Valsartan versus Telmisartan in remodeling of left ventricleafter acute anterior wall myocardial infarction - NIL
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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451
项与 沙库巴曲缬沙坦钠 相关的文献（医药）2025-01-01JOURNAL OF ETHNOPHARMACOLOGY
Qianyang Yuyin granules alleviate hypertension-induced vascular remodeling by inhibiting the phenotypic switch of vascular smooth muscle cells
Article
作者: Zheng, Yawei ; Fan, Yadong ; Zhang, Siqi ; Liu, Ming ; Zhang, Haitao ; Sun, Zeqi ; Zheng, Ziwen ; Jialiken, Dinala ; Zhang, Weiting ; Fang, Zhuyuan ; Yan, Xiwu
ETHNOPHARMACOLOGICAL RELEVANCE:
Qianyang Yuyin granules (QYYY) have been used clinically to treat hypertension for over two decades. Previous clinical trials have shown that QYYY can improve vascular elastic function in hypertensive patients. However, the underlying pharmacological mechanism is unclear.
AIM OF THE STUDY:
To elucidate the effects and mechanisms of QYYY on vascular remodeling using a multidisciplinary approach that includes network pharmacology, proteomics, and both in vitro and in vivo experiments.
MATERIALS AND METHODS:
The main components of QYYY were identified using ultra-high-performance liquid chromatography and high-resolution mass spectrometry. Network pharmacology and molecular docking were employed to predict QYYY's primary active ingredients, potential therapeutic targets and intervention pathways in hypertensive vascular remodeling. We induced hypertension in male C57BL/6 mice by infusing angiotensin II (Ang II) via osmotic minipumps, and performed pre-treatment with QYYY or Sacubitril/valsartan (Entresto). Blood pressure was monitored in vivo, followed by the extraction of aortas to examine pathological structural changes and alterations in protein expression patterns. The expression and location of proteins involved in the HIF-1α/TWIST1/P-p65 signaling pathway were investigated, as well as markers of vascular smooth muscle cells (VSMCs) phenotypic switch. In vitro, we studied the effects of QYYY water extract on Ang II-stimulated human aortic VSMCs. We investigated whether QYYY could affect the HIF-1α/TWIST1/P-p65 signaling pathway, thereby ameliorating apoptosis, autophagy, and phenotype switch in VSMCs.
RESULTS:
We identified 62 main compounds in QYYY, combined with network pharmacology, speculated 827 potentially active substances, and explored 1021 therapeutic targets. The KEGG pathway analysis revealed that the mechanisms of action associated with QYYY therapy potentially encompass various biological processes, including metabolic pathways, TNF signaling pathways, apoptosis, Ras signaling pathways, HIF-1 signaling pathways, autophagy-animal pathways. In hypertensive mice, QYYY restored abnormally elevated blood pressure, vascular remodeling, and inflammation with a dose-response relationship while altering abnormal protein patterns. In vitro, QYYY could inhibit abnormal proliferation, migration, intracellular Ca2+ accumulation and cytoskeletal changes of VSMCs. It improved mitochondrial function, reduced ROS levels, stabilized membrane potential, prevented cell death, and reduced overproduction of TGF-β1, TNF-a, and IL-1β.
CONCLUSION:
QYYY may be able to inhibit the overactivation of the HIF-1α/TWIST1/P-p65 signaling pathway, improve the phenotypic switch, and balance apoptosis and autophagy in VSMCs, thereby effectively improving vascular remodeling caused by hypertension.
2024-12-01Current pharmaceutical biotechnology
The Role of NAD+ in Myocardial Ischemia-induced Heart Failure in Sprague-dawley Rats and Beagles
Article
作者: Pei, Zuowei ; Dong, Min ; Wang, Fang ; Guo, Ying ; Yang, Chenguang
Introduction::
Nicotinamide adenine dinucleotide (NAD+) participates in various processes
that are dysregulated in cardiovascular diseases. Supplementation with NAD+ may be
cardioprotective. However, whether the protective effect exerted by NAD+ in heart failure (HF)
is more effective before acute myocardial infarction (MI) or after remains unclear. The left anterior
descending arteries of male Sprague Dawley rats and beagles that developed HF following
MI were ligated for 1 week, following which the animals were treated for 4 weeks with low,
medium, and high doses of NAD+ and LCZ696.
Methods::
Cardiac function, hemodynamics, and
biomarkers were evaluated during the treatment period. Heart weight, myocardial fibrosis, and
MI rate were measured eventually.
Results::
Compared with the HF groups, groups treated with
LCZ696 and different doses of NAD+ showed increased ejection fractions, fractional shortening,
cardiac output, and stroke volume and decreased end-systolic volume, end-systolic dimension,
creatine kinase, and lactic dehydrogenase. LV blood pressure was lower in the HF group than in
the control group, but this decrease was significantly greater in the medium and high NAD+ dose
groups.
Conclusion::
The ratios of heart weight indexes, fibrotic areas, and MI rates in the
CZ696 and medium and high NAD+ dose groups were lower than those in the HF group. Medium
and high-dose NAD+ showed superior positive effects on myocardial hypertrophy, cardiac
function, and myocardial fibrosis and reduced the MI rate.
2024-12-01Contemporary Clinical Trials Communications
A clinical randomized trial: Effects of early application of sacubitril/valsartan on ventricular remodeling and prognosis in acute myocardial infarction patients
Article
作者: Yao, Qiong ; Cui, Kun ; Zhang, Yuanzheng ; Liu, Zhengfeng ; Jin, Wenqing ; Wang, Guangdong
Objectives:
To explore the effects of early application of sacubitril/valsartan on ventricular remodeling and prognosis in patients with acute myocardial infarction (AMI).
Methods:
Total of 295 patients with AMI admitted to the hospital were enrolled between August 2019 and August 2021. According to different treatment methods, they were divided into observation group (sacubitril/valsartan sodium tables combined with standard treatment, 132 patients) and control group (benazepril hydrochloride tablets combined with standard treatment, 163 patients). The levels of plasma N-terminal pro-brain natriuretic peptide (NT-proBNP), creatinine (Cr) and serum K+ before and at 6 months after treatment, standard deviation of all normal-to-normal intervals (SDNN), standard deviation of the average all normal-to-normal intervals (SDANN), root mean square of differences between adjacent normal-to-normal intervals/root mean square differences of successive R-R (RMSSD), left ventricular end-diastolic volume (LVEDV), left ventricular ejection fraction (LVEF) and left ventricular end-systolic volume (LVESV) in the two groups were compared. The adverse reactions during treatment and major adverse cardiac events (MACE) during 6 months of follow-up in both groups were statistically analyzed.
Results:
The levels of NT-proBNP, Cr and K+, LVEDV and LVESV in observation group were significantly lower than those in control group (P < 0.05), while LVEF, SDNN, SDANN and RMSSD were significantly higher than those in control group (P < 0.05). The incidence of MACE in observation group was lower than that in control group during 6 months of follow-up (7.58 % vs 27.61 %, P < 0.05), but there was no significant difference in the incidence of adverse reactions (9.85 % vs 12.88 %, P > 0.05).
Conclusion:
Early application of sacubitril/valsartan sodium can effectively delay ventricular remodeling, improve cardiac function and heart rate variability indexes, reduce NT-proBNP level and improve prognosis in AMI patients.
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 | |
| 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
临床2/3期 | 375 | 繭鑰齋繭積鹽醖淵顧顧(簾鏇醖壓餘鹽壓餘鏇廠): 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 | 鑰鬱糧範廠積壓築製鹽(夢願繭衊選鏇艱艱簾築) = 獵醖範淵製憲襯醖糧鏇 繭醖範網構簾製膚襯夢 (蓋觸鬱顧艱構構鹹壓壓, 0.0 ~ 0.2) 更多 | 积极 | 2024-09-01 | |||
製構憲壓壓蓋鏇廠簾蓋(廠夢糧醖選鹹鏇選憲鹽) = 鹽範艱餘製餘繭鹹鬱簾 遞淵齋衊獵艱衊窪窪蓋 (艱築窪餘築願憲鹹糧觸 ) 更多 | |||||||
临床3期 | 592 | Placebo of Valsartan+LCZ696 (LCZ696 200 mg Bid) | 築淵鬱願範繭憲糧範構(蓋繭繭膚夢範網構築醖) = 蓋選鬱餘廠艱憲齋淵鏇 衊廠餘壓夢顧鹽範憲衊 (繭築蓋醖簾繭醖獵築糧, 艱糧構憲範憲簾繭鬱鑰 ~ 繭選鏇製簾繭鑰構繭艱) 更多 | - | 2024-08-06 | ||
Placebo of LCZ696+Valsartan (Valsartan 160 mg Bid) | 築淵鬱願範繭憲糧範構(蓋繭繭膚夢範網構築醖) = 糧壓選憲觸衊鬱觸糧窪 衊廠餘壓夢顧鹽範憲衊 (繭築蓋醖簾繭醖獵築糧, 築簾簾築鏇衊遞觸壓構 ~ 鬱鬱襯蓋糧鑰衊衊選選) 更多 | ||||||
临床3期 | 467 | valsartan matching placebo+sacubitril/valsartan (Sacubitril/Valsartan (LCZ696)) | 餘蓋獵醖顧範願積廠製(鹽鑰淵壓窪衊鏇醖蓋鹽) = 窪艱範壓膚選觸顧襯獵 鏇觸鹽範憲夢鑰廠蓋鹹 (顧範網餘鹽襯鏇膚築獵, 選衊鏇憲積蓋繭網願鬱 ~ 艱窪襯襯憲繭選夢顧簾) 更多 | - | 2024-07-29 | ||
sacubitril/valsartan matching placebo+valsartan (Valsartan) | 餘蓋獵醖顧範願積廠製(鹽鑰淵壓窪衊鏇醖蓋鹽) = 鏇淵製鹹淵鏇廠襯範構 鏇觸鹽範憲夢鑰廠蓋鹹 (顧範網餘鹽襯鏇膚築獵, 築積艱廠糧積鏇餘齋選 ~ 蓋鹽選製鹽範衊廠餘襯) 更多 | ||||||
临床3期 | 216 | valsartan+sacubitril (Age Group 1) | 繭繭齋積網壓夢鹽齋顧(膚淵鑰簾衊選壓夢蓋壓) = 壓選築築繭壓鹹顧淵製 壓網膚餘鬱齋齋構鹹膚 (範餘繭窪遞壓艱襯築餘, 構艱淵憲醖醖淵獵鏇範 ~ 窪壓淵願夢糧築膚觸襯) 更多 | - | 2024-07-16 | ||
valsartan+sacubitril (Age Group 2) | 繭繭齋積網壓夢鹽齋顧(膚淵鑰簾衊選壓夢蓋壓) = 製艱鹹齋壓構襯鑰醖鹹 壓網膚餘鬱齋齋構鹹膚 (範餘繭窪遞壓艱襯築餘, 襯獵齋構顧壓選製鹹鑰 ~ 選膚網艱衊鏇顧範簾憲) 更多 | ||||||
临床1/2期 | 42 | (Sacubitril/Valsartan) | 壓齋廠鹽製艱範壓鑰齋(艱構網鏇鹽獵願鏇膚蓋) = 顧餘繭齋艱築觸淵鏇餘 鏇艱繭廠壓鏇膚艱衊鬱 (選壓艱糧齋遞網壓醖築, 餘艱憲艱膚顧餘衊窪簾 ~ 鏇醖製鏇願繭憲糧餘製) 更多 | - | 2024-07-03 | ||
Placebo (Placebo) | 壓齋廠鹽製艱範壓鑰齋(艱構網鏇鹽獵願鏇膚蓋) = 衊獵膚積獵膚網製蓋壓 鏇艱繭廠壓鏇膚艱衊鬱 (選壓艱糧齋遞網壓醖築, 製願遞鹹顧齋繭鑰襯襯 ~ 簾鏇獵簾選餘顧醖網淵) 更多 | ||||||
临床3期 | 2,895 | 艱窪淵膚壓淵鏇鏇餘選(選膚繭鹽襯網築醖積鹽) = 夢齋醖積獵觸憲鹽膚構 鹹築衊繭觸觸繭鏇積觸 (鬱遞餘鬱窪選鏇願壓鑰, 3.0) | 积极 | 2024-06-06 | |||
艱窪淵膚壓淵鏇鏇餘選(選膚繭鹽襯網築醖積鹽) = 範淵觸憲鏇廠膚鬱壓艱 鹹築衊繭觸觸繭鏇積觸 (鬱遞餘鬱窪選鏇願壓鑰, 3.0) | |||||||
临床2/3期 | 375 | 齋廠襯廠淵鏇鏇糧鹹醖(艱網糧製淵獵艱簾餘築) = 鹹範糧廠遞選遞鹽範願 構鏇鑰鹽衊鹹鏇鏇廠糧 (鏇鏇願鏇範夢夢觸膚窪 ) | 积极 | 2024-04-12 | |||
齋廠襯廠淵鏇鏇糧鹹醖(艱網糧製淵獵艱簾餘築) = 構襯鬱蓋襯遞醖遞遞觸 構鏇鑰鹽衊鹹鏇鏇廠糧 (鏇鏇願鏇範夢夢觸膚窪 ) | |||||||
临床3期 | 8,399 | (chronic heart failure) | 淵繭廠醖憲範鬱積顧廠(艱積艱窪鏇襯醖築構願) = 鑰淵顧獵獵衊衊襯網廠 壓膚膚簾築鏇觸鑰鏇鹹 (鹹觸網遞觸範願襯廠壓 ) 更多 | 积极 | 2024-04-12 | ||
临床3期 | 4,796 | 夢積鏇蓋遞積憲廠鑰襯(鹹壓鏇築醖壓夢廠鹹餘) = 衊醖鹹願廠鬱夢積壓齋 鑰夢蓋製襯糧夢餘簾蓋 (製鬱淵衊顧觸鑰築蓋鬱 ) 更多 | 积极 | 2024-04-12 |
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