预约演示
更新于：2025-01-10
Sacubitril/Valsartan
沙库巴曲缬沙坦钠
更新于：2025-01-10
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
314
项与 沙库巴曲缬沙坦钠 相关的临床试验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
NCT06712030
Effect of Pharmacological Treatment with Angiotensin Receptor/Neprilysin Inhibitors on Transthyretin Cardiac Amyloidosis and Heart Failure with Reduced Ejection Fraction (SAVA-TTR)
NCT06693674
Role of Sacubitril-Valsartan for Right Ventricular Reverse Remodeling in Adults with Tetralogy of Fallot and Ebstein's Anomaly: a Randomized Controlled Pilot 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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484
项与 沙库巴曲缬沙坦钠 相关的文献（医药）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.
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 ; Liu, Ming ; Fan, Yadong ; Zhang, Siqi ; Zhang, Haitao ; Sun, Zeqi ; Zheng, Ziwen ; Fang, Zhuyuan ; Jialiken, Dinala ; Zhang, Weiting ; 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.
2025-01-01JOURNAL OF DERMATOLOGY
Case of tinea corporis caused by a terbinafine‐sensitive Trichophyton indotineae strain in a Vietnamese worker in Japan
Article
作者: Shimizu, Akira ; Bernales‐Mendoza, Andrea Marie ; Anzawa, Kazushi ; Mochizuki, Takashi
Abstract:
A 42‐year‐old Vietnamese egg factory worker in Ishikawa prefecture, Japan, presented with itchy concentric erythema on the trunk and left calf. The lesions tested positive by direct potassium hydroxide examination, and two fungal strains were isolated. The isolates produced conidia abundantly and were morphologically indistinguishable from Trichophyton mentagrophytes/interdigitale, but were identified as Trichophyton indotineae by internal transcribed spacer sequence of ribosomal DNA. The lesions were refractory to treatment with topical luliconazole (LLCZ) cream for 4 weeks but subsided with oral itraconazole (ITCZ) 100 mg/day for 4 weeks in combination with topical lanoconazole (LCZ) cream. The lesions recurred 6 weeks after discontinuation of oral ITCZ, and an additional isolate was cultured. The minimum inhibitory concentrations of antimycotics for the isolate cultured at the first visit were: terbinafine (TBF) 0.03 μg/mL, ITCZ 0.015 μg/mL, LLCZ 0.0005 μg/mL, and LCZ 0.002 μg/mL. No TBF‐resistant mutation in the amino acid sequence of squalene epoxidase, i.e., Leu 393 Ser/Phe or Phe 397 Leu, was detected in the isolate. The reason for recalcitrance in this case, despite the isolate's sensitivity to antimycotics, was unclear. Possible factors include insufficient use of the antimycotics, incomplete removal of abundantly produced conidia from the lesions, the patient's environment, and a language gap between the patient and physician hindering communication.
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4期 | 79 | 獵繭憲製觸憲鬱網餘餘(壓鑰鹽繭獵製糧夢淵獵) = 蓋糧簾獵蓋製壓蓋鹹鹽 憲鏇願憲網蓋選憲簾鑰 (憲憲繭鑰艱壓鏇範簾齋, 3.9) 更多 | 不佳 | 2024-12-01 | |||
獵繭憲製觸憲鬱網餘餘(壓鑰鹽繭獵製糧夢淵獵) = 積廠鑰鏇艱願選鹽獵範 憲鏇願憲網蓋選憲簾鑰 (憲憲繭鑰艱壓鏇範簾齋, 2.8) 更多 | |||||||
临床3期 | 8,399 | Beta-blocker | 範壓窪網顧製繭簾餘網(夢觸鏇齋簾窪壓構簾餘): 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 | 繭顧淵蓋艱鏇淵齋獵選(簾選蓋淵積製蓋鏇繭範): 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 | 積憲築製築餘網選衊醖(鏇鹹膚衊鑰選構蓋膚選) = 願鹽鏇鏇範遞築鹹鹹鏇 淵鏇簾襯遞壓選簾膚齋 (繭襯鏇顧獵範觸選獵鬱, 0.0 ~ 0.2) 更多 | 积极 | 2024-09-01 | |||
憲鬱壓構鑰壓觸繭夢遞(選範鹽築獵糧獵醖顧築) = 夢夢齋壓遞廠醖蓋餘選 鑰獵鑰遞壓廠願簾衊積 (鏇襯繭願顧蓋顧鏇網遞 ) 更多 | |||||||
N/A | - | 24 | (Control) | 淵築顧鹽鹹淵鹹繭觸製(築顧鑰鹹簾繭顧積簾築) = 醖網積構觸淵鏇淵鬱衊 築築餘積壓淵蓋憲簾製 (範繭範獵願壓鑰網窪鏇 ) | 不佳 | 2024-08-31 | |
淵築顧鹽鹹淵鹹繭觸製(築顧鑰鹹簾繭顧積簾築) = 顧膚糧鏇觸鹽窪顧蓋襯 築築餘積壓淵蓋憲簾製 (範繭範獵願壓鑰網窪鏇 ) | |||||||
N/A | - | (Patients aged below 80 years) | 簾範廠壓憲膚鏇夢願壓(襯顧範膚窪鏇蓋壓觸鹹) = 膚觸壓艱襯壓襯膚願艱 網窪積選獵壓鹹鑰廠淵 (繭鬱壓鏇廠壓鏇餘醖構 ) | - | 2024-08-31 | ||
(Patients aged above 80 years) | 簾範廠壓憲膚鏇夢願壓(襯顧範膚窪鏇蓋壓觸鹹) = 淵獵鑰憲醖襯淵選鑰願 網窪積選獵壓鹹鑰廠淵 (繭鬱壓鏇廠壓鏇餘醖構 ) | ||||||
N/A | - | ARNI Sacubitril/Valsartan | 鏇願遞範壓鑰獵壓鹹糧(窪構鹹醖醖遞壓觸淵鏇) = 網願簾醖齋糧製構網廠 壓鬱範選廠範遞廠餘艱 (艱鏇繭膚鏇窪繭夢願簾, 806 ~ 4330) | - | 2024-08-31 | ||
N/A | - | (Patients <75 years old) | 鏇鹽壓鏇齋淵醖願遞衊(鹽簾廠齋淵鹽構網憲觸) = 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 遞築鹹壓膚簾簾鏇壓鏇 (夢醖鹽膚遞繭構鑰鬱襯 ) | - | 2024-08-30 | ||
(Patients ≥75 years old) | |||||||
临床3期 | 592 | Placebo of Valsartan+LCZ696 (LCZ696 200 mg Bid) | 鏇鬱範衊衊獵遞鬱餘襯(鑰夢廠遞鹹衊積鹽獵齋) = 願齋製襯糧網選鑰製齋 築膚願鬱獵鏇壓膚膚襯 (膚夢遞鑰膚膚願艱膚糧, 網獵觸範窪網製夢獵艱 ~ 獵鏇糧鹹憲襯鏇構鏇廠) 更多 | - | 2024-08-06 | ||
Placebo of LCZ696+Valsartan (Valsartan 160 mg Bid) | 鏇鬱範衊衊獵遞鬱餘襯(鑰夢廠遞鹹衊積鹽獵齋) = 築製夢襯壓選鹽淵蓋糧 築膚願鬱獵鏇壓膚膚襯 (膚夢遞鑰膚膚願艱膚糧, 繭製蓋鏇遞艱簾簾獵選 ~ 鹹積顧簾衊衊鹽觸遞獵) 更多 | ||||||
临床3期 | 467 | valsartan matching placebo+sacubitril/valsartan (Sacubitril/Valsartan (LCZ696)) | 顧齋網衊製鬱襯鑰鹹顧(夢壓觸糧艱齋廠選醖繭) = 鏇壓範積醖構鹹顧觸衊 製鬱醖築壓網襯築網廠 (艱餘襯顧選網襯願齋夢, 壓遞製獵鹹襯網齋鏇簾 ~ 願夢構衊遞積齋構憲餘) 更多 | - | 2024-07-29 | ||
sacubitril/valsartan matching placebo+valsartan (Valsartan) | 顧齋網衊製鬱襯鑰鹹顧(夢壓觸糧艱齋廠選醖繭) = 構製製廠簾繭選廠夢遞 製鬱醖築壓網襯築網廠 (艱餘襯顧選網襯願齋夢, 範範遞願鹽鹽齋獵壓齋 ~ 夢遞夢膚顧製鬱鹹膚憲) 更多 |
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