预约演示
更新于：2026-01-29
Sacubitril/Valsartan
沙库巴曲缬沙坦钠
更新于：2026-01-29
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
370
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
NCT06536309
Neprilysin Inhibition to Reduce Myocardial Fibrosis in Heart Failure With Preserved Ejection Fraction
ChiCTR2500115657
Effect of sacubitril/valsartan and ACEI/ARB on left ventricular remodeling in patients with STEMI after PCI: a prospective, superiority randomized controlled 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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662
项与 沙库巴曲缬沙坦钠 相关的文献（医药）2026-02-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Quality-by-design-steered development of luliconazole-loaded ultra-deformable ethosomes for topical delivery: improved dermatokinetics and antifungal activity
Article
作者: Mahajan, Akanksha ; Katare, Om Prakash ; Dennison, Sarah R ; Singh, Kamalinder K ; Singh, Bhupinder ; Sharma, Gajanand
This work reports the first systematic formulation strategy guided by Quality-by-Design (QbD) principles to create an ultra-deformable ethosomes (UDEs) based nanocarrier for luliconazole (LCZ). The approach addresses the long-standing barriers of poor solubility, limited skin penetration, and rapid drug clearance in dermatophytosis therapy. A Box-Behnken design identified the optimal composition, including phospholipid (PL 90G), Span® 20, and ethanol: propylene glycol, yielding highly elastic nanosized vesicles (particle size 196.97 ± 1.57 nm; polydispersity index 0.158 ± 0.03) with exceptional percent drug entrapment (91.0%) and sustained release (62% over 12 h). Incorporation into a Carbopol 980 gel conferred favourable shear-thinning behaviour, enhanced spreadability, and superior texture as compared to a marketed 1% LCZ cream (MKT-LF). Ex vivo permeation across rat skin demonstrated a 2.4-fold higher flux and 11.3-fold greater cutaneous deposition than MKT-LF, attributed to synergistic vesicle deformability and ethanol-induced fluidization of stratum corneum. LCZ-UDEs demonstrated deep epidermal penetration of intact fluorescently labelled vesicles. Dermatokinetic profiling revealed a 3.4-fold increase in epidermal AUC0-12, prolonged half-life, and delayed Tmax, indicating enhanced skin retention. Antifungal assays demonstrated a two-fold reduction in MIC, and rapid fungicidal kinetics against Trichophyton rubrum compared with LCZ solution and MKT-LF. Biocompatibility studies validated >90% HaCaT cell viability, no haemolysis, and absence of dermal irritation. Sustained intradermal LCZ levels minimized sub-therapeutic exposure that drives fungal resistance. By uniting nanoscale vesicle engineering, ethanol-enhanced skin permeation, and QbD-optimized composition, this study delivers a stable, safe, and efficacious topical nanoplatform with potential to transform dermatophytosis management and mitigate antifungal resistance.
2026-02-01NEUROPHARMACOLOGY
The enhanced Wnt/β-catenin pathway upregulation by sacubitril/valsartan via neprilysin inhibition compared to valsartan in the rotenone induced Parkinson's disease rat model
Article
作者: Nofal, Shahira ; Awny, Magdy M. ; El-Sayed, Elsayed K. ; Awny, Magdy M ; Elkhial, Rania Tarek
Parkinson's disease (PD), the second most common neurodegenerative disorder, is characterized by the progressive loss of dopaminergic neurons in the basal ganglia, particularly in the substantia nigra, and the accumulation of α-synuclein into Lewy bodies. Recently, the WNT/β-catenin signaling pathway has emerged as a potential neuroprotective mechanism in PD, activated by natriuretic peptides (NPs) such as ANP, BNP, and CNP. Sacubitril/valsartan (SAC/VAL) is an FDA-approved medication for chronic heart failure. SAC contains neprilysin inhibition, while VAL is an angiotensin receptor blocker used to treat hypertension. This study aimed to determine whether SAC/VAL could activate the WNT/β-catenin pathway by increasing NP levels. To isolate the effect of SAC, VAL was administered separately. Male Wistar rats were injected with 2 mg/kg rotenone subcutaneously (S.C.) for 35 days to induce a PD-like model. VAL and SAC/VAL were administered orally at 20 mg/kg/day and 40 mg/kg/day, respectively, one week before rotenone treatment for six weeks. SAC/VAL was more effective than VAL in reducing rotenone-induced behavioral deficits, mitigating dopaminergic injury, normalizing dopamine (DA), tyrosine hydroxylase (TH), and NP levels, and activating the WNT/β-catenin pathway. SAC/VAL also suppressed oxidative stress and neuroinflammation. In conclusion, SAC/VAL exhibited greater neuroprotection against PD-induced neurodegeneration than VAL, likely due to neprilysin inhibition by the SAC component, which activates the WNT/β-catenin pathway.
2026-01-06JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION
Sacubitril/Valsartan vs Enalapril in Heart Failure Due to Chagas Disease
Article
Importance:
The efficacy and safety of guideline-recommended treatments for heart failure (HF) are uncertain in patients with Chagas disease.
Objective:
To evaluate the efficacy and safety of the angiotensin receptor-neprilysin inhibitor sacubitril/valsartan in patients with HF with reduced ejection fraction due to Chagas disease.
Design, Setting, and Participants:
From December 10, 2019, through September 13, 2023, patients with HF, confirmed diagnosis of Chagas disease, left ventricular ejection fraction of 40% or less, and N-terminal pro-B-type natriuretic peptide (NT-proBNP) of 600 pg/mL or greater (or B-type natriuretic peptide [BNP] ≥150 pg/mL) or 400 pg/mL or greater (or BNP ≥100 pg/mL) if hospitalized for HF within the previous 12 months were screened at 83 sites in Argentina, Brazil, Colombia, and Mexico. Statistical analysis was conducted between May and July 2025.
Interventions:
Patients were randomized to receive sacubitril/valsartan (target dose, 200 mg twice daily) or enalapril (target dose, 10 mg twice daily), in addition to standard therapy.
Main Outcomes and Measures:
The primary end point was a hierarchical composite outcome tested, in order, of death from cardiovascular causes, hospitalization for HF, or relative change in NT-proBNP from baseline to 12 weeks. The primary analysis was done using a win ratio approach.
Results:
Overall, 462 participants were randomized to receive sacubitril/valsartan and 460 to receive enalapril (mean [SD] age, 64.2 [10.8] years; 387 [42.0%] were female). Over a median (IQR) follow-up of 25.2 (18.4-33.2) months, cardiovascular death occurred in 110 patients (23.8% [18.3% wins in the hierarchical comparison]) in the sacubitril/valsartan group and 117 patients (25.4% [17.5% wins]) in the enalapril group. A total of 102 patients (22.1% [7.7% wins]) in the sacubitril/valsartan group and 111 (24.1% [6.9% wins]) in the enalapril group experienced a first hospitalization for HF. Patients in the sacubitril/valsartan group had a median (IQR) decrease in NT-proBNP of 30.6% (−54.3% to −0.9%) at 12 weeks, leading to 22.5% wins, while those in the enalapril group had a 5.5% (−31.9% to 37.5%) decrease (7.2% wins). The resulting stratified win ratio was 1.52 (95% CI, 1.28-1.82;
P
< .001) for sacubitril/valsartan compared with enalapril.
Conclusions and Relevance:
In patients with HF with reduced ejection fraction due to Chagas disease, there was no significant difference in clinical outcomes between sacubitril/valsartan and enalapril, but there was a greater reduction in NT-proBNP at 12 weeks in patients in the sacubitril/valsartan group.
Trial Registration:
ClinicalTrials.gov Identifier:
NCT04023227
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 |
|---|---|---|---|---|
| 心肌梗塞后综合征 | 临床3期 | - | 2021-05-26 | |
| 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 | |
| 急性心肌梗塞 | 临床3期 | 比利时 | 2016-12-09 | |
| 急性心肌梗塞 | 临床3期 | 巴西 | 2016-12-09 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 922 | 顧窪鹽構選醖醖廠醖顧(網鹽簾繭構積淵積糧鏇) = 積衊襯齋願餘鬱顧獵醖 餘糧顧醖憲鏇鬱顧艱糧 (觸廠醖餘獵網選壓觸蓋 ) 更多 | 不佳 | 2025-12-03 | |||
顧窪鹽構選醖醖廠醖顧(網鹽簾繭構積淵積糧鏇) = 壓鹹鏇選選範壓願構衊 餘糧顧醖憲鏇鬱顧艱糧 (觸廠醖餘獵網選壓觸蓋 ) 更多 | |||||||
临床3期 | 12,974 | 觸餘廠夢築鏇窪廠網築(觸衊積醖獵構鏇顧壓夢): OR = 1.16 (95.0% CI, 1.08 ~ 1.24) 更多 | 积极 | 2025-11-04 | |||
临床4期 | 190 | 齋衊憲選醖壓鹽遞簾壓(憲醖願壓鏇積鬱選遞顧) = 齋範蓋鬱衊膚醖製鑰膚 顧願簾鏇憲鑰獵廠衊醖 (艱製鑰夢遞選願齋齋願 ) | 积极 | 2025-11-01 | |||
齋衊憲選醖壓鹽遞簾壓(憲醖願壓鏇積鬱選遞顧) = 夢願積憲製鑰窪膚憲繭 顧願簾鏇憲鑰獵廠衊醖 (艱製鑰夢遞選願齋齋願 ) | |||||||
临床3期 | 心脏衰竭 NT-proBNP | LVEF | 847 | 顧顧獵夢顧壓願簾醖憲(鹽壓製鏇膚憲淵積構襯): rate ratio = 0.6 (95% CI, 0.37 ~ 0.99), P-Value = 0.046 更多 | 积极 | 2025-11-01 | ||
临床2期 | 138 | 鹽憲鏇鹹範獵夢壓顧糧(範壓簾築觸鬱鏇繭壓壓): Difference = 0.3 (95.0% CI, 0.05 ~ 0.6) 更多 | 不佳 | 2025-10-21 | |||
Placebo | |||||||
临床3期 | 心脏衰竭 amino terminal pro-B type natriuretic peptide (NT-proBNP) | - | 淵觸廠觸膚餘蓋網艱窪(簾襯鑰衊範憲製夢積顧): ratio of change = 0.85 (95% CI, 0.73 ~ 0.999) | 积极 | 2025-10-01 | ||
临床4期 | 4 | (LCZ696) | 選鹽廠顧醖糧願願淵獵(憲繭餘鬱鹹獵鹹範構網) = 壓艱願鑰壓鹹膚鏇廠蓋 構餘淵淵廠願繭齋壓糧 (窪蓋蓋築憲願鑰積鹹網, 鑰蓋鏇願觸鑰蓋顧獵壓 ~ 廠憲夢積築觸襯選壓觸) | - | 2025-08-03 | ||
(Valsartan) | 選鹽廠顧醖糧願願淵獵(憲繭餘鬱鹹獵鹹範構網) = 製製膚膚遞鹽窪鏇鹹醖 構餘淵淵廠願繭齋壓糧 (窪蓋蓋築憲願鑰積鹹網, 糧簾齋餘構範築獵鏇願 ~ 顧遞積壓顧鹽願窪膚觸) 更多 | ||||||
临床3期 | 心脏衰竭 N-terminal pro-B type natriuretic peptide (NT-proBNP) | - | 鹽鬱網齋積襯淵淵鹽遞(衊積繭廠衊醖艱觸鑰遞) = 簾夢鏇鏇構鹹窪繭艱繭 簾憲糧衊網遞糧餘襯網 (鏇艱醖獵膚製鏇鏇糧壓, 5.3 ~ 6.5) | 积极 | 2025-06-01 | ||
临床3期 | 8,399 | 鹹築顧齋獵鏇範顧積廠(壓願鑰鬱醖蓋廠衊遞夢): P-Value = 0.62 更多 | 积极 | 2025-05-06 | |||
临床3期 | 心脏衰竭 N-terminal pro-B-type natriuretic peptide (NT-proBNP) | 466 | 廠簾廠醖壓壓淵襯製積(餘獵築糧糧製衊齋構網) = 衊鏇齋選鑰鬱獵鏇築鏇 膚艱艱廠窪鑰選鹹廠積 (製遞衊餘鏇襯鏇淵繭鏇, 1.04 ~ 1.56) 更多 | 积极 | 2025-02-01 |
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