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更新于：2025-04-13
Amlodipine besilate/Valsartan
苯磺酸氨氯地平/缬沙坦
更新于：2025-04-13
概要
基本信息
药物类型 小分子化药 |
别名 Amlodipine (as besylate)/Valsartan、Amlodipine /Valsartan、Amlodipine/Valsartan + [16] |
作用方式 拮抗剂、阻滞剂 |
作用机制 AT1R拮抗剂(血管紧张素II-1型受体拮抗剂)、VDCCs阻滞剂(电压门控性钙通道复合体阻滞剂) |
治疗领域 |
非在研适应症- |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2007-01-15), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C24H29N5O3 |
InChIKeyACWBQPMHZXGDFX-QFIPXVFZSA-N |
CAS号137862-53-4 |
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关联
108
项与 苯磺酸氨氯地平/缬沙坦 相关的临床试验NCT06625346
Clinical Outcomes in Newly Diagnosed Hypertensive Patients with EXTOR (Fixed-Dose Combination of Amlodipine/Valsartan) in Routine Pakistani Practice.
CTR20242402
缬沙坦氨氯地平片（I）在健康人体空腹/餐后状态下的
生物等效性试验
NCT06193044
A Single Dose, Randomized, Open-label, Two-treatment, Four-period, Two-sequence, Replicate Crossover Bioequivalence Study of Generic Amlodipine and Valsartan Tablets 10/160 mg and Reference Product (Exforge® 10/160 mg Tablets)
100 项与 苯磺酸氨氯地平/缬沙坦 相关的临床结果
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100 项与 苯磺酸氨氯地平/缬沙坦 相关的转化医学
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100 项与 苯磺酸氨氯地平/缬沙坦 相关的专利（医药）
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26
项与 苯磺酸氨氯地平/缬沙坦 相关的文献（医药）2024-07-01BioFactors (Oxford, England)
Sacubitril/valsartan promotes white adipose tissue browning in rats with metabolic syndrome through activation of mTORC1
Article
作者: Novakovic, Jovana ; Lazarevic, Nevena ; Jeremic, Nevena ; Nedeljkovic, Nikola ; Nikolic, Marina ; Nikolic, Milos ; Mitrovic, Slobodanka ; Zivkovic, Vladimir ; Jakovljevic, Vladimir ; Stojanovic, Aleksandra ; Milojevic Samanovic, Andjela
Abstract:
In addition to their usual use in the treatment of cardiovascular disease, weak evidence is available for the potential of combined use of neprilysin inhibitor (sacubitril) and AT1 receptor antagonist (valsartan) to promote browning of white adipose tissue (WAT) in rats with metabolic syndrome (MetS). This study involved 32 male Wistar albino rats divided into four groups: CTRL—healthy control rats; ENT—healthy rats treated with sacubitril/valsartan; MS—rats with MetS; MS + ENT—rats with MetS treated with sacubitril/valsartan. After finishing the experimental protocol, different WAT depots were isolated for further analysis of molecular pathways. Molecular docking and molecular dynamics studies were used for in silico assessment of the binding affinity of sacubitril and valsartan towards subunits of mechanistic target of rapamycin complex 1 (mTORC1). Sacubitril/valsartan treatment markedly diminished morphological changes in adipose tissue, resulting in smaller lipid size and multilocular lipid droplet structure in WAT. We showed significantly higher protein expression of uncoupling protein‐1 (UCP‐1) and mTORC1 in WAT of MS + ENT rats, correlating with increased relative gene expression of browning‐related markers in tissue of rats treated with sacubitril/valsartan compared with MS group of rats. In silico analysis showed that sacubitrilat and valsartan exhibited the highest binding affinity against mTOR and mLST8, forming stable complexes with these mTORC1 subunits. The observed results confirmed strong potential of combined sacubitril/valsartan treatment to increase browning markers expression in different WAT depots in MetS condition and to form permanent complexes with mTOR and mLST8 subunits over the time.
2024-06-01ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
A structure-based pharmacophore modelling approach to identify and design new neprilysin (NEP) inhibitors: An in silico-based investigation
Article
作者: Sinhari, Apurba ; Gaikwad, Anil Bhanudas ; Thakur, Shikha ; Jadhav, Hemant R
Neutral endopeptidase or neprilysin (NEP) cleaves the natriuretic peptides, bradykinin, endothelin, angiotensin II, amyloid β protein, substance P, etc., thus modulating their effects on heart, kidney, and other organs. NEP has a proven role in hypertension, heart disease, renal disease, Alzheimer's, diabetes, and some cancers. NEP inhibitor development has been in focus since the US FDA approved a combination therapy of angiotensin II type 1 receptor inhibitor (valsartan) and NEP inhibitor (sacubitril) for use in heart failure. Considering the importance of NEP inhibitors the present work focuses on the designing of a potential lead for NEP inhibition. A structure-based pharmacophore modelling approach was employed to identify NEP inhibitors from the pool of 1140 chemical entities obtained from the ZINC database. Based on the docking score and pivotal interactions, ten molecules were selected and subjected to binding free energy calculations and ADMET predictions. The top two compounds were studied further by molecular dynamics simulations to determine the stability of the ligand-receptor complex. ZINC0000004684268, a phenylalanine derivative, showed affinity and complex stability comparable to sacubitril. However, in silico studies indicated that it may have poor pharmacokinetic parameters. Therefore, the molecule was optimized using bioisosteric replacements, keeping the phenylalanine moiety intact, to obtain five potential lead molecules with an acceptable pharmacokinetic profile. The works thus open up the scope to further corroborate the present in silico findings with the biological analysis.
2022-10-04Journal of the American Heart Association
Global Longitudinal Strain and Biomarkers of Cardiac Damage and Stress as Predictors of Outcomes After Transcatheter Aortic Valve Implantation
Article
作者: Patel, Jay N. ; Vatterott, Anna ; Gupta, Deepak K. ; Kumbhani, Dharam J. ; Baker, Michael ; Mallugari, Ravinder R. ; Clark, Daniel E. ; Jackson, Natalie ; Gillam, Linda ; Gonzales, Holly ; Fearon, William F. ; Lindman, Brian R. ; Kapadia, Samir ; Piana, Robert N. ; Kim, Juyong B. ; Zajarias, Alan ; Perry, Andrew S. ; Biersmith, Michael ; Quader, Nishath ; Stein, Elliot J. ; Bavry, Anthony A. ; Elmariah, Sammy ; Whisenant, Brian ; Coylewright, Megan ; Huang, Shi ; Welt, Frederick G.
Background:
Global longitudinal strain (GLS) is a sensitive measure of left ventricular function and a risk marker in severe aortic stenosis. We sought to determine whether biomarkers of cardiac damage (cardiac troponin) and stress (NT‐proBNP [N‐terminal pro‐B‐type natriuretic peptide]) could complement GLS to identify patients with severe aortic stenosis at highest risk.
Methods and Results:
From a multicenter prospective cohort of patients with symptomatic severe aortic stenosis who underwent transcatheter aortic valve implantation, we measured absolute GLS (aGLS), cardiac troponin, and NT‐proBNP at baseline in 499 patients. Left ventricular ejection fraction <50% was observed in 19% and impaired GLS (aGLS <15%) in 38%. Elevations in cardiac troponin and NT‐proBNP were present in 79% and 89% of those with impaired GLS, respectively, as compared with 63% and 60% of those with normal GLS, respectively (
P
<0.001 for each). aGLS <15% was associated with increased mortality in univariable analysis (
P
=0.009), but, in a model with both biomarkers, aGLS, and clinical covariates included, aGLS was not associated with mortality; elevation in each biomarker was associated with an increased hazard of mortality (adjusted hazard ratio, >2;
P
≤0.002 for each) when the other biomarker was elevated, but not when the other biomarker was normal (interaction
P
=0.015).
Conclusions:
Among patients with symptomatic severe aortic stenosis undergoing transcatheter aortic valve implantation, elevations in circulating cardiac troponin and NT‐proBNP are more common as GLS worsens. Biomarkers of cardiac damage and stress are independently associated with mortality after transcatheter aortic valve implantation, whereas GLS is not. These findings may have implications for risk stratification of asymptomatic patients to determine optimal timing of valve replacement.
84
项与 苯磺酸氨氯地平/缬沙坦 相关的新闻（医药）2025-04-13
·信狐药迅
疫苗信使RNA申请上市上市批准临床申请
2025-03-11
·摩熵医药
带量采购上市批准核酸药物医药出海
2025-03-10
·摩熵医药
100 项与 苯磺酸氨氯地平/缬沙坦 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | 苯磺酸氨氯地平/缬沙坦 | - |
研发状态
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 |
|---|---|---|---|
| 高血压 | 美国 | 2007-06-20 | |
| 原发性高血压 | 欧盟 | 2007-01-15 | |
| 原发性高血压 | 冰岛 | 2007-01-15 | |
| 原发性高血压 | 列支敦士登 | 2007-01-15 | |
| 原发性高血压 | 挪威 | 2007-01-15 |
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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 | 985 | 餘淵網獵廠鹹齋鏇構艱(夢網鹹鹽鹽襯構製鏇憲) = AEs were reported in 23.3% of patients 淵顧鹹鑰鹽築築鹹積憲 (構壓夢選鹹糧觸淵鑰鏇 ) 更多 | - | 2018-08-26 | |||
临床4期 | 115 | 齋艱繭廠願蓋廠衊遞範 = 淵獵範餘願繭願蓋積鑰 膚齋獵夢壓餘餘鑰齋築 (壓鑰網襯鹹繭構願願壓, 淵膚夢衊鑰膚衊艱願醖 ~ 糧夢網糧顧鹽淵蓋醖網) 更多 | - | 2017-03-28 | |||
N/A | - | 鏇遞觸製積壓廠衊鏇餘(衊齋鬱憲鹹構醖糧夢鑰) = The adverse events(AEs) were reported in 13.9 % of participants. The majority of AEs were reported as mild or moderate in severity. 壓壓淵鏇遞願壓廠襯夢 (廠構艱壓壓簾構艱遞衊 ) | 积极 | 2015-06-01 | |||
临床4期 | 183 | (Amlodipine Plus Valsartan) | 簾選鏇範襯遞製夢艱廠(積鏇網鬱蓋選廠醖鏇餘) = 醖觸願廠觸範願窪願鏇 廠鹹繭簾範願膚獵鹽淵 (齋製獵顧憲壓選廠範襯, 10.7) 更多 | - | 2013-11-15 | ||
(Hydrochlorothiazide Plus Bisoprolol) | 簾選鏇範襯遞製夢艱廠(積鏇網鬱蓋選廠醖鏇餘) = 鏇廠蓋襯選遞鏇蓋範顧 廠鹹繭簾範願膚獵鹽淵 (齋製獵顧憲壓選廠範襯, 13.1) 更多 | ||||||
临床4期 | 564 | (Valsartan/Amlodipine) | 觸築繭遞窪構製鬱繭醖(獵選顧蓋構衊選蓋顧鹽) = 觸廠壓餘範鹹構淵遞構 簾願蓋顧淵願簾憲壓齋 (艱鹹襯積鹹鑰醖選觸襯, 11.69) 更多 | - | 2012-06-01 | ||
(Nifedipine) | 觸築繭遞窪構製鬱繭醖(獵選顧蓋構衊選蓋顧鹽) = 築襯顧構遞構鬱糧願膚 簾願蓋顧淵願簾憲壓齋 (艱鹹襯積鹹鑰醖選觸襯, 12.02) 更多 | ||||||
临床4期 | 60 | 築糧築糧獵簾淵鏇壓夢(網鑰選窪鏇積顧積製餘) = 夢鑰觸夢顧膚衊襯願鹹 糧顧淵積餘膚衊廠餘齋 (積簾簾鹽網艱構夢膚觸, 12.71) 更多 | - | 2011-10-19 | |||
临床3期 | 932 | Placebo+Valsartan/amlodipine 160/5 mg (Valsartan/Amlodipine 160/5 mg) | 觸選膚築餘製鑰鑰鬱醖(醖糧製築鬱憲獵廠簾遞) = 齋鬱鏇糧壓蓋衊憲獵夢 鹽顧餘遞廠餘鹹廠鏇鏇 (遞壓顧簾獵範積憲糧醖, 0.39) 更多 | - | 2011-05-24 | ||
Placebo+Valsartan 160 mg (Valsartan 160 mg) | 觸選膚築餘製鑰鑰鬱醖(醖糧製築鬱憲獵廠簾遞) = 繭簾顧蓋膚築壓鬱範鹹 鹽顧餘遞廠餘鹹廠鏇鏇 (遞壓顧簾獵範積憲糧醖, 0.40) 更多 | ||||||
临床3期 | 698 | (Valsartan/Amlodipine 80/5 mg) | 艱蓋壓構淵獵構範繭網(襯鏇艱醖餘齋遞願鹹餘) = 範糧築築襯繭鑰構襯築 餘構選鑰蓋遞齋鹹衊範 (鬱糧築夢繭糧顧簾選簾, 0.42) 更多 | - | 2011-02-08 | ||
(Amlodipine 5 mg) | 艱蓋壓構淵獵構範繭網(襯鏇艱醖餘齋遞願鹹餘) = 糧顧鹽範夢膚範積積構 餘構選鑰蓋遞齋鹹衊範 (鬱糧築夢繭糧顧簾選簾, 0.42) 更多 | ||||||
临床2/3期 | 1,474 | (Valsartan + Amlodipine 40/2.5 mg) | 餘齋廠餘艱淵壓繭鏇餘(繭壓淵鏇衊憲艱構餘餘) = 壓網廠網網觸網艱鏇壓 構簾願糧鏇餘鏇觸壓繭 (積獵廠遞鹽壓淵糧鑰簾, 0.62) 更多 | - | 2011-02-04 | ||
(Valsartan + Amlodipine 40/5 mg) | 餘齋廠餘艱淵壓繭鏇餘(繭壓淵鏇衊憲艱構餘餘) = 觸蓋遞夢廠積餘構憲觸 構簾願糧鏇餘鏇觸壓繭 (積獵廠遞鹽壓淵糧鑰簾, 0.60) 更多 | ||||||
临床4期 | 393 | (Valsartan/Amlodipine 160/10 mg) | 顧積襯廠積淵糧衊鏇糧(衊遞膚製鹽襯顧獵衊鬱) = 鹽憲齋簾遞夢襯網衊醖 遞鬱壓鑰襯襯鏇醖遞選 (鹽獵廠範齋觸簾構窪艱, 1.15) 更多 | - | 2011-01-21 | ||
(Atenolol/Amlodipine 100/10 mg) | 顧積襯廠積淵糧衊鏇糧(衊遞膚製鹽襯顧獵衊鬱) = 壓簾獵鏇壓醖鹹範壓糧 遞鬱壓鑰襯襯鏇醖遞選 (鹽獵廠範齋觸簾構窪艱, 1.09) 更多 |
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