盐酸奈必洛尔/缬沙坦(Nebivolol Hydrochloride/Valsartan) - 药物靶点：AT1R x β1-adrenergic receptor_在研适应症：高血压_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Byvalson、Nebivolol/valsartan、Valsartan/nebivolol

靶点

AT1R x β1-adrenergic receptor

作用机制

AT1R拮抗剂(血管紧张素II-1型受体拮抗剂)、β1-adrenergic receptor拮抗剂(β1-肾上腺素能受体拮抗剂)

治疗领域

心血管疾病

在研适应症

高血压

非在研适应症-

原研机构

Allergan Ltd. (Ireland)

在研机构

Prinston Pharmaceutical, Inc.

非在研机构

AbbVie, Inc.

最高研发阶段批准上市

首次获批日期

美国 (2016-06-03),

高血压

最高研发阶段(中国)-

特殊审评-

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结构

分子式C46H54F2N6O7

InChIKeySCTCSYRLAUPSSW-KXUDKMLBSA-N

CAS号1562428-72-1

关联

2

项与盐酸奈必洛尔/缬沙坦相关的临床试验

NCT05170061 / Completed临床3期IIT

Ambulatory 24-Hour Cardiac Oxygen Consumption and Blood Pressure-Heart Rate Variability: Effects of Nebivolol and Valsartan Alone and in Combination

A randomized,double-blind,double-dummy,active controlled,15 week study to evaluate the effects of nebivolol and valsartan alone and in combination on 24-hour ambulatory cardiac work and variability of heart rate-mean central systolic pressure product.

开始日期2013-02-01

申办/合作机构

State University of New York at Buffalo

NCT01415505 / Completed临床3期

A Multicenter, Open-Label, Single-Arm, Free Tablet Combination, Long-Term Study to Evaluate the Safety of Nebivolol in Combination With Valsartan in Patients With Stage 1 or Stage 2 Essential Hypertension

The purpose of this study is to evaluate the safety and tolerability of nebivolol and valsartan given as a free tablet combination in patient with stage 1 or stage 2 essential hypertension.

开始日期2011-08-01

申办/合作机构

Forest Laboratories, Inc.

100 项与盐酸奈必洛尔/缬沙坦相关的临床结果

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100 项与盐酸奈必洛尔/缬沙坦相关的转化医学

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100 项与盐酸奈必洛尔/缬沙坦相关的专利（医药）

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3

项与盐酸奈必洛尔/缬沙坦相关的文献（医药）

2023-09-01·Journal of AOAC International

A Novel, Sustainable, and Eco-Friendly Spectrophotometric and Chemometric Approach for Determination of Severely Overlapped Spectrum via Unified Regression Equation: Greenness and Whiteness Assessment.

Article

作者: Farouk, Maha ; Hemdan, Ahmed ; Fares, Nermine V ; Magdy, Ragaa

BACKGROUNDNebivolol and valsartan (VAL) in combination with each other successfully control blood pressure and improve hypertension patient outcomes.OBJECTIVETo develop and validate innovative, simple, and sustainable spectrophotometric methods for the simultaneous analysis of nebivolol and valsartan.METHODThe new modified difference amplitude modulation (MD-AM) method uses only unified regression equation and does not require any resolution techniques. Other different approaches were also applied for the determination of the same mixture including univariate and multivariate spectrophotometric methods. The multivariate methods were PLS and PCR, whereas the univariate methods were derivative ratio (DD1), ratio difference (RD), constant center (CC), constant center spectrum subtraction (CC-SS), constant value coupled with amplitude difference (CV-AD), advanced concentration value (ACV), and amplitude difference (AD). The proposed methods use a green solvent; thus, the environmental impact of the presented procedures was evaluated qualitatively and quantitatively using six well-known evaluation tools.RESULTSAll methods were applied successfully for the analysis of the studied drugs in their bulk powder, pharmaceutical dosage form Byvalson®, and in vitro release at intestinal pH (7.4) using a USP dissolution tester. Results obtained were compared statistically with the reported method and with each other using a one-way ANOVA statistical test, and no significant differences were found.CONCLUSIONSAll green and white analytical chemistry evaluation tools results confirm the safety, sustainability, and cost-effectiveness of the approaches, indicating that the methods are regarded green and sustainable. Results were agreeable, encouraging their applicability in quality control laboratories for dosage form and making these methods an eco-friendly substitute for the analysis of this combined dosage form and for evaluating the dissolution profile.HIGHLIGHTSFor the first time, a severely overlapped spectrum was determined using a unified regression equation without the need of extended part or zero contribution regions by the novel method MD-AM. The proposed methods are the first study of in vitro dissolution profiling of nebivolol hydrochloride (NEB) and VAL and the first sustainable and green methods applied without compromising the analytical criteria.

2018-08-01·Pharmacology & Therapeutics1区 · 医学

Discovery of Leonuri and therapeutical applications: From bench to bedside

1区 · 医学

Review

作者: Yi Zhun Zhu ; Xinhua Liu ; Qing Zhu ; Weijun Wu

Despite several advances in percutaneous coronary intervention and the discovery of new drugs, the incidence of myocardial infarction and deaths due to cardiovascular diseases (CVD) has not decreased markedly in China. The quality of life is affected seriously, which further results in great social and family burden. Many drugs, from the century-old aspirin to the newly FDA-approved Byvalson, have been proven to be effective in the treatment and prevention of CVD. As clinically reported, those life-saving drugs still have their side effects in regards to the narrow therapeutic indexes influenced by individual genetic variations. Herba Leonuri, also known as Chinese Motherwort, which are naturally present in plants and traditionally are used for the uterotonic action, postpartum blood stasis, breast pain as well as other gynecological disorders in China for thousands of years. Since the last two decades, our group has reported leonurine, a unique alkaloid found in Herba Leonuri, exhibits various bioactivities such as antioxidant, anti-apoptotic effects, free radical scavenging and anti-inflammatory effects, in addition to improving micro-circulation. These bioactivities are related to the underlying mechanisms of ischemic heart diseases and cardiac fibrosis. Pharmacological studies have proven leonurine to be effective in treating CVD in various ways, particularly ischemic heart diseases. Besides the cardio protective effects, which are similar in the central nervous system, more specifically, inhibited mitochondrial reactive oxygen species production together with the restored mitochondrial function and redox state were observed in middle cerebral artery occlusion rats by leonurine treatment, which strongly reveals its neuroprotective effects and carries a therapeutic potential for recovery and prevention of stroke. Based on their mode of action, we propose that leonurine can be developed as drugs to treat ischemic heart diseases. Taking advantage of the most recent findings in pharmacological research including the effects of low toxicity and good pharmacokinetics characteristics, leonurine has a very attractive prospect of clinical application. Our recent promising pharmacological results may be able to eradicate the barrier hindering its sale on market. In sum, from bench to bedside is no longer a long way for leonurine.

2016-09-12·The Medical letter on drugs and therapeutics4区 · 医学

Byvalson--a beta blocker/ARB combination for hypertension.

4区 · 医学

Article

100 项与盐酸奈必洛尔/缬沙坦相关的药物交易

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