磷酸卡维地洛(Carvedilol Phosphate) - 药物靶点：α-adrenergic receptor x β1-adrenergic receptor_在研适应症：心脏衰竭，高血压，左心室功能不全_专利_临床

概要

基本信息

药物类型

小分子化药

别名

COREG MR、Carvedilol、Carvedilol phosphate (USAN)

+ [4]

靶点

α-adrenergic receptor x β1-adrenergic receptor

作用机制

α-adrenergic receptor拮抗剂(α-肾上腺素能受体家族拮抗剂)、β1-adrenergic receptor拮抗剂(β1-肾上腺素能受体拮抗剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Waylis Therapeutics LLC

非在研机构

GSK Plc

最高研发阶段批准上市

首次获批日期

美国 (2006-10-20),

心脏衰竭高血压左心室功能不全

最高研发阶段(中国)-

特殊审评-

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结构

分子式C48H60N4O17P2

InChIKeyLHNYXTULDSJZRB-UHFFFAOYSA-N

CAS号610309-89-2

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关联

19

项与磷酸卡维地洛相关的临床试验

RBR-4ccdqh6 / Active, not recruitingN/AIIT

Removable Partial Dentures with Co-Cr versus PEEK structure: clinical crossover study

开始日期2022-01-01

申办/合作机构-

NCT03169426 / Completed临床4期IIT

Effect of Beta-blocker on Cardioprotective Effect of Remote Ischemic Conditioning

Remote ischemic conditioning has been shown to protect myocardium from ischemia-reperfusion injury during cardiac intervention or cardiac surgery. However, effect of beta-blocker, commonly used cardiovascular medication in patients with cardiac diseases such as hypertension or angina pectoris, on cardioprotective role of remote ischemic conditioning has not been well documented. The purpose of the study is to investigate the effect of beta-blocker on remote ischemic conditioning in healthy volunteers.

开始日期2017-05-17

申办/合作机构

Seoul National University Hospital

CTR20150261 / Active, not recruiting

硫酸卡维地洛缓释胶囊（规格：72 mg）在中国健康男性受试者中的单次剂量、随机、开放生物等效性研究

研究健康男性受试者在空腹状态或进食高脂食物后，单次口服由江苏恒瑞医药股份有限公司生产的硫酸卡维地洛缓释胶囊（规格：72 mg）和葛兰素史克制药有限公司生产的磷酸卡维地洛缓释胶囊的相对生物利用度，评价两制剂间的生物等效性。评价食物对硫酸卡维地洛缓释胶囊（规格：72 mg）人体内生物利用度的影响。

开始日期2014-09-30

申办/合作机构

江苏恒瑞医药股份有限公司

100 项与磷酸卡维地洛相关的临床结果

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100 项与磷酸卡维地洛相关的转化医学

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100 项与磷酸卡维地洛相关的专利（医药）

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20

项与磷酸卡维地洛相关的文献（医药）

2022-10-01·Journal of Pharmaceutical and Biomedical Analysis

Functional group-specific multilateral derivatization cum extraction method for simultaneous quantification of genotoxic impurities in carvedilol phosphate drug using GC-MS and their toxicity assessments

Article

作者: Thenmozhi, Kathavarayan ; Elumalai, Sambandan ; Sabarinathan, Subbaramanian ; Ponnusamy, Vinoth Kumar ; Senthilkumar, Sellappan

A simple and facile functional group-specific multilateral derivatization cum extraction method coupled with GC-MS based analytical methodology has been developed for the rapid identification and determination of five potential genotoxic impurities (GTIs), including epichlorohydrin, hydrazine, phenylhydrazine, 3-chloro-1,2-propanediol and 1-(2-chloroethoxy)- 2-methoxybenzene in the carvedilol phosphate (CRV-P) drug active pharmaceutical ingredient (API). A generic synthetic route has been explored to apply the current investigation to the majority of the market available synthetic routes for the carvedilol process. Five significant GTIs were identified, and their toxicity was examined using in-silico model. The pharmacokinetic and pharmacodynamic properties of the impurities were compared with the drug molecule to evince the associated risk of impurities during therapeutic action. Furthermore, a quantitative comparison has been made for each impurity with the drug molecule for their ADMET properties, and the potential nature of the impurities has been thoroughly assessed. The developed method encompasses simple derivatization cum extraction-oriented GC-MS method for the reported GTIs, which was also validated as per current ICH guidelines. The obtained LOD and LOQ for the method were between 0.06 ~ 0.61 µg/g and 0.17 ~ 1.8 µg/g, respectively, and the r² values (0.994 ~ 0.997) show that the method is very sensitive and linear over a wide range (LOQ to 120 % of the target concentration). The percentage recoveries and relative standard deviation obtained were between 85.3 and 109.5 and 0.1-4.7, respectively, showing fit for purpose. Moreover, method precision, intermediate precision, and robustness of the method have also been successfully demonstrated. Thus, this method could be directly engaged as the quality forecasting tool for the marketed drug samples aimed at the estimation of the reported GTIs at trace level.

2019-04-01·Carbohydrate Polymers1区 · 化学

Smart karaya-locust bean gum hydrogel particles for the treatment of hypertension: Optimization by factorial design and pre-clinical evaluation

1区 · 化学

Article

作者: Sen, Kalyan Kumar ; Laha, Bibek ; Maiti, Sabyasachi ; Goswami, Rimpa

This investigation was undertaken to unveil the controlled drug delivery and preclinical anti-hypertensive potential of a novel interpenetrating biopolymer-based network of karaya gum and carboxymethyl locust bean gum (CLBG). The Williamson synthesis of CLBG was confirmed after analyzing FTIR spectra, degree of O-carboxymethyl group substitution and viscosity. The hydrogel particles (HPs) were developed using aluminium chloride solution as cross-linker. A full 3² factorial design approach was adopted for the optimization of two responses: drug entrapment efficiency and drug release (%) in simulated gastrointestinal conditions at 10 h. FE-SEM images and EDX spectra supported the formation of spherical HPs and successful entrapment of the drug in the HPs. Depending upon formulation variables, the drug entrapment efficiency of the HPs lied in the range of 84-98%. The HP matrix was chemically compatible for carvedilol phosphate as was suggested by infrared, thermal and x-ray analyses. The swelling kinetics of HPs corroborated well with the pH-dependent in vitro drug discharge characteristics. The drug release from HPs was found to follow anomalous transport mechanism with varying contribution of simple diffusion and polymer relaxation as was elucidated by Peppas-Sahlin model equation. Preclinical data suggested that the optimized HPs had an excellent blood pressure lowering activity in male Swiss albino mice up to 10 h.

2017-06-01·American Heart Journal2区 · 医学

Lisinopril or Coreg CR in reducing cardiotoxicity in women with breast cancer receiving trastuzumab: A rationale and design of a randomized clinical trial

2区 · 医学

Article

作者: Krischer, Jeffrey ; Guglin, Maya ; Munster, Pamela ; Fink, Angelina

BACKGROUNDTrastuzumab (TZB) is an established therapy for HER2-positive breast cancer. The use of TZB is commonly associated with cardiotoxicity manifesting as asymptomatic decrease in left ventricular ejection fraction (LVEF) or overt heart failure. Several studies demonstrated favorable effects of angiotensin-converting enzyme (ACE) inhibitors and β-blockers (BBs) in the prevention of chemotherapy-induced cardiotoxicity. We hypothesize that patients, randomized to receive an ACE inhibitor or a BB during trastuzumab therapy for breast cancer, will maintain a higher LVEF than patients randomized to placebo.METHODS AND RESULTSWe designed a prospective, multicenter, randomized, phase II placebo-controlled clinical trial to evaluate the effects of an ACE inhibitor (lisinopril) and a BB (carvedilol phosphate-extended release) on cardiotoxicity in patients with breast cancer who are receiving adjuvant or neoadjuvant TZB therapy. The primary objectives include (1) comparison of incidence of cardiotoxicity and (2) comparison of LVEF as a continuous variable in between the arms. Cardiotoxicity was defined as an absolute decrease in LVEF from baseline of ≥10% at follow-up or an absolute decrease of ≥5% in LVEF from baseline for individuals with <50% LVEF at follow-up. The target accrual is 468 participants, representing patients both with and without anthracycline exposure. The enrollment is completed. The trial is co-sponsored by University of South Florida and National Cancer Institute. The LVEF is being evaluated by echocardiography or multigated acquisition scan.CONCLUSIONSIf we can demonstrate that the use of an ACE inhibitor or a BB can reduce the degree of TZB-induced cardiotoxicity, it is hoped that patients will receive complete and uninterrupted TZB therapy for breast cancer without compromising cardiac function.

100 项与磷酸卡维地洛相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03415	磷酸卡维地洛	C07AG02	DB01136

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
心脏衰竭	美国	Waylis Therapeutics LLC	2006-10-20
高血压	美国	Waylis Therapeutics LLC	2006-10-20
左心室功能不全	美国	Waylis Therapeutics LLC	2006-10-20

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
原发性高血压	临床1期	美国	GSK Plc	2007-10-01
高血压	临床1期	美国	GSK Plc	2006-01-05
高血压	临床1期	波多黎各	GSK Plc	2006-01-05
高血压	临床1期	加拿大	GSK Plc	2006-01-05

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01009918 (Lisinopril or Coreg CR in Reducing Side Effects in Women With Breast Cancer Receiving Trastuzumab, CTgov)	临床2期	心脏毒性 \| 乳腺癌	468	lisinopril (Arm I Lisinopril)	鹽淵壓蓋鏇餘壓餘鏇窪(夢鏇繭艱範蓋觸膚鬱蓋) = 製製壓積願醖壓築餘積鏇蓋齋醖顧齋願築鏇網 (積範憲衊蓋憲窪築膚醖, 簾製願淵憲簾鑰窪範艱 ~ 製觸築窪糧齋憲構築壓) 更多	-	2021-03-30
				Coreg CR® (Arm II Coreg CR®)	鹽淵壓蓋鏇餘壓餘鏇窪(夢鏇繭艱範蓋觸膚鬱蓋) = 艱廠夢顧鏇糧夢鬱淵鹹鏇蓋齋醖顧齋願築鏇網 (積範憲衊蓋憲窪築膚醖, 積窪餘繭鑰壓壓窪餘憲 ~ 衊壓淵願壓衊鬱遞艱觸) 更多
NCT00742508 (CTgov)	临床1期	慢性心力衰竭	41	CRV-IR+carvedilol (CRV) (CRV-IR)	蓋壓鑰艱艱鏇願範醖範(餘積糧鏇醖憲鹹觸簾艱) = 鏇願製夢繭製膚鏇鹹觸糧繭壓繭範鹽積獵獵夢 (遞膚淵積顧築窪鑰憲餘, 獵壓觸鏇鏇窪夢顧獵淵 ~ 遞醖齋獵繭餘齋鹽獵願) 更多	-	2010-08-19
				carvedilol (SK&F-105517-D)+SK&F-105517-D (SK&F-105517-D)	蓋壓鑰艱艱鏇願範醖範(餘積糧鏇醖憲鹹觸簾艱) = 觸齋範糧積獵廠願衊繭糧繭壓繭範鹽積獵獵夢 (遞膚淵積顧築窪鑰憲餘, 簾鏇鬱遞齋製構繭廠淵 ~ 襯蓋壓襯鑰獵鹽廠觸獵) 更多
NCT00273052 (CTgov)	临床3期	高血压	514	Carvedilol Phosphate (Coreg CR)	襯選觸選膚願窪獵醖襯(積築糧構構範顧襯觸膚) = 壓衊壓壓繭齋壓願鹹憲壓淵鏇鏇衊遞廠壓選鹽 (範鹹蓋夢齋糧憲觸餘網, 鹽糧獵淵繭願積製範壓 ~ 餘鑰築範鬱鹽顧獵鬱糧) 更多	-	2010-02-01
				Toprol XL (Toprol XL)	襯選觸選膚願窪獵醖襯(積築糧構構範顧襯觸膚) = 齋蓋廠艱淵齋築鹽鬱淵壓淵鏇鏇衊遞廠壓選鹽 (範鹹蓋夢齋糧憲觸餘網, 糧獵齋壓蓋鏇製構廠膚 ~ 選壓醖鹹鹹廠衊夢網製) 更多