磷酸卡维地洛(Carvedilol Phosphate) - 药物靶点：α-adrenergic receptor x β1-adrenergic receptor_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

作用方式

拮抗剂

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

心血管疾病

在研适应症-

非在研适应症

慢性心力衰竭原发性高血压心脏衰竭+ [3]

原研机构

GSK Plc

在研机构-

非在研机构

GSK PlcWaylis Therapeutics LLC

权益机构-

最高研发阶段撤市

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/序列

分子式C48H60N4O17P2

InChIKeyLHNYXTULDSJZRB-UHFFFAOYSA-N

CAS号610309-89-2

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关联

18

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-

CTR20150261

/ Active, not recruitingN/A

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

CTR20150260

/ Active, not recruiting临床1期

硫酸卡维地洛缓释胶囊（规格：9 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：9 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：9 mg）人体内生物利用度的影响。

开始日期2014-08-17

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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4,974

项与磷酸卡维地洛相关的文献（医药）

2025-06-01·Carbohydrate Polymers

Bespoke hydroxypropyl methylcellulose-based solid foams loaded with poorly soluble drugs by tunable modular design

Article

作者: He, Wuzhong ; Genina, Natalja ; Mu, Huiling

A tunable modular design (TMD) as a new approach was proposed to tailor the dose and drug release profile of poorly water-soluble drugs from hydroxypropyl methylcellulose (HPMC)-based solid foams by combining two manufacturing principles: (1) freeze-drying aqueous HPMC-based gels to yield porous sturdy modules with specific doses of an active pharmaceutical ingredient (API) with the step size of 3 mg, and (2) fine-tuning the desired dose of the API with the step size of 0.1 mg by inkjet printing of the API-loaded ink onto the modules. Carvedilol (CAR) was used as a model poorly water-soluble API that requires frequent dose adjustment. The limitation of poor CAR solubility was overcome by designing pharmaceutically approved co-solvent systems. This approach ensured printable inks of a high drug content, and sturdy and flexible modules with uniform distribution of CAR to achieve effective and accurate doses of CAR. The tailored release rate of CAR from TMD products was succeeded by varying the composition, particularly, the content and grade of HPMC, and physical dimensions of modules. The TMD approach holds potential for designing bespoke high-quality products, containing hydrophilic cellulose ethers such as HPMC and poorly water-soluble APIs.

2025-05-01·Drug Delivery and Translational Research

In vitro and in vivo evaluation of in situ forming polyester implants for the extended release of carvedilol

Article

作者: Alsalem, Mohammad ; Saed, Husam ; Shnewer, Khaldoun ; Abulateefeh, Samer R ; Abuhamdan, Raghad M

Polyester based in situ forming implants (ISFIs) are injectable long-acting drug delivery systems that offer a wide range of unique advantages. As a result of these advantages, two relatively high molecular weight, ester terminated grades of poly (D,L-lactide-co-glycolide) (PLGA) and poly(D,L-lactide) (PLA) were evaluated for their ability (i) to form ISFIs loaded with carvedilol, and (ii) to control its release both in vitro and in vivo. At a polymeric concentration of 40% w/w, implant solutions were syringeable, injectable, and able to encapsulate carvedilol to a high degree (encapsulated drug% > 97%). When visualized using scanning electron microscopy (SEM), implants were found to have a dense thin surface atop porous sublayers. As for their in vitro evaluation, PLGA and PLA implants were able to maintain drug release over the course of 49 and 84 days, respectively. On the other hand, in vivo drug release from both implants was almost identical and lasted for only 42 days. This may be due to the overriding effect of the similar host environment at the injection site that diminished the effect of polymeric physiochemistry on phase inversion and drug release. Lastly, while the polymer-free drug/NMP solution completely released its drug content within the initial half hour in vitro, the formulation extended drug release in vivo. This could be due to a yet to be investigated interaction between carvedilol and NMP under in vivo conditions. These results cement the significance of formulating carvedilol loaded ISFIs for the management of chronic conditions.

2025-03-24·Journal of Biomolecular Structure and Dynamics

Bioprospecting of Meliaceae family phytomolecules for the treatment of monkeypox virus infection: a QSAR modeling and MD simulation approach

Article

作者: AlShehail, Bashayer M. ; Al Kaabi, Nawal A. ; Alotaibi, Nouf ; Alissa, Mohammed ; Alsomali, Ghaneema ; Alqahtani, Ali S. ; Al-Subaie, Maha F. ; Rabaan, Ali A. ; Almansour, Zainab H. ; Alshehri, Ahmad A. ; Halwani, Muhammad A. ; Khamis, Faryal

Recent monkeypox virus (MPXV) infections show the risk of MPXV transmission that persists today and the significance of surveillance and quick response methods to stop the virus's spread. Currently, the monkeypox virus infection is not specifically treated. In this study, QSAR models were designed using known inhibitors of cysteine proteinase from the vaccinia virus, where the Random Forest model and Ridge model had showed the best correlation between predicted and observed EC₅₀. These models were used to screen Maliaceae family phytochemicals against MPXV cysteine proteinase. The compound, IMPHY010637 was detected in top 5 from both the QSAR screening models and showed best docked score (-8.6 kcal/mol) and thus selected for further investigation. Further, the IMPHY010637 showed interaction with the catalytic residue His²⁴¹ of the protein as reported in earlier studies. The ADMET analysis of the compound showed the acceptable drug-like properties of IMPHY010637. However, these properties could be improved after experimental validation of protein-ligand binding. Both docked complex and poses created in 100 ns MD simulation of the protein-ligand complex showed the presence of multiple hydrogen bonds. RMSD and conformation analysis showed stable binding of IMPHY010637 with the cysteine proteinase of MPXV at its active site. Compared to the known inhibitor, IMPHY010637 showed better binding with the protein as observed by the PCA and MM/GBSA analysis. This study concluded IMPHY010637 as a potential inhibitor for the cysteine proteinase of MPXV using computational methods that could be tested in in-vitro experiments.

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

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
慢性心力衰竭	临床1期	日本	GSK Plc	2008-08-28
高血压前期	临床1期	美国	GSK Plc	2007-11-01
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	Waylis Therapeutics LLC	2006-10-20

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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)	願廠憲鹹淵蓋醖鬱鹹簾(選淵獵淵艱觸夢窪鬱選) = 觸願窪鹹製壓醖夢醖鹹糧鬱鹽選艱艱鏇餘積艱 (襯夢鹽鹹餘觸廠憲艱淵, 憲艱糧糧網網鏇製顧獵 ~ 衊選廠襯壓構鏇簾餘醖) 更多	-	2021-03-30
				Coreg CR® (Arm II Coreg CR®)	願廠憲鹹淵蓋醖鬱鹹簾(選淵獵淵艱觸夢窪鬱選) = 糧範艱膚顧鏇壓襯膚築糧鬱鹽選艱艱鏇餘積艱 (襯夢鹽鹹餘觸廠憲艱淵, 積繭蓋壓鏇齋窪廠憲網 ~ 蓋鑰構選衊廠願齋築淵) 更多
NCT00742508 (CTgov)	临床1期	慢性心力衰竭	41	CRV-IR+carvedilol (CRV) (CRV-IR)	觸膚衊願齋願獵憲膚鑰(觸網艱願構範顧糧醖廠) = 網鹽壓鬱鏇選範顧壓糧觸範遞艱範網築憲範遞 (範築艱鏇獵襯網獵獵範, 餘遞鹹襯糧鑰淵顧壓願 ~ 廠範鏇艱鹹範鏇餘構願) 更多	-	2010-08-19
				carvedilol (SK&F-105517-D)+SK&F-105517-D (SK&F-105517-D)	觸膚衊願齋願獵憲膚鑰(觸網艱願構範顧糧醖廠) = 壓淵簾壓醖鏇繭鑰構艱觸範遞艱範網築憲範遞 (範築艱鏇獵襯網獵獵範, 鹽醖廠糧廠糧繭淵衊製 ~ 淵網醖觸鬱鏇範鹹繭膚) 更多
NCT00273052 (CTgov)	临床3期	高血压	514	Carvedilol Phosphate (Coreg CR)	鏇衊窪壓簾願衊遞鏇鹹(艱鹹範夢糧襯範鏇鹹繭) = 夢鏇膚遞鏇餘願鏇艱積獵蓋餘願網範製窪鬱獵 (齋遞範繭蓋憲鹽選憲構, 窪糧願製衊鹽鏇顧築齋 ~ 餘顧鹹積製夢構窪觸網) 更多	-	2010-02-01
				Toprol XL (Toprol XL)	鏇衊窪壓簾願衊遞鏇鹹(艱鹹範夢糧襯範鏇鹹繭) = 齋壓壓範製鑰範鏇壓鏇獵蓋餘願網範製窪鬱獵 (齋遞範繭蓋憲鹽選憲構, 襯築築齋構網蓋淵夢窪 ~ 繭繭願蓋網衊餘夢夢製) 更多