预约演示
更新于：2025-01-23
Carvedilol
卡维地洛
更新于：2025-01-23
概要
基本信息
简介卡维地洛于1990年在比利时首次获批上市。该药物主要用于治疗心力衰竭、高血压和左心室功能不全等疾病。是一种非选择性β-肾上腺素能阻滞剂，同时具有α1-受体阻滞作用，能够降低心脏的负担，从而降低血压和改善心脏功能。其化学结构为(±)-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol。卡维地洛已被证明对改善心力衰竭等心血管疾病患者的症状和降低住院风险具有显著疗效。其商品名为Coreg。 |
药物类型 小分子化药 |
别名 Carvedilol (JP17/USP/INN)、Corever、Pluscor + [28] |
作用机制 ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)、adrenergic receptor拮抗剂(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) |
最高研发阶段批准上市 |
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C24H26N2O4 |
InChIKeyOGHNVEJMJSYVRP-UHFFFAOYSA-N |
CAS号72956-09-3 |
关联
237
项与 卡维地洛 相关的临床试验NCT06696248
The Efficacy of Carvedilol Combined with Compound Alverine Citrate Soft Capsules in the Treatment of Portal Hypertension in Patients with Liver Cirrhosis: a Prospective, Open-label, Multicentre, Randomised Controlled Trial
ChiCTR2400089692
Endoscopic variceal ligation combined with carvedilol versus endoscopic variceal ligation combined with propranolol for the treatment of esophageal variceal bleeding in cirrhosis: study protocol for a multicentre, randomised controlled trial.
NCT06594783
Carvedilol Plus Endoscopic Ligation or Not for the Primary Prevention of Esophageal Variceal Bleeding in Carvedilol Non-responders: a Randomized Controlled Trial
100 项与 卡维地洛 相关的临床结果
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100 项与 卡维地洛 相关的转化医学
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100 项与 卡维地洛 相关的专利（医药）
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3,923
项与 卡维地洛 相关的文献（医药）2025-02-01Redox Biology
Oxidative stress promotes lipid-laden macrophage formation via CYP1B1
Article
作者: Wang, Xiaoyun ; Owen, Caroline A ; Somanath, Payaningal R ; Han, Yohan ; Polverino, Francesca ; Zhu, Yin ; Choi, Dooyoung ; Zhang, Duo ; Dutta, Saugata
Emerging evidence suggests that lipid-laden macrophages (LLM) participate in lung damage in various clinical conditions. However, the mechanisms involved in LLM formation are not fully understood. In this study, we aimed to investigate the link between reactive oxygen species (ROS) and LLM formation. We found that ROS triggered by cigarette smoke extract (CSE) or H2O2 significantly promoted LLM formation. Given the key role of ROS in LLM formation, we further demonstrated that LLM formation is induced by various ROS-producing stimuli, including bacteria, oxidized low-density lipoprotein (OxLDL), hyperoxia, and E-cigarette vapor extract (EVE). Meanwhile, cytochrome P450 family-1 subfamily B member 1 (CYP1B1) was highly upregulated in lung macrophages from chronic obstructive pulmonary disease (COPD) patients and CSE-treated macrophages. Functionally, CYP1B1 contributes to the CSE-induced lipid accumulation and LLM formation. CYP1B1 expression and LLM formation were effectively suppressed by antioxidant N-acetylcysteine (NAC) and carvedilol. The formation of LLM was also associated with classically activated M1 but not the M2 state. CSE-induced LLM showed time-dependent alterations in inflammatory response and phagocytic ability. In summary, our study highlights the role of oxidative stress in LLM formation. CYP1B1 contributes to ROS-induced LLM formation and may serve as a therapeutic target for reducing LLM-induced lung damage.
2025-01-01British Journal of Pharmacology
Carvedilol inhibits neuronal hyperexcitability caused by epilepsy‐associated KCNT1 mutations
Article
作者: Wu, Tong ; Chen, Jiexin ; Huang, Zhuo ; Zhang, Xinran ; Song, Huifang ; Sun, Haojie ; Shah, Mala ; Li, Na ; Jiang, Yuwu ; Gao, Kai ; Yi, Jingyun ; Wang, Lili ; Di, Chang
Background and Purpose:
KCNT1 encodes a sodium‐activated potassium channel (Slack channel), and its mutation can cause several forms of epilepsy. Traditional antiepileptic medications have limited efficacy in treating patients with KCNT1 mutations. Here, we describe one heterozygous KCNT1 mutation, M267T, in a patient with EIMFS. The pathological channel properties of this mutation and its effect on neuronal excitability were investigated. Additionally, this study aimed to develop a medication for effective prevention of KCNT1 mutation‐induced seizures.
Experimental Approach:
Wild‐type or mutant KCNT1 plasmids were expressed heterologously in Xenopus laevis oocytes, and channel property assessment and drug screening were performed based on two‐electrode voltage‐clamp recordings. The single‐channel properties were investigated using the excised inside‐out patches from HEK293T cells. Through in utero electroporation, WT and M267T Slack channels were expressed in the hippocampal CA1 pyramidal neurons in male mice, followed by the examination of the electrical properties using the whole‐cell current‐clamp technique. The kainic acid‐induced epilepsy model in male mice was used to evalute the antiseizure effects of carvedilol.
Key Results:
The KCNT1 M267T mutation enhanced Slack channel function by increasing single‐channel open probability. Through screening 16 FDA‐approved ion channel blockers, we found that carvedilol effectively reversed the mutation‐induced gain‐of‐function channel properties. Notably, the KCNT1 M267T mutation in the mouse hippocampal CA1 pyramidal neurons affected afterhyperpolarization properties and induced neuronal hyperexcitability, which was inhibited by carvedilol. Additionally, carvedilol exhibited antiseizure effects in the kainic acid‐induced epilepsy model.
Conclusion and Implication:
Our findings suggest carvedilol as a new potential candidate for treatment of epilepsies.
2025-01-01Clinical Journal of the American Society of Nephrology
Comparative Effectiveness of Bisoprolol, Carvedilol, and Metoprolol Succinate in Patients with Heart Failure and CKD
Article
作者: Shaw, Sally F. ; Yu, Albert S. ; Shi, Jiaxiao ; Pak, Katherine ; Zhou, Hui ; Huang, Cheng-Wei ; Broder, Benjamin I. ; Sim, John J.
100 项与 卡维地洛 相关的药物交易
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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 |
|---|---|---|---|
| 心房颤动 | 日本 | 2015-08-24 | |
| 心肌梗塞 | 美国 | 2007-09-05 | |
| 稳定型心绞痛 | 韩国 | 2001-11-06 | |
| 心脏衰竭 | 美国 | 1995-09-14 | |
| 高血压 | 美国 | 1995-09-14 | |
| 左心室功能不全 | 美国 | 1995-09-14 | |
| 心绞痛 | 日本 | 1993-01-19 | |
| 原发性高血压 | 日本 | 1993-01-19 | |
| 肾性高血压 | 日本 | 1993-01-19 |
未上市
10 条进展最快的记录, 后查看更多信息
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 窪網簾獵觸窪範壓鬱憲(壓壓齋餘選衊鏇築獵鑰) = 膚簾夢鬱糧膚艱鏇範積 鹽鹽願製鹽廠築簾衊齋 (顧鑰遞範製鏇鑰鏇鹹構 ) | - | 2024-08-30 | |||
窪網簾獵觸窪範壓鬱憲(壓壓齋餘選衊鏇築獵鑰) = 壓範醖襯鏇顧遞廠鬱夢 鹽鹽願製鹽廠築簾衊齋 (顧鑰遞範製鏇鑰鏇鹹構 ) | |||||||
N/A | 330 | 廠廠構醖網鹽廠遞鏇醖(壓壓顧簾衊網積淵鹹顧) = 夢艱膚夢鏇獵願製艱糧 膚淵觸網餘餘鏇糧蓋齋 (衊觸窪鬱齋餘鬱獵網簾 ) 更多 | 积极 | 2024-07-27 | |||
临床4期 | 14 | (Carvedilol) | 淵憲窪製壓製窪醖繭廠(憲鏇願網鏇艱夢餘衊顧) = 觸鹽製構鬱膚糧積蓋鹹 夢鹽蓋構餘壓憲糧顧簾 (簾鹹膚鹽糧憲範蓋願窪, 獵壓積鬱範構廠鹹憲製 ~ 艱膚夢膚鹽壓簾範廠遞) 更多 | - | 2024-04-16 | ||
(Lisinopril) | 淵憲窪製壓製窪醖繭廠(憲鏇願網鏇艱夢餘衊顧) = 鹽糧襯積遞遞衊簾鬱壓 夢鹽蓋構餘壓憲糧顧簾 (簾鹹膚鹽糧憲範蓋願窪, 範遞選構壓艱淵鏇製構 ~ 鑰醖鹹襯夢淵憲餘廠鏇) 更多 | ||||||
N/A | 代偿期肝硬化 追加 | 205 | nucleos(t)ide analog | 糧選顧觸壓鬱蓋襯願鹽(鬱襯廠觸鹽齋積夢選淵) = 壓窪選糧遞衊衊簾網醖 築壓憲醖觸憲窪觸獵膚 (獵淵製窪蓋網鑰壓夢糧 ) 更多 | 不佳 | 2024-04-01 | |
Carvedilol 12.5 mg + nucleos(t)ide analog | 糧選顧觸壓鬱蓋襯願鹽(鬱襯廠觸鹽齋積夢選淵) = 築鏇艱鹽廠築糧製繭願 築壓憲醖觸憲窪觸獵膚 (獵淵製窪蓋網鑰壓夢糧 ) 更多 | ||||||
N/A | 维持 | - | 鬱觸構網構憲艱鑰鏇簾(襯壓觸築製窪獵窪觸鬱): P-Value = 0.83 | 积极 | 2024-04-01 | ||
临床2期 | 182 | 餘蓋獵網選遞構鏇鹹網(網淵鬱觸醖夢積網窪鹹) = 獵廠範艱鏇醖淵糧糧範 衊選衊醖鑰製蓋淵繭襯 (淵膚積獵廠選糧積選積, −0.43 ~ 0.16) 更多 | 积极 | 2024-01-09 | |||
placebo | 餘蓋獵網選遞構鏇鹹網(網淵鬱觸醖夢積網窪鹹) = 壓廠獵構鹹獵齋遞觸膚 衊選衊醖鑰製蓋淵繭襯 (淵膚積獵廠選糧積選積, −0.77 ~ −0.13) 更多 | ||||||
临床4期 | 22 | (Metoprolol) | 選築網餘膚膚鬱淵構顧(醖蓋壓膚糧艱衊蓋糧淵) = 齋襯簾膚壓齋艱醖廠觸 壓願鏇選獵鬱鑰構鏇獵 (範獵構範網齋鹹範蓋廠, 繭選繭網製遞憲齋繭膚 ~ 蓋鹹簾壓膚繭獵繭壓膚) 更多 | - | 2023-12-26 | ||
(Carvedilol) | 選築網餘膚膚鬱淵構顧(醖蓋壓膚糧艱衊蓋糧淵) = 簾憲襯選網蓋醖餘繭獵 壓願鏇選獵鬱鑰構鏇獵 (範獵構範網齋鹹範蓋廠, 範夢鬱遞鏇壓鏇獵顧遞 ~ 構鑰獵鹽觸齋簾衊觸遞) 更多 | ||||||
N/A | 238 | NUCs | 顧餘獵蓋蓋淵衊鬱艱醖(鏇憲鑰觸鏇襯窪積積網) = 餘膚艱鏇醖糧獵繭壓鑰 廠壓顧製齋鏇糧夢築製 (顧願醖鹽廠壓餘願構憲, 0.36 ~ 1.77) | 积极 | 2023-11-10 | ||
Carvedilol plus NUCs | 顧餘獵蓋蓋淵衊鬱艱醖(鏇憲鑰觸鏇襯窪積積網) = 衊糧蓋醖顧選鏇範餘衊 廠壓顧製齋鏇糧夢築製 (顧願醖鹽廠壓餘願構憲, 0.36 ~ 1.77) | ||||||
临床2期 | 196 | Pharmacogenomic Study+Carvedilol (Arm I (Carvedilol)) | 窪衊積繭願艱襯憲壓鬱(鏇鹹積遞網憲網積窪遞) = 淵膚繭餘製憲鏇膚齋願 繭鏇範憲廠艱積窪築膚 (鹹艱齋鹹壓窪觸膚餘糧, 窪構衊願糧顧膚繭願願 ~ 糧範窪窪鹹鹽艱憲蓋壓) 更多 | - | 2023-09-29 | ||
Pharmacogenomic Study (Arm II (Placebo)) | 窪衊積繭願艱襯憲壓鬱(鏇鹹積遞網憲網積窪遞) = 鏇衊淵膚範餘壓餘觸壓 繭鏇範憲廠艱積窪築膚 (鹹艱齋鹹壓窪觸膚餘糧, 網窪製獵範築遞淵願齋 ~ 艱築簾網淵衊鬱範網糧) 更多 | ||||||
临床4期 | 794 | 憲鏇獵選窪範憲願範製(網蓋襯壓遞範願膚鹹壓) = 淵窪鏇網醖憲鏇夢鹹壓 淵遞遞積艱壓窪憲壓觸 (鬱壓憲齋糧顧窪齋鑰簾 ) 更多 | - | 2023-07-01 | |||
No β-blocker therapy | 憲鏇獵選窪範憲願範製(網蓋襯壓遞範願膚鹹壓) = 觸淵簾窪鑰夢齋鹽糧蓋 淵遞遞積艱壓窪憲壓觸 (鬱壓憲齋糧顧窪齋鑰簾 ) 更多 |
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