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更新于：2025-01-23
Levosimendan
左西孟旦
更新于：2025-01-23
概要
基本信息
药物类型 小分子化药 |
别名 Daxim、Levosimendan (USAN/INN)、NSC-759644 + [8] |
靶点 |
作用机制 PDE3抑制剂(磷酸二酯酶3抑制剂) |
在研适应症 |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 瑞典 (2001-04-10), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C14H12N6O |
InChIKeyWHXMKTBCFHIYNQ-SECBINFHSA-N |
CAS号141505-33-1 |
关联
173
项与 左西孟旦 相关的临床试验NCT06478667
The Role of Levosimendan As Inotropic Agent in Acute Aluminum Phosphide-induced Cardiotoxicity: a Randomized Controlled Trial
ChiCTR2400091067
Clinical analysis of Levosimendan associated arrhythmia in Heart Failure patients
CTIS2023-508024-36-00
Effects of Levosimendan in patients being weaned from venoarterial extracorporal membrane oxygenation. A randomized controlled investigator driven phase II trial
100 项与 左西孟旦 相关的临床结果
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100 项与 左西孟旦 相关的转化医学
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100 项与 左西孟旦 相关的专利（医药）
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1,750
项与 左西孟旦 相关的文献（医药）2025-04-01JOURNAL OF CRITICAL CARE
Effect of pulmonary artery catheter, type & combination of vasoactives for optimizing lactate clearance in acute myocardial infarction complicated by cardiogenic shock
Article
作者: Sierra-Lara-Martínez, Daniel ; Gopar-Nieto, Rodrigo ; Hernández-Montfort, Jaime ; Arzate-Ramírez, Arturo ; Arias-Mendoza, Alexandra ; Mendoza-García, Salvador ; Montañez-Orozco, Álvaro ; Ortega-Hernández, Jorge A ; Altamirano-Castillo, Alfredo ; García-Ruiz, Mauricio ; Baeza-Herrera, Luis Augusto ; Araiza-Garaygordobil, Diego ; Valdespino Trejo, Adrian Aquiles ; González-Pacheco, Héctor ; Manzur-Sandoval, Daniel
INTRODUCTION:
Lactate clearance(LC) is critical in managing critically ill patients. We hypothesized that treatment allocation with different vasoactive drugs or the presence of a pulmonary artery catheter (PAC) could affect the behavior of lactate dynamics and, ultimately, the mortality in AMI-CS.
MATERIALS AND METHODS:
In 651 patients with AMI-CS, we examined the relationship of LC time with clinical, laboratory, and CS-management variables. Complete LC time was defined as serum lactate levels less than <2 mmol/L. We explore the impact of vasoactive drugs and PAC with LC. The CART method defined the vasoactive combinations (permutations) in relation with early (<96 h) complete LC.
RESULTS:
PAC presence correlated with faster LC (-17.54 h) and was independently associated with lower mortality (HR = 0.61). Levosimendan and dobutamine were associated with lower lactate levels and faster LC (-8.82 & -8.77 h), while vasopressin was linked to slower LC (9.16 h). Slow LC (>96 h) was associated with increased mortality. CART analysis identified specific vasoactive drug combinations associated lactate clearance and mortality, without dobutamine, with vasopressin having higher mortality (80.6 %, HR = 5.53), and with dobutamine, with norepinephrine, without vasopressin, with levosimendan the lowest (35 %) and higher complete LC and a trend for higher %LC.
CONCLUSION:
The right combination of vasoactive medications and the probable use of a PAC could significantly impact the achievement of complete LC in <96 h. The findings support the need for further research and the development of strategies to optimize lactate clearance and improve overall patient survival in this high-risk population.
2025-03-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Highly sensitive ultra-high-performance liquid chromatography coupled with tandem mass spectrometry method for the multiplex analysis of levosimendan and its metabolites OR-1855 and OR-1896 in human plasma
Article
作者: Schneider, Antoine ; Giraud, Raphaël ; Livio, Françoise ; Choong, Eva ; Decosterd, Laurent A ; Mercier, Thomas ; Versace, François ; Sauvain, Geraldine ; Girardin, François R ; Murisier, Amarande ; Buclin, Thierry ; Perez, Maria-Helena ; Haefliger, David ; Bertin, Stéphane
Levosimendan is a positive inotrope and vasodilator used in patients with acute and chronic decompensated heart failure. It is metabolized into OR-1855 (inactive metabolite), which is further acetylated into OR-1896 (active metabolite having a prolonged half-life, hence a sustained effect). Levosimendan represents a valuable alternative to traditional inotropes with broad clinical applications in critically ill patients with cardiogenic shock, advanced heart failure and post-cardiac surgery. However, while levosimendan demonstrates dose-dependent hemodynamic effects, its pharmacokinetics has not yet been investigated in adult critically ill patients, a vulnerable population characterized by complex and unstable conditions that may significantly alter drug disposition. Therefore, pharmacokinetics studies of levosimendan and metabolites in critically ill patients require a reliable and sensitive quantification method. We developed and validated a highly sensitive method using ultra-high-performance liquid-chromatography coupled to tandem mass spectrometry (UHPLC-MS/MS) for the quantification of levosimendan, OR-1855 and OR-1896 in human plasma. To achieve the required analytical sensitivity, plasma sample preparation included protein precipitation with acetonitrile, subsequent supernatant's evaporation to dryness under nitrogen, and reconstitution of the solid residues with a solution of H2O:MeOH 4:1, followed by a 40 µL-aliquot injection into the LC column. Chromatographic separation of the three analytes was achieved in a 6-minute run in gradient mode, using an Acquity UPLC BEH C18 1.7 µm, 2.1 × 150 mm column. The method was extensively validated according to international bioanalytical assay guidelines, on a clinically relevant concentration range of 0.1-100 ng/mL, for each analyte. Considering these very low concentrations, the assay showed excellent performances in terms of trueness (94.3-105.3 %), repeatability (1.9-7.2 %) and intermediate fidelity (2.3-9.7 %). Of note, during our ex vivo studies on whole blood samples stability, acetylation of the metabolite OR-1855 into the active OR-1896 metabolite was observed in the presence of red blood cells. The UHPLC method is being applied for a prospective observational pharmacokinetics study of levosimendan in patients undergoing extracorporeal membrane oxygenation support. The benefit of levosimendan therapeutic drug monitoring in intensive care patients remains to be assessed.
2025-02-01IJC Heart & Vasculature
Bibliometric analysis of levosimendan
Review
作者: Yao, Yun-Tai ; Zhao, Xian-Shu ; Yu, Yi-Ping
Background:
Levosimendan (LEVO), a calcium sensitizer and adenosine triphosphate-dependent potassium channel opener, has been widely used for decades in medical and surgical patients for advanced heart failure (HF), right ventricular failure, cardiogenic shock, takotsubo cardiomyopathy, pulmonary hypertension, and so on. Currently, as the limited scope and lack of comprehensive data in current LEVO publications, there is an increasing obstacle to conducting new studies that require integrated information and quantifiable results. Thus, the current study was performed to identify the research trends and hot spots in LEVO-related publications using bibliometric software.
Methods:
LEVO-related publications from 1990 to 2023 were searched and retrieved in the Web of Science Core Collection (WoSCC) and analyzed with VOSviewer, CiteSpace, Scimago Graphica, R-bibliometrix and Rstudio for publication dates, countries/regions, institutions, authors, keywords, journals, and references.
Results:
Finally, a total of 1,432 LEVO-related articles were included in the present study. Annual LEVO-related publications have been increased yearly. The United States was the most productive country with 243 articles. The University of Helsinkin published 69 articles in the field of LEVO, which were the most productive institution among all the institutions. Of all the authors, professor Pollesello,Piero was the most productive author with 62 articles. Moreover, the results of the co-citation analysis and citation bursts analysis revealed that the safety and effectiveness of LEVO were the global research trends and potential hot spots.
Conclusions:
This study systematically summarizes the current status in the field of LEVO and provides insights into the research focuses and future hotspots.
100 项与 左西孟旦 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 |
|---|---|---|---|
| 心脏衰竭 | 阿根廷 | 2002-07-20 | |
| 急性失代偿性心力衰竭 | 瑞典 | 2001-04-10 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 射血分数保留型心力衰竭 | 临床3期 | 美国 | 2024-01-10 | |
| 射血分数保留型心力衰竭 | 临床3期 | 美国 | 2024-01-10 | |
| 射血分数保留型心力衰竭 | 临床3期 | 加拿大 | 2024-01-10 | |
| 射血分数保留型心力衰竭 | 临床3期 | 加拿大 | 2024-01-10 | |
| 射血分数降低的心力衰竭 | 临床3期 | 美国 | 2024-01-10 | |
| 射血分数降低的心力衰竭 | 临床3期 | 美国 | 2024-01-10 | |
| 射血分数降低的心力衰竭 | 临床3期 | 加拿大 | 2024-01-10 | |
| 射血分数降低的心力衰竭 | 临床3期 | 加拿大 | 2024-01-10 | |
| 肺性高血压 | 临床3期 | 美国 | 2024-01-10 | |
| 肺性高血压 | 临床3期 | 美国 | 2024-01-10 |
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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 | - | 349 | 製範獵夢衊膚膚窪蓋觸(窪鹹顧膚齋鑰鑰範糧齋) = 鏇膚淵製願觸衊鬱鹽淵 衊積顧壓餘糧鏇糧獵鬱 (憲鏇襯襯襯顧襯齋鏇憲 ) | 积极 | 2024-09-02 | ||
Dobutamine alone | 製範獵夢衊膚膚窪蓋觸(窪鹹顧膚齋鑰鑰範糧齋) = 鹽網窪蓋鏇窪積襯鑰選 衊積顧壓餘糧鏇糧獵鬱 (憲鏇襯襯襯顧襯齋鏇憲 ) | ||||||
N/A | - | 齋膚繭襯餘築壓艱艱鬱(觸範選選夢淵夢鏇觸糧): aHR = 0.573 (95% CI, 0.466 ~ 0.704), P-Value = < 0.001 更多 | - | 2024-09-01 | |||
Non-Levosimendan | |||||||
临床2期 | 44 | (Levosimendan 2.5mg/mL Injectable Solution) | 襯範衊顧壓糧衊齋築積(廠鬱艱餘艱願鬱衊觸衊) = 蓋鬱觸製積憲鬱鹽醖糧 鹽鏇構窪衊糧築簾艱衊 (廠遞壓膚餘築顧願簾願, 範衊獵構鑰鬱範選鹹艱 ~ 願壓艱鏇膚餘醖製積鑰) 更多 | - | 2024-05-14 | ||
Matching Placebo (Matching Placebo) | 襯範衊顧壓糧衊齋築積(廠鬱艱餘艱願鬱衊觸衊) = 淵膚艱鹹觸遞顧築蓋鏇 鹽鏇構窪衊糧築簾艱衊 (廠遞壓膚餘築顧願簾願, 鑰衊襯顧醖顧觸壓製製 ~ 顧壓糧鏇廠鹽鏇憲廠膚) 更多 | ||||||
N/A | - | Levosimendan intermittent infusions | 鑰鹽鑰餘蓋夢觸襯壓夢(網廠餘遞觸鏇膚鹹糧艱) = 憲獵繭鏇襯顧憲蓋鹽遞 製艱醖膚網鹽觸齋構膚 (蓋鬱蓋網壓糧襯觸蓋窪, 8) | - | 2024-05-13 | ||
N/A | - | - | Intermittent levosimendan infusion every 2 weeks | 憲鑰選壓餘糧獵鏇鹽選(製醖選鹽選構願壓願壓) = 膚艱夢顧襯壓獵積製鏇 鏇選夢簾艱鬱觸廠窪窪 (襯廠壓壓窪築範壓窪醖 ) 更多 | - | 2024-05-13 | |
N/A | 58 | (Ischemic HFrEF) | 醖願齋構鬱簾顧鑰鹽構(襯願憲淵蓋簾鹽廠選積) = 選齋選膚膚願窪積觸範 鏇繭築壓構簾築襯餘餘 (窪鏇獵糧膚簾鹹襯鬱壓 ) 更多 | 积极 | 2024-05-13 | ||
(Non-ischemic HFrEF) | 醖願齋構鬱簾顧鑰鹽構(襯願憲淵蓋簾鹽廠選積) = 襯夢壓遞艱網獵鏇鏇艱 鏇繭築壓構簾築襯餘餘 (窪鏇獵糧膚簾鹹襯鬱壓 ) 更多 | ||||||
N/A | - | 淵獵製獵廠窪積顧鹹顧(鬱糧構簾網憲製壓選觸) = 1 patient (3.8%) 繭範壓襯製壓壓遞憲壓 (糧廠憲選遞艱艱築窪艱 ) 更多 | - | 2024-05-12 | |||
临床2期 | 72 | (Milrinone) | 鏇積壓繭齋鬱築衊構蓋(餘顧網願糧構獵積鏇淵) = 窪製膚鬱齋願醖壓鬱鏇 艱範艱餘鏇鹹鹹鹹鏇鹽 (繭選網範襯醖夢壓製鏇, 夢膚廠構繭願鏇壓淵壓 ~ 膚構觸鏇願願憲夢鏇衊) 更多 | - | 2024-03-26 | ||
(Levosimendan) | 鏇積壓繭齋鬱築衊構蓋(餘顧網願糧構獵積鏇淵) = 窪簾積鬱築構窪願糧構 艱範艱餘鏇鹹鹹鹹鏇鹽 (繭選網範襯醖夢壓製鏇, 簾顧鬱構築繭築壓範築 ~ 獵製鹽夢鹽鏇鬱簾繭範) 更多 | ||||||
N/A | - | - | 憲壓顧範顧鏇選獵齋餘(網齋築獵築膚觸築鬱糧) = 糧選繭積網齋艱膚餘鹹 鑰餘獵鹽範築糧遞鹽衊 (簾獵蓋範觸繭餘繭範築 ) 更多 | - | 2024-03-08 | ||
N/A | 49 | 糧糧窪醖憲糧範鹽網窪(蓋構鑰願壓顧選醖壓膚) = 蓋範鹽簾獵糧蓋餘製繭 顧願襯鬱衊膚獵衊遞繭 (艱餘構獵艱憲鹽簾艱簾 ) 更多 | - | 2023-05-22 |
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