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Recombinant human H2 relaxin (serelaxin) as a cardiovascular drug: aiming at the right target.
Drug Discovery Today ( IF 7.4 ) Pub Date : 2020-04-29 , DOI: 10.1016/j.drudis.2020.04.014
Daniele Bani 1
Affiliation  

Serelaxin (recombinant human relaxin-2 hormone; RLX-2) had raised expectations as a new medication for cardiovascular diseases. Evidence from preclinical studies indicated that serelaxin has chronotropic, inotropic, and anti-arrhythmic actions on the myocardium and cardioprotective effects mediated by vasodilation, angiogenesis, and inhibition of inflammation and fibrosis. However, clinical trials with serelaxin in patients with acute heart failure (AHF) gave inconclusive results. A critical reappraisal of the comprehensive cardiovascular actions of serelaxin clearly delineates acute myocardial infarction (AMI) as a feasible therapeutic target. Serelaxin acts at multiple levels on the pathogenic mechanisms of AMI and previous in vivo studies suggest that its administration at reperfusion affords myocardial salvage. Thus, serelaxin could be an effective adjunctive medical therapy to coronary angioplasty.



中文翻译:

重组人 H2 松弛素(serelaxin)作为心血管药物:瞄准正确的目标。

Serelaxin(重组人松弛素 2 激素;RLX-2)作为一种新的心血管疾病药物引起了人们的期望。来自临床前研究的证据表明,serelaxin 对心肌具有变时性、正性肌力和抗心律失常作用,并具有由血管舒张、血管生成和抑制炎症和纤维化介导的心脏保护作用。然而,在急性心力衰竭 (AHF) 患者中使用 Serelaxin 的临床试验给出了不确定的结果。对 serelax 综合心血管作用的批判性重新评估清楚地将急性心肌梗死 (AMI) 定为可行的治疗靶点。Serelaxin 在多个水平上作用于 AMI 和以前的体内致病机制研究表明,再灌注时给予它可以挽救心肌。因此,serelaxin 可能是冠状动脉成形术的有效辅助药物治疗。

更新日期:2020-04-29
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