Ng Tien M H, Goland Sorel, Elkayam Uri
From the *Departments of Clinical Pharmacy and Medicine, University of Southern California, Los Angeles, CA; †Heart Institute, Kaplan Medical Center, Rehovot, Israel; and ‡Department of Medicine, Division of Cardiology, University of Southern California, Los Angeles, CA.
Cardiol Rev. 2016 Jul-Aug;24(4):194-204. doi: 10.1097/CRD.0000000000000089.
Acute heart failure remains a major cause of morbidity, and its treatment requires an increasing investment of the health care system. Whereas success in treating chronic heart failure has been achieved over the last decades, several pharmacological approaches for acute heart failure have been introduced but have failed to demonstrate any clinical benefit. Serelaxin is a recombinant human relaxin-2 vasoactive peptide that causes systemic and renal vasodilation. Data suggest that the clinical benefits may be attributable to a potential combination of multiple actions of serelaxin, including improving systemic, cardiac, and renal hemodynamics, and protecting cells and organs from damage via neurohormonal, anti-inflammatory, antiremodeling, antifibrotic, anti-ischemic, and proangiogenic effects. Recently, a number of clinical trials have demonstrated that serelaxin infusion over 48 hours improved dyspnea with more rapid relief of congestion during the first days after admission for heart failure. In addition, administration of serelaxin diminished cardiac, renal, and hepatic damage, which were associated with improved long-term mortality. Available data support substantial clinical benefits and significant promise for serelaxin as a treatment option for patients with acute heart failure. This review focuses on the pharmacology and mechanisms of action of serelaxin and provides a detailed discussion of the clinical evidence for this novel therapy in acute heart failure.
急性心力衰竭仍然是发病的主要原因，其治疗需要医疗保健系统投入越来越多的资源。尽管在过去几十年中慢性心力衰竭的治疗取得了成功，但针对急性心力衰竭的几种药物治疗方法已经推出，但未能显示出任何临床益处。Serelaxin是一种重组人松弛素-2血管活性肽，可引起全身和肾血管舒张。数据表明，临床益处可能归因于Serelaxin多种作用的潜在组合，包括改善全身、心脏和肾脏血流动力学，以及通过神经激素、抗炎、抗重塑、抗纤维化、抗缺血和促血管生成作用保护细胞和器官免受损伤。最近，一些临床试验表明，在心力衰竭入院后的头几天内，输注Serelaxin 48小时可改善呼吸困难，并更快缓解充血症状。此外，给予Serelaxin可减少心脏、肾脏和肝脏损伤，这与长期死亡率的改善有关。现有数据支持Serelaxin作为急性心力衰竭患者的治疗选择具有显著的临床益处和巨大前景。本综述重点关注Serelaxin的药理学和作用机制，并详细讨论了这种新型疗法在急性心力衰竭中的临床证据。
