非奈利酮治疗慢性心力衰竭的研究进展

Research progress on finerenone in the treatment of chronic heart failure

盐皮质激素受体拮抗剂(mineralocorticoid receptor antagonist,MRA)因其在治疗心力衰竭(heart failure,HF)、难治性高血压(hypertension)和各种肾脏疾病中的效用而广为人知,是治疗慢性心力衰竭(chronic heart failure,CHF)的推荐用药。在已有的甾体类MRA中,螺内酯(spironolactone)与盐皮质激素受体(mineralocorticoid receptor,MR)结合力虽高,但选择性较差,容易出现类固醇受体交叉反应;依普利酮(eplerenone)虽然对MR选择性更高,但结合力较低,还存在高钾血症(hyperkalemia)及肾功能恶化风险,均未能在临床中广泛使用。新型非甾体类MRA非奈利酮(finerenone),较螺内酯对MR的选择性更高,较依普利酮对MR的结合力更强,安全性和耐受性较好,多项试验和小型研究均显示出在治疗CHF方面有较好的应用前景。本文对非奈利酮治疗CHF的研究进展作一综述。

Mineralocorticoid receptor antagonists (MRAs) are well known for their utility in treating heart failure,refractory hypertension,and various kidney diseases.They are recommended medications for chronic heart failure (CHF).However,the available MRAs spironolactone has high binding ability but poor selectivity with mineralocorticoid receptor (MR),which is prone to steroid receptor cross-reaction.While eplerenone has higher selectivity to MR,but low binding ability.High risk of adverse events such as hyperkalemia and worsening renal function limit their clinical use.Finerenone,as a novel non-steroidal MRA,has higher selectivity towards MR compared to spironolactone and stronger affinity than eplerenone,as well as good safety profile and tolerability.Encouraging results had been shown in multiple trials and smaller studies,showing promising prospects for treating CHF.This article reviewed the research progress of finerenone in the treatment of CHF.