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摘要: 盐皮质激素受体拮抗剂在治疗心力衰竭方面起着至关重要的作用。目前认为，螺内酯、依普利酮等甾体类盐皮质激素受体拮抗剂可使心力衰竭和慢性肾脏疾病患者获益，但易导致高钾血症等不良反应，降低了临床使用率。非奈利酮是一种新型非甾体盐皮质激素受体拮抗剂，不仅在治疗心力衰竭和慢性肾脏疾病等方面具有更好的安全性和有效性，在心房颤动和心肌梗死等疾病的治疗中也发挥着重要作用。本文对非奈利酮在心血管及相关疾病治疗中的研究进展进行综述。
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关键词:
- 非奈利酮 /
- 非甾体类盐皮质激素受体拮抗剂 /
- 心血管疾病
Abstract: Mineralocorticoid receptor antagonists(MRAs) play a vital role in the treatment of heart failure. Although MRAs such as spironolactone and eplerenone have been shown to benefit patients with heart failure and chronic kidney disease, their clinical use is limited due to more side effects such as hyperkalemia. Finerenone, as a new type of highly selective non-steroidal MRA, has better safety profile and tolerance in the treatment of heart failure and chronic kidney disease. In recent years, a number of studies and basic experiments have shown that finerenone has great potential in the treatment of hypertension and myocardial infarction. In this paper, we review the latest research progress of the efficacy and safety of finerenone in cardiovascular and other related diseases. -
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表 1 螺内酯、依普利酮和非奈利酮的药物特点比较
Table 1. Characteristics of spironolactone, eplerenone, and finerenone
项目 螺内酯 依普利酮 非奈利酮 化学结构 
类别 甾体类 甾体类 二氢吡啶 对MR的选择性 非选择性 选择性 高选择性 半衰期/h 1.4 (活性代谢物12~35) 4~6 2 MR IC50/nM 24 990 17.8 AR IC50/nM 77 ≥21200 ≥10000 PR EC50/nM 740 ≥31200 ≥10000 注：AR，雄激素受体；PR，孕激素受体；EC50，达到50%所需的配体浓度。 
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| 引用本文: |
余万乾, 沈文, 杨萍萍, 等. 非奈利酮在心血管及相关疾病的研究进展[J]. 临床心血管病杂志, 2022, 38(11): 916-920. doi: 10.13201/j.issn.1001-1439.2022.11.013
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| Citation: |
YU Wanqian, SHEN Wen, YANG Pingping, et al. Finerenone in treatment of cardiovascular and related diseases[J]. J Clin Cardiol, 2022, 38(11): 916-920. doi: 10.13201/j.issn.1001-1439.2022.11.013
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