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醛固酮受体拮抗剂——肾脏保护的证据,新型药物的试验。

Mineralocorticoid Receptor Antagonists-Evidence for Kidney Protection, Trials With Novel Agents.

机构信息

Department of Medicine, Am. Heart Assoc. Comprehensive Hypertension Center, University of Chicago Medicine, Chicago, IL.

Department of Medicine, Am. Heart Assoc. Comprehensive Hypertension Center, University of Chicago Medicine, Chicago, IL.

出版信息

Adv Chronic Kidney Dis. 2021 Jul;28(4):371-377. doi: 10.1053/j.ackd.2021.07.005.

Abstract

The area of aldosterone blockade has exploded in the last decade with the development of four new compounds of a different class referred to as nonsteroidal mineralocorticoid receptor antagonists (MRAs). Their chemistry and clinical charatcteristics are distinctly different from their steroidal cousins. Apart from blocking aldosterone activity, albeit in a different way than the steroidal MRAs, they have much less blood pressure (BP) effects and are better tolerated. The spectrum of nonsteroidal MRAs includes one agent with significant BP reduction, KBP-5074, to agents with minimal BP effects yet have demonstrated significant cardiorenal risk reduction in diabetic kidney disease, finerenone. The paper reviews the development and pharmacology of these different agents and tries to provide a perspective as to their place in the spectrum of aldosterone excess disorders.

摘要

在过去的十年中,随着四种不同类别被称为非甾体类盐皮质激素受体拮抗剂(MRA)的新化合物的开发,醛固酮阻断领域取得了巨大进展。它们的化学结构和临床特征与甾体类 MRA 明显不同。除了阻断醛固酮的活性(尽管方式与甾体类 MRA 不同),它们对血压的影响要小得多,而且耐受性更好。非甾体 MRA 的范围包括一种具有显著降压作用的药物 KBP-5074,以及一些对血压影响较小但已在糖尿病肾病中证明具有显著心脏和肾脏风险降低作用的药物,如非奈利酮。本文综述了这些不同药物的开发和药理学,并试图提供一个视角,探讨它们在醛固酮过多症中的地位。

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