Mineralocorticoid Receptor Antagonists: An Overview of History and Evolution.

Q3 Medicine
B C Kalmath, Mangesh Tiwaskar, Gattu R Kumar, Hemant Khemani, Amit Singh, Rajeev Kishore, Arvind Chouhan, B L Harikrishnan, Sarita Choudhary, Manish Goyal, Arun Pradhan, Febin Francis, Amarnath Sugumaran, Senthilnathan Mohanasundaram
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引用次数: 0

Abstract

Mineralocorticoid receptor antagonists (MRAs) have significantly evolved since the introduction of the first steroidal MRA, spironolactone, in the 1950s. Initially discovered for treating hypertension and heart failure (HF), the clinical applications of MRAs have been expanded to chronic kidney disease (CKD) and diabetic nephropathy. Steroidal MRAs, such as spironolactone and eplerenone, effectively suppress mineralocorticoid receptor activation but are associated with side effects like hyperkalemia and endocrine abnormalities. Current research aims to optimize MRAs further for broader therapeutic applications, including nondiabetic kidney and cardiovascular diseases, and to improve safety profiles. In this review, we reflect on the historical development, classification, evolution, major clinical trials, and future prospects of MRAs.

矿物皮质激素受体拮抗剂:历史和进化概述。
矿物皮质激素受体拮抗剂(MRAs)自20世纪50年代引入第一种甾体MRA螺内酯以来,已经有了显著的发展。mra最初被发现用于治疗高血压和心力衰竭(HF),临床应用已扩展到慢性肾脏疾病(CKD)和糖尿病肾病。甾体MRAs,如螺内酯和依普利酮,有效抑制矿皮质激素受体的激活,但与高钾血症和内分泌异常等副作用相关。目前的研究旨在进一步优化mra,以实现更广泛的治疗应用,包括非糖尿病肾病和心血管疾病,并提高安全性。本文就mra的历史发展、分类、演变、主要临床试验及未来展望进行综述。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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CiteScore
0.80
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