Current Hypertension Reports ( IF 3.9 ) Pub Date : 2022-04-30 , DOI: 10.1007/s11906-022-01177-6 Yuta Tezuka 1 , Sadayoshi Ito 1, 2
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Purpose of Review
The study aims to verify the advantages of nonsteroidal mineralocorticoid receptor blockers (MRBs) in the management of hypertension and cardiovascular and renal diseases, comparing with conventional MRBs.
Recent Findings
Based on the unique structures, the nonsteroidal MRBs have higher selectivity for mineralocorticoid receptors (MRs) and show no agonist activity for major steroid hormone receptors in contrast to steroidal MRBs. Today, there are two nonsteroidal MRBs, esaxerenone and finerenone, which completed phase 3 clinical trials. Series of clinical trials have shown that both agents achieve similar MR blockade with smaller doses as compared with steroidal MRBs, but have no off-target side effect such as gynecomastia. Esaxerenone has persistent blood pressure-lowering effects in various hypertensive populations, including essential hypertension and those with diabetes and/or chronic kidney disease, while finerenone has demonstrated reduction of the cardiovascular risk rather than blood pressure in patients with diabetes and chronic kidney disease.
Summary
Nonsteroidal MRBs are a more refined agent which contributes to appropriate MR blocking with minimized unpleasant adverse effects.
中文翻译：
是时候重新考虑盐皮质激素受体阻断策略了：非甾体盐皮质激素受体阻断剂的到来
审查目的
本研究旨在验证非甾体盐皮质激素受体阻滞剂 (MRB) 与传统 MRB 相比在治疗高血压、心血管和肾脏疾病方面的优势。
最近的发现
基于独特的结构，非甾体 MRBs 对盐皮质激素受体 (MRs) 具有更高的选择性，并且与甾体 MRBs 相比，对主要的甾体激素受体没有激动剂活性。今天，有两种非甾体 MRBs，esaxerenone 和finerenone，它们完成了 3 期临床试验。一系列临床试验表明，与甾体 MRB 相比，两种药物都能以较小的剂量实现相似的 MR 阻断，但没有男性乳房发育等脱靶副作用。Esaxerenone 在各种高血压人群中具有持续的降血压作用，包括原发性高血压和糖尿病和/或慢性肾病患者，而 Finerenone 已证明降低了糖尿病和慢性肾病患者的心血管风险而不是血压。
概括
非甾体 MRB 是一种更精细的药物，有助于适当的 MR 阻断，同时将令人不快的不良反应降至最低。
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