Department of Cardiovascular Medicine, Graduate School of Medical Sciences, Kumamoto University, 1-1-1, Honjo, Chuo-ku, Kumamoto City, 860-8556, Japan.
Curr Hypertens Rep. 2020 Feb 29;22(3):21. doi: 10.1007/s11906-020-1023-y.
Recently, nonsteroidal mineralocorticoid receptor (MR) antagonists (MRAs), which have been proposed to be called MR blockers (MRBs), have become available for clinical use, but their clinical role is unknown. We reviewed the clinical roles of MRAs and MRBs based on previous knowledge and as demonstrated in representative clinical trials.
Steroidal MRAs, such as spironolactone and eplerenone, inhibit the action of aldosterone and cortisol in MRs expressed in several organs and cell types, and accumulating clinical studies have revealed that they exert hypotensive and cardiorenal protective effects. Recently, MRBs, including finerenone and esaxerenone, have been developed and are expected to lower the risk of hyperkalemia, which is common when steroidal MRAs are used. Although the differences between MRAs and MRBs in clinical practice have not yet been established, further studies in this field are expected to broaden our understanding. MRBs exert antihypertensive and cardiorenal protective effects, and their potency is thought to be far superior to that of MRAs, because MRBs have both strong MR inhibitory action and high selectivity. Thus, MRBs could be a promising agent for the treatment of hypertension and cardiorenal, cerebral, and metabolic disorders.
最近，非甾体类盐皮质激素受体（MR）拮抗剂（MRAs）已可用于临床，其被提议称为 MR 阻滞剂（MRBs），但其临床作用尚不清楚。我们根据既往知识和代表性临床试验结果，综述了 MRA 和 MRB 的临床作用。
甾体类 MRA，如螺内酯和依普利酮，可抑制在多个器官和细胞类型中表达的 MR 对醛固酮和皮质醇的作用，大量临床研究表明其具有降压和心脏肾脏保护作用。最近，开发了 MRBs，包括非奈利酮和 esaxerenone，预计可降低甾体类 MRA 常见的高钾血症风险。尽管 MRA 和 MRB 在临床实践中的差异尚未确定，但该领域的进一步研究有望拓宽我们的认识。MRBs 具有降压和心脏肾脏保护作用，其效力被认为远优于 MRA，因为 MRBs 具有强大的 MR 抑制作用和高选择性。因此，MRBs 可能成为治疗高血压和心脏肾脏、大脑和代谢紊乱的有前途的药物。
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