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Mineralocorticoid Receptor Blockers: Novel Selective Nonsteroidal Mineralocorticoid Receptor Antagonists

  • Prevention of Hypertension: Public Health Challenges(Y Yano, Section Editor)
  • Published:
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Abstract

Purpose of Review

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.

Recent Findings

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.

Summary

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.

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Acknowledgments

We thank all paramedical staff and clinical secretaries for their kind support during the course of this work.

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Authors and Affiliations

  1. Department of Cardiovascular Medicine, Graduate School of Medical Sciences, Kumamoto University, 1-1-1, Honjo, Chuo-ku, Kumamoto City, 860-8556, Japan

    Daisuke Sueta, Eiichiro Yamamoto & Kenichi Tsujita

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  1. Daisuke Sueta
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  2. Eiichiro Yamamoto
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  3. Kenichi Tsujita
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Correspondence to Daisuke Sueta.

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Conflict of Interest

K.T. has received honoraria from Amgen Astellas BioPharma K.K.; Bayer Yakuhin, Ltd.; Daiichi Sankyo Co., Ltd.; MSD K.K.; and Sanofi K.K. and has received grants from AstraZeneca K.K.; Astellas Pharma Inc.; Bayer Yakuhin, Ltd.; Boehringer Ingelheim, Japan; Boston Scientific Japan K.K.; Chugai Pharmaceutical Co., Ltd.; Daiichi Sankyo Co., Ltd.; Eisai Co., Ltd., Kowa Pharmaceutical Co., Ltd.; Mitsubishi Tanabe Pharma; MSD K.K.; Pfizer Japan Inc.; Sanofi K.K.; Shionogi & Co., Ltd.; and Takeda Pharmaceutical Co., Ltd. The remaining authors have nothing to disclose.

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Sueta, D., Yamamoto, E. & Tsujita, K. Mineralocorticoid Receptor Blockers: Novel Selective Nonsteroidal Mineralocorticoid Receptor Antagonists. Curr Hypertens Rep 22, 21 (2020). https://doi.org/10.1007/s11906-020-1023-y

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