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依斯巴伦诺:全球首次获批。

Esaxerenone: First Global Approval.

机构信息

Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand.

出版信息

Drugs. 2019 Mar;79(4):477-481. doi: 10.1007/s40265-019-01073-5.

DOI:10.1007/s40265-019-01073-5
PMID:30806972
Abstract

Esaxerenone (MINNEBRO™)-a novel oral, non-steroidal, selective mineralocorticoid receptor blocker-is being developed by Daiichi Sankyo for the treatment of hypertension and diabetic nephropathies. In January 2019, based on positive results from a phase III trial conducted in Japan in patients with essential hypertension, esaxerenone received marketing approval in Japan for the treatment of hypertension. This article summarizes the milestones in the development of esaxerenone leading to this first global approval for the treatment of hypertension.

摘要

依普利酮(MINNEBRO™)-一种新型口服、非甾体类、选择性盐皮质激素受体拮抗剂,由第一三共株式会社开发,用于治疗高血压和糖尿病肾病。2019 年 1 月,基于在日本进行的一项针对原发性高血压患者的 III 期临床试验的积极结果,依普利酮在日本获得批准上市,用于治疗高血压。本文总结了依普利酮开发过程中的重要里程碑,最终使其在全球范围内首次获批用于治疗高血压。

相似文献

1
Esaxerenone: First Global Approval.依斯巴伦诺:全球首次获批。
Drugs. 2019 Mar;79(4):477-481. doi: 10.1007/s40265-019-01073-5.
2
Synergistic reduction in albuminuria in type 2 diabetic mice by esaxerenone (CS-3150), a novel nonsteroidal selective mineralocorticoid receptor blocker, combined with an angiotensin II receptor blocker.新型非甾体类选择性盐皮质激素受体阻滞剂依斯巴群(CS-3150)与血管紧张素 II 受体阻滞剂联合应用可协同降低 2 型糖尿病小鼠的蛋白尿。
Hypertens Res. 2020 Nov;43(11):1204-1213. doi: 10.1038/s41440-020-0495-0. Epub 2020 Jul 2.
3
Efficacy and safety of esaxerenone (CS-3150) in Japanese patients with type 2 diabetes and macroalbuminuria: a multicenter, single-arm, open-label phase III study.在日本 2 型糖尿病伴大量白蛋白尿患者中的疗效和安全性:一项多中心、单臂、开放标签的 III 期研究。
Clin Exp Nephrol. 2021 Oct;25(10):1070-1078. doi: 10.1007/s10157-021-02075-y. Epub 2021 Jun 10.
4
Efficacy and safety of esaxerenone (CS-3150) for the treatment of essential hypertension: a phase 2 randomized, placebo-controlled, double-blind study.依普利酮治疗原发性高血压的疗效和安全性:一项 2 期随机、安慰剂对照、双盲研究。
J Hum Hypertens. 2019 Jul;33(7):542-551. doi: 10.1038/s41371-019-0207-x. Epub 2019 May 21.
5
Cardioprotective Effects of a Nonsteroidal Mineralocorticoid Receptor Blocker, Esaxerenone, in Dahl Salt-Sensitive Hypertensive Rats.非甾体类盐皮质激素受体阻滞剂依斯巴伦诺对达尔盐敏感型高血压大鼠的心脏保护作用。
Int J Mol Sci. 2021 Feb 19;22(4):2069. doi: 10.3390/ijms22042069.
6
Exposure-response analysis of the efficacy and safety of esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker, in hypertensive patients with or without diabetic kidney disease.在伴有或不伴有糖尿病肾病的高血压患者中,新型非甾体类盐皮质激素受体阻滞剂 esaxerenone 的疗效和安全性的暴露-反应分析。
Drug Metab Pharmacokinet. 2024 Apr;55:100535. doi: 10.1016/j.dmpk.2023.100535. Epub 2023 Oct 19.
7
Long-term phase 3 study of esaxerenone as mono or combination therapy with other antihypertensive drugs in patients with essential hypertension.依普利酮单药或与其他抗高血压药物联合治疗原发性高血压患者的长期 3 期研究。
Hypertens Res. 2019 Dec;42(12):1932-1941. doi: 10.1038/s41440-019-0314-7. Epub 2019 Sep 25.
8
Effect of a novel nonsteroidal selective mineralocorticoid receptor antagonist, esaxerenone (CS-3150), on blood pressure and renal injury in high salt-treated type 2 diabetic mice.新型非甾体选择性盐皮质激素受体拮抗剂依斯巴伦诺(CS-3150)对高盐处理的 2 型糖尿病小鼠血压和肾脏损伤的影响。
Hypertens Res. 2019 Jun;42(6):892-902. doi: 10.1038/s41440-019-0211-0. Epub 2019 Jan 21.
9
Esaxerenone (CS-3150) in Patients with Type 2 Diabetes and Microalbuminuria (ESAX-DN): Phase 3 Randomized Controlled Clinical Trial.依帕司他(CS-3150)治疗 2 型糖尿病合并微量白蛋白尿患者(ESAX-DN)的 III 期随机对照临床试验。
Clin J Am Soc Nephrol. 2020 Dec 7;15(12):1715-1727. doi: 10.2215/CJN.06870520. Epub 2020 Nov 25.
10
Esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker (MRB) in hypertension and chronic kidney disease.依普利酮,一种新型非甾体类盐皮质激素受体拮抗剂(MRB),用于治疗高血压和慢性肾脏病。
J Hum Hypertens. 2021 Feb;35(2):148-156. doi: 10.1038/s41371-020-0377-6. Epub 2020 Jul 13.

引用本文的文献

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Rationale and Design of the ESPIAL Trial - A Prospective, Randomized, Exploratory Study to Evaluate the Effect of Esaxerenone on Reduction of Urinary Albumin to Creatinine Ratio in Hypertensive Patients Concomitant With Heart Failure and Albuminuria.依普利酮治疗试验(ESPIAL)的原理与设计——一项前瞻性、随机、探索性研究,旨在评估依普利酮对降低合并心力衰竭和蛋白尿的高血压患者尿白蛋白与肌酐比值的效果。
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Emerging Pharmacological Approaches for the Treatment of Arterial Hypertension.治疗动脉高血压的新兴药理学方法
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本文引用的文献

1
Pharmacokinetics, Metabolism, and Excretion of [C]Esaxerenone, a Novel Mineralocorticoid Receptor Blocker in Humans.在人体中[C]依普利酮,一种新型的盐皮质激素受体阻断剂的药代动力学、代谢和排泄。
Drug Metab Dispos. 2019 Mar;47(3):340-349. doi: 10.1124/dmd.118.084897. Epub 2018 Dec 12.
2
Single- and multiple-dose escalation study to assess pharmacokinetics, pharmacodynamics and safety of oral esaxerenone in healthy Japanese subjects.一项在健康日本受试者中评估口服 esaxerenone 的药代动力学、药效学和安全性的单次和多次递增剂量研究。
Br J Clin Pharmacol. 2018 Aug;84(8):1821-1829. doi: 10.1111/bcp.13616. Epub 2018 Jun 7.
3
Mineralocorticoid receptor as a therapeutic target in chronic kidney disease and hypertension.
Aldosterone's impact on kidney health: exploring the benefits of mineralocorticoid receptor antagonists for renal protection.
醛固酮对肾脏健康的影响:探索盐皮质激素受体拮抗剂对肾脏保护的益处。
Am J Transl Res. 2024 Aug 15;16(8):4246-4255. doi: 10.62347/NRGG6465. eCollection 2024.
4
Esaxerenone Attenuates Aldosterone-Induced Mitochondrial Damage-Mediated Pyroptosis in Mouse Aorta and Rat Vascular Smooth Muscle Cells.依沙克瑞诺可减轻醛固酮诱导的小鼠主动脉和大鼠血管平滑肌细胞线粒体损伤介导的焦亡。
Life (Basel). 2024 Jul 31;14(8):967. doi: 10.3390/life14080967.
5
Clinical Properties and Non-Clinical Testing of Mineralocorticoid Receptor Antagonists in In Vitro Cell Models.在体外细胞模型中,盐皮质激素受体拮抗剂的临床特性和非临床测试。
Int J Mol Sci. 2024 Aug 22;25(16):9088. doi: 10.3390/ijms25169088.
6
Intellectual landscapes and emerging trends of non-steroidal mineralocorticoid receptor antagonists: a bibliometric and visual analysis.非甾体类盐皮质激素受体拮抗剂的知识图谱和新兴趋势:文献计量学和可视化分析。
Int Urol Nephrol. 2024 Sep;56(9):3079-3090. doi: 10.1007/s11255-024-04059-9. Epub 2024 Apr 25.
7
Unique characteristics of Asians with hypertension: what is known and what can be done?亚洲高血压患者的独特特征:已知情况与应对措施
J Hypertens. 2024 Sep 1;42(9):1482-1489. doi: 10.1097/HJH.0000000000003706. Epub 2024 Mar 12.
8
Adverse Effects of Aldosterone: Beyond Blood Pressure.醛固酮的不良反应:不仅仅是血压。
J Am Heart Assoc. 2024 Apr 2;13(7):e030142. doi: 10.1161/JAHA.123.030142. Epub 2024 Mar 18.
9
Mineralocorticoid receptor overactivation: targeting systemic impact with non-steroidal mineralocorticoid receptor antagonists.醛固酮受体过度激活:用非甾体类醛固酮受体拮抗剂靶向全身影响。
Diabetologia. 2024 Feb;67(2):246-262. doi: 10.1007/s00125-023-06031-1. Epub 2023 Dec 21.
10
Investigating the Impact of Selective Modulators on the Renin-Angiotensin-Aldosterone System: Unraveling Their Off-Target Perturbations of Transmembrane Ionic Currents.探究选择性调节剂对肾素-血管紧张素-醛固酮系统的影响:揭示其对跨膜离子流的非靶向干扰。
Int J Mol Sci. 2023 Sep 12;24(18):14007. doi: 10.3390/ijms241814007.
盐皮质激素受体作为慢性肾脏病和高血压的治疗靶点
Hypertens Res. 2017 Mar;40(3):221-225. doi: 10.1038/hr.2016.137. Epub 2016 Oct 20.
4
CS-3150, a Novel Nonsteroidal Mineralocorticoid Receptor Antagonist, Shows Preventive and Therapeutic Effects On Renal Injury in Deoxycorticosterone Acetate/Salt-Induced Hypertensive Rats.新型非甾体类盐皮质激素受体拮抗剂CS-3150对醋酸脱氧皮质酮/盐诱导的高血压大鼠肾损伤具有预防和治疗作用。
J Pharmacol Exp Ther. 2016 Sep;358(3):548-57. doi: 10.1124/jpet.116.234765. Epub 2016 Jul 6.
5
CS-3150, a novel non-steroidal mineralocorticoid receptor antagonist, prevents hypertension and cardiorenal injury in Dahl salt-sensitive hypertensive rats.CS-3150,一种新型非甾体盐皮质激素受体拮抗剂,可预防 Dahl 盐敏感性高血压大鼠的高血压和心脏肾脏损伤。
Eur J Pharmacol. 2015 Dec 15;769:266-73. doi: 10.1016/j.ejphar.2015.11.028. Epub 2015 Nov 26.
6
Pharmacological profile of CS-3150, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.新型高效选择性非甾体盐皮质激素受体拮抗剂CS-3150的药理学特性
Eur J Pharmacol. 2015 Aug 15;761:226-34. doi: 10.1016/j.ejphar.2015.06.015. Epub 2015 Jun 11.
7
Mineralocorticoid receptor blockade in the protection of target organ damage.盐皮质激素受体阻断在靶器官损伤保护中的作用
Cardiovasc Hematol Agents Med Chem. 2006 Jan;4(1):75-91. doi: 10.2174/187152506775268776.