Mineralocorticoid receptors (MRs) are implicated in the pathology of hypertension. MR blockers are recommended for the treatment of salt-sensitive or resistant hypertension. However, use of currently available MR blockers is limited by adverse events. This phase 3 multicenter, randomized, double-blind study compared the efficacy and safety of esaxerenone, a new selective nonsteroidal MR blocker, at 2.5 and 5 mg/day and eplerenone 50 mg/day in Japanese patients with essential hypertension. After a 4-week washout period, 1001 eligible adults with hypertension were randomized evenly to esaxerenone 2.5 or 5 mg/day or eplerenone 50 mg/day treatments, taken orally once daily for 12 weeks. Primary end points were changes in sitting systolic or diastolic blood pressure (BP) from baseline at the end of treatment. Esaxerenone 2.5 mg/day was noninferior to eplerenone for reductions in sitting and 24-hour BP. Reductions in BP with esaxerenone 5 mg/day were significantly greater than those with esaxerenone 2.5 mg/day. Changes in diurnal BP showed persistent 24-hour antihypertensive effects in all treatment groups. The proportions of patients achieving target sitting BP (<140/90 mm Hg) were 31.5%, 41.2%, and 27.5% with esaxerenone 2.5 and 5 mg/day and eplerenone 50 mg/day, respectively. Incidences of adverse events (all mild or moderate) were similar across treatment groups. These results indicate that esaxerenone is an effective and well-tolerated MR blocker in Japanese patients with essential hypertension, with BP-lowering activity at least equivalent to eplerenone. Clinical Trial Registration -URL: http://www.clinicaltrials.gov. Unique identifier: NCT02890173.

中文翻译：

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比较 Esaxerenone (CS-3150) 和 Eplerenone 在原发性高血压患者中的双盲随机 3 期研究（ESAX-HTN 研究）

盐皮质激素受体 (MR) 与高血压病理有关。推荐使用 MR 阻滞剂治疗盐敏感或难治性高血压。然而，目前可用的 MR 阻滞剂的使用受到不良事件的限制。这项 3 期多中心、随机、双盲研究比较了日本原发性高血压患者中 2.5 和 5 毫克/天的依普利酮（一种新型选择性非甾体 MR 阻滞剂）和依普利酮 50 毫克/天的疗效和安全性。经过 4 周的清除期后，1001 名符合条件的成年高血压患者被随机随机分配至 esaxerenone 2.5 或 5 mg/天或依普利酮 50 mg/天治疗组，每天口服一次，持续 12 周。主要终点是治疗结束时坐位收缩压或舒张压 (BP) 相对于基线的变化。2. 艾沙司酮 5 毫克/天在减少坐姿和 24 小时血压方面不劣于依普利酮。使用 esaxerenone 5 mg/天的血压降低显着大于使用 esaxerenone 2.5 mg/天的血压降低。在所有治疗组中，昼夜血压的变化显示出持续的 24 小时抗高血压作用。达到目标坐姿血压 (<140/90 mmHg) 的患者比例分别为 31.5%、41.2% 和 27.5%，使用依普利酮 2.5 和 5 毫克/天以及依普利酮 50 毫克/天。各治疗组的不良事件发生率（均为轻度或中度）相似。这些结果表明，esaxerenone 在日本原发性高血压患者中是一种有效且耐受性良好的 MR 阻滞剂，其降压活性至少与依普利酮相当。临床试验注册 - URL：http://www.clinicaltrials.gov。唯一标识符：NCT02890173。