Abstract
This study investigated the long-term antihypertensive effects of esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker, alone or in combination with a calcium channel blocker (CCB) or a renin–angiotensin system (RAS) inhibitor, in Japanese patients with essential hypertension. Patients were treated with esaxerenone starting at 2.5 mg/day increasing to 5 mg/day if required to achieve blood pressure (BP) targets as a monotherapy or with a CCB or RAS inhibitor. After the first 12 weeks of treatment, an additional antihypertensive agent could be added if required to achieve the target BP; the total treatment period was 28 or 52 weeks. The primary endpoint was a change from baseline in sitting BP. Of the 368 enrolled patients, 245 received monotherapy, and 59 and 64, respectively, took a CCB or RAS inhibitor concurrently. Mean changes from baseline in sitting systolic/diastolic BP (95% confidence intervals) at weeks 12, 28 and 52 were −16.1 (−17.3, −14.9)/−7.7 (−8.4, −6.9), −18.9 (−20.2, −17.7)/−9.9 (−10.7, −9.2), and −23.1 (−25.0, −21.1)/−12.5 (−13.6, −11.3) mmHg, respectively (all P < 0.0001 vs baseline). Similar BP reductions at these weeks were observed between all patient subgroups stratified by age, and the observed decreases in 24-h ambulatory BP were consistent with the efficacy observed in sitting BP. Esaxerenone was also well-tolerated with a rate of hyperkalemia at 5.4% (serum potassium ≥5.5 mEq/L), indicating a good safety profile for treatment over the long-term or in combination with a CCB or RAS inhibitor. In conclusion, esaxerenone may be a promising treatment option for patients with hypertension.
Highlights
IntroductionIncreasing aldosterone levels have been associated with an increased incidence and severity of hypertension [1,2,3,4,5]
Supplementary information The online version of this article contains supplementary material, which is available to authorized users.Aldosterone acts on mineralocorticoid receptors (MRs) on renal tubular epithelial cells to regulate electrolyte levels and blood fluid volume by promoting sodium reabsorption and urinary potassium (K+) excretion
Aldosterone has been linked with the development and progression of a number of comorbidities associated with hypertension, including endothelial dysfunction, left ventricular hypertrophy, chronic kidney disease, heart failure, stroke, and obstructive sleep apnea [6,7,8,9,10,11,12,13,14]
Summary
Increasing aldosterone levels have been associated with an increased incidence and severity of hypertension [1,2,3,4,5]. Aldosterone has been linked with the development and progression of a number of comorbidities associated with hypertension, including endothelial dysfunction, left ventricular hypertrophy, chronic kidney disease, heart failure, stroke, and obstructive sleep apnea [6,7,8,9,10,11,12,13,14]. Agents that block the action of aldosterone at MRs have therapeutic activity in a number of conditions, such as hypertension, heart failure, and microalbuminuria [15,16,17,18,19,20,21,22,23].
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