Esaxerenone is a nonsteroidal mineralocorticoid receptor blocker that is being studied for its effectiveness for diabetes-associated mineralocorticoid receptor-related hypertension.
Esaxerenone showed significant reductions for systolic and diastolic blood pressure as well as decreases in metabolic measures for patients with type 2 diabetes (T2D) or prediabetes and hypertension, according to results published in the Endocrine Journal. Esaxerenone is a nonsteroidal mineralocorticoid receptor blocker that is being studied for its effectiveness for diabetes-associated mineralocorticoid receptor-related hypertension.1
Esaxerenone is a nonsteroidal mineralocorticoid receptor blocker that is being studied for its effectiveness for diabetes-associated mineralocorticoid receptor-related hypertension. | Image Credit: neirfy - stock.adobe.com
“In the present study, we characterized the changes in BP [blood pressure] and various blood parameters that occur following Esax[erenone] administration in hypertensive subjects with T2D or prediabetes,” the study authors stated.1 “Esax[erenone] administration was found to be associated with a significantly larger reduction in SBP [systolic blood pressure] than Amlo[dipine] administration, as well as larger reductions in circulating liver enzyme activities and urinary albumin concentration.”
According to authors of a commentary in Nature, esaxerenone was developed as a highly selective mineralocorticoid receptor with a longer half-life than previous medications in the same class. It has been shown to show reductions in hypertension with fewer contraindications than other drugs in the class. It has also shown effects of lowering blood pressure without inducing reflex sympathetic nervous system activation as well as protectiveness of the organs, according to results of another study.2
There has been a focus on treating cardiometabolic diseases, which is when obesity and diabetes are present alongside cardiovascular disease, such as ischemic heart diseases and heart failure. There have been advancements in treating ischemic heart diseases, but treating metabolic disorders and obesity has not kept up, according to a commentary in eBioMedicine. The authors stated a prevalence of overweight and obesity, T2D, and metabolic syndrome has been increasing, exacerbating cardiometabolic disease burden.4
In the current study, investigators aimed to examine the effects of esaxerenone on blood pressure and metabolic parameters of hypertension for patients with T2D or prediabetes, comparing the effects with amlodipine. Patients from 7 medical institutes between May 2019 and May 2022 were included in the study. Patients had hypertension with either T2D or prediabetes, were 20 years and older, and had initiated esaxerenone and received it for at least 6 months during the study period.1
The investigators included 26 men and 20 women that received esaxerenone at administration and 58 patients that started amlodipine. The results showed that systolic blood pressure significantly decreased from approximately 155.2 mmHg at baseline to 132.9 mmHg after 6 months with esaxerenone and diastolic decreased from 83.3 mmHg to 72.3 mmHg. Furthermore, investigators reported that body mass index, glycated hemoglobin, aspartate aminotransferase, alanine aminotransferase, total cholesterol, low-density lipoprotein cholesterol, estimated glomerular filtration rate, and urine albumin/creatinine ratio decreased significantly. However, they found that both serum K and creatinine concentrations increased during the study, but there were no serious adverse events reported.1
Furthermore, investigators examined the effect on the liver, especially for the 13 patients that had liver enzyme activity above the reference range. They stated that “the median AST and ALT activities decreased from 33.0 [31.0–42.5] U/L to 28.0 [24.0–40.0] U/L (p = 0.07) and 48.0 [30.5–74.5] U/L to 35.0 [26.0–59.5] U/L (p < 0.01), respectively.”1
READ MORE: Diabetes Resource Center
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