Endothelin Receptor Antagonists (ERA) in Hypertension and Chronic Kidney Disease: a Rose with Many Thorns

Abstract

The discovery of endothelin created a lot of enthusiasm and paved new therapeutic avenues for the treatment of arterial hypertension. Endothelin plays a significant role in blood pressure regulation through pronounced vasoconstriction and modulation of sodium and water reabsorption in the kidneys. Endothelin receptor antagonists have been tested in many clinical trials in patients with arterial hypertension, heart failure, pulmonary arterial hypertension, systemic sclerosis, chronic kidney disease, and diabetic nephropathy. However, the results were usually disappointing, except in pulmonary hypertension and scleroderma digital ulcers. The future of ERAs for the treatment of arterial hypertension and chronic kidney disease does not seem bright, and only the combination with other classes of antihypertensive drugs might offer a way out.