The potential of endothelin antagonism as a therapeutic approach

Expert Opin Investig Drugs. 2004 Nov;13(11):1419-35. doi: 10.1517/13543784.13.11.1419.


Endothelin (ET) is a pivotal physiological regulator of blood pressure through its effects on blood vessels, heart, lung and kidneys, and the ET system can be overactive in disorders such as pulmonary hypertension, heart failure and renal disease. Such observations stimulated interest among scientists and pharmaceutical companies that have set up high-throughput screens to search for antagonists of ET receptors. The emerging compounds have been tested in animals with exciting results, leading to great hope that such inhibitors could be translated into human drugs with desirable therapeutic activities and few side effects. This review will describe the most relevant results obtained in experimental animals in a wide variety of disease conditions and focus on the data of selected compounds that have been employed in clinical trials.

Publication types

  • Review

MeSH terms

  • Clinical Trials as Topic*
  • Drug Evaluation, Preclinical*
  • Endothelin Receptor Antagonists
  • Endothelins / antagonists & inhibitors*
  • Endothelins / genetics
  • Endothelins / metabolism*
  • Humans
  • Receptors, Endothelin / metabolism


  • Endothelin Receptor Antagonists
  • Endothelins
  • Receptors, Endothelin