Endothelin receptor antagonists for pulmonary arterial hypertension: an overview

Cardiovasc Ther. 2010 Oct;28(5):e65-71. doi: 10.1111/j.1755-5922.2010.00158.x.


The last decade has seen major advances in the pharmacotherapy of pulmonary arterial hypertension (PAH). One of these advances has been the discovery of endothelin receptor antagonists (ERAs). ERAs are a class of potent vasodilators and antimitotic substances, which could specifically dilate and remodel pulmonary arterial system, and have been proposed as an alternative to traditional therapies for PAH. Current available evidence suggests that ERAs improve exercise capacity, functional status, pulmonary hemodynamics, and delay the time to clinical worsening for patients with PAH. This review attempts to provide an overview of the pharmacology, therapeutic benefits, and safety profile of ERAs in patients with PAH.

Publication types

  • Review

MeSH terms

  • Animals
  • Antihypertensive Agents / adverse effects
  • Antihypertensive Agents / pharmacokinetics
  • Antihypertensive Agents / therapeutic use*
  • Blood Pressure / drug effects
  • Drug Interactions
  • Endothelin Receptor Antagonists*
  • Endothelins / metabolism*
  • Evidence-Based Medicine
  • Familial Primary Pulmonary Hypertension
  • Humans
  • Hypertension, Pulmonary / drug therapy
  • Hypertension, Pulmonary / metabolism
  • Hypertension, Pulmonary / physiopathology
  • Receptors, Endothelin / metabolism
  • Treatment Outcome
  • Vasodilator Agents / adverse effects
  • Vasodilator Agents / pharmacokinetics
  • Vasodilator Agents / therapeutic use*


  • Antihypertensive Agents
  • Endothelin Receptor Antagonists
  • Endothelins
  • Receptors, Endothelin
  • Vasodilator Agents