• Dermot S O'Callaghan, Laurent Savale, Azzedine Yaïci, Delphine Natali, Xavier Jaïs, Florence Parent, David Montani, Marc Humbert, Gérald Simonneau, and Olivier Sitbon.
• Université Paris-Sud, Faculté de Médecine, Le Kremlin-Bicêtre, F 94276, France.
• Expert Opin Pharmacother. 2011 Jul 1; 12 (10): 1585-96.

IntroductionEndothelin is a key mediator in the pathophysiology of pulmonary arterial hypertension (PAH). Its effects are mediated through the activation of two associated receptor subtypes, termed A and B. Therapeutic strategies that modulate the activity of endothelin are, therefore, of interest to improve the functional status of patients with PAH.Areas CoveredThe rationale for the use of endothelin receptor antagonists as a therapeutic class in PAH and pertinent data from important clinical studies are presented in this review. Areas for future research are also suggested.Expert OpinionThe availability of the endothelin receptor antagonist class of agents represents a significant addition to the therapeutic armamentarium which is available for the treatment of PAH. Comparative studies are warranted to establish whether selective endothelin-A receptor antagonism is more advantageous than dual receptor antagonism. Future studies of endothelin receptor antagonists will increasingly focus on the potential of a combination of different PAH therapeutic classes and will employ 'harder' clinical end points. This is of crucial importance to ensure that future developments are both worthwhile and acceptable to patients, physicians, health system payers and regulatory authorities.© 2011 Informa UK, Ltd.

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