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Endothelin receptor antagonists – their role in pulmonary medicine - 18/11/11

Doi : 10.1016/j.rmr.2009.07.001 
S. Boniface a, M. Reynaud-Gaubert b, , c
a Cabinet de pneumologie, 4, avenue de Delphes, 13006 Marseille, France 
b Service de pneumologie, CHU Nord, chemin des Bourrely, 13015 Marseille, France 
c URMITE, UMR 6236, CNRS, université de la Méditerranée, Aix Marseille-II, 13015 Marseille, France 

Corresponding author.

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Summary

Introduction

Understanding of the function of endothelin-1 in the pathophysiology of endothelial disease, in particular pulmonary arterial hypertension (PAH), has paved the way for the development of endothelin-receptor antagonists (ERAs) and explains the leading role they now play in the treatment armamentarium for this disease.

Background

Three active ERA drugs (bosentan, sitaxentan, ambrisentan) are currently approved for the treatment of PAH in France. Several randomised clinical trials have demonstrated their efficacy and safety in PAH.

Perspectives and conclusion

Besides its vasoconstrictor effect, endothelin-1 (ET-1) plays a pivotal role in cell proliferation and apoptosis. ERAs are innovative drugs potentially useful in some pulmonary disorders such as idiopathic pulmonary fibrosis or systemic sclerosis, even though the preliminary results published remain insufficient or controversial.

Conclusion

ERAs play a major role in the management of pulmonary vascular disease. Other drugs, still under study, could prove useful in the treatment of infiltrating pneumonias.

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Keywords : Pulmonary arterial hypertension, Endothelin-receptor antagonists, Bosentan, Ambrisentan, Sitaxentan, Pulmonary fibrosis


Plan


 This article is the English translation of the following manuscript, which was originally published in French in Revue des Maladies Respiratoires. Please cite this article as : “Boniface S, Reynaud-Gaubert M. Les antagonistes des récepteurs de l’endothéline : leur place dans les maladies pulmonaires. Rev Mal Respir 2010;27:103–5”.


© 2011  Publié par Elsevier Masson SAS.
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Vol 28 - N° 8

P. e94-e107 - octobre 2011 Retour au numéro
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