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Endothelin receptor antagonists in pulmonary arterial hypertension

Richard N. Channick, MD^*,*, Olivier Sitbon, MD, Robyn J. Barst, MD, Alessandra Manes, MD and Lewis J. Rubin, MD^*

^* Pulmonary and Critical Care Division, University of California, San Diego, California, USA
Division of Pulmonary and Critical Care Medicine, University of Paris-Sud, Paris, France
Division of Pediatric Cardiology, Columbia–Presbyterian Hospital, New York, New York, USA
Institute of Cardiology, University of Bologna, Bologna, Italy

Manuscript received January 13, 2004; accepted February 3, 2004.

^* Reprint requests and correspondence: Dr. Richard N. Channick, UCSD Medical Center, 9300 Campus Point Drive, La Jolla, California 92037, USA.
rchannick{at}ucsd.edu

Endothelin receptor antagonism has emerged as an important therapeutic strategy in pulmonary arterial hypertension (PAH). Laboratory and clinical investigations have clearly shown that endothelin (ET)-1 is overexpressed in several forms of pulmonary vascular disease and likely plays a significant pathogenetic role in the development and progression of pulmonary vasculopathy. Oral endothelin receptor antagonists (ERAs) have been shown to improve pulmonary hemodynamics, exercise capacity, functional status, and clinical outcome in several randomized placebo-controlled trials. Bosentan, a dual-receptor antagonist, is approved by the U.S. Food and Drug Administration for class III and IV patients with PAH, based on two phase III trials. In addition to its efficacy as sole therapy, bosentan may have a role as part of a combination of drugs such as a prostanoid or sildenafil. The selective endothelin receptor-A antagonists sitaxsentan and ambrisentan are currently undergoing investigation.

Abbreviations and Acronyms   CTEPH = chronic thromboembolic pulmonary hypertension   ERAs = endothelin receptor antagonists   ET = endothelin   ETA = endothelin receptor A   ETB = endothelin receptor B   IPAH = idiopathic pulmonary arterial hypertension   6MWT = 6-min walk test   PAH = pulmonary arterial hypertension   WHO = World Health Organization   NYHA = New York Heart Association

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