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Endothelin receptor antagonists in pulmonary arterial hypertension

Authors :
Channick, Richard N.
Sitbon, Olivier
Barst, Robyn J.
Manes, Alessandra
Rubin, Lewis J.
Source :
Journal of the American College of Cardiology (JACC). Jun2004, Vol. 43 Issue 12, pS62-S67. 0p.
Publication Year :
2004

Abstract

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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
07351097
Volume :
43
Issue :
12
Database :
Academic Search Index
Journal :
Journal of the American College of Cardiology (JACC)
Publication Type :
Academic Journal
Accession number :
13435192
Full Text :
https://doi.org/10.1016/j.jacc.2004.02.042