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Endothelin receptor antagonists in pulmonary arterial hypertension.

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.

journal_name

J Am Coll Cardiol

journal_title

Journal of the American College of Cardiology

authors

Channick RN,Sitbon O,Barst RJ,Manes A,Rubin LJ

doi

10.1016/j.jacc.2004.02.042

subject

Has Abstract

pub_date

2004-06-16 00:00:00

pages

62S-67S

issue

12 Suppl S

eissn

0735-1097

issn

1558-3597

pii

S073510970400511X

journal_volume

43

pub_type

杂志文章,评审

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