Document Detail


Ambrisentan for the treatment of pulmonary arterial hypertension.
MedLine Citation:
PMID:  19920913     Owner:  NLM     Status:  PubMed-not-MEDLINE    
Abstract/OtherAbstract:
Ambrisentan is an endothelin receptor antagonist (ERA) that was recently approved for treatment of pulmonary arterial hypertension (PAH). Endothelin (ET) is a potent vasoconstrictor with mitogenic, hypertrophic and pro-inflammatory properties that is upregulated in pulmonary hypertensive diseases. The biologic effects of ET are mediated by 2 cell surface receptors termed ET(A) and ET(B). ET(A) mediates the vasoconstrictor effect of ET on vascular smooth muscle, whereas ET(B) is expressed primarily on vascular endothelial cells where it induces nitric oxide synthesis and acts to clear ET from the circulation. Ambrisentan is the first ET(A) selective ERA approved for use in the US. Recently published clinical trials in patients with PAH demonstrate improvement in functional capacity and pulmonary hemodynamics similar to other ET(A) selective and non-selective ERAs. Its once daily dosing and lower incidence of serum aminotransferase elevation offer potential advantages over other ERAs, but further experience with this agent is needed to fully understand its long-term efficacy and safety. This review discusses the endothelin family of proteins and receptors and their role in the pathophysiology of pulmonary hypertensive diseases. It also examines the development process, safety profile and clinical trials that have resulted in ambrisentan being approved for treatment of PAH.
Authors:
Brian Casserly; James R Klinger
Publication Detail:
Type:  Journal Article     Date:  2009-02-06
Journal Detail:
Title:  Drug design, development and therapy     Volume:  2     ISSN:  1177-8881     ISO Abbreviation:  Drug Des Devel Ther     Publication Date:  2009  
Date Detail:
Created Date:  2009-11-20     Completed Date:  2010-06-28     Revised Date:  2013-05-23    
Medline Journal Info:
Nlm Unique ID:  101475745     Medline TA:  Drug Des Devel Ther     Country:  New Zealand    
Other Details:
Languages:  eng     Pagination:  265-80     Citation Subset:  -    
Affiliation:
Division of Pulmonary Medicine, The Memorial Hospital of Rhode Island, 593 Eddy Street, Pawtucket, RI 02903, USA.
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