Document Detail

Sitaxsentan: a novel endothelin-A receptor antagonist for pulmonary arterial hypertension.
MedLine Citation:
PMID:  16292989     Owner:  NLM     Status:  MEDLINE    
Sitaxsentan is an orally active, selective endothelin-A receptor antagonist that may benefit patients with pulmonary arterial hypertension by blocking the vasoconstrictive effects of endothelin-A receptors, while maintaining the vasodilator and endothelin-1 clearance functions of the endothelin-B receptors. In its first randomized, placebo-controlled study, sitaxsentan improved exercise capacity assessed by the 6-min walk test, New York Heart Association functional class, cardiac index and pulmonary vascular resistance in New York Heart Association Class II, III and IV patients with idiopathic pulmonary arterial hypertension and pulmonary arterial hypertension related to connective tissue disease or congenital heart disease. Although doses of 100 and 300 mg once daily demonstrated equivalent efficacy, the lower dose had a better safety profile. Additional studies are ongoing to assess the relative safety and efficacy of 50 and 100 mg once-daily dosing. The most common side effects include rhinitis, headache, peripheral edema, chest pain, nausea, constipation, increased prothrombin time/international normalized ratio (in patients on warfarin), flushing and insomnia. As with other endothelin receptor antagonists, increases in hepatic transaminases have been observed with sitaxsentan. Initial studies using the selective oral endothelin-A receptor antagonist sitaxsentan in pulmonary arterial hypertension patients have revealed a favorable risk-benefit therapeutic profile with the 100 mg once-daily dose.
Allison C Widlitz; Robyn J Barst; Evelyn M Horn
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Expert review of cardiovascular therapy     Volume:  3     ISSN:  1744-8344     ISO Abbreviation:  Expert Rev Cardiovasc Ther     Publication Date:  2005 Nov 
Date Detail:
Created Date:  2005-11-18     Completed Date:  2006-07-20     Revised Date:  2008-06-05    
Medline Journal Info:
Nlm Unique ID:  101182328     Medline TA:  Expert Rev Cardiovasc Ther     Country:  England    
Other Details:
Languages:  eng     Pagination:  985-91     Citation Subset:  IM    
Pulmonary Hypertension Center, Columbia University College of Physicians and Surgeons, BHN 2-255, New York, NY 10032, USA.
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MeSH Terms
Clinical Trials as Topic
Hypertension, Pulmonary / drug therapy*
Isoxazoles / adverse effects,  therapeutic use*
Receptors, Endothelin / antagonists & inhibitors*
Thiophenes / adverse effects,  therapeutic use*
Reg. No./Substance:
0/Isoxazoles; 0/Receptors, Endothelin; 0/Thiophenes; 0/sitaxsentan

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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