sitaxsentan

endothelin A receptor antagonist; structure in first source

Also Known As:

N-(4-chloro-3-methyl-5-isoxazolyl)-2-((4,5-(methylenedioxy)-O-toly)acetyl)-3-thiophenesulfonamide; N-(4-chloro-3-methyl-5-isoxazolyl)-2-(3,4-(methylenedioxy)-6-methyl)phenylacetyl-3-thiophenesulfonamide; TBC 11251; TBC-11251; TBC11251

Networked: 68 relevant articles (9 outcomes, 22 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Barst, Robyn J: 10 articles (10/2008 - 06/2002)
2.	Langleben, David: 6 articles (12/2015 - 02/2004)
3.	Horn, Evelyn M: 5 articles (11/2007 - 06/2002)
4.	Frost, Adaani E: 4 articles (12/2015 - 06/2005)
5.	Naeije, Robert: 4 articles (10/2010 - 05/2006)
6.	Benza, Raymond L: 3 articles (12/2015 - 01/2007)
7.	Torbicki, Adam: 3 articles (12/2015 - 03/2011)
8.	Dhaun, Neeraj: 3 articles (04/2011 - 11/2007)
9.	Goddard, Jane: 3 articles (04/2011 - 11/2007)
10.	Webb, David J: 3 articles (04/2011 - 11/2007)

Related Diseases

1.	Pulmonary Arterial Hypertension 04/08/2004 - "In a phase 2b/3 pulmonary arterial hypertension trial, once a day treatment of 100 mg of sitaxsentan statistically significantly improved 6-min walk distance and NYHA class at 12 weeks (Barst et al. Am. J. " 02/01/2012 - "To assess safety and efficacy of sitaxsentan 50 and 100 mg in patients with pulmonary arterial hypertension (PAH). " 02/01/2012 - "Safety and efficacy of sitaxsentan 50 and 100 mg in patients with pulmonary arterial hypertension." 11/01/2004 - "STRIDE-1, a 12-week randomized, doubleblind, placebo-controlled trial of sitaxsentan for pulmonary arterial hypertension showed significant benefit in 6-minute walk distance, functional class and hemodynamics. " 10/01/2008 - "Sitaxsentan for the treatment of pulmonary arterial hypertension: a 1-year, prospective, open-label observation of outcome and survival."
2.	Congenital Heart Defects (Congenital Heart Defect) 11/01/2004 - "In its first randomised, placebo-controlled study, Sitaxsentan to Relieve Impaired Exercise-1 (STRIDE-1), sitaxsentan improved exercise capacity assessed by 6 min walk, 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 PAH, PAH related to connective tissue disease or PAH related to congenital heart disease. " 01/01/2007 - "Forty-eight patients with idiopathic PAH or PAH associated with connective-tissue disease or congenital heart disease were randomized (double-blind) to a single daily dose of either 50 mg or 100 mg sitaxsentan. " 06/01/2005 - "STRIDE I evaluated the selective endothelin A receptor antagonist, sitaxsentan (SITAX), in a 12-week randomized, double-blind, trial (178 patients) employing placebo (PBO), 100 mg or 300 mg SITAX orally once daily in PAH and included patients with NYHA class II, congenital heart disease and a BL 6MW>450 m, groups often excluded from previous trials. " 02/15/2004 - "Patients with pulmonary arterial hypertension that was idiopathic, related to connective tissue disease or congenital heart disease, were randomized to receive placebo (n = 60), sitaxsentan 100 mg (n = 55), or sitaxsentan 300 mg (n = 63) orally once daily for 12 weeks. " 11/01/2005 - "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. "
3.	Connective Tissue Diseases (Connective Tissue Disease) 11/01/2004 - "In its first randomised, placebo-controlled study, Sitaxsentan to Relieve Impaired Exercise-1 (STRIDE-1), sitaxsentan improved exercise capacity assessed by 6 min walk, 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 PAH, PAH related to connective tissue disease or PAH related to congenital heart disease. " 03/01/2009 - "Further evaluation of sitaxsentan in patients with connective tissue diseases suffering from ischemic skin ulcers is required." 05/01/2008 - "Is sitaxsentan a good therapeutic option for pulmonary arterial hypertension associated with connective tissue disease?" 01/01/2007 - "Forty-eight patients with idiopathic PAH or PAH associated with connective-tissue disease or congenital heart disease were randomized (double-blind) to a single daily dose of either 50 mg or 100 mg sitaxsentan. " 02/15/2004 - "Patients with pulmonary arterial hypertension that was idiopathic, related to connective tissue disease or congenital heart disease, were randomized to receive placebo (n = 60), sitaxsentan 100 mg (n = 55), or sitaxsentan 300 mg (n = 63) orally once daily for 12 weeks. "
4.	Familial Primary Pulmonary Hypertension 11/01/2005 - "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. "
5.	Hypoxia (Hypoxemia) 11/01/2010 - "Sitaxsentan decreased PVR in acute and chronic hypoxia (both p<0.001), and partly restored V'(O(2),max), by 30 % in acute hypoxia (p<0.001) and 10% in chronic hypoxia (p<0.05). " 01/01/2000 - "The same dose of sitaxsentan delivered iv 50 min after the onset of hypoxia reversed the established pulmonary vasoconstriction. " 10/15/2012 - "Whereas under hypoxia, theophylline significantly increased muscular blood flow, and sitaxsentan increased tissue oxygenation, the combination improved both parameters but in a reduced manner. " 07/01/2001 - "Horses were exposed to a 10 min period of hypoxia (F(I)O2 approximately 0.11) on 2 occasions, with and without pretreatment with the selective ET(A) receptor antagonist TBC11251 (10 mg/kg bwt i.v.). " 01/01/2000 - "In a 2-week model of hypoxia using 10% O(2), treatment with sitaxsentan (15 mg/kg per day in drinking water) attenuated pulmonary hypertension and the associated right ventricular hypertrophy, and prevented the remodeling of small pulmonary arteries (50-100 microM) without affecting systemic arterial blood pressure or heart rate. "

Related Drugs and Biologics

1.	Endothelin A Receptor
2.	Endothelin Receptor Antagonists
3.	Theophylline (Theon)
4.	Bosentan (Tracleer)
5.	Sodium
6.	ambrisentan
7.	Endothelins (Endothelin)
8.	Endothelin Receptors (Endothelin Receptor)
9.	Atrasentan
10.	Collagen Type I (Type I Collagen)

Related Therapies and Procedures

1.	Therapeutics
2.	Cardiopulmonary Bypass (Heart-Lung Bypass)
3.	Subcutaneous Injections
4.	Drug Therapy (Chemotherapy)