Chengde Wu, E Radford Decker, Natalie Blok, Huong Bui, Tony J You, Junmei Wang, Andree R Bourgoyne, Vippra Knowles, Kurt L Berens, George W Holland, Tommy A Brock, Richard A F Dixon
Sitaxsentan (1) (Wu et al. J. Med. Chem. 1997, 40, 1690) is our first endothelin antagonist being evaluated in clinical trials. It has demonstrated biological effects in an acute hemodynamic study in CHF (Givertz et al. Circulation 2000, 101, 2922), an open-label 20-patient pulmonary hypertension trial (Barst et al. Chest 2002, 121, 1860-1868), and a 31-patient trial in essential hypertension (Calhoun et al. AHA Scientific Sessions 2000). 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...
April 8, 2004: Journal of Medicinal Chemistry