Sitaxsentan: a selective endothelin-A receptor antagonist, for the treatment of pulmonary arterial hypertension.
Pulmonary arterial hypertension (PAH) is a progressive, life-threatening condition. Sitaxsentan, a selective endothelin-A receptor antagonist, is an effective, safe and well-tolerated endothelin receptor antagonist for the treatment of PAH in adult patients. Multi-center, randomized, placebo-controlled clinical trials have demonstrated that sitaxsentan has beneficial effects on exercise capacity (i.e., 6-min walk distance), functional class and hemodynamic parameters in PAH patients. Sitaxsentan has a low incidence of acute hepatotoxicity. Patients on concomitant warfarin require a decrease in warfarin dose to maintain a therapeutic international normalized ratio. The demonstration of clinical efficacy and low incidence of acute hepatotoxicity support the potential use of sitaxsentan for the treatment of PAH.
Barst
Robyn J
RJ
Columbia University College of Physicians and Surgeons, 3959 Broadway, BHN 2-255, New York, NY 10032, USA. rjb3@columbia.edu
D065130:Endothelin A Receptor Antagonists; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy* / Q000453:epidemiology / Q000503:physiopathology; D007555:Isoxazoles / Q000494:pharmacology* / Q000627:therapeutic use*; D015337:Multicenter Studies as Topic; D016032:Randomized Controlled Trials as Topic; D044022:Receptor, Endothelin A / Q000502:physiology; D013876:Thiophenes / Q000494:pharmacology* / Q000627:therapeutic use*
D065130:Endothelin A Receptor Antagonists; D007555:Isoxazoles; D044022:Receptor, Endothelin A; D013876:Thiophenes; C106276:sitaxsentan