A review of sitaxsentan sodium in patients with pulmonary arterial hypertension.
Pulmonary arterial hypertension (PAH) is a life threatening, progressive condition which eventually leads to fatal right heart failure. Endothelin-1 (ET-1), a potent vasoconstrictor peptide, is increased in the pulmonary arteries of patients with pulmonary hypertension. Endothelin-1 acts through the stimulation of 2 subtypes of receptors (endothelin receptor subtypes A [ET(A)] and B [ET(B)]). In PAH patients, ETRAs block the deleterious vasoconstrictor effects of ET-1, and ETRA treatment in PAH patients has been shown to be safe and efficacious. Sitaxsentan is an orally active, highly ET(A) selective ETRA that, in clinical trials, has demonstrated improvements in exercise capacity, functional class and hemodynamics in PAH patients. Sitaxsentan has been shown to be safe, well tolerated, and associated with a lower incidence of liver toxicity than other approved ETRAs.
Waxman
Aaron B
AB
Department of Internal Medicine, Pulmonary Critical Care Unit, Harvard Medical School, Massachusetts General Hospital, Boston, MA 02114-2621, USA. abwaxman@partners.org
D002986:Clinical Trials as Topic; D065128:Endothelin Receptor Antagonists; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy*; D007555:Isoxazoles / Q000627:therapeutic use*; D011669:Pulmonary Wedge Pressure / Q000187:drug effects; D013876:Thiophenes / Q000627:therapeutic use*; D016896:Treatment Outcome
D065128:Endothelin Receptor Antagonists; D007555:Isoxazoles; D013876:Thiophenes; C106276:sitaxsentan