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Sitaxsentan: a selective endothelin-A receptor antagonist, for the treatment of pulmonary arterial hypertension

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EXPERT OPINION ON PHARMACOTHERAPY
卷 8, 期 1, 页码 95-109

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TAYLOR & FRANCIS LTD
DOI: 10.1517/14656566.8.1.95

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endothelin-1; endothelin receptor antagonist; pulmonary arterial hypertension

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Pulmonary arterial hypertension (PAH) is a progressive, life-threatening condition. Sitaxsentan, a selective enclothelin-A receptor antagonist, is an effective, safe and well-tolerated enclothelin 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.

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