Sitaxentan sodium Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
In November Encysive Pharmaceuticals launched Thelin®
(sitaxsentan sodium) in the U.K. for the treatment of pulmonary
arterial hypertension (PAH), following European Commission
approval in August 2006. Sitaxsentan is the first
selective endothelin A (ETA) receptor antagonist, and the
first once-daily oral treatment available for patients with
PAH. It is 6,500-fold selective in the targeting of ETA versus ETB receptors. Sitaxsentan is indicated for improving
exercise capacity in PAH patients classified as World Health
Organization (WHO) functional class III. Efficacy has been
shown in primary pulmonary hypertension and pulmonary
hypertension associated with connective tissue disease. In
the U.S., Encysive has submitted a complete response to an
approvable letter received from the FDA in July.
Verwenden
Selective endothelin A (ETA) receptor antagonist. Antihypertensive. Used in treatment of chronic heart failure.
Allgemeine Beschreibung
Sitaxentan sodium, belongs to thesulfonamide class of endothelin receptor antagonists.Although it has 6,000-fold selectivity for the ETA receptor,clinical trials have not demonstrated a greater efficacyover bosentan. However, it has much lower liver toxicitythan bosentan. The manufacturer is attempting to meetefficacy outcomes set by the FDA, which must be met beforeapproval of sitaxsentan as a therapeutic agent will begranted.
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