sitaxsentan

Sitaxsentan is a small molecule, selective endothelin-A (ET-A) receptor antagonist developed for the treatment of pulmonary arterial hypertension (PAH). It acts by competitively blocking the binding of endothelin, a potent vasoconstrictor, to ET-A receptors on vascular smooth muscle cells. This blockade leads to decreased pulmonary vascular resistance and improved exercise capacity in patients with PAH. Sitaxsentan has much higher selectivity for ET-A over ET-B receptors compared to other drugs in its class such as bosentan. It was originally marketed under the brand name Thelin by Encysive Pharmaceuticals and later Pfizer but was withdrawn from global markets due to concerns about hepatotoxicity[1][2][3][4].

Brand names

Thelin

Other names

sitaxentansitaxsentan sodiumN-(4-chloro-3-methyl-5-isoxazolyl)-2-(3,4-(methylenedioxy)-6-methyl)phenylacetyl-3-thiophenesulfonamide