Sitaxentan

Products Sitaxentan had been on the market in the EU since 2006 in the form of film-coated tablets (Thelin 100 mg, Pfizer). It was withdrawn from the market in 2010 because of liver-toxic side effects. Structure and properties Sitaxentan (C18H15ClN2O6S2, Mr = 454.9 g/mol) is an oxazole, thiophene, benzodioxole, and sulfonamide derivative. It is present … Sitaxentan

Ambrisentan

Products Ambrisentan is commercially available in the form of film-coated tablets (Volibris). It has been approved in many countries since 2008. Generic versions were registered in 2020. Structure and properties Ambrisentan (C22H22N2O4, Mr = 378.4 g/mol) is a dimethylpyrimidine, diphenyl and propionic acid derivative and exists as a white crystalline powder that is practically insoluble … Ambrisentan

Macitentan

Products Macitentan is commercially available in the form of film-coated tablets (Opsumit). It was approved in the United States in October 2013 and in many countries in 2014. Macitentan was launched as a successor to bosentan (Tracleer) as it loses patent protection. Structure and properties Macitentan (C19H20Br2N6O4S, Mr = 588.3 g/mol) is a brominated pyrimidine … Macitentan

Bosentan

Products Bosentan is commercially available in the form of tablets and dispersible tablets (Tracleer). It has been approved in many countries since 2002. Generic versions were registered in 2017. Structure and properties Bosentan (C27H29N5O6S, Mr = 551.6 g/mol) is present in drugs as bosentan monohydrate, a white to yellowish powder that is poorly soluble in … Bosentan