API Product   :    Macitentan*
CEP   :    -
WCC   :    -
Therapeutic Use    :    Other cardiovascular products; Antihypertensives
Originator   :    Actelion Pharmaceuticals Ltd.
CAS No.    :    441798-33-0
Trade Name.   :    OPSUMIT
Molecular Weight   :    588.28 g/ mol
Molecular Formula   :    C19H20Br2N6O4S
Macitentan is used to treat high blood pressure in the lungs (pulmonary arterial hypertension). This condition is thought to be caused by increased levels of a certain natural substance (endothelin-1).
Macitentan (trade name Opsumit) is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH).[1] The other two ERAs marketed as of 2014 are bosentan and ambrisentan.[1] Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB.[1] However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype.