Active Pharmaceutical Ingredients (APIs)

  • Macitentan*

    • 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

    Application

    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).

    General Description

    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.