Macitentan

Macitentan tablets are an endothelin receptor antagonist (ERA) indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) in adults to reduce the risks of disease progression and hospitalization for PAH ( 1.1 ). 1.1 Pulmonary Arterial Hypertension Macitentan tablets are an endothelin receptor antagonist (ERA) indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) in adults to reduce the risks of disease progression and hospitalization for PAH.

12.1 Mechanism of Action Endothelin (ET)-1 and its receptors (ET A and ET B ) mediate a variety of deleterious effects, such as vasoconstriction, fibrosis, proliferation, hypertrophy, and inflammation. In disease conditions such as PAH, the local ET system is upregulated and is involved in vascular hypertrophy and in organ damage. Macitentan is an endothelin receptor antagonist that inhibits the binding of ET-1 to both ET A and ET B receptors. Macitentan displays high affinity and sustained occupancy of the ET receptors in human pulmonary arterial smooth muscle cells.

Following administration (10 mg/1 Tablet, Film Coated), Macitentan achieves F ≈ 47%–59% systemic availability after standard oral Macitentan administration bioavailability and time to peak concentration spans 1 to 2 hrs under macitentan maintenance onset, governed by a Terminal t½ estimated at 7–19 hrs depending on renal/hepatic reserve (Macitentan) terminal half-life through macitentan undergoes cyp3a4/cyp2c9-mediated hepatic metabolism prior to excretion.

Before initiating Macitentan at 10 mg/1 Tablet, Film Coated, clinical safety checklists rule out 4 contraindications; hypersensitivity ( 4.2 ) 4.1 pregnancy macitentan may cause fetal harm when administered to a pregnant woman.; macitentan is contraindicated in females who are pregnant.. Logged tolerability patterns center on headache (11.6% of reports), nausea (7.5% of reports), nasopharyngitis (6.1% of reports).