Macitentan

Macitentan is an endothelin receptor antagonist used to treat pulmonary arterial hypertension (PAH). It works by blocking endothelin receptors on vascular smooth muscle and blood vessels, reducing vasoconstriction, vascular remodeling, inflammation, fibrosis, and cell proliferation, thereby improving pulmonary blood flow. Macitentan carries a high risk of embryo-fetal toxicity and is contraindicated during pregnancy, requiring strict pregnancy prevention measures in women of childbearing potential.

Macitentan is an endothelin receptor antagonist used to manage pulmonary arterial hypertension to delay disease progression.

Macitentan is indicated for patients with pulmonary arterial hypertension.

• Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)

Macitentan blocks simulators of hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction.

Macitentan is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Macitentan binds to the receptors, endothelin A and B (ETA and ETB), which prevents the agonist endothelin -1 (ET-1) from binding and stimulating the ETA and ETB receptors.

Macitentan is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached.

Macitentan has a volume of distribution of 50L.

Macitentan is >99% bound to plasma proteins, which are mainly albumin

Eliminated 50% through urine and 24% through feces.

The half life of macitentan is 16 hours, and the half life of it's active metabolite is 48 hours.

Clearance data was not found.

Macitentan has a black box warning of embryo-fetal toxicity. Special precautions must be taken for all females of child-bearing age, and women who are pregnant must not be given macitentan.

• Take with or without food.