Dosing & Uses
Pulmonary Arterial Hypertension
Fixed-dose combination pending FDA approval for treatment of pulmonary arterial hypertension (PAH)
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Pharmacology
Mechanism of Action
Macitentan: Endothelin receptor antagonist (ERA); prevents binding of endothelin (ET)-1 to both ET-A and ET-B receptors with high affinity to ET receptors in pulmonary arterial smooth muscle cells; active metabolite 20% as potent as parent compound
Tadalafil: Inhibits PDE-5, increasing cGMP to allow relaxation of pulmonary vascular smooth-muscle cells and vasodilation of pulmonary vasculature
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Images
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.
