Clinical Pharmacokinetics and Pharmacodynamics of the Endothelin Receptor Antagonist Macitentan

摘要: Pulmonary arterial hypertension (PAH) is a progressive disease of the lung vascular system, which leads to right-sided heart failure and ultimately death if untreated. Treatments regulate pulmonary pressure target prostacyclin, nitric oxide, endothelin (ET) pathways. Macitentan, an oral, once-daily, dual ETA ETB receptor antagonist with high affinity sustained binding first ET show significant reduction risk morbidity mortality in PAH patients large-scale phase III study long-term outcome. Here we present review available clinical pharmacokinetic, pharmacodynamic, pharmacokinetic/pharmacodynamic relationship, drug–drug interaction data macitentan healthy subjects, PAH, special populations.