What are the clinical pharmacokinetics, pharmacodynamics, and drug-drug interactions of macitentan in healthy subjects and PAH patients?
This review summarizes the clinical pharmacokinetics and pharmacodynamics of macitentan, an endothelin receptor antagonist used for pulmonary arterial hypertension.
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 to regulate the pulmonary vascular pressure target the prostacyclin, nitric oxide, and endothelin (ET) pathways. Macitentan, an oral, once-daily, dual ETA and ETB receptor antagonist with high affinity and sustained receptor binding is the first ET receptor antagonist to show significant reduction of the risk of morbidity and mortality in PAH patients in a large-scale phase III study with a long-term outcome. Here we present a review of the available clinical pharmacokinetic, pharmacodynamic, pharmacokinetic/pharmacodynamic relationship, and drug-drug interaction data of macitentan in healthy subjects, patients with PAH, and in special populations.
Sidharta et al. (Thu,) studied this question.