title: Macitentan for the treatment of pulmonary arterial hypertension.
abstract: Macitentan is a novel, dual endothelin receptor antagonist recently approved for the treatment of WHO Group I pulmonary arterial hypertension. Its pharmacologic mechanism of action as well as the pharmacokinetics, pharmacodynamics and potential drug-drug interactions have been demonstrated in multiple phase I and II trials. The pivotal randomized, placebo-controlled, event-driven clinical trial revealed a significant reduction in morbidity. The most common adverse events were rarely clinically significant, nor did they result in a high rate of discontinuation. Of note, macitentan is contraindicated in pregnant women due to embryo-fetal toxicity.
authors.affiliation: University of Kansas Medical Center, Kansas City, Kansas, USA. LSpikes@kumc.edu.
authors.forename: L
authors.initials: L
authors.lastname: Spikes
authors.affiliation: University of Kansas Medical Center, Kansas City, Kansas, USA.
authors.forename: T
authors.initials: T
authors.lastname: Williamson
authors.affiliation: University of Kansas Medical Center, Kansas City, Kansas, USA.
authors.forename: L
authors.initials: L
authors.lastname: Satterwhite
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D062186:Arterial Pressure / Q000187:drug effects*; D004347:Drug Interactions; D065130:Endothelin A Receptor Antagonists; D065627:Familial Primary Pulmonary Hypertension; D005260:Female; D005333:Fetus / Q000187:drug effects; D006801:Humans; D006976:Hypertension, Pulmonary / Q000175:diagnosis / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D061214:Patient Safety; D011247:Pregnancy; D011651:Pulmonary Artery / Q000187:drug effects* / Q000378:metabolism / Q000503:physiopathology; D011743:Pyrimidines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D044022:Receptor, Endothelin A / Q000378:metabolism; D013449:Sulfonamides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016896:Treatment Outcome
chemical_list: D000959:Antihypertensive Agents; D065130:Endothelin A Receptor Antagonists; D011743:Pyrimidines; D044022:Receptor, Endothelin A; D013449:Sulfonamides; C533860:macitentan
keywords: Actelion-1; Endothelin receptor antagonist (ERA); Macitentan; Pulmonary arterial hypertension (PAH)