Macitentan for the treatment of pulmonary arterial hypertension.
BACKGROUND
Pulmonary arterial hypertension (PAH) is a serious disease characterized by elevation of pulmonary artery pressures and right ventricular failure. It is a progressive disease with a poor 5-year survival despite recent advances in treatment. Endothelin plays an important role in the development and progression of the disease. Endothelin receptor blockers have been used to treat PAH since 2001. More recently, macitentan was approved for treatment of PAH.


METHODS
This review covers the preclinical and clinical data on macitentan.


CONCLUSIONS
Macitentan is a more potent ERA and has been shown to delay progression of the disease. It does not appear to have any significant hepatotoxicity and has a convenient once-a-day dosing. In the large event driven trial, macitentan significantly reduced morbidity in patients with PAH. It was safe and well tolerated and the benefit was seen in treatment-naïve patients and those already receiving PAH therapy.
Associate ProfessorThe Ohio State University , Columbus, OH 43210 , USA sood.7@osu.edu.
Namita
N
Sood
D002986:Clinical Trials as Topic; D065128:Endothelin Receptor Antagonists / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D006207:Half-Life; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy*; D011743:Pyrimidines / Q000493:pharmacokinetics / Q000627:therapeutic use*; D017466:Receptors, Endothelin / Q000737:chemistry / Q000378:metabolism; D013449:Sulfonamides / Q000493:pharmacokinetics / Q000627:therapeutic use*
D065128:Endothelin Receptor Antagonists; D011743:Pyrimidines; D017466:Receptors, Endothelin; D013449:Sulfonamides; C533860:macitentan
endothelin; macitentan; pulmonary arterial hypertension