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Safety, efficacy, and clinical utility of macitentan in the treatment of pulmonary arterial hypertension

Authors Monaco T, Davila C

Received 11 December 2015

Accepted for publication 3 March 2016

Published 18 May 2016 Volume 2016:10 Pages 1675—1682


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Prof. Dr. Wei Duan

Thomas J Monaco,1 Carlos D Davila2

1Division of Pulmonary and Critical Care Medicine, Baylor College of Medicine, Houston, TX, 2Department of Medicine, Einstein Medical Center, Philadelphia, PA, USA

Abstract: Pulmonary arterial hypertension is a progressive, debilitating disease caused by a dysregulation of the pulmonary vascular tone that inevitably leads to right heart failure and death without treatment. Until relatively recently, the treatment options for those afflicted by pulmonary arterial hypertension were limited; today, a greater understanding of the pathophysiology behind this disease has led to several evidence-based therapies that can improve pulmonary function and quality of life for these patients. One of the primary mediators of pulmonary vascular tone is endothelin-1, which is a potent and long-lasting vasoconstrictor. Macitentan is a second-generation endothelin receptor antagonist that acts selectively as a pulmonary vasodilator without the significant side effects noted with previous endothelin receptor antagonists. This review focuses on the mechanism of action and pharmacokinetics of macitentan, as well as the adverse effects, efficacy, and clinical uses of macitentan in the clinical trials to date. In addition, the authors briefly review clinical trials currently underway to illustrate possible future directions for the use of macitentan.

Keywords: pulmonary arterial hypertension, macitentan, endothelin receptor antagonist

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