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Macitentan: A Review of Its Use in Patients with Pulmonary Arterial Hypertension

Abstract

Macitentan (Opsumit®) is an orally active, dual endothelin receptor antagonist (ERA) with tissue targeting properties. Macitentan was approved recently in the EU (as monotherapy or combination therapy) for the long-term treatment of pulmonary arterial hypertension (PAH) in adults of WHO functional class II or III, and in the USA for the treatment of PAH (WHO group I) to delay disease progression and reduce hospitalization for PAH. This article reviews the pharmacological properties, efficacy and tolerability data relevant to the use of macitentan in this indication. Treatment with macitentan 10 mg once daily significantly reduced the risk for the primary composite endpoint of morbidity and mortality in patients with PAH (mostly WHO functional class II or III) in the large, randomized, placebo-controlled SERAPHIN study. Other efficacy outcomes, including exercise capacity, haemodynamic parameters and health-related quality of life also improved significantly with macitentan relative to placebo. Macitentan was generally well tolerated in this study. As with other ERAs, haemoglobin levels decreased with macitentan therapy; however, these were not progressive and stabilized following longer-term treatment. Although comparative studies are needed to definitively position macitentan with respect to other approved agents, current evidence suggests that macitentan is a useful treatment option for initial therapy in patients with WHO functional class II or III PAH, which has the potential advantage of once-daily administration.

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Disclosure

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made by the author on the basis of scientific and editorial merit. Sohita Dhillon is a salaried employee of Adis/Springer.

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Correspondence to Sohita Dhillon.

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The manuscript was reviewed by: N. Galie, Institute of Cardiology, University of Bologna, Bologna, Italy; L.J. Rubin, Division of Pulmonary and Critical Care Medicine, Department of Medicine, University of California San Diego School of Medicine, La Jolla (CA), USA.

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Dhillon, S. Macitentan: A Review of Its Use in Patients with Pulmonary Arterial Hypertension. Drugs 74, 1495–1507 (2014). https://doi.org/10.1007/s40265-014-0266-9

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  • DOI: https://doi.org/10.1007/s40265-014-0266-9

Keywords

  • Pulmonary Arterial Hypertension
  • Idiopathic Pulmonary Fibrosis
  • Functional Class
  • Bosentan
  • PDE5 Inhibitor