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Abstract
Macitentan is an orally active, dual endothelin receptor antagonist (ERA) with tissue targeting properties. Macitentan was approved recently in the EU for the long-term treatment of pulmonary arterial hypertension (PAH) in adults of WHO functional class II or III, and in the US 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.