Which medications in the drug class Endothelin-Receptor Antagonists are used in the treatment of Pulmonary Arterial Hypertension?

Updated: Apr 25, 2018
  • Author: Kristin E Schwab, MD; Chief Editor: Zab Mosenifar, MD, FACP, FCCP  more...
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Answer

Endothelin-Receptor Antagonists

Endothelin-receptor antagonists competitively bind to the endothelin-1 receptors EtA and EtB, causing reductions in pulmonary arterial pressure, pulmonary vascular resistance, and mean right atrial pressure.

Bosentan (Tracleer)

Bosentan is indicated for the treatment of PAH in patients with WHO class III or IV symptoms to improve exercise ability and decrease the rate of clinical decline. It inhibits vessel constriction and elevation of blood pressure by competitively binding to EtA and EtB receptors in endothelium and vascular smooth muscle. This leads to a significant increase in cardiac index associated with significant reductions in pulmonary arterial pressure, pulmonary vascular resistance, and mean right atrial pressure. Because of its teratogenic potential, bosentan can be prescribed only through the Tracleer Access Program (phone: 1-866-228-3546).

Ambrisentan (Letairis)

Ambrisentan inhibits vessel constriction and elevation of blood pressure by competitively binding to EtA and EtB receptors in endothelium and vascular smooth muscle. This leads to a significant increase in cardiac index associated with significant reductions in pulmonary arterial pressure, pulmonary vascular resistance, and mean right atrial pressure. Ambrisentan is indicated for the treatment of WHO group 1 PAH in patients to improve exercise ability and delay clinical worsening. It is also indicated in combination with tadalafil to reduce the risks of disease progression and hospitalization for worsening PAH, and to improve exercise ability. Because of the risks of hepatic injury and potential teratogenesis, ambrisentan is available only through the Letairis Education and Access Program (LEAP). Prescribers and pharmacies must register with LEAP in order to prescribe and dispense. For more information, see http://www.letairis.com or call (866) 664-LEAP (5327).

Macitentan (Opsumit)

Macitentan is a dual endothelin receptor antagonist that prevents binding of ET1 to both EtA and EtB receptors. It is indicated to delay disease progression of PAH (WHO group I).


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