Endothelin receptor antagonist

An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors.

Three main kinds of ERAs exist:

• selective ET_A receptor antagonists (sitaxentan, ambrisentan, atrasentan, BQ-123, zibotentan, edonentan), which affect endothelin A receptors.
• dual antagonists (bosentan, macitentan, tezosentan), which affect both endothelin A and B receptors.
• selective ET_B receptor antagonists (BQ-788 and A192621) which affect endothelin B receptors are used in research but have not yet reached the clinical trial stage.

Macitentan, ambrisentan and bosentan are mainly used for the treatment of pulmonary arterial hypertension, while atrasentan is an experimental anti-cancer drug.