Endothelin receptor antagonist
Drug that blocks endothelin receptors
An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors.
Three main kinds of ERAs exist:
- Dual ET Receptor Antagonists, which affect both endothelin A (ETA) and B receptors (ETB) [1]
- aprocitentan, bosentan, macitentan, tezosentan
- Selective ETA Receptor Antagonists, which affect endothelin A receptors
- sitaxentan, ambrisentan, atrasentan, BQ-123, sparsentan, zibotentan, avosentan, edonentan, clazosentan
- Selective ETB Receptor Antagonists, which affect endothelin B receptors
- BQ-788 and A192621 are used in research but have not yet reached 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.
References
- ^ Endothelin receptor antagonists
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