Harman Patil (Editor)

Endothelin receptor antagonist

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

Three main kinds of ERAs exist:

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

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

    Edonentan is an endothelin receptor antagonist drug.

    References

    Endothelin receptor antagonist Wikipedia
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