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Endothelin Receptor Antagonist

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Endothelin Receptor Antagonist, Bosentan, Tracleer, Ambrisentan, Letairis, Macitentan, Opsumit, Sitaxsentan

  • See Also
  1. Aprocitentan
  • Indications
  1. Pumonary Arterial Hypertension
    1. Bosentan (Tracleer)
    2. Ambrisentan (Letairis)
    3. Macitentan (Opsumit)
    4. Sitaxsentan
  2. Hypertension (fourth-line, refractory)
    1. Aprocitentan
  3. Cancer (e.g. Prostate Cancer, Colorectal Cancer, experimental)
    1. Endothelins inhibition may decrease tumor growth, progression, and Angiogenesis
  • Mechanism
  1. Endothelin is a vasonstrictor and Aldosterone mediator
  2. Endothelin Receptor Antagonists inhibit endothelin activity, resulting in vasodilation
  1. Bosentan (Tracleer)
    1. Start 62.5 mg orally twice daily (may increase to 125 mg twice daily)
  2. Ambrisentan (Letairis)
    1. Start 5 mg daily (may increase to 10 mg daily)
  3. Macitentan (Opsumit)
    1. Start 10 mg orally daily
  4. Sitaxsentan
  • Drug Interactions
  1. Oral Contraceptives (OCP)
    1. May reduce OCP efficacy
  2. Warfarin
    1. Increased INR
  • Adverse Effects
  1. Peripheral Edema
  2. Flushing
  3. Headache
  4. Liver Function Test abnormalities
  • Safety
  1. FDA pregnancy category X
  2. Monitoring
    1. Liver Function Testing monthly (hepatotoxicity risk)