Products
Endothelin receptor antagonists are commercially available in the form of film-coated and dispersible tablets. The first agent in this group to be approved was bosentan (Tracleer) in the United States in 2001 and in the EU and Switzerland in 2002.
Effects
- Antivasoconstrictive
- Reduce pulmonary and systemic vascular resistance
- Higher blood flow volume without increasing heart rate
Endothelin receptor antagonists are antagonists at the ETA and/or ETB receptor. They abolish the effects of endothelin, thereby decreasing pulmonary and systemic vascular resistance, resulting in higher blood output without increasing heart rate.
Indications
- For the treatment of pulmonary arterial hypertension.
- Reduction in the number of new digital ulcerations in patients with systemic sclerosis with active digital ulcer disease.
Agents
- Ambrisentan (Volibris)
- Bosentan (Tracleer)
- Macitentan (Opsumit)
- Sitaxentan (Thelin, out of commerce)
