Endothelin A receptor antagonist
- Prevents the most potent endogenous vasoconstrictor
- Pulmonary vasodilation → ↓ pulmonary arterial pressure
- Systemic vasodilation → ↓ blood pressure
- Fluid retention and teratogenicity are class effects
- Vasodilation in pulmonary arterial hypertension
- Hepatotoxicity and fluid retention; contraindicated in pregnancy
Drugs with this mechanism (5)
- Ambrisentan — Endothelin-A antagonist for pulmonary arterial hypertension.
- Aprocitentan — Endothelin-receptor antagonist added for hypertension resistant to standard multidrug therapy.
- Bosentan — Endothelin antagonist for pulmonary hypertension; hepatotoxic, teratogenic.
- Macitentan — Once-daily endothelin antagonist for pulmonary hypertension.
- Sparsentan — Dual endothelin ETA and AT1 antagonist for IgA nephropathy; hepatotoxicity and fetal toxicity REMS.
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