Ambrisentan is a selective type A endothelin receptor antagonist used to treat primary pulmonary arterial hypertension and pulmonary arterial hypertension based on diagnostic classifications. It is approved in Europe, Canada and the United States for use as a single agent to improve exercise ability and delay clinical worsening.
- Mechanism
- Curator reviewed
Endothelin-1 (ET-1) is an endogenous peptide that acts on the endothelin type A (ETA) and endothelin type B (ETB) receptors in vascular smooth muscle and endothelium. ETA-mediated actions include vasoconstriction and cell proliferation, whereas ETB predominantly mediates vasodilation, anti-proliferation, and ET-1 clearance. In patients with pulmonary arterial hypertension, ET-1 levels are increased and correlate with increased right arterial pressure and severity of disease. Ambrisentan is one of several newly developed vasodilator drugs that selectively target the endothelin type A (ETA) receptor, inhibiting its action and preventing vasoconstriction. Selective inhibition of the ETA receptor prevents phospholipase C-mediated vasoconstriction and protein kinase C-mediated cell proliferation. Endothelin type B (ETB) receptor function is not significantly inhibited, and nitric oxide and prostacyclin production, cyclic GMP- and cyclic AMP-mediated vasodilation, and endothelin-1 (ET-1) clearance is preserved.
- Primary indication
- Ambrisentan is indicated for treatment of idiopathic (‘primary’) pulmonary arterial hypertension (IPAH) and pulmonary arterial hypertension (PAH) associated with connective tissue disease in patients with WHO functional class II or III symptoms.Curator reviewed · 1 structured indication
- Formula / weight
- C22H22N2O4 · 378.428 g/mol (avg)
- First approval
- Canada, 2008 · United States, 2007 · European Union, 2016
- Code names
- BSF-208075 · GSK-1325760 · GSK-1325760A · LU-208075
- Brand names
Resolves to
OUJTZYPIHDYQMC-LJQANCHMSA-NSMILESCOC([C@H](OC1=NC(C)=CC(C)=N1)C(O)=O)(C1=CC=CC=C1)C1=CC=CC=C1What you can answer from here — as of May 03, 2025
Which drugs share a target with Ambrisentan, and which of those have an active Phase 3 trial?
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