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Ambrisentan is an orally active, selective endothelin type A (ETA) receptor antagonist used for the treatment of pulmonary arterial hypertension (PAH), specifically WHO Group 1 PAH in patients with functional class II or III symptoms. It works by blocking the action of endothelin-1, a potent vasoconstrictor and mitogen that is elevated in PAH. By selectively antagonizing endothelin type A receptor (ETA) on vascular smooth muscle cells, ambrisentan reduces vasoconstriction and cellular proliferation while allowing ETB-mediated vasodilation and clearance of endothelin-1 to continue. This results in relaxation of pulmonary blood vessels, improved exercise capacity, delayed clinical worsening, and reduced risk of disease progression or hospitalization. Ambrisentan can be used as monotherapy or in combination with tadalafil for enhanced efficacy[1][2][3][5][6][8].
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