Drug intelligence / Profile preview

ambrisentan

Development stage
Approved
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

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].

Brand names
LetairisVolibrisPulmonext
Other names
ambrisentan [INN]Gilead brand of ambrisentan
02

Targets

EDNRA (Endothelin receptor type A)

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