Ambrisentan

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable, selective antagonist of the endothelin type-A (ETA) receptor that may be used for the treatment of pulmonary arterial hypertension (PAH). Upon administration, ambrisentan targets and binds to ETA receptor, which prevents the binding of endothelin-1 (ET-1) to the ETA receptor and ET-1/ETA-mediated vasoconstriction and cell proliferation. This may lead to vasodilation. ET-1 concentrations are increased in plasma as well as lung tissue in PAH, and ET-1 may play a key role in the pathogenesis of PAH.

**Synonyms:** - (+-)-(2S)-2-((4,6-Dimethylpyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic Acid - AMBRISENTAN - BSF-208075 - LU-208075 - Letairis - Pulmonext - Volibris