enarsentan

Enarsentan is a small molecule dual endothelin receptor antagonist (ERA) that targets both the endothelin-A (ETA) and endothelin-B (ETB) receptors. It is primarily being investigated for the prevention and treatment of acute mountain sickness (AMS) and high-altitude pulmonary edema (HAPE). The drug's mechanism involves blocking the binding of endothelin-1 (ET-1), a potent endogenous vasoconstrictor that is significantly upregulated during exposure to high-altitude hypoxia. By inhibiting these receptors, enarsentan helps to mitigate hypoxia-induced pulmonary hypertension and vascular permeability, which are central to the pathophysiology of altitude-related illnesses. Clinical development has been notably active in China, where it has been evaluated in Phase 4 studies involving healthy adults ascending to high altitudes.

Other names

enrasentanSB 217242SB217242SB-217242依那生坦