enrasentan

Enrasentan is an orally active small molecule drug that acts as a mixed endothelin A (ETA) and endothelin B (ETB) receptor antagonist, with approximately 100-fold greater affinity for the ETA receptor. It was developed primarily for the treatment of cardiovascular diseases such as congestive heart failure and pulmonary hypertension. In preclinical animal models, enrasentan reduced blood pressure, prevented cardiac hypertrophy, preserved myocardial function, normalized blood pressure in hyperinsulinemic hypertensive rats, and reduced ischemic brain area in stroke models. However, clinical trials did not demonstrate favorable effects on ventricular remodeling in heart failure patients. The drug reached phase II clinical development before its discontinuation[1][2][3][4][7].

Other names

enrasentanEnrasentan [INN]167256-08-8