darusentan

Darusentan is a selective endothelin ETA receptor antagonist and a small molecule drug. It acts by selectively blocking the binding of endothelin-1 (ET-1) to the endothelin type-A (ETA) receptor, thereby inhibiting ET-1-induced vasoconstriction and reducing blood pressure. Darusentan is orally bioavailable, with maximum plasma concentrations reached within 1–2 hours post-dose and a mean elimination half-life greater than 15 hours, supporting once-daily dosing. The drug was primarily developed for the treatment of resistant hypertension and congestive heart failure. Clinical trials demonstrated dose-dependent reductions in systolic and diastolic blood pressure in patients with moderate or resistant hypertension; however, phase III trials did not meet all primary efficacy endpoints for resistant hypertension, leading to discontinuation of further development for this indication. The most common adverse events reported were peripheral edema and headache[1][2][3][4][5][7].

Other names

171714-84-4