etamicastat

Etamicastat is a peripherally selective, reversible inhibitor of dopamine β-hydroxylase (DBH), the enzyme responsible for converting dopamine to noradrenaline in sympathetic nerves. By inhibiting DBH, etamicastat reduces noradrenaline levels and increases dopamine levels in peripheral tissues, leading to decreased sympathetic nervous system activity. This results in dose-dependent reductions in systolic and diastolic blood pressure without affecting heart rate. Etamicastat was developed as an oral antihypertensive agent with potential benefits for heart failure due to its ability to lower blood pressure and improve renal function parameters such as vasodilation, diuresis, and natriuresis. The drug was specifically designed not to cross the blood–brain barrier to minimize central side effects seen with earlier DBH inhibitors like nepicastat. Clinical trials demonstrated its efficacy in lowering blood pressure; however, development for hypertension and heart failure has been discontinued[1][4][5][6][7].

Other names

Etamicastat [INN]760173-05-5UNII-9X96V6DBU4UNII9X96V6DBU4UNII 9X96V6DBU4