Drug intelligence / Profile preview

Tasosartan

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Tasosartan is a selective, potent, orally active, and long-acting nonpeptide angiotensin II type 1 (AT1) receptor antagonist. It blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor in vascular smooth muscle and the adrenal gland. By blocking these receptors, tasosartan causes vasodilation, reduces secretion of vasopressin (ADH), decreases production and secretion of aldosterone, and ultimately lowers blood pressure. Its antihypertensive effect is attributed to both direct antagonism of angiotensin II-induced vasoconstriction and reduction in aldosterone-mediated sodium retention. Tasosartan was developed for the treatment of hypertension and heart failure but was withdrawn from FDA review after phase III clinical trials due to safety concerns[1][3][4][5].

02

Targets

AGTR1 (Angiotensin II Type-1 receptor)AGTR2 (AT2)

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