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Saprisartan is a selective, potent, orally active, and long-acting nonpeptide angiotensin II type 1 (AT1) receptor antagonist. It was developed for the treatment of hypertension and heart failure. Saprisartan works by blocking the renin-angiotensin-aldosterone system (RAAS) at the AT1 receptor level in vascular smooth muscle and adrenal gland tissue. This antagonism leads to decreased sodium reabsorption and vasoconstriction, resulting in lower blood pressure. The drug is based on losartan’s prototypical chemical structure but features insurmountable/noncompetitive antagonism likely due to slow dissociation kinetics from the AT1 receptor. Despite its promising pharmacological profile and high oral bioavailability, clinical development of saprisartan was discontinued[1][2][3][4][5][7].
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