Drug intelligence / Profile preview

aliskiren + furosemide

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

**Aliskiren + furosemide** is a combination of two pharmaceutical drugs used together for their antihypertensive and diuretic effects. - **Aliskiren** is a direct renin inhibitor that blocks the conversion of angiotensinogen to angiotensin I by inhibiting renin. This leads to lower plasma concentrations of angiotensin I and II, reducing blood pressure primarily through decreased vasoconstriction and aldosterone-mediated sodium retention[2][4][6]. - **Furosemide** is a loop diuretic that inhibits the sodium-potassium-chloride cotransporter (NKCC2) in the thick ascending limb of the loop of Henle. This promotes diuresis by preventing sodium and chloride reabsorption, leading to increased excretion of water, sodium, chloride, and other electrolytes[5]. When coadministered, aliskiren significantly reduces the plasma concentration and exposure of furosemide (decreased AUC by 28% and Cmax by 49%), which may diminish its diuretic effect and requires monitoring[1][2][3][7]. The combination is primarily considered for patients with hypertension who benefit from both renin-angiotensin system blockade and potent diuresis.

02

Targets

REN (Renin)NKCC2 (Sodium-potassium-chloride cotransporter 2)NKCC (Sodium-potassium-chloride cotransporter)

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