Drug intelligence / Profile preview

aliskiren + valsartan

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

Overview

Aliskiren + valsartan is a fixed-dose combination antihypertensive drug that combines two agents targeting the renin-angiotensin-aldosterone system (RAAS) at different points. Aliskiren is a direct renin inhibitor that blocks the conversion of angiotensinogen to angiotensin I, thereby reducing plasma renin activity and subsequent formation of angiotensin II. Valsartan is an angiotensin II receptor blocker (ARB) that selectively inhibits the binding of angiotensin II to the AT1 receptor, preventing vasoconstriction and aldosterone secretion. The complementary mechanisms provide more complete RAAS inhibition than either agent alone, resulting in significant reductions in blood pressure and related biomarkers such as plasma renin activity, angiotensin I, angiotensin II, and aldosterone. This combination was primarily indicated for hypertension but was withdrawn from the U.S. market in 2012 due to safety concerns in certain populations[1][4][5][8].

Brand names
Valturna
Other names
aliskiren and valsartanaliskiren/valsartanvalsartan + aliskirenvalsartan/aliskiren
02

Targets

REN (Renin)AGTR1 (Angiotensin II Type-1 receptor)

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