Drug intelligence / Profile preview

aliskiren + valsartan + ramipril

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

Overview

Aliskiren + valsartan + ramipril is a hypothetical triple combination of antihypertensive agents, each targeting different points in the renin-angiotensin-aldosterone system (RAAS). Aliskiren is a direct renin inhibitor that blocks the conversion of angiotensinogen to angiotensin I, thereby reducing downstream production of angiotensin II and aldosterone[6]. Valsartan is an angiotensin II receptor blocker (ARB) that prevents angiotensin II from binding to its receptor, inhibiting vasoconstriction and aldosterone secretion[1][4]. Ramipril is an angiotensin-converting enzyme (ACE) inhibitor that blocks the conversion of angiotensin I to angiotensin II. The combined use of these three drugs would result in comprehensive RAAS blockade. However, clinical guidelines and regulatory agencies strongly advise against combining all three due to increased risks of renal impairment, hyperkalemia, and hypotension[2][3]. Dual combinations (e.g., aliskiren with either an ARB or ACE inhibitor) have been studied but are associated with significant safety concerns.

02

Targets

REN (Renin)ACE (Angiotensin Converting Enzyme)AGTR1 (Angiotensin II Type-1 receptor)

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