Drug intelligence / Profile preview

aliskiren + valsartan + amlodipine

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

Overview

Aliskiren + valsartan + amlodipine is a hypothetical triple combination of antihypertensive agents: - **Aliskiren** is a direct renin inhibitor, which blocks the activity of renin and decreases formation of angiotensin I, thereby lowering blood pressure. - **Valsartan** is an angiotensin II receptor blocker (ARB), which blocks the binding of angiotensin II to its receptor in blood vessels, leading to vasodilation and decreased blood pressure. - **Amlodipine** is a dihydropyridine calcium channel blocker (CCB), which inhibits the influx of calcium ions into vascular smooth muscle and cardiac muscle, also causing vasodilation and lower blood pressure. While fixed-dose triple combination products containing aliskiren + amlodipine + hydrochlorothiazide (Amturnide) and amlodipine + valsartan + hydrochlorothiazide (Exforge HCT) have been approved, there is no evidence a triple combination of aliskiren + valsartan + amlodipine (without hydrochlorothiazide) is approved, marketed, or under development as a fixed-dose product. Coadministration of aliskiren with ARBs (such as valsartan) is contraindicated in patients with diabetes and not recommended in those with renal impairment due to increased risk of adverse renal outcomes, hyperkalemia, and hypotension[6].

02

Targets

LTCC (Voltage-gated calcium channel (L-type))REN (Renin)AGTR1 (Angiotensin II Type-1 receptor)

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