Drug intelligence / Profile preview

amlodipine + azilsartan

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Amlodipine + azilsartan is a fixed-dose combination therapy used for the management of hypertension. It combines amlodipine, a dihydropyridine calcium channel blocker (CCB), with azilsartan medoxomil, an angiotensin II receptor blocker (ARB). Amlodipine works by inhibiting the influx of calcium ions into vascular smooth muscle and cardiac muscle cells by blocking L-type calcium channels, leading to peripheral vasodilation and reduced blood pressure. Azilsartan medoxomil is a prodrug that is converted to azilsartan, which selectively inhibits the binding of angiotensin II to the AT1 receptor, thereby blocking the renin-angiotensin-aldosterone system (RAAS) and preventing vasoconstriction and aldosterone release. This dual mechanism provides synergistic blood pressure lowering effects. The combination is particularly studied in patients with comorbid conditions such as coronary artery disease and those undergoing percutaneous coronary intervention (PCI) to evaluate its effectiveness in blood pressure control and clinical outcomes.

Brand names
Zacras
Other names
amlodipine besylate + azilsartan medoxomilamlodipine + azilsartan medoxomil
02

Targets

CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)AGTR1 (Angiotensin II Type-1 receptor)

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