Drug intelligence / Profile preview

azilsartan medoxomil + nifedipine

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

Overview

Azilsartan medoxomil + nifedipine is an oral fixed-dose combination of two antihypertensive agents: azilsartan medoxomil, an angiotensin II receptor blocker (ARB), and nifedipine, a dihydropyridine calcium channel blocker. **Azilsartan medoxomil** is a prodrug hydrolyzed to azilsartan, which selectively blocks the angiotensin II type 1 (AT1) receptor in the renin-angiotensin-aldosterone system, inhibiting vasoconstriction and sodium/water retention, leading to reduced blood pressure. **Nifedipine** blocks voltage-dependent L-type calcium channels in vascular smooth muscle and myocardial cells, inhibiting calcium entry, inducing vasodilation, and reducing peripheral vascular resistance. The combination offers complementary and additive blood pressure–lowering effects, useful for patients with hypertension not adequately controlled by monotherapy. There is extensive evidence justifying the use of ARB and calcium channel blocker combinations for enhanced blood pressure control, although most clinical evidence and fixed-dose products involve amlodipine rather than nifedipine in combination with azilsartan medoxomil.

02

Targets

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

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