Drug intelligence / Profile preview

amlodipine + azelnidipine

Development stage
Unknown
Lead developer
Pfizer
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Amlodipine + azelnidipine is a fixed-dose combination of two dihydropyridine calcium channel blockers, amlodipine and azelnidipine, used for the treatment of hypertension. Both agents act as vasodilators by inhibiting L-type calcium channels in vascular smooth muscle, leading to relaxation of blood vessels and reduction in blood pressure. Amlodipine is widely used globally for hypertension and angina, while azelnidipine is primarily approved in Japan and some Asian countries for hypertension. The combination aims to provide additive antihypertensive effects with potentially improved tolerability or efficacy compared to monotherapy. Both drugs have high vasoselectivity with minimal negative inotropic effects; however, studies suggest that azelnidipine may have a less pronounced negative effect on cardiac contractility than amlodipine[1][2][3]. The primary indication for this combination is the management of mild to moderate essential hypertension.

02

Targets

CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)CACNA1D (Voltage-dependent L-type calcium channel subunit alpha-1D)

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