Drug intelligence / Profile preview

nifedipine + telmisartan

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

Overview

Nifedipine + telmisartan is a fixed-dose combination of two antihypertensive agents used for the treatment of hypertension, particularly in patients at high or very high cardiovascular risk. Nifedipine is a calcium channel blocker (specifically, a dihydropyridine calcium-channel antagonist) that inhibits the influx of calcium ions into vascular smooth muscle and cardiac muscle, resulting in vasodilation and reduced blood pressure. Telmisartan is an angiotensin II receptor blocker (ARB) that selectively antagonizes the angiotensin II type 1 (AT1) receptor on vascular smooth muscle and adrenal gland tissue, leading to vasodilation and decreased aldosterone-mediated sodium retention. Telmisartan also exhibits partial agonist activity at peroxisome proliferator-activated receptor gamma (PPARγ), which may confer additional metabolic benefits such as improved insulin sensitivity. The combination provides greater and earlier blood pressure reduction than either agent alone, with maintenance of favorable metabolic indices[1][3][8].

02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)LTCC (Voltage-gated calcium channel (L-type))AGTR1 (Angiotensin II Type-1 receptor)

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