Drug intelligence / Profile preview

olmesartan medoxomil + levamlodipine besilate

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

Olmesartan medoxomil + levamlodipine besilate is a fixed-dose combination (FDC) therapy developed by Beijing Fuyuan Pharmaceutical for the treatment of hypertension. This combination pairs olmesartan medoxomil, a prodrug that is hydrolyzed to the active angiotensin II receptor type 1 (AT1) antagonist olmesartan, with levamlodipine besilate, the pharmacologically active (S)-enantiomer of the calcium channel blocker amlodipine. Olmesartan works by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle, thereby inhibiting vasoconstriction and aldosterone secretion. Levamlodipine acts as a dihydropyridine calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle, leading to vasodilation. The use of the (S)-enantiomer of amlodipine is intended to maintain antihypertensive efficacy while potentially reducing the incidence of side effects, such as peripheral edema, which are often associated with the (R)-enantiomer found in racemic amlodipine. This FDC provides a synergistic approach to blood pressure management by targeting two distinct physiological pathways.

Other names
(S)-amlodipine besilate + olmesartan medoxomillevamlodipine besylate + olmesartan medoxomilolmesartan medoxomil + levamlodipine besylate
02

Targets

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

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