Drug intelligence / Profile preview

nebivolol

Development stage
Approved
Lead developer
Menarini
Modality
Small Molecules
Administration
Oral
01

Overview

Nebivolol is a highly selective beta-blocker (beta adrenergic receptor antagonist) used primarily to treat hypertension (high blood pressure) and, in some regions, heart failure. It is a racemic mixture of two enantiomers: d-nebivolol, which acts as a selective beta-1 adrenergic receptor antagonist, and l-nebivolol, which has beta-3 adrenergic receptor agonist activity. The drug lowers blood pressure by blocking the effects of catecholamines at the beta receptors in the heart and vascular smooth muscle—slowing heart rate and relaxing blood vessels. Additionally, its action on beta-3 receptors stimulates endothelial nitric oxide synthase to increase nitric oxide production, leading to vasodilation. Nebivolol was developed by Menarini/Biofarma and is marketed under brand names such as Bystolic[1][2][5][9].

Brand names
Bystolic
Other names
NarbivololNebivololum
02

Targets

ADRB1 (β1)ADRB2 (β2)ADRB3 (β3)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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