Drug intelligence / Profile preview

celiprolol

Development stage
Phase 4
Lead developer
Zevra Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Celiprolol is a unique beta-blocker used primarily for the management of mild to moderate hypertension and effort-induced angina pectoris. It is characterized by its selective β1-adrenoceptor antagonist activity, partial β2-adrenoceptor agonist activity, and weak α2-adrenoceptor antagonist properties. This pharmacological profile distinguishes it from other beta-blockers, providing antihypertensive effects with mild vasodilation and minimal negative impact on cardiac function at rest. Celiprolol has also been investigated for the prevention of vascular complications in patients with vascular Ehlers–Danlos syndrome (vEDS), where it may reduce arterial events by lowering heart rate and pulsatile pressure, thus decreasing mechanical stress on fragile blood vessels[1][2][5]. The drug was patented in 1973 and approved for medical use in 1982[5].

Brand names
CelectolCeliprolol PCH
Other names
celiprolol
02

Targets

ADRA2A (α2A)ADRB1 (β1)ADRB2 (β2)

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