Drug intelligence / Profile preview

etafenone

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Etafenone is a propiophenone derivative that functions as a coronary vasodilator and antiarrhythmic agent. It primarily acts as a calcium channel antagonist, inhibiting the slow inward calcium current in myocardial and vascular smooth muscle cells, which results in negative inotropic effects and reduced vascular resistance. Additionally, etafenone exhibits potent sodium channel blocking activity, contributing to its antiarrhythmic properties. Beyond its cardiovascular effects, it has been shown to inhibit platelet aggregation and phosphodiesterase activity. Historically marketed under brand names such as Dialicor and Baxacor for the treatment of coronary heart disease and angina, its clinical use has largely been superseded by newer agents. Notably, research has identified that etafenone can induce Parkinsonism-like symptoms, likely due to its diethylaminomethyl moiety which facilitates the blockade of dopamine D2 receptors in the striatum.

Brand names
DialicorBaxacor
Other names
etafenone hydrochloride2'-[2-(diethylamino)ethoxy]-3-phenylpropiophenone2-(2-diethylaminoethoxy)phenyl 2-phenylethyl ketone
02

Targets

LTCC (Voltage-gated calcium channel (L-type))NaV (Voltage-gated sodium channels)

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