Drug intelligence / Profile preview

desethylamiodarone

Development stage
Unknown
Modality
Small Molecules
Administration
Not Applicable (not Administered Directly; Formed In Vivo From Amiodarone)
01

Overview

desethylamiodarone is the major active metabolite of amiodarone, formed by N-demethylation. It is detectable in the serum of patients treated with amiodarone and retains antiarrhythmic properties similar to the parent drug. Desethylamiodarone acts primarily by blocking cardiac potassium channels, leading to the prolongation of the action potential duration and QT interval, but also exhibits inhibitory effects on sodium and calcium channels, and beta-adrenergic receptors. In addition to cardiac effects, desethylamiodarone has been shown in preclinical studies to induce apoptosis and cell cycle arrest in certain cancer cell models (e.g., bladder carcinoma), suggesting potential cytostatic properties[1][5][7][9].

Other names
N-desethylamiodaroneDEA
02

Targets

SCN5A (Sodium channel protein type 5 subunit alpha)SPHK2 (Sphingosine kinase 2)KCNH2 (Voltage-gated potassium channel subfamily H member 2)Kir (Inward-rectifier potassium channels)

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