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celivarone
- Development stage
- Phase 3
- Lead developer
- Sanofi
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Celivarone is a non-iodinated benzofuran derivative developed as an antiarrhythmic agent for the treatment of atrial fibrillation and the prevention of ventricular arrhythmias. Structurally related to amiodarone and dronedarone, it was designed to provide similar multi-channel blocking efficacy without the iodine-related organ toxicities (such as thyroid and pulmonary dysfunction) associated with amiodarone. Celivarone exhibits electrophysiological properties including the inhibition of multiple ion currents, such as the rapid and slow components of the delayed rectifier potassium current (IKr and IKs), the inward rectifier potassium current (IK1), L-type calcium channels, and sodium channels. It also possesses non-competitive anti-adrenergic activity. Despite promising early results, clinical development by Sanofi was discontinued following Phase 2 trials (MAIA and CORYFEE) which failed to demonstrate significant efficacy in maintaining sinus rhythm or reducing interventions from implantable cardioverter-defibrillators (ICDs) compared to placebo.
- Other names
- celivarone
02
Targets
ADRB1 (β1)KACh (G protein–activated inwardly rectifying potassium channel)KCNA5 (Ultra-rapid delayed rectifier potassium channel)IKs (Slowly activating delayed rectifier potassium channel (KCNQ1/KCNE1))SCN5A (Sodium channel protein type 5 subunit alpha)KCNH2 (Voltage-gated potassium channel subfamily H member 2)ADRA1 (Alpha-1 adrenergic receptor family)KCNJ2 (Inward rectifier potassium channel Kir2.1)KCNQ1 (Potassium voltage-gated channel subfamily KQT member 1)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)
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