Drug intelligence / Profile preview

vernakalant

Development stage
Phase 4
Lead developer
Advanz Pharma
Modality
Small Molecules
Administration
Intravenous
01

Overview

Vernakalant is a small molecule antiarrhythmic drug developed for the rapid conversion of recent-onset atrial fibrillation to sinus rhythm. It is classified as an atypical class III antiarrhythmic, with unique atrial-selective properties. Vernakalant acts by blocking multiple ion channels in the atria, including voltage-gated sodium channels (with dose- and frequency-dependent inhibition), ultra-rapid delayed rectifier potassium channels (Kv1.5/IKur), acetylcholine-activated potassium channels (IKAch), and transient outward potassium currents (Kv4.3/Ito). This results in prolongation of the atrial refractory period and selective suppression of abnormal electrical activity in the atria, while having minimal effects on ventricular tissue. Its affinity for sodium channel blockade increases at higher heart rates, making it particularly effective during episodes of rapid arrhythmia such as atrial fibrillation[1][2][3][6]. Vernakalant has a short half-life and is administered intravenously for acute cardioversion.

Brand names
Brinavess
Other names
vernakalant hydrochloride
02

Targets

KACh (G protein–activated inwardly rectifying potassium channel)KCND3 (Potassium voltage-gated channel subfamily D member 3 with KChIP2 coexpression complex)KCNA5 (Ultra-rapid delayed rectifier potassium channel)SCN5A (Sodium channel protein type 5 subunit alpha)KCNH2 (Voltage-gated potassium channel subfamily H member 2)

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