Drug intelligence / Profile preview

mexiletine

Development stage
Approved
Lead developer
Boehringer Ingelheim
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Mexiletine is an orally active small molecule antiarrhythmic drug classified as a Class 1B antiarrhythmic agent. It is structurally similar to lidocaine and acts primarily by blocking fast voltage-gated sodium channels (notably the sodium channel protein type 5 subunit alpha) in cardiac myocytes and nerve cells, thereby inhibiting the inward sodium current during phase 0 of the cardiac action potential. This action shortens the action potential duration and refractory period, stabilizing cardiac rhythm. Mexiletine is used mainly for treating documented life-threatening ventricular arrhythmias such as sustained ventricular tachycardia, especially when associated with long QT syndrome (notably LQT3). It may also be used off-label for chronic pain syndromes and muscle stiffness related to myotonic disorders[1][4][5][8].

Brand names
Mexitil
Other names
mexiletine hydrochloride
02

Targets

SCN5A (Sodium channel protein type 5 subunit alpha)

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