MEXILETINE HYDROCHLORIDE · MACLEODS PHARMS LTD
Mexiletine hydrochloride is indicated for the treatment of documented, life-threatening ventricular arrhythmias, such as sustained ventricular tachycardia. Due to its proarrhythmic potential, its use for lesser arrhythmias is generally not recommended, and treatment of patients with asymptomatic ventricular premature contractions should be avoided. Because of the risk of inducing new arrhythmias, therapy should be initiated in a hospital setting. It is important to note that antiarrhythmic drugs have not been shown to enhance survival in patients with ventricular arrhythmias.
How MEXILETINE HYDROCHLORIDE Works
Mexiletine hydrochloride is an orally active local anesthetic and antiarrhythmic agent, structurally similar to lidocaine. It functions by inhibiting the inward sodium current, which reduces the rate of rise (Phase 0) of the action potential. In Purkinje fibers, mexiletine decreases the effective refractory period (ERP) and the action potential duration (APD); however, because the decrease in APD is more pronounced, the ERP/APD ratio is increased, helping to stabilize cardiac rhythm.
Details
- Status
- Prescription
- First Approved
- 1985-12-30
- Routes
- ORAL
- Dosage Forms
- CAPSULE
Companies
MEXILETINE HYDROCHLORIDE Approval History
What MEXILETINE HYDROCHLORIDE Treats
2 indicationsMEXILETINE HYDROCHLORIDE is approved for 2 conditions since its original approval in 1995. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Ventricular Arrhythmia
- Ventricular Tachycardia
MEXILETINE HYDROCHLORIDE Boxed Warning
BOXED WARNING WARNINGS Mortality In the National Heart, Lung and Blood Institute’s Cardiac Arrhythmia Suppression Trial (CAST), a long-term, multicentered, randomized, double-blind study in patients with asymptomatic non-life-threatening ventricular arrhythmias who had a myocardial infarction more than six days but less than two years previously, an excessive mortality or non-fatal cardiac arrest rate (7.7%) was seen in patients treated with encainide or flecainide compared with that seen in pat...
BOXED WARNING WARNINGS Mortality In the National Heart, Lung and Blood Institute’s Cardiac Arrhythmia Suppression Trial (CAST), a long-term, multicentered, randomized, double-blind study in patients with asymptomatic non-life-threatening ventricular arrhythmias who had a myocardial infarction more than six days but less than two years previously, an excessive mortality or non-fatal cardiac arrest rate (7.7%) was seen in patients treated with encainide or flecainide compared with that seen in patients assigned to carefully matched placebo-treated groups (3.0%). The average duration of treatment with encainide or flecainide in this study was ten months. The applicability of the CAST results to other populations (e.g., those without recent myocardial infarction) is uncertain. Considering the known proarrhythmic properties of mexiletine and the lack of evidence of improved survival for any antiarrhythmic drug in patients without life-threatening arrhythmias, the use of mexiletine as well as other antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmia. Acute Liver Injury In postmarketing experience abnormal liver function tests have been reported, some in the first few weeks of therapy with mexiletine hydrochloride. Most of these have been observed in the setting of congestive heart failure or ischemia and their relationship to mexiletine hydrochloride has not been established.
MEXILETINE HYDROCHLORIDE Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
MoA expansion candidates
Same target(s), different indications — where else is this mechanism being explored?
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
Drugs Similar to MEXILETINE HYDROCHLORIDE
3 of 11FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
1 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT06862596 Med-SBMA | CAMCR-026 jRCT2041240174 | Ph 2, Ph 3 | recruiting | Clinical Trial of Mexiletine Hydrochloride for Spinal and Bulbar Muscular Atrophy |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
MEXILETINE HYDROCHLORIDE FDA Label Details
Indications & Usage
FDA Label (PDF)Mexiletine Hydrochloride Capsules USP are indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life- threatening. Because of the proarrhythmic effects of mexiletine, its use with lesser arrhythmias is generally not recommended. Treatment of patients with asymptomatic ventricular premature contractions should be avoided. Initiation of mexiletine treatment, as with other antiarrhythmic agents used to treat life-threatening arrhythmias, should be carried out in the hospital. Antiarrhythmic drugs h...
BOXED WARNING WARNINGS Mortality In the National Heart, Lung and Blood Institute’s Cardiac Arrhythmia Suppression Trial (CAST), a long-term, multicentered, randomized, double-blind study in patients with asymptomatic non-life-threatening ventricular arrhythmias who had a myocardial infarction more t...
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Full clinical data, patents, trials, and competitive landscape for mexiletine hydrochloride.
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.