mexiletine
Trade name: mexitil
Approved
Dec 30, 1985
Mexiletine is a non-selective voltage-gated sodium channel blocker which belongs to the Class IB anti-arrhythmic group of medicines. It is used to treat heart arrhythmias. Mexiletine is also used to treat refractory pain and muscle stiffness resulting in myotonic dystrophy or myotonia congenita. Mexiletine was approved for commercial use in 1985 under the brand name Mexitil, but most marketing efforts have since been discontinued. There has been a continued effort to identify other therapeutic use cases and a number of clinical trials have been conducted including ALS and chronic pain from amputation. — NCATS
Clinical trial activity
28 trials · 36 clinical orgs · 17 marketing orgs
Earliest trial started Jul 1, 1985 (NCT00000518)
Timeline
1980s
- Jan 1, 1985
Earliest Phase 3 Sponsor(trial)
- Dec 30, 1985
Boehringer Ingelheim — Earliest FDA Approval
- Dec 30, 1985
Boehringer Ingelheim — NDA Secondary Org
- Dec 30, 1985
Boehringer Ingelheim — NDA Organization
1990s
- May 16, 1995
Teva — Marketing Organization
- May 16, 1996
Ani Pharmaceuticals — Marketing Organization
- Jan 1, 1997
Earliest Phase 2 Sponsor(trial)
- Feb 26, 1997
Watson Pharmaceuticals — Marketing Organization
2010s
- Jan 1, 2012
Earliest Phase 1 Sponsor(trial)
2020s
- Jul 22, 2020
Crossmedika Sa — Marketing Organization
- Jan 25, 2021
RiconPharma — Marketing Organization
- Jan 25, 2021
Novast Labs — Marketing Organization
- Jan 25, 2021
Ingenus Pharmaceuticals — Marketing Organization
- Oct 1, 2021
Senores Pharms — Marketing Organization
- Oct 1, 2021
Aavis Pharma — Marketing Organization
- Aug 26, 2022
Aucta Pharms — Marketing Organization
- Aug 26, 2022
Rising Pharmaceuticals — Marketing Organization
- Aug 26, 2022
ZENARA — Marketing Organization
- Nov 9, 2022
Annora Pharma — Marketing Organization
- Feb 27, 2023
Leading Pharma Llc — Marketing Organization
- Feb 27, 2023
Quagen Pharma — Marketing Organization
- Mar 23, 2026
Macleods Pharmaceuticals, Ltd — Marketing Organization
Indications
Studied for
- Amputation, Surgical · Phase 2
- Amyotrophic Lateral Sclerosis · Phase 4
- Arrhythmias, Cardiac · Phase 3
- Blepharospasm · Phase 2
- Cardiotoxicity · Phase 1
- Cardiovascular Diseases · Phase 3
- Charcot-Marie-Tooth Disease · Phase 2
- Chronic Pain · Phase 2
- Death, Sudden, Cardiac · Phase 3
- Diabetic Neuropathies · Phase 3
- Dystonia · Phase 2
- Heart Arrest · Phase 3
- Heart Diseases · Phase 3
- HIV Infections · Phase 2
- Irritable Bowel Syndrome · Phase 1
- Myocardial Infarction · Phase 3
- Myotonia · Phase 3
- Myotonia Congenita · Phase 3
- Myotonic Disorders · Phase 3
- Myotonic Dystrophy · Phase 3
- Pain · Phase 3
- Paresthesia · Phase 3
- Peripheral Nervous System Diseases · Phase 2
- Pharmacokinetics · Phase 1
- Polyradiculoneuropathy · Phase 4
- Spasm · Phase 2
- Tachycardia · Phase 4
- Tachycardia, Ventricular · Phase 3
- Ventricular Fibrillation · Phase 3
Mechanism of action
- Sodium channel alpha subunitBLOCKER
Sodium channel alpha subunit blocker
- Sodium channel protein type 1 subunit alpha (SCN1A) ↗
- Sodium channel protein type 5 subunit alpha (SCN5A) ↗
- Sodium channel protein type 4 subunit alpha (SCN4A) ↗
- Sodium channel protein type 7 subunit alpha (SCN7A) ↗
- Sodium channel protein type 2 subunit alpha (SCN2A) ↗
- Sodium channel protein type 9 subunit alpha (SCN9A) ↗
- Sodium channel protein type 3 subunit alpha (SCN3A) ↗
- Sodium channel protein type 11 subunit alpha (SCN11A) ↗
- Sodium channel protein type 8 subunit alpha (SCN8A) ↗
- Sodium channel protein type 10 subunit alpha (SCN10A) ↗
- Sodium channel protein type I alpha subunit
- Sodium channel protein type V alpha subunit
- Sodium channel protein type IV alpha subunit
- Sodium channel protein type VII alpha subunit
- Sodium channel protein type IX alpha subunit
- Sodium channel protein type II alpha subunit
- Sodium channel protein type III alpha subunit
- Sodium channel protein type XI alpha subunit
- Sodium channel protein type VIII alpha subunit
- Sodium channel protein type X alpha subunit
- Sodium channel alpha subunits; brain (Types I, II, III)
Approval history
- approvedPriority reviewDec 30, 1985
Chemistry & pharmacology
SMILES
Cc1cccc(C)c1OCC(C)N- Mol. weight
- 179.26 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL558 ↗
- WikipediaMexiletine ↗
- NCATS1U511HHV4Z ↗
- ChEMBLCHEMBL1200606 ↗
Also known as
- 1-(2',6'-dimethylphenoxy)-2-aminopropane
- 1-(2',6'-dimethylphenoxy)-2-aminopropane
- 1-(2,6-dimethylphenoxy)-2-propanamine
- 1-(2,6-dimethylphenoxy)-2-propanamine
- (+-)-1-(2,6-dimethylphenoxy)propan-2-amine
- (+-)-1-(2,6-dimethylphenoxy)propan-2-amine
- 1-methyl-2-(2,6-xylyloxy)ethanamine
- 1-methyl-2-(2,6-xylyloxy)ethanamine
- (2rs)-1-(2,6-dimethylphenoxy)-2-aminopropane
- (2rs)-1-(2,6-dimethylphenoxy)-2-aminopropane
- dl-mexiletine
- ko-1173 cl
- ko-1173 cl
- ko-1173-cl
- ko-1173-cl
- mexetil
- mexiletina
- mexiletina
- mexiletine
- mexiletine
- mexiletine
- mexiletine
- mexiletine
- mexiletine
- mexiletine
- mexiletine
- mexiletine
- mexiletine
- (+/-)-mexiletine
- mexilétine
- mexilétine
- mexiletine hcl
- mexiletine hcl
- mexiletine hcl
- mexiletine hydrochloride
- mexiletine hydrochloride
- mexiletine hydrochloride
- mexiletine hydrochloride
- mexiletin hcl
- mexiletin hydrochloride
- mexiletinum
- mexiletinum
- mexitil
- mexitil
- mexitil
- mexitil p.l.
- (rs)-mexiletine
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07097701 | Phase 3 | Oct 1, 2025 | Lupin |
| NCT06549400 | Phase 3 | Feb 27, 2025 | Lupin |
| NCT06669299 | N/A | Dec 31, 2024 | — |
| NCT06523400 | Phase 3 | Sep 27, 2024 | Lupin |
| NCT05639257 | N/A | Dec 5, 2022 | Government of Denmark, Lupin, University of Copenhagen, ZiteLab |
| NCT05619120 | N/A | Nov 10, 2022 | Jiao Tong University |
| NCT05017155 | Phase 3 | Aug 12, 2021 | University of London |
| NCT04700046 | Phase 3 | Jul 6, 2021 | Lupin |
| NCT04622553 | N/A | Feb 1, 2021 | Lupin, University of Paris |
| NCT04624750 | Phase 3 | Nov 16, 2020 | Lupin, University of Paris |
| NCT02781454 | Phase 2 | Oct 1, 2016 | Harvard University, University of Washington |
| NCT02561702 | Phase 2 | Sep 1, 2015 | University of Rochester |
| NCT02260388 | Phase 4 | Oct 1, 2014 | Cancer Research Network, University of Kansas |
| NCT02308748 | Phase 1 | May 1, 2014 | Food and Drug Administration, Spaulding Clinical Research Inc. |
| NCT02045667 | Phase 2 | Jan 1, 2014 | Radboud University, University of Groningen, ZonMw: The Netherlands Organisation for Health Research and Development |
| NCT01849770 | Phase 2 | Jul 1, 2013 | University of Washington |
| NCT01811355 | Phase 4 | May 1, 2013 | ALS Association, University of California, Davis |
| NCT01717404 | Phase 1 | Oct 1, 2012 | Mayo Clinic |
| NCT01406873 | Phase 2 | Jun 1, 2011 | University of Rochester |
| NCT02336477 | Phase 3 | Jun 1, 2011 | University of Paris |
Organizations
Research & Development (36)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Lupin | For profit | 7 | 6 | 2 | 2020 |
| University of Paris | Academic/Hospital | 3 | 1 | 2 | 2011 |
| University of Washington | Academic/Hospital | 3 | 3 | 2 | 1987 |
| Harvard University | Academic/Hospital | 2 | 0 | 2 | 2009 |
| National Heart, Lung, and Blood Institute (NHLBI) | Government | 2 | 0 | 1 | 1985 |
| University of Kansas | Academic/Hospital | 2 | 2 | 2 | 2008 |
| University of Rochester | Academic/Hospital | 2 | 2 | 1 | 2011 |
| ALS Association | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Biosense Webster, Inc. | For profit | 1 | 0 | 1 | 2009 |
| Boehringer Ingelheim | For profit | 1 | 0 | 1 | 1999 |
| Canadian Institutes of Health Research (CIHR) | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Cancer Research Network | Academic/Hospital | 1 | 0 | 1 | 2014 |
| Food and Drug Administration | Government | 1 | 1 | 1 | 2014 |
| Government of Canada | Government | 1 | 0 | 1 | 2009 |
| Government of Denmark | Government | 1 | 0 | 1 | 2022 |
| Jiao Tong University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Johns Hopkins University | Academic/Hospital | 1 | 0 | 1 | 1997 |
| Mayo Clinic | Academic/Hospital | 1 | 1 | 1 | 2012 |
| National Center for Research Resources (NCRR) | Government | 1 | 1 | 1 | 1993 |
| National Institute of Allergy and Infectious Diseases (NIAID) | Government | 1 | 1 | 1 | 1999 |
Marketing (19)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Aavis Pharma | For profit | MKTG | Oct 1, 2021 |
| Ani Pharmaceuticals | For profit | MKTG | May 16, 1996 |
| Ani Pharmaceuticals | For profit | SYN | May 16, 1996 |
| Annora Pharma | For profit | MKTG | Nov 9, 2022 |
| Aucta Pharms | For profit | MKTG | Aug 26, 2022 |
| Boehringer Ingelheim | For profit | NDA2 | Dec 30, 1985 |
| Boehringer Ingelheim | For profit | NDA | Dec 30, 1985 |
| Crossmedika Sa | For profit | MKTG | Jul 22, 2020 |
| Ingenus Pharmaceuticals | For profit | MKTG | Jan 25, 2021 |
| Leading Pharma Llc | For profit | MKTG | Feb 27, 2023 |
| Macleods Pharmaceuticals, Ltd | For profit | MKTG | Mar 23, 2026 |
| Novast Labs | For profit | MKTG | Jan 25, 2021 |
| Quagen Pharma | For profit | MKTG | Feb 27, 2023 |
| RiconPharma | For profit | MKTG | Jan 25, 2021 |
| Rising Pharmaceuticals | For profit | MKTG | Aug 26, 2022 |
| Senores Pharms | For profit | MKTG | Oct 1, 2021 |
| Teva | For profit | MKTG | May 16, 1995 |
| Watson Pharmaceuticals | For profit | MKTG | Feb 26, 1997 |
| ZENARA | For profit | MKTG | Aug 26, 2022 |