zonisamide
Trade name: Zonegran
Approved
Mar 27, 2000
Zonisamide is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodium and calcium channels, which leads to the suppression of neuronal hypersynchronization (i.e. convulsions). Sonisamide has also been found to potentiate dopaminergic and serotonergic neurotransmission but does not appear to potentiate syanptic activity by GABA (gamma amino butyric acid). Zonisamide binds to sodium channels and voltage sensitive calcium channels, which suppresses neuronal depolarization and hypersynchronization. Zonisamide also inhibits carbonic anhydrase to a weaker extent, but such an effect is not thought to contribute substantially to the drug's anticonvulsant activity. Zonisamide is approved in the United States, United Kingdom, and Australia for adjunctive treatment of partial seizures in adults and in Japan for both adjunctive and monotherapy for partial seizures (simple, complex, secondarily generalized), generalized (tonic, tonic-clonic (grand mal), and atypical absence) and combined seizures. — NCATS
Clinical trial activity
72 trials · 79 clinical orgs · 28 marketing orgs
Earliest trial started Feb 1, 2002 (NCT00056576)
Timeline
2000s
- Mar 27, 2000
Advanz Pharma — Earliest FDA Approval
- Mar 27, 2000
Sunovion — NDA Secondary Org
- Mar 27, 2000
Advanz Pharma — Marketing Organization
- Mar 27, 2000
Advanz Pharma — NDA Secondary Org
- Mar 27, 2000
Advanz Pharma — NDA Organization
- Jan 1, 2002
Earliest Phase 2 Sponsor(trial)
- Jan 1, 2002
Earliest Phase 3 Sponsor(trial)
- Jan 1, 2003
- Dec 22, 2005
Rising Pharmaceuticals — Marketing Organization
- Dec 22, 2005
Ani Pharmaceuticals — Marketing Organization
- Dec 22, 2005
Apotex — Marketing Organization
- Dec 22, 2005
Aurobindo Pharma — Marketing Organization
- Dec 22, 2005
Mylan — Marketing Organization
- Dec 22, 2005
Roxane Laboratories — Marketing Organization
- Dec 22, 2005
Upsher-Smith Laboratories — Marketing Organization
- Dec 22, 2005
Wockhardt — Marketing Organization
- Dec 22, 2005
Celltrion — Marketing Organization
- Dec 22, 2005
Granules India — Marketing Organization
- Dec 22, 2005
Boehringer Ingelheim — Marketing Organization
- Dec 22, 2005
PHARMOBEDIENT — Marketing Organization
- Jan 30, 2006
Glenmark Pharmaceuticals — Marketing Organization
- Mar 17, 2006
Sun Pharmaceuticals — Marketing Organization
- Apr 20, 2006
Watson Pharmaceuticals — Marketing Organization
- Apr 20, 2006
Heritage Pharma — Marketing Organization
- Apr 20, 2006
Chartwell Pharmaceuticals — Marketing Organization
- May 31, 2006
Invagen Pharms — Marketing Organization
- Aug 16, 2006
Bluepharma — Marketing Organization
- Aug 16, 2006
Bionpharma Inc — Marketing Organization
- Oct 16, 2006
Zydus Discovery DMCC — Marketing Organization
- Oct 16, 2006
Cadila Healthcare — Marketing Organization
- Feb 21, 2007
Epic Pharma Llc — Marketing Organization
2020s
- Jan 26, 2021
Unichem — Marketing Organization
- Jul 15, 2022
Azurity — Marketing Organization
- Jul 15, 2022
Azurity — NDA Secondary Org
- May 12, 2025
Macleods Pharmaceuticals, Ltd — Marketing Organization
Indications
Studied for
- Alcohol-Induced Disorders · Phase 2
- Alcoholism · Phase 4
- Bipolar Disorder · Phase 4
- Cocaine-Related Disorders · Phase 1/Phase 2
- Drug Resistant Epilepsy · Phase 4
- Dyskinesias · Phase 4
- Dystonia · Phase 3
- Epilepsies, Partial · Phase 4
- Epilepsy, Complex Partial · Phase 3
- Epilepsy, Tonic-Clonic · Phase 4
- Essential Tremor · Phase 2
- Fibromyalgia · Phase 4
- Glioma · Phase 4
- Healthy Volunteers · Phase 1
- Hearing Loss, Noise-Induced · Phase 2
- Intellectual Disability · Phase 4
- Migraine Disorders · Phase 4
- Obesity · Phase 4
- Parkinson Disease · Phase 4
- Parkinsonian Disorders · Phase 4
- Psychotic Disorders · Phase 3
- Schizophrenia · Phase 3
- Seizures · Phase 4
- Sleep Apnea, Obstructive · Phase 2
- Sleep Apnea Syndromes · Phase 2
- Smoking Cessation · Phase 3
- Stress Disorders, Post-Traumatic · Phase 2
- Tobacco Use Disorder · Phase 1/Phase 2
- Weight Gain · 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
- approvedMar 27, 2000
Chemistry & pharmacology
SMILES
NS(=O)(=O)CC1=NOC2=C1C=CC=C2- Mol. weight
- 212.226 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaZonisamide ↗
- NCATS459384H98V ↗
- ChEMBLCHEMBL750 ↗
Also known as
- 1,2-benzisoxazole-3-methanesulfonamide
- 1,2-benzisoxazole-3-methanesulfonamide
- 1,2-benzisoxazole-3-methanesulfonamide
- 3-(sulfamoylmethyl)-1,2-benzisoxazole
- 3-(sulfamoylmethyl)-1,2-benzisoxazole
- 3-sulfamoylmethyl-1,2-benzisoxazole
- ad 810
- ad-810
- ad-810
- ad-810
- benzo[d]isoxazol-3-yl-methanesulfonamide
- benzo[d]isoxazol-3-yl-methanesulfonamide
- ci 912
- ci-912
- ci-912
- ci-912
- elan brand of zonisamide
- exceglan
- excegram
- excegran
- pd-110843
- pd-110843
- zonegran
- zonegran
- zonegran
- zonegran
- zonegran
- zonegran
- zonisamida
- zonisamida
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide
- zonisamide monosodium
- zonisamidum
- zonisamidum
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06534502 | Phase 4 | Sep 30, 2024 | Azurity Pharmaceuticals |
| NCT06967012 | Phase 4 | Aug 1, 2024 | Nantong University |
| NCT06347497 | Phase 3 | Apr 1, 2024 | Kafrelsheikh University |
| NCT06361446 | Phase 3 | Mar 29, 2024 | Kafrelsheikh University |
| NCT05134857 | Phase 2 | Dec 31, 2021 | Washington State University |
| NCT05205811 | Phase 3 | Dec 14, 2021 | Foundation for a Smoke-Free World, Rose Research Center, LLC |
| NCT04774250 | Phase 2 | Oct 31, 2021 | Department of Defense, Gateway Biotechnology, Inc., University of Texas, Galveston, Washington University in St. Louis |
| NCT04768569 | Phase 2 | Aug 31, 2021 | Department of Defense, Gateway Biotechnology, Inc., University of Akron, University of Texas, Galveston, Washington University in St. Louis |
| NCT04939675 | N/A | Jul 1, 2021 | National Taiwan University |
| NCT04650204 | Phase 4 | Dec 15, 2020 | Mayo Clinic, National Cancer Institute (NCI) |
| NCT04388319 | Phase 3 | Jun 1, 2020 | Foundation for a Smoke-Free World, Rose Research Center, LLC |
| NCT04182399 | N/A | Dec 15, 2019 | Ain Shams University |
| NCT03689114 | Phase 4 | Jan 31, 2019 | Azienda Ospedaliera San Gerardo di Monza, Government of Italy, Mario Negri Institute |
| NCT03376139 | Phase 2 | Oct 1, 2018 | Baylor University, Department of Defense, Department of Veteran Affairs, Pharmacotherapies for Alcohol and Substance Abuse Consortium |
| NCT02707965 | Phase 4 | Jul 1, 2017 | Food and Drug Administration, University of Maryland |
| NCT02049073 | Phase 1/Phase 2 (Phase 2) | Jun 1, 2017 | Washington University in St. Louis |
| NCT02900352 | Phase 1 | Oct 1, 2016 | Yale University |
| NCT02901041 | Phase 3 | Sep 1, 2016 | Boston University, Mclean Hospital, University of Houston |
| NCT03034538 | Phase 4 | Apr 8, 2016 | Rowan University |
| NCT02368431 | Phase 3 | Mar 1, 2015 | Department of Veteran Affairs |
Organizations
Research & Development (79)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Eisai | For profit | 23 | 19 | 3 | 2002 |
| Boston University | Academic/Hospital | 4 | 4 | 3 | 2006 |
| Department of Defense | Government | 4 | 0 | 1 | 2013 |
| Department of Veteran Affairs | Government | 4 | 2 | 3 | 2003 |
| National Institute on Alcohol Abuse and Alcoholism (NIAAA) | Government | 3 | 0 | 2 | 2006 |
| Orexigen Therapeutics, Inc | For profit | 3 | 3 | 1 | 2006 |
| Washington University in St. Louis | Academic/Hospital | 3 | 3 | 1 | 2017 |
| Yale University | Academic/Hospital | 3 | 3 | 2 | 2012 |
| Dr. Reddy's Laboratories | For profit | 2 | 2 | 1 | 2005 |
| Duke University | Academic/Hospital | 2 | 1 | 2 | 2006 |
| Elan Pharmaceuticals | For profit | 2 | 2 | 2 | 2002 |
| Eli Lilly | For profit | 2 | 1 | 1 | 2006 |
| Foundation for a Smoke-Free World | Academic/Hospital | 2 | 0 | 1 | 2020 |
| Gateway Biotechnology, Inc. | For profit | 2 | 0 | 1 | 2021 |
| Johns Hopkins University | Academic/Hospital | 2 | 2 | 1 | 2010 |
| Kafrelsheikh University | Academic/Hospital | 2 | 2 | 1 | 2024 |
| Kendle International Inc. | For profit | 2 | 0 | 1 | 2003 |
| Mutual Pharmaceutical | For profit | 2 | 2 | 1 | 2005 |
| Mylan | For profit | 2 | 2 | 1 | 2003 |
| PharmaNet (2006) | For profit | 2 | 0 | 1 | 2005 |
Marketing (42)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Advanz Pharma | For profit | MKTG | Mar 27, 2000 |
| Advanz Pharma | For profit | NDA2 | Mar 27, 2000 |
| Advanz Pharma | For profit | NDA | Mar 27, 2000 |
| Advanz Pharma | For profit | SYN | Mar 27, 2000 |
| Ani Pharmaceuticals | For profit | MKTG | Dec 22, 2005 |
| Ani Pharmaceuticals | For profit | SYN | Dec 22, 2005 |
| Apotex | For profit | MKTG | Dec 22, 2005 |
| Apotex | For profit | SYN | Dec 22, 2005 |
| Aurobindo Pharma | For profit | MKTG | Dec 22, 2005 |
| Azurity | For profit | MKTG | Jul 15, 2022 |
| Azurity | For profit | NDA2 | Jul 15, 2022 |
| Bionpharma Inc | For profit | MKTG | Aug 16, 2006 |
| Bionpharma Inc | For profit | SYN | Aug 16, 2006 |
| Bluepharma | For profit | MKTG | Aug 16, 2006 |
| Boehringer Ingelheim | For profit | MKTG | Dec 22, 2005 |
| Cadila Healthcare | For profit | MKTG | Oct 16, 2006 |
| Celltrion | For profit | MKTG | Dec 22, 2005 |
| Chartwell Pharmaceuticals | For profit | MKTG | Apr 20, 2006 |
| Epic Pharma Llc | For profit | MKTG | Feb 21, 2007 |
| Glenmark Pharmaceuticals | For profit | MKTG | Jan 30, 2006 |
| Glenmark Pharmaceuticals | For profit | SYN | Jan 30, 2006 |
| Glenmark Pharmaceuticals | For profit | SYN | Jan 30, 2006 |
| Granules India | For profit | MKTG | Dec 22, 2005 |
| Heritage Pharma | For profit | SYN | Apr 20, 2006 |
| Heritage Pharma | For profit | MKTG | Apr 20, 2006 |
| Invagen Pharms | For profit | MKTG | May 31, 2006 |
| Macleods Pharmaceuticals, Ltd | For profit | MKTG | May 12, 2025 |
| Mylan | For profit | MKTG | Dec 22, 2005 |
| Mylan | For profit | SYN | Dec 22, 2005 |
| PHARMOBEDIENT | For profit | MKTG | Dec 22, 2005 |
| Rising Pharmaceuticals | For profit | MKTG | Dec 22, 2005 |
| Rising Pharmaceuticals | For profit | SYN | Dec 22, 2005 |
| Roxane Laboratories | For profit | MKTG | Dec 22, 2005 |
| Sun Pharmaceuticals | For profit | MKTG | Mar 17, 2006 |
| Sun Pharmaceuticals | For profit | SYN | Dec 22, 2005 |
| Sunovion | For profit | NDA2 | Mar 27, 2000 |
| Unichem | For profit | MKTG | Jan 26, 2021 |
| Upsher-Smith Laboratories | For profit | MKTG | Dec 22, 2005 |
| Watson Pharmaceuticals | For profit | MKTG | Apr 20, 2006 |
| Wockhardt | For profit | MKTG | Dec 22, 2005 |
| Zydus Discovery DMCC | For profit | MKTG | Oct 16, 2006 |
| Zydus Discovery DMCC | For profit | SYN | Oct 16, 2006 |