ethosuximide

Trade name: zarontin

Small moleculeapproved

Approved

Nov 2, 1960

Ethosuximide is a succinimide anticonvulsant, used in the treatment of epilepsy. Ethosuximide suppresses the paroxysmal three cycle per second spike and wave activity associated with lapses of consciousness which is common in absence (petit mal) seizures. The frequency of epileptiform attacks is reduced, apparently by depression of the motor cortex and elevation of the threshold of the central nervous system to convulsive stimuli. Binds to T-type voltage sensitive calcium channels. Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-voltage activated (LVA)" group and are strongly blocked by mibefradil. A particularity of this type of channels is an opening at quite negative potentials and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes. Ethosuximide is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system. — NCATS

Clinical trial activity

13 trials · 25 clinical orgs · 14 marketing orgs

Phase 1
2
Phase 2
11
Phase 3
2
Phase 4
1

Earliest trial started Jul 1, 2004 (NCT00088452)

Timeline

1960s

  1. Nov 2, 1960

    Parke-Davis — Earliest FDA Approval

  2. Nov 2, 1960

    Parke-Davis — NDA Organization

1970s

  1. Feb 13, 1974

    Parke-Davis — Marketing Organization

  2. Feb 13, 1974

    Warner Lambert — Marketing Organization

1990s

  1. Jul 30, 1993

    Teva — Marketing Organization

2000s

  1. Nov 22, 2000

    Pharmaceutical Associates — Marketing Organization

  2. Oct 28, 2002

    Bionpharma Inc — Marketing Organization

  3. Dec 22, 2003

    Mikart — Marketing Organization

  4. Dec 22, 2003

    Chartwell Pharmaceuticals — Marketing Organization

  5. Jan 1, 2004

    Earliest Phase 3 Sponsor(trial)

  6. Jan 1, 2006

    Earliest Phase 2 Sponsor(trial)

  7. May 28, 2008

    Akorn, Inc. — Marketing Organization

  8. May 28, 2008

    Epic Pharma Llc — Marketing Organization

2010s

  1. Jan 1, 2011

    Earliest Phase 1 Sponsor(trial)

  2. Sep 25, 2012

    Heritage Pharma — Marketing Organization

  3. Sep 25, 2012

    Emcure — Marketing Organization

  4. Feb 19, 2019

    Strides Pharma Science — Marketing Organization

  5. Feb 19, 2019

    ONESOURCE SPECIALTY — Marketing Organization

2020s

  1. Mar 16, 2020

    Puracap Pharmaceutical — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedPriority reviewNov 2, 1960

Chemistry & pharmacology

Loading structure…

SMILES

CCC1(C)CC(=O)NC1=O
Mol. weight
141.1677 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

Also known as

  • (+-)-2-ethyl-2-methylsuccinimide
  • (+-)-2-ethyl-2-methylsuccinimide
  • (±)-2-ethyl-2-methylsuccinimide
  • (±)-2-ethyl-2-methylsuccinimide
  • 2-ethyl-2-methylsuccinimide
  • 2-ethyl-2-methylsuccinimide
  • 2-methyl-2-ethylsuccinimide
  • 2-methyl-2-ethylsuccinimide
  • 3-ethyl-3-methyl-2,5-pyrrolidinedione
  • 3-ethyl-3-methyl-2,5-pyrrolidinedione
  • 3-ethyl-3-methylsuccinimide
  • 3-ethyl-3-methylsuccinimide
  • 3-methyl-3-ethylpyrrolidine-2,5-dione
  • 3-methyl-3-ethylpyrrolidine-2,5-dione
  • 3-methyl-3-ethylsuccinimide
  • 3-methyl-3-ethylsuccinimide
  • 3-methyl-3-ethylsuccinimide
  • aethosuximide
  • aethosuximide
  • alpha-ethyl-alpha-methylsuccinimide
  • alpha-ethyl-alpha-methylsuccinimide
  • alpha-methyl-alpha-ethylsuccinimide
  • alpha-methyl-alpha-ethylsuccinimide
  • atysmal
  • atysmal
  • ci-366
  • ci-366
  • cn-10395
  • cn-10395
  • emeside
  • emeside
  • ethosuxide
  • ethosuximid
  • ethosuximid
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximide
  • ethosuximidum
  • ethosuximidum
  • etosuximid
  • etosuximida
  • etosuximida
  • gamma-ethyl-gamma-methyl-succinimide
  • gamma-ethyl-gamma-methyl-succinimide
  • gamma-methyl-gamma-ethyl-succinimide
  • gamma-methyl-gamma-ethyl-succinimide
  • pm-671
  • pm-671
  • suxinutin
  • suxinutin
  • t2000
  • thilopemal
  • thilopemal
  • zarontin
  • zarontin
  • zarontin
  • γ-ethyl-γ-methyl-succinimide
  • γ-ethyl-γ-methyl-succinimide

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT04431778Phase 2Sep 1, 2020University Clermont Auvergne
NCT04217733Phase 3Nov 1, 2019Tanta University
NCT03887624Early Phase 1 (Phase 1)Apr 15, 2019Zhejiang University
NCT02973542Phase 2Feb 1, 2017University Clermont Auvergne
NCT02205931Phase 4Jan 1, 2015Lancashire Teaching Hospitals NHS Foundation Trust, National Institute for Health Research, United Kingdom, Newcastle University, Sheffield Hallam University, University of Birmingham, University of Bristol, University of Cambridge, University of Leeds, University of Liverpool, University of London, University of Manchester
NCT02100046Phase 2Mar 1, 2014Fondation Apicil, University Clermont Auvergne
NCT01122381Phase 1/Phase 2 (Phase 2)Dec 1, 2011Department of Veteran Affairs, Thomas Jefferson University, University of Pittsburgh
NCT01278004Phase 2May 1, 2010Royal Marsden Hospital NHS Trust, University of London
NCT00689585Phase 2Sep 1, 2008McGill University
NCT00655278Phase 2Aug 1, 2007Taro Pharmaceuticals
NCT00506012Phase 2Aug 1, 2007Taro Pharmaceuticals
NCT00321087Phase 2Aug 1, 2006Taro Pharmaceuticals
NCT00088452Phase 3Jul 1, 2004Children's National Medical Center, National Institute of Neurological Disorders and Stroke (NINDS), University of Cincinnati, University of Pennsylvania
Showing 13 of 13 trials
Page 1 / 1

Organizations

Research & Development (25)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Taro PharmaceuticalsFor profit3312006
University Clermont AuvergneAcademic/Hospital3312014
University of LondonAcademic/Hospital2122010
Children's National Medical CenterAcademic/Hospital1012004
Department of Veteran AffairsGovernment1112011
Fondation ApicilAcademic/Hospital1012014
Lancashire Teaching Hospitals NHS Foundation TrustAcademic/Hospital1012015
McGill UniversityAcademic/Hospital1112008
National Institute for Health Research, United KingdomGovernment1012015
National Institute of Neurological Disorders and Stroke (NINDS)Government1012004
Newcastle UniversityAcademic/Hospital1012015
Royal Marsden Hospital NHS TrustAcademic/Hospital1112010
Sheffield Hallam UniversityAcademic/Hospital1012015
Tanta UniversityAcademic/Hospital1112019
Thomas Jefferson UniversityAcademic/Hospital1012011
University of BirminghamAcademic/Hospital1012015
University of BristolAcademic/Hospital1012015
University of CambridgeAcademic/Hospital1012015
University of CincinnatiAcademic/Hospital1112004
University of LeedsAcademic/Hospital1012015
25 organizations
Page 1 / 2

Marketing (16)

OrganizationOrg typeRelationshipDate
Akorn, Inc.For profitMKTGMay 28, 2008
Bionpharma IncFor profitMKTGOct 28, 2002
Bionpharma IncFor profitSYNOct 28, 2002
Chartwell PharmaceuticalsFor profitMKTGDec 22, 2003
EmcureFor profitMKTGSep 25, 2012
Epic Pharma LlcFor profitMKTGMay 28, 2008
Heritage PharmaFor profitMKTGSep 25, 2012
MikartFor profitMKTGDec 22, 2003
ONESOURCE SPECIALTYFor profitMKTGFeb 19, 2019
Parke-DavisFor profitMKTGFeb 13, 1974
Parke-DavisFor profitNDANov 2, 1960
Pharmaceutical AssociatesFor profitMKTGNov 22, 2000
Puracap PharmaceuticalFor profitMKTGMar 16, 2020
Strides Pharma ScienceFor profitMKTGFeb 19, 2019
TevaFor profitMKTGJul 30, 1993
Warner LambertFor profitMKTGFeb 13, 1974