tiagabine

Trade name: gabitril

Small moleculeapproved

Approved

Sep 30, 1997

Tiagabine (trade name Gabitril) is an anticonvulsant medication used in the treatment of Partial Seizures. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enhance the activity of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, Tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. Tiagabine is approved by U.S. Food and Drug Administration (FDA) as an adjunctive treatment for partial seizures in individuals of age 12 and up. It may also be prescribed off-label by physicians to treat anxiety disorders and panic disorder as well as neuropathic pain (including fibromyalgia). For anxiety and neuropathic pain, tiagabine is used primarily to augment other treatments. Tiagabine may be used alongside selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, or benzodiazepines for anxiety, or antidepressants, gabapentin, other anticonvulsants, or opioids for neuropathic pain. The most common side effect of tiagabine is dizziness. Other side effects that have been observed with a rate of statistical significance relative to placebo include asthenia, somnolence, nervousness, memory impairment, tremor, headache, diarrhea, and depression. — NCATS

Clinical trial activity

14 trials · 12 clinical orgs · 5 marketing orgs

Phase 1
1
Phase 2
10
Phase 3
6
Phase 4
3

Earliest trial started Aug 1, 2001 (NCT00218166)

Timeline

1990s

  1. Sep 30, 1997

    Cephalon — Earliest FDA Approval

  2. Sep 30, 1997

    Cephalon — NDA Organization

  3. Sep 30, 1997

    Cephalon — NDA Secondary Org

2000s

  1. Jan 1, 2001

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2003

    Cephalon — Earliest Phase 3 Sponsor(trial)

2010s

  1. Jan 1, 2011

    Earliest Phase 1 Sponsor(trial)

  2. Nov 4, 2011

    Sun Pharmaceuticals — Marketing Organization

  3. Oct 13, 2017

    Wilshire Pharmaceuticals — Marketing Organization

  4. Dec 8, 2017

    Amneal Pharmaceuticals — Marketing Organization

2020s

  1. Nov 16, 2021

    MSN Laboratories — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedSep 30, 1997

Chemistry & pharmacology

Loading structure…

SMILES

Cc1ccsc1C(=CCCN1CCC[C@@H](C(=O)O)C1)c1sccc1C
Mol. weight
375.56 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • a-70569-1
  • a-70569-1
  • abbott-70569
  • abbott-70569
  • abbott-70569-1
  • abbott-70569-1
  • abbott-70569.1
  • abbott-70569.1
  • abbott-70569.hcl
  • abbott-70569.hcl
  • abt-569
  • abt-569
  • gabatril
  • gabitril
  • gabitril
  • gabitril
  • gabitril
  • n-(4,4-di(3-methylthien-2-yl)but-3-enyl)nipecotic acid
  • nnc-05-0328
  • nnc-05-0328
  • no-05-0328
  • no-05-0328
  • no 328
  • no-328
  • no 329
  • no-329
  • (r)-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)-3-piperidinecarboxylic acid, hydrochloride
  • (r)-tiagabine
  • tiagabina
  • tiagabina
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine
  • tiagabine hcl
  • tiagabine hcl
  • tiagabine hcl
  • tiagabine hydrochloride
  • tiagabine hydrochloride
  • tiagabine hydrochloride
  • tiagabine hydrochloride
  • tiagabine, (s)-isomer
  • tiagabinum
  • tiagabinum
  • tigabine

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02387710Phase 2Mar 1, 2015Harvard University
NCT01904487Phase 1Apr 1, 2011University of Pittsburgh
NCT00855738Phase 4May 1, 2007Pfizer
NCT00214994Phase 3Jan 1, 2005Cephalon
NCT00129298Phase 2Dec 1, 2004National Institute on Drug Abuse (NIDA), Yale University
NCT00236015Phase 3Nov 1, 2004Cephalon
NCT00236054Phase 3Oct 1, 2004Cephalon
NCT00236067Phase 3Oct 1, 2004Cephalon
NCT00174850Phase 4Jul 1, 2004State University of New York, State University of New York, Syracuse
NCT00179465Phase 3Nov 1, 2003Dartmouth University, Harvard University
NCT00233675Phase 3Aug 1, 2003Cephalon
NCT00086255Phase 2Oct 1, 2002Department of Veteran Affairs, National Institute on Drug Abuse (NIDA), University of Cincinnati
NCT00208741Phase 4Jun 1, 2002Cephalon, Emory University
NCT00218166Phase 2Aug 1, 2001National Institute on Drug Abuse (NIDA)
Showing 14 of 14 trials
Page 1 / 1

Organizations

Research & Development (12)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
CephalonFor profit6522002
National Institute on Drug Abuse (NIDA)Government3312001
Harvard UniversityAcademic/Hospital2222003
Dartmouth UniversityAcademic/Hospital1012003
Department of Veteran AffairsGovernment1012002
Emory UniversityAcademic/Hospital1112002
PfizerFor profit1112007
State University of New YorkAcademic/Hospital1112004
State University of New York, SyracuseAcademic/Hospital1012004
University of CincinnatiAcademic/Hospital1012002
University of PittsburghAcademic/Hospital1112011
Yale UniversityAcademic/Hospital1012004
12 organizations
Page 1 / 1

Marketing (6)

OrganizationOrg typeRelationshipDate
Amneal PharmaceuticalsFor profitMKTGDec 8, 2017
CephalonFor profitNDASep 30, 1997
CephalonFor profitNDA2Sep 30, 1997
MSN LaboratoriesFor profitMKTGNov 16, 2021
Sun PharmaceuticalsFor profitMKTGNov 4, 2011
Wilshire PharmaceuticalsFor profitMKTGOct 13, 2017