tiagabine
Trade name: gabitril
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
Earliest trial started Aug 1, 2001 (NCT00218166)
Timeline
1990s
2000s
2010s
- Jan 1, 2011
Earliest Phase 1 Sponsor(trial)
- Nov 4, 2011
Sun Pharmaceuticals — Marketing Organization
- Oct 13, 2017
Wilshire Pharmaceuticals — Marketing Organization
- Dec 8, 2017
Amneal Pharmaceuticals — Marketing Organization
2020s
- Nov 16, 2021
MSN Laboratories — Marketing Organization
Indications
Approved for
Mechanism of action
- GABA transporter 1INHIBITOR
SLC6A1 inhibitor
reuptake inhibitor
Approval history
- approvedSep 30, 1997
Chemistry & pharmacology
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
- ChEMBLCHEMBL1027 ↗
- WikipediaTiagabine ↗
- NCATSZ80I64HMNP ↗
- ChEMBLCHEMBL1695 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02387710 | Phase 2 | Mar 1, 2015 | Harvard University |
| NCT01904487 | Phase 1 | Apr 1, 2011 | University of Pittsburgh |
| NCT00855738 | Phase 4 | May 1, 2007 | Pfizer |
| NCT00214994 | Phase 3 | Jan 1, 2005 | Cephalon |
| NCT00129298 | Phase 2 | Dec 1, 2004 | National Institute on Drug Abuse (NIDA), Yale University |
| NCT00236015 | Phase 3 | Nov 1, 2004 | Cephalon |
| NCT00236054 | Phase 3 | Oct 1, 2004 | Cephalon |
| NCT00236067 | Phase 3 | Oct 1, 2004 | Cephalon |
| NCT00174850 | Phase 4 | Jul 1, 2004 | State University of New York, State University of New York, Syracuse |
| NCT00179465 | Phase 3 | Nov 1, 2003 | Dartmouth University, Harvard University |
| NCT00233675 | Phase 3 | Aug 1, 2003 | Cephalon |
| NCT00086255 | Phase 2 | Oct 1, 2002 | Department of Veteran Affairs, National Institute on Drug Abuse (NIDA), University of Cincinnati |
| NCT00208741 | Phase 4 | Jun 1, 2002 | Cephalon, Emory University |
| NCT00218166 | Phase 2 | Aug 1, 2001 | National Institute on Drug Abuse (NIDA) |
Organizations
Research & Development (12)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Cephalon | For profit | 6 | 5 | 2 | 2002 |
| National Institute on Drug Abuse (NIDA) | Government | 3 | 3 | 1 | 2001 |
| Harvard University | Academic/Hospital | 2 | 2 | 2 | 2003 |
| Dartmouth University | Academic/Hospital | 1 | 0 | 1 | 2003 |
| Department of Veteran Affairs | Government | 1 | 0 | 1 | 2002 |
| Emory University | Academic/Hospital | 1 | 1 | 1 | 2002 |
| Pfizer | For profit | 1 | 1 | 1 | 2007 |
| State University of New York | Academic/Hospital | 1 | 1 | 1 | 2004 |
| State University of New York, Syracuse | Academic/Hospital | 1 | 0 | 1 | 2004 |
| University of Cincinnati | Academic/Hospital | 1 | 0 | 1 | 2002 |
| University of Pittsburgh | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Yale University | Academic/Hospital | 1 | 0 | 1 | 2004 |
Marketing (6)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Amneal Pharmaceuticals | For profit | MKTG | Dec 8, 2017 |
| Cephalon | For profit | NDA | Sep 30, 1997 |
| Cephalon | For profit | NDA2 | Sep 30, 1997 |
| MSN Laboratories | For profit | MKTG | Nov 16, 2021 |
| Sun Pharmaceuticals | For profit | MKTG | Nov 4, 2011 |
| Wilshire Pharmaceuticals | For profit | MKTG | Oct 13, 2017 |