Tiagabine
Gabitril, Tiagabine (tiagabine) is a small molecule pharmaceutical. Tiagabine was first approved as Gabitril on 1997-09-30. It is used to treat bipolar disorder, epilepsy, and partial epilepsies in the USA. The pharmaceutical is active against sodium- and chloride-dependent GABA transporter 1.
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| nervous system diseases | D009422 |
| mental disorders | D001523 |
Trade Name
FDA
EMA
Gabitril, Tiagabine (discontinued: Gabitril, Tiagabine)
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| gabitril | New Drug Application | 2016-08-06 |
| tiagabine hydrochloride | ANDA | 2023-12-30 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| epilepsy | EFO_0000474 | D004827 | G40.9 |
| partial epilepsies | EFO_0004263 | D004828 | — |
| bipolar disorder | EFO_0000289 | D001714 | F30.9 |
Agency Specific
FDA
EMA
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Patent Expiration
No data
HCPCS
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Clinical
Clinical Trials
21 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Anxiety disorders | D001008 | EFO_0006788 | F41.1 | — | — | 5 | 1 | — | 6 |
| Social phobia | D000072861 | EFO_1001917 | F40.1 | — | — | — | 1 | — | 1 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Generalized anxiety disorder | D000098647 | — | — | — | — | 2 | — | — | 2 |
Indications Phases 2
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Indications Phases 1
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Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Tiagabine |
| INN | tiagabine |
| Description | Tiagabine is a piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy. It has a role as a GABA reuptake inhibitor and an anticonvulsant. It is a piperidinemonocarboxylic acid, a beta-amino acid, a member of thiophenes and a tertiary amino compound. It is functionally related to a (R)-nipecotic acid. It is a conjugate base of a tiagabine(1+). |
| Classification | Small molecule |
| Drug class | gabamimetics |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | Cc1ccsc1C(=CCCN1CCC[C@@H](C(=O)O)C1)c1sccc1C |
Identifiers
| PDB | — |
| CAS-ID | 115103-54-3 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1027 |
| ChEBI ID | 9586 |
| PubChem CID | 60648 |
| DrugBank | DB00906 |
| UNII ID | Z80I64HMNP (ChemIDplus, GSRS) |
Target
Agency Approved
SLC6A1
SLC6A1
Organism
Homo sapiens
Gene name
SLC6A1
Gene synonyms
GABATR, GABT1, GAT1
NCBI Gene ID
Protein name
sodium- and chloride-dependent GABA transporter 1
Protein synonyms
GABA transporter 1, solute carrier family 6 (neurotransmitter transporter), member 1, solute carrier family 6 (neurotransmitter transporter, GABA), member 1, Solute carrier family 6 member 1
Uniprot ID
Mouse ortholog
Slc6a1 (232333)
sodium- and chloride-dependent GABA transporter 1 (P31648)
Alternate
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Variants
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Gabitril – Cephalon
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Estimated US medical usage
Tiagabine
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Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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881 adverse events reported
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