Drug intelligence / Profile preview

tiagabine

Development stage
Approved
Lead developer
Teva Pharmaceutical Industries
Modality
Small Molecules
Administration
Oral
01

Overview

Tiagabine is a small molecule anticonvulsant medication primarily indicated as adjunctive therapy for the treatment of partial seizures in adults and children 12 years of age and older. Developed through a collaboration between Novo Nordisk and Abbott Laboratories, it represents a unique class of antiepileptic drugs that target the GABAergic system. Its mechanism of action involves the potent and selective inhibition of the GABA transporter 1 (GAT-1), the primary protein responsible for the reuptake of gamma-aminobutyric acid (GABA) from the synaptic cleft into presynaptic neurons and surrounding glial cells. By blocking GAT-1, tiagabine increases the extracellular concentration and duration of GABA at inhibitory synapses, thereby enhancing GABA-mediated inhibitory neurotransmission and elevating the seizure threshold.

Brand names
Gabitril
Other names
tiagabine hydrochloride
02

Targets

SLC6A1 (Sodium- and chloride-dependent GABA transporter 1)

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