E2730 is a selective and noncompetitive inhibitor of the gamma-aminobutyric acid (GABA) transporter 1 (GAT1) that exhibits oral availability as well as antiepileptic properties. Its inhibition of GAT1 is dependent on the prevailing GABA concentrations and specifically targets GAT1-mediated GABA uptake. Demonstrating in vivo effectiveness, E2730 has been tested at doses ranging from 5-50 mg/kg orally in various models, including the rat amygdala kindling and the mouse corneal kindling models, as well as in drug-resistant psychomotor epilepsy, fragile X syndrome at 2.5-300 mg/kg, and Dravet syndrome at dosages of 10 mg/kg and 20 mg/kg [1].