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TRTL-729

Development stage: Phase 1
Lead developer: Tortugas Neuroscience
Modality: Small Molecules

Overview

TRTL-729 is a small molecule uncompetitive inhibitor of the gamma-aminobutyric acid transporter 1 (GAT-1), currently in preclinical development by Tortugas Neuroscience for the treatment of focal epilepsy. Unlike traditional competitive GAT-1 inhibitors, TRTL-729 utilizes an uncompetitive mechanism of action to reduce GABA reuptake and increase extracellular GABA levels. This activity-dependent approach is designed to enhance inhibitory neurotransmission specifically during periods of high synaptic activity, potentially offering a superior safety and efficacy profile compared to existing GABAergic therapies for brain disorders.

Targets

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

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