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GSK-424887

Development stage: Phase 1
Lead developer: GSK
Modality: Small Molecules
Administration: Oral

Overview

GSK-424887 is an investigational small molecule drug developed by GlaxoSmithKline (GSK) as a dual antagonist of the human neurokinin 1 receptor and inhibitor of the serotonin transporter. It was studied for its potential use in treating depressive disorder and anxiety disorder. The compound acts as both a selective competitive antagonist at the neurokinin 1 (NK1) receptor and an inhibitor of serotonin reuptake, aiming to combine antidepressant and anxiolytic effects. Clinical development reached phase 1 trials, but further development was discontinued[3][4][5][6].

Other names: IYI99KCF2TIYI-99KCF2TIYI 99KCF2TN-((1S)-1-(3-chloronaphthalen-1-yl)ethyl)-2-(4-(4-fluorophenyl)-1-methylpiperidin-4-yl)-N-methylacetamide

Targets

TACR1 (Neurokinin‑1 Receptor)SERT (Sodium-dependent serotonin transporter)

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