Drug intelligence / Profile preview

GSK163090

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK163090 is a potent, selective, and orally active small molecule antagonist of the serotonin 1A receptor (5‑HT1A), serotonin 1B receptor (5‑HT1B), and serotonin 1D receptor (5‑HT1D). It was developed by GSK as a potential fast-onset antidepressant and anxiolytic. The drug advanced to phase II clinical trials for major depressive disorder (MDD) and anxiety disorders but did not demonstrate significant efficacy compared to placebo in MDD trials. Development for these indications has been discontinued[1][2][6][7].

Other names
1-(3-(2-(4-(2-Methyl-5-quinolinyl)-1-piperazinyl)ethyl)phenyl)-2-imidazolidinone1-[3-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]phenyl]imidazolidin-2-oneUNII-7XI927X82BUNII7XI927X82BUNII 7XI927X82B
02

Targets

HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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