Drug intelligence / Profile preview

PCT-3012

Development stage
Preclinical
Lead developer
PolyCore Therapeutics
Modality
Small Molecules
01

Overview

**PCT-3012** is a novel small molecule developed by PolyCore Therapeutics as a G protein-biased agonist of the dopamine D3 receptor (D3R) for treating motor symptoms in early- to mid-stage Parkinson's disease without inducing levodopa-associated dyskinesia, tolerance, or impulse control disorders. Unlike traditional dopamine agonists like L-dopa, which signal through both G-protein and β-arrestin pathways—where β-arrestin recruitment leads to receptor desensitization and side effects—PCT-3012 selectively activates G-protein signaling while avoiding β-arrestin recruitment, thereby maintaining therapeutic efficacy on motor function while minimizing long-term receptor desensitization and hyperactivation of neurons.[1][2][7]

02

Targets

DRD3 (Dopamine receptor D3)

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