Drug intelligence / Profile preview

GPR17

Development stage
Preclinical
Lead developer
Rewind Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

GPR17 (also known as RWT020016) is a first-in-class, orally active, brain-penetrant small molecule GPR17 antagonist being developed by Rewind Therapeutics for the treatment of demyelinating diseases, including multiple sclerosis, optic neuritis, and nerve injuries. GPR17 (G protein-coupled receptor 17) is a key regulator of oligodendrocyte precursor cell (OPC) maturation. Chronic upregulation of GPR17 in OPCs following myelin injury halts their differentiation into mature, myelin-producing oligodendrocytes. By selectively blocking GPR17, the drug releases this differentiation block, promoting OPC maturation and facilitating structural and functional remyelination. The program is currently in preclinical development.

Other names
GPR17 antagonistGPR-17 antagonistGPR 17 antagonistGPR17 inhibitorGPR-17 inhibitorGPR 17 inhibitorGPR17 modulatorGPR-17 modulatorGPR 17 modulator
02

Targets

CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)LTE4R (G protein-coupled receptor 17)

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