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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.
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