GSK3179106

GSK3179106 is a potent and selective small molecule inhibitor of the rearranged during transfection (RET) tyrosine kinase receptor. It is designed to be gut-restricted and acts as a pyridone hinge binder with high selectivity for RET (IC50 ~0.3–0.4 nM). The drug was developed as a first-in-class candidate for the treatment of irritable bowel syndrome (IBS), targeting neuronal growth factor signaling in the enteric nervous system to normalize neuronal function and alleviate IBS symptoms. In addition to its activity against RET kinase, GSK3179106 also exhibits inhibitory effects on p38 mitogen‐activated protein kinase (MAPK), contributing to anti-inflammatory properties observed in preclinical models such as acute lung injury. The compound has undergone phase I clinical trials in healthy volunteers for safety and pharmacokinetics[1][7][5][6].

Other names

RET Kinase inhibitor 12-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-N-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamideDY8BBK4G3CDY-8BBK4G3CDY 8BBK4G3C