Cadefrecitinib (GLPG3667) is a potent, reversible and selective, ATP-competitive TYK2 inhibitor with IC50 of 2.3 nM.
GLPG3667 is a selective TYK2 inhibitor in human PBMC and whole blood assays.
GLPG3667 shows dose-dependent inhibition of IFNα-induced STAT1 phosphorylation (JAK1/TYK2-dependent, IC50=70 nM), IL-2-induced STAT5 phosphorylation (JAK1/JAK3-dependent) and granulocyte macrophage colony-stimulating factor (GM-CSF)-induced STAT5 phosphorylation (JAK2-dependent).
GLPG3667 displays general kinase selectivity against a panel of 365 kinases.
GLPG3667 reduced dermal ear inflammation in an IL-23-induced in vivo mouse model of psoriasis.
