GLPG3312

GLPG3312 is a potent and selective pan-salt-inducible kinase (SIK) inhibitor developed by Galapagos. It targets all three SIK isoforms—SIK1, SIK2, and SIK3—with low nanomolar potency. The drug was designed as part of the "Toledo" program to modulate inflammatory responses through a dual mechanism of action: reducing pro-inflammatory cytokine production while increasing immunoregulatory cytokines. Preclinical studies demonstrated anti-inflammatory and immunoregulatory effects in human primary myeloid cells and mouse models. A first-in-human Phase 1 clinical trial evaluated its safety, pharmacokinetics, and pharmacodynamics in healthy volunteers using both immediate-release (IR) and modified-release (MR) oral tablet formulations[6][7][8]. Although initially considered for further development in inflammatory diseases such as ulcerative colitis, the program appears to have been superseded by more selective next-generation compounds[4][7].

Other names

GLPG 3312GLPG3312GLPG-3312