molecules of the month


oral IRAK4 inhibitor

promising activity in mouse model for atopic dermatitis

HTS of kinase-focused 25K cmpd library vs. IRAK4 catalytic domain

Sci. Trans. Med., February 15, 2023

Galapagos, FR + BE

GLPG2534, oral IRAK4 inhibitor, promising activity in mouse model for atopic dermatitis, GALAPAGOS SASU, FR + NV, BE
5 mins read

Preclinical validation for IRAK4 inhibitors for dermatology from activity in human biopsies. Interleukin-1 receptor-associated kinase (IRAK4) is downstream of toll-like receptors (TLRs), which are established mediators of inflammation. Like many immune-signaling nodes (JAK, BTK), this has been of interest for potential treatment of immunological diseases and blood cancers with immune-cell lineages. Paralleling the development of JAK inhibitors, IRAK4 biology was preclinically validated for RA and SLE initially, and now Galapagos is disclosing preclinical validation for dermatology, the ATP-competitive clinical candidate, GLPG2534. Particularly notable here is that IRAK4 inhibition with Galapagos’ compound ameliorated pathogenic molecular signatures in biopsies of diseased human tissue. IRAK4, the “JAK” or “BTK” of innate immunity? Given the massive success of molecules targeting T-cell receptor signaling mediators…

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