Delgocitinib CAS# 1263774-59-9 迪高替尼

Delgocitinib is a pan-JAK inhibitor targeting JAK1, JAK2, JAK3, and TYK2 with nanomolar potency (IC₅₀ values generally 2–30 nM across isoforms). In cellular assays, it suppressed cytokine-induced STAT phosphorylation, including IL-4, IL-13, IL-22, IL-31, and IFN-γ pathways relevant to inflammatory skin disease. In mouse dermatitis models, topical delgocitinib reduced epidermal hyperplasia, pruritus-associated cytokines, and inflammatory cell infiltration, leading to marked improvements in skin barrier function. Toxicology studies indicated low systemic exposure after topical dosing and good local tolerability, supporting its development for chronic inflammatory dermatoses such as atopic dermatitis.