A JAK1 inhibitor
Abrocitinib is a JAK1 inhibitor (IC50 = 0.029 ?M).1 It is selective for JAK1 over JAK2, JAK3, and TYK2 (IC50s = 0.803, >10, and 1.253 ?M, respectively) and a panel of 40 kinases at 1 ?M. Abrocitinib inhibits IFN-α-, IL-21-, or IL-27-induced phosphorylation of STAT3 (IC50s = 0.189, 0.511, and 0.271 ?M, respectively) and IFN-γ-induced phosphorylation of STAT1 (IC50 = 0.163 ?M) in isolated human whole blood. It reduces paw edema in a rat model of adjuvant-induced arthritis when administered at doses of 1, 5, and 15 mg/kg. Formulations containing abrocitinib have been used in the treatment of atopic dermatitis.
1.Vazquez, M.L., Kaila, N., Strohbach, J.W., et al.Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A selective JAK1 clinical candidate for the treatment of autoimmune diseasesJ. Med. Chem.61(3)1130-1152(2018)
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