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Baricitinib is an inhibitor of JAK1 and JAK2 (IC50s = 0.0059 and 0.0057 µM, respectively).1 It is selective for JAK1 and JAK2 over JAK3, TYK2, c-Met, and checkpoint kinase 2 (Chk2; IC50s = >0.4, 0.053, >10, and >1 µM, respectively). Baricitinib inhibits IL-6-induced phosphorylation of STAT3 in isolated human peripheral blood mononuclear cells (PBMCs) and rat whole blood (IC50s = 0.044 and 0.128 µM, respectively). It reduces disease severity in a type II collagen-induced mouse model of arthritis when administered at doses of 3 and 10 mg/kg. Baricitinib (4 mg/animal) also decreases lung macrophage infiltration and disease severity in rhesus monkeys infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2).2 Formulations containing baricitinib have been used in the treatment of rheumatoid arthritis.
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1. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: Preclinical characterization of INCB028050. J. Immunol. 184(9), 5298-5307 (2010).
2. Baricitinib treatment resolves lower-