Baricitinib

Baricitinib is a highly potent JAK1 and JAK2 inhibitor (IC50 values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC50 = 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC50 = 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1 in vitro (Kd values are 17.2, 39.8, 134.4 and 68.5 nM, respectively). Inhibits IL-6-induced STAT phosphorylation and subsequent pro-inflammatory chemokine (MPC-1) and cytokine (IL-17 and IL-22) production in PBMCs and T-cells. Displays anti-inflammatory and disease modifying effects in the rat adjuvant arthritis model. In silico modelling predicts inhibition of SARS-CoV-2 cell entry.