BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor.

CYP2C9:12 μM, CYP2D6:41 μM, CYP2C19:9 μM, CYP3A4:8 μM, CYP1A2:50 μM

BI 653048 exhibits improved drug-like properties, inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19, and CYP3A4 (IC50s: 50 μM, 41 μM, 12 μM, 9 μM, and 8 μM). BI 653048 reduces affinity for the hERG ion channel with an IC50>30 μM in recombinant HEK293 cells expressing the human ERG potassium channel. BI 653048 inhibits TNF-stimulated IL-6 production in mouse RAW cells (IC50: 100 nM) [2].

BI 653048 (p.o.; 3, 10, and 30 mg/kg) at 3 mg/kg has nonsignificant decreases for all measured histology parameters (ankle inflammation, cartilage damage, pannus formation, and bone resorption), Mid-dose (10 mg/kg) treatment significantly decreases pannus and bone resorption (33%) as well as summed scores (27%), while at high dose (30 mg/kg), all parameters are significantly decreased (87–96%). The ED50 value for the summed scores is 14 mg/kg [2].