Evobrutinib is an inhibitor of Bruton's tyrosine kinase (BTK; IC = 8.9 nM). It is selective for BTK over a panel of 233 kinases at 1 μM. It inhibits BTK in peripheral blood mononuclear cells (PBMCs; IC = 61 nM). Evobrutinib inhibits B cell activation and proliferation in vitro (ICs = 18.4 and 10.9 nM, respectively). It inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis when administered at doses of 3.95, 19.8, and 39.5 mg/kg. Evobrutinib (1 and 3 mg/kg) reduces cartilage destruction in a rat model of collagen-induced arthritis. It also decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of systemic lupus erythematosus (SLE).