RO5461111 a highly specific and orally active antagonist of Reduced the activation and expansion of spleen dendritic cells, CD4, double-negative T cells and plasma cells.
Reduced plasma levels of IL-10 and TNF-α.
[1]. Rupanagudi KV, et al. Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming. Ann Rheum Dis. 2015 Feb;74(2):452-63.
[2]. Sanchez RA, et al. Preparation of proline dipeptidyl nitrile derivatives as cathepsin, particularly cathepsin S and L, inhibitors: United States, US20100267722. 2010-10-21.