CPL409116

CPL409116 is a first-in-class, orally administered small molecule that acts as a dual inhibitor of Janus kinases (JAK) and Rho-associated coiled-coil containing protein kinases (ROCK). Developed by Celon Pharma, often in collaboration with the National Centre for Research and Development, it is designed to simultaneously inhibit inflammation and fibrogenesis. The drug primarily targets JAK1 and JAK3 with less activity against JAK2 and Tyk2, as well as both ROCK isoforms. Its mechanism aims to reduce inflammatory cytokine release—thereby decreasing lymphocyte activation/proliferation—and modulate cellular processes such as cytoskeleton organization, cell adhesion/motility, proliferation, apoptosis, and smooth muscle contraction. This dual action may be particularly beneficial in autoimmune diseases like rheumatoid arthritis (including those with interstitial lung disease), where both inflammation and fibrosis are key pathological features. Phase I studies demonstrated safety/tolerability in healthy volunteers; phase II trials showed dose-dependent efficacy in patients with active rheumatoid arthritis who had inadequate response to methotrexate[1][2][4][5][6][9][10].

Other names

CPL'116CPL-409116CPL409116CPL 409116