Safety and Pharmacokinetics of JAK/ROCK Inhibitor in Healthy Volunteers

In BRG we are just starting Study for Healthy People with an Immune Drug - Part B. The aim of the following clinical trial is to determine safety and pharmacokinetic parameters in healthy volunteers after oral administration of Janus kinases and Rho-kinases inhibitor (JAK/ROCKi), called CPL409116.Janus kinase (JAK) inhibitors are a new class of small molecule drugs that modulate inflammatory pathways by blocking one or more JAK receptors. In recent years, JAK inhibitors have emerged as a new option for the treatment of various inflammatory diseases, including rheumatoid arthritis, psoriatic arthritis, spondyloarthritis, skin disorders and others. CPL409116 inhibits JAK1 and JAK3 with less inhibitory activity against JAK2 and Tyk2. Inhibition of these kinases decreases inflammatory cytokine release which in turn decreases lymphocyte activation and proliferation. Moreover, CPL409116 blocks Rho-kinases (ROCKs), which are involved in diverse cellular processes including actin cytoskeleton organization, cell adhesion and motility, proliferation, apoptosis as well as smooth muscle contraction.  Dual inhibition of JAK/ROCK kinases may be beneficial for patients suffering from fibrotic complications of inflammatory disease. More information about the study you can find on

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