Zetomipzomib (KZR-616) is a first-in-class, selective immunoproteasome inhibitor for a range of autoimmune diseases. Immunoproteasomes play an important role in regulating the normal function of the immune system and when inhibited, multiple pathways involved in inflammatory cytokine production and immune effector cell activity – including macrophages, B cells and T cells – are also inhibited. Since the pathways regulated by immunoproteasomes are involved in the pathogenesis of many autoimmune diseases, zetomipzomib offers a “pipeline in a drug” approach, with the potential to be a treatment option for a broad range of autoimmune conditions.

Most approaches for treating autoimmune diseases focus on suppressing the immune system, like steroids, or targeting a single immune signal to help counter the chronic inflammatory state that is often present. Zetomipzomib, however, can broadly modulate the immune system when it is dysregulated. This candidate has the potential to act as a steroid sparing agent, which would fill a major unmet need in the autoimmune treatment landscape.