ISM3830

ISM3830 is a novel, orally bioavailable small-molecule inhibitor of Cbl-b (Casitas B-lineage lymphoma proto-oncogene b), an intracellular E3 ubiquitin ligase that serves as an immune checkpoint by negatively regulating the activation of T cells, NK cells, and dendritic cells. Developed by Insilico Medicine, ISM3830 is designed to restore innate and adaptive immune responses within the immunosuppressive tumor microenvironment. Preclinical data presented at AACR 2026 demonstrate that ISM3830 enhances the release of IL-2 and IFN-γ, restores the function of exhausted T cells, and exhibits potent antitumor activity in syngeneic mouse models. Furthermore, it shows significant synergy when combined with anti-PD-1 therapy, leading to high rates of tumor growth inhibition and complete regression in animal models. ISM3830 possesses a favorable pharmacokinetic profile and a safety margin that supports its clinical development for the treatment of various solid tumors.