tolinapant

Tolinapant is an orally bioavailable, non-peptidomimetic small molecule antagonist of the cellular and X-linked inhibitors of apoptosis proteins (cIAP1, cIAP2, and XIAP). By selectively binding to and inhibiting these IAPs, which are often overexpressed in cancer cells and contribute to tumor survival and resistance to therapy, tolinapant restores apoptotic signaling pathways leading to cancer cell death. In addition to its direct pro-apoptotic effects, it also exerts immunomodulatory activity by inducing immunogenic forms of cell death such as necroptosis. This results in activation of both the innate and adaptive immune systems against tumor cells. Tolinapant is being developed primarily for hematologic malignancies such as peripheral T-cell lymphoma (PTCL) and cutaneous T-cell lymphoma (CTCL), as well as advanced solid tumors including head and neck squamous cell carcinoma (HNSCC) and cervical carcinoma. The drug was designed using fragment-based drug design technology.

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tolinapant