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Motolimod is a synthetic small molecule that acts as a potent and selective agonist of Toll-like receptor 8 (TLR8), which is primarily expressed on myeloid dendritic cells, monocytes/macrophages, and mast cells. By binding to TLR8, motolimod activates the central transcription factor NF-kB, leading to the secretion of proinflammatory cytokines and other mediators. This results in a Th1-weighted antitumoral cellular immune response and mobilizes both innate and adaptive immunity against tumors. Motolimod has been investigated as an immunostimulant in various cancers—including ovarian cancer, lymphoma, tongue cancer, fallopian tube cancer, peritoneal carcinoma, B-cell lymphoma, squamous cell carcinoma of the head and neck—and has reached up to phase II clinical trials for these indications. The drug was originally developed under the code name VTX-2337[1][2][3][5][7].
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