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Ifupinostat is a novel, orally available small molecule that acts as a dual inhibitor of phosphatidylinositol 3-kinase alpha (PI3Kα) and histone deacetylases (HDACs). By simultaneously inhibiting both PI3Kα and HDACs, ifupinostat disrupts key tumor cell signaling networks involved in cancer cell proliferation and survival. This dual-targeting approach is designed to enhance antitumor efficacy by blocking two critical pathways implicated in oncogenesis. Ifupinostat has demonstrated potent nanomolar inhibitory activity against PI3Kα (IC50 <0.1 μM) and HDACs (IC50 0.1–1 μM)[7][4][9]. It is being developed primarily for the treatment of hematologic malignancies such as relapsed/refractory diffuse large B-cell lymphoma[8][4].
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