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Roginolisib is a first-in-class, orally available, highly selective small molecule inhibitor and allosteric modulator of phosphatidylinositol 3-kinase delta (PI3Kδ). It blocks PI3Kδ-dependent signaling in both tumor cells and regulatory T cells (Tregs), thereby inhibiting cancer cell growth, survival, and migration. Roginolisib demonstrates a unique binding mode with high selectivity for PI3Kδ compared to earlier generation inhibitors, which is expected to improve safety and tolerability. The drug has shown efficacy in pretreated solid tumors and hematologic malignancies—including uveal melanoma, follicular lymphoma, chronic lymphocytic leukemia (CLL), myelofibrosis, non-small cell lung cancer (NSCLC), peripheral T-cell lymphoma, malignant melanoma, mesothelioma, non-Hodgkin's lymphoma—and can synergize with other agents such as venetoclax or immune checkpoint inhibitors. Roginolisib is being developed by iOnctura[1][2][4][5][6].
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