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Imatinib (ST571) is a small molecule tyrosine kinase inhibitor primarily targeting BCR-ABL, c-KIT, and PDGFR, widely used in the treatment of chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GIST). Alpelisib (BYL719) is a selective phosphatidylinositol 3-kinase alpha (PI3Kα) inhibitor that blocks the ATP-binding site of PI3K p110α, a catalytic subunit frequently mutated in various cancers. Alpelisib is approved for use in certain types of breast cancer with PIK3CA mutations and for PIK3CA-related overgrowth spectrum disorders. The combination of imatinib and alpelisib represents an investigational approach to target both tyrosine kinase-driven signaling pathways and PI3K/AKT/mTOR pathway dysregulation in cancer therapy[1][2][4][5].
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