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Serabelisib is an orally bioavailable, selective inhibitor of the class I phosphoinositide 3‑kinase alpha isoform (PI3Kα), including mutant forms of PIK3CA, a key component in the PI3K/Akt/mTOR signaling pathway. By inhibiting PI3Kα, serabelisib disrupts downstream signaling involved in tumor cell growth, survival, and resistance to therapy. This targeted mechanism may induce apoptosis and inhibit proliferation in PI3Kα-expressing tumor cells. Serabelisib has demonstrated efficacy in preclinical models with both wild-type and mutant p110α and is being investigated primarily for solid tumors such as endometrial cancer, renal cell carcinoma, and triple-negative breast cancer. The drug was originally developed by Intellikine and has been further developed by Takeda Oncology and other collaborators[1][2][3][4][5][6][7].
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