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PIK-101 (also known as PIKTOR) is an orally bioavailable small molecule dual inhibitor of the phosphoinositide 3-kinase alpha (PI3Kα) isoform and the mechanistic target of rapamycin complexes 1 and 2 (mTORC1/2). Developed by Faeth Therapeutics, PIK-101 is designed to treat PIK3CA-mutated and pathway-dependent malignancies, specifically hormone receptor-positive, HER2-negative (HR+/HER2-) metastatic breast cancer. The drug's clinical development is unique in its integration with the Faeth Metabolic Platform, which utilizes a precision insulin-suppressing diet to enhance therapeutic efficacy. By simultaneously blocking PI3Kα and mTORC1/2 while metabolically suppressing insulin, PIK-101 aims to prevent the compensatory insulin feedback loop that typically limits the effectiveness of PI3K inhibitors. It is currently undergoing Phase 1 clinical evaluation.
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