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LXI-15029 (also known as MTI-31) is an orally bioavailable, ATP-competitive dual inhibitor of the mammalian target of rapamycin (mTOR) complexes 1 and 2 (mTORC1 and mTORC2). Developed by Shandong Luoxin Pharmaceutical Group, it is designed to overcome the limitations of first-generation mTOR inhibitors (rapalogs) by preventing the feedback activation of AKT that typically occurs when only mTORC1 is inhibited. By binding to the catalytic domain of the mTOR kinase, LXI-15029 inhibits the phosphorylation of downstream substrates such as S6K1, 4E-BP1, and AKT (at Ser473). It has been investigated in Phase 1 clinical trials for the treatment of advanced malignant solid tumors and hormone receptor-positive, HER2-negative breast cancer, both as a monotherapy and in combination with endocrine therapies like exemestane.
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