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This is a combination of two small molecule drugs: - Letrozole is a non-steroidal aromatase inhibitor that suppresses estrogen biosynthesis by inhibiting the aromatase enzyme. It is primarily used in hormone receptor-positive breast cancer to reduce estrogen levels and slow tumor growth. - Voxtalisib (SAR245409, XL765) is an orally available dual inhibitor of phosphoinositide 3-kinases (PI3K) and mammalian target of rapamycin complexes 1 and 2 (mTORC1/mTORC2). By blocking these kinases, voxtalisib disrupts key signaling pathways involved in cell proliferation, survival, and metabolism. The combination has been investigated for use in hormone-receptor-positive, HER2-negative metastatic breast cancer that is resistant to prior endocrine therapy[1][3]. The rationale for combining these agents lies in targeting both hormonal signaling via estrogen suppression and compensatory survival pathways mediated by PI3K/mTOR activation.
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