Drug intelligence / Profile preview

letrozole + voxtalisib

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

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.

Brand names
Femara
Other names
SAR-245409 (voxtalisib)XL-765 (voxtalisib)
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)Mechanistic target of rapamycin complex 1CYP19A1 (Aromatase)

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