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everolimus + exemestane + radium-223 dichloride

Development stage: Discontinued
Lead developer: Bayer
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration: Oral, Intravenous

Overview

A combination therapy consisting of everolimus (an mTOR inhibitor), exemestane (an aromatase inhibitor), and radium-223 dichloride (an alpha-emitting radiopharmaceutical). This combination targets hormone receptor-positive (HR+), HER2-negative breast cancer with bone metastases through multiple mechanisms: inhibiting mTOR signaling, reducing estrogen production, and selectively targeting bone metastases with alpha radiation.

Brand names: Xofigo
Other names: radium-223 dichloride + exemestane + everolimus

Targets

mTOR (Mammalian target of rapamycin kinase)HydroxyapatiteCYP19A1 (Aromatase)

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