Drug intelligence / Profile preview

radium-223 + enzalutamide

Development stage
Unknown
Lead developer
Bayer
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

Radium-223 + enzalutamide is a combination therapy under clinical development for the treatment of metastatic castration-resistant prostate cancer (mCRPC) with bone metastases. Radium-223 dichloride is a radiopharmaceutical that mimics calcium and selectively targets bone metastases, delivering alpha particle radiation that induces double-stranded DNA breaks in cancer cells, leading to cell death. Enzalutamide is an androgen receptor inhibitor that blocks the action of male hormones (androgens), thereby inhibiting prostate cancer cell growth and survival. The combination leverages their distinct mechanisms—radium-223’s targeted radiotherapy and enzalutamide’s hormonal blockade—to improve outcomes and potentially delay resistance to treatment. Recent phase 3 trial data show significant improvements in radiological progression-free survival (rPFS) and overall survival (OS) compared to monotherapy[1][2][5][6].

Brand names
XofigoXtandi
Other names
radium-223 dichlorideradium223 dichlorideradium 223 dichlorideenzalutamide
02

Targets

AR (Adrenergic receptors)

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