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radium-223 + enzalutamide
- Development stage
- Phase 3
- Lead developer
- Bayer
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules
- 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].
- Other names
- radium-223 dichlorideradium223 dichlorideradium 223 dichlorideenzalutamide
02
Targets
AR (Adrenergic receptors)
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