Drug intelligence / Profile preview

radium Ra 223 dichloride + abiraterone acetate + prednisone

Development stage
Phase 2
Lead developer
Bayer
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen of three drugs used in the treatment of metastatic castration-resistant prostate cancer (mCRPC) with bone metastases. Radium Ra 223 dichloride is a targeted alpha-particle radiopharmaceutical that selectively binds to areas of increased bone turnover, delivering cytotoxic radiation to bone metastases and disrupting tumor cell activity. Abiraterone acetate is an androgen biosynthesis inhibitor that blocks CYP17, reducing androgen production and thereby inhibiting prostate cancer growth. Prednisone is a synthetic glucocorticoid used to manage side effects associated with abiraterone and provide additional anti-tumor effects. While each drug individually has demonstrated efficacy in mCRPC, clinical trials have shown that combining all three increases the risk of fractures and mortality without improving skeletal event-free survival compared to standard regimens; thus, this combination is not recommended outside clinical trials[2][5][6].

Other names
radium-223radium223radium 223Ra 223Ra223Ra-223abiraterone
02

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)

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