Drug intelligence / Profile preview

darolutamide + radium-223

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

Overview

Darolutamide + radium-223 is a combination therapy under investigation for the treatment of metastatic castration-resistant prostate cancer (mCRPC) with bone metastases. Darolutamide is an orally administered second-generation androgen receptor inhibitor that blocks androgen receptor signaling, thereby inhibiting the growth of prostate cancer cells. Radium-223 dichloride is a targeted alpha-emitting radiopharmaceutical that mimics calcium and selectively binds to areas of increased bone turnover associated with bone metastases; it induces double-strand DNA breaks in adjacent tumor cells through alpha particle emission. Preclinical studies have demonstrated synergistic antitumor efficacy when these agents are combined, likely due to downregulation of DNA damage response pathways and enhanced suppression of tumor-induced pathological effects in bone[1][2]. Both drugs are approved individually for specific indications in prostate cancer.

Other names
darolutamideradium-223 dichlorideradium223 dichlorideradium 223 dichloride
02

Targets

AR (Adrenergic receptors)DNA

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