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radium-223 + tasquinimod
- Development stage
- Phase 1
- Lead developer
- Active Biotech
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
A combination therapy consisting of Radium-223 dichloride and tasquinimod, currently under investigation for the treatment of bone-only metastatic castration-resistant prostate cancer (mCRPC). Radium-223 is a first-in-class alpha-emitting radiopharmaceutical that acts as a calcium mimetic, selectively targeting areas of high bone turnover associated with metastases and delivering high-LET radiation to induce double-strand DNA breaks in tumor cells. Tasquinimod is an oral small molecule quinoline-3-carboxamide derivative that functions as an anti-angiogenic and immunomodulatory agent by binding to and inhibiting histone deacetylase 4 (HDAC4) and the S100A9 protein, thereby modulating the tumor microenvironment and blocking survival signaling. This combination approach, led by the Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, seeks to enhance therapeutic efficacy by combining bone-targeted cytotoxic radiation with systemic microenvironment modulation.
- Other names
- Radium-223 dichloride + tasquinimodXofigo + tasquinimodRa-223 + tasquinimod
02
Targets
DNAHDAC4S100A9 (Myeloid-related protein 14)THBS1 (Thrombospondin-1)
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