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225Ac-macropa-PSMA
- Development stage
- Preclinical
- Lead developer
- Helmholtz-Zentrum Dresden-Rossendorf
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
225Ac-macropa-PSMA is a preclinical targeted alpha therapy (TAT) radiopharmaceutical designed for the treatment of prostate cancer, specifically metastatic castration-resistant prostate cancer (mCRPC). Developed by the Helmholtz-Zentrum Dresden-Rossendorf (HZDR) and Palacky University Olomouc, the agent consists of the alpha-emitting radionuclide actinium-225 (225Ac) complexed with a macropa-derived chelator and conjugated to a prostate-specific membrane antigen (PSMA)-targeting ligand. The macropa chelator enables rapid, high-yield radiolabeling under mild, room-temperature conditions, outperforming traditional DOTA-based chelators by preserving temperature-sensitive biomolecules and maintaining high complex stability. Preclinical evaluations of both monomeric (mcp-M-PSMA) and dimeric (mcp-D-PSMA) variants have demonstrated high binding affinity, rapid whole-body clearance, and significant tumor uptake and retention in PSMA-positive prostate cancer models.
- Other names
- 225Ac-mcp-D-PSMA225Ac-mcp-M-PSMA225Ac-mcp-PSMA[225Ac]Ac-macropa-PSMA[225Ac]Ac-mcp-D-PSMA[225Ac]Ac-mcp-M-PSMAactinium-225-macropa-PSMAactinium225-macropa-PSMAactinium 225-macropa-PSMA
02
Targets
PSMA (Prostate-specific membrane antigen)
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