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actinium-225 PSMA-617
- Development stage
- Phase 3
- Lead developer
- Novartis
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Actinium-225-PSMA-617 is an investigational radiopharmaceutical designed for targeted alpha therapy (TAT) in patients with prostate cancer. It consists of the alpha-emitting radionuclide actinium-225 conjugated to the small-molecule ligand PSMA-617. The ligand binds with high affinity to Prostate-Specific Membrane Antigen (PSMA), a protein significantly overexpressed on the surface of prostate cancer cells. Upon binding and subsequent cellular internalization, the actinium-225 isotope undergoes decay, releasing high-energy alpha particles with a short path length. These particles induce lethal double-strand DNA breaks within the cancer cell, maximizing tumor cell killing while minimizing radiation exposure to adjacent healthy tissues. Initially developed by the German Cancer Research Center (DKFZ) and University Hospital Heidelberg, the therapy is currently being advanced by Novartis, primarily for metastatic castration-resistant prostate cancer (mCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC).
- Brand names
- None (investigational)
- Other names
- Actinium (225Ac) vipivotide tetraxetanActinium-225 PSMA-617Actinium225 PSMA-617Actinium 225 PSMA-617
02
Targets
PSMA (Prostate-specific membrane antigen)DNA
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