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[225Ac]FR96
- Development stage
- Preclinical
- Lead developer
- Helmholtz-Zentrum Dresden-Rossendorf
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
[225Ac]FR96 is a novel macropa-based prostate-specific membrane antigen (PSMA)-targeting radioligand modified with an albumin-binding moiety. It is labeled with the alpha-emitting radionuclide actinium-225 ([225Ac]) for targeted alpha therapy (TAT) of prostate cancer, specifically metastatic castration-resistant prostate cancer (mCRPC). The incorporation of the albumin-binding moiety is designed to enhance blood retention, prolong circulation half-life, and increase tumor uptake, thereby improving therapeutic efficacy. Preclinical studies in LNCaP tumor-bearing mice have demonstrated high tumor accumulation and significant DNA damage (indicated by gamma-H2AX staining) in tumor tissues with low toxicity in healthy organs such as the kidneys.
- Other names
- [225Ac]-FR96225Ac-FR96
02
Targets
PSMA (Prostate-specific membrane antigen)
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