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177Lu-AF03
- Development stage
- Phase 1
- Lead developer
- Yong He
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
177Lu-AF03 is a bispecific heterodimeric peptide radiolabeled with Lutetium-177 (177Lu) that simultaneously targets fibroblast activation protein (FAP) and integrin αvβ6. FAP is highly expressed on cancer-associated fibroblasts in the tumor stroma, while integrin αvβ6 is upregulated on the surface of various epithelial tumor cells. By concurrently binding to both targets, 177Lu-AF03 aims to overcome tumor heterogeneity and enhance tumor uptake and retention while minimizing off-target accumulation. Developed by Zhongnan Hospital of Wuhan University, the radiopharmaceutical is being evaluated in early-phase clinical trials for safety, biodistribution, radiation dosimetry, and preliminary diagnostic efficacy via SPECT/CT imaging in patients with malignant solid tumors.
- Other names
- 177Lu-labeled AF03Lutetium (177Lu) AF03Lutetium-177 AF03Lutetium177 AF03Lutetium 177 AF03
02
Targets
FAP (Fibroblast activation protein alpha)αVβ6 (Integrin αVβ6)
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