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[64Cu]Cu-DOTHA2-FAPI-04
- Development stage
- Preclinical
- Lead developer
- Université de Sherbrooke
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Positron Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
[64Cu]Cu-DOTHA2-FAPI-04 is a copper-64 radiolabeled small-molecule fibroblast activation protein (FAP) inhibitor developed by the Université de Sherbrooke. It consists of the FAP-targeting moiety FAPI-04 conjugated to the novel hydroxamate-based bifunctional chelator DOTHA2, which is radiolabeled with the positron emitter copper-64 (64Cu). DOTHA2 provides rapid and highly stable chelation of copper-64 under mild conditions, minimizing in vivo demetallation and off-target accumulation. [64Cu]Cu-DOTHA2-FAPI-04 is designed as a diagnostic PET imaging agent to visualize FAP-expressing tumor stroma and cancer-associated fibroblasts (CAFs) in various solid tumors, including prostate cancer, pancreatic cancer, melanoma, and head and neck cancer, offering a wider imaging time window compared to gallium-68 labeled tracers.
- Other names
- 64Cu-DOTHA2-FAPI[64Cu]Cu-DOTHA2-FAPI
02
Targets
FAP (Fibroblast activation protein alpha)
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