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64Cu-DOTHA2-FAPI (also referred to as 64Cu-DOTHA2-FAPI-04) is a novel radiolabeled small molecule fibroblast activation protein inhibitor (FAPI) developed for positron emission tomography (PET) imaging. It consists of the FAP-targeting ligand DOTHA2-FAPI (derived from the FAPI-04 scaffold) chelated with the positron-emitting radioisotope copper-64 (64Cu). The tracer specifically binds to fibroblast activation protein alpha (FAP), which is highly overexpressed on cancer-associated fibroblasts (CAFs) in the tumor stroma of various solid tumors, including head and neck squamous cell carcinoma (HNSCC), prostate cancer, and melanoma. Developed by researchers at the Université de Sherbrooke and the Centre d'Imagerie Moléculaire de Sherbrooke (CIMS), 64Cu-DOTHA2-FAPI is utilized in preclinical research to visualize tumor stroma, evaluate tumor heterogeneity, and monitor therapeutic responses to immunotherapies such as nivolumab.
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