Drug intelligence / Profile preview

64Cu-DOTHA2-FAPI

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-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.

Other names
64Cu-labeled DOTHA2-FAPI[64Cu]Cu-DOTHA2-FAPI[64Cu]Cu-DOTHA2-FAPI-04copper-64 DOTHA2-FAPIcopper64 DOTHA2-FAPIcopper 64 DOTHA2-FAPI
02

Targets

FAP (Fibroblast activation protein alpha)

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