Drug intelligence / Profile preview

68Ga-TCR-FAPI

Development stage
Unknown
Lead developer
Peking Union Medical College Hospital
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

68Ga-TCR-FAPI is a targeted covalent radiopharmaceutical (TCR) designed for Positron Emission Tomography (PET) imaging. It consists of the positron-emitting radioisotope gallium-68 conjugated to a ligand that targets Fibroblast Activation Protein (FAP), an enzyme highly expressed on cancer-associated fibroblasts within the tumor stroma of various solid tumors. Unlike conventional FAPI tracers that bind reversibly, TCR-FAPI is engineered to form a covalent bond with the FAP protein. This covalent mechanism significantly increases tumor uptake and prolongs retention of the tracer within the tumor microenvironment, leading to improved image contrast and diagnostic sensitivity. It is currently being evaluated for its ability to guide surgical precision in medullary thyroid carcinoma (MTC) and for the detection of various other malignant tumors.

Other names
68Ga-labeled targeted covalent radiopharmaceutical fibroblast activation protein inhibitorGa-68 TCR-FAPIGa68 TCR-FAPIGa 68 TCR-FAPI
02

Targets

FAP (Fibroblast activation protein alpha)

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