Drug intelligence / Profile preview

gallium Ga 68 fapi

Development stage
Unknown
Lead developer
Heidelberg University Hospital
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Gallium-68-labeled FAPI (Fibroblast Activation Protein Inhibitor) is a diagnostic radiopharmaceutical used in positron emission tomography (PET) imaging. It targets fibroblast activation protein alpha (FAP), a cell-surface glycoprotein that is highly expressed on cancer-associated fibroblasts (CAFs) within the tumor stroma of various solid malignancies. Unlike conventional metabolic imaging with 18F-FDG, which measures glucose metabolism, FAPI-PET visualizes the tumor microenvironment at the stromal level. This approach offers high tumor-to-background contrast due to low physiological uptake in most normal tissues, making it particularly sensitive for detecting tumors with high stromal content or low metabolic activity, such as pancreatic, gastric, and breast cancers. Several variants of the ligand exist, including FAPI-04, FAPI-46, and FAPI-74, which are typically small-molecule quinoline derivatives labeled with the positron-emitting isotope gallium-68.

Other names
gallium-68-labeled fibroblast activation protein inhibitorgallium68-labeled fibroblast activation protein inhibitorgallium 68-labeled fibroblast activation protein inhibitor[68Ga]Ga-FAPIgallium-68-labeled FAPIgallium68-labeled FAPIgallium 68-labeled FAPI
02

Targets

FAP (Fibroblast activation protein alpha)

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