Drug intelligence / Profile preview

[68Ga]Ga-DOTA.SA.FAPi

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

Overview

[68Ga]Ga-DOTA.SA.FAPi is a next-generation radiopharmaceutical diagnostic agent designed for positron emission tomography (PET) imaging. It targets Fibroblast Activation Protein (FAP), an enzyme highly overexpressed on the surface of cancer-associated fibroblasts (CAFs) within the tumor stroma of most epithelial cancers. The molecule utilizes a squaric acid (SA) linker, which has been shown to enhance the binding affinity and pharmacokinetic profile of FAP inhibitors compared to earlier versions. By chelating the positron-emitting isotope Gallium-68 via a DOTA moiety, the tracer allows for high-contrast visualization of various malignancies, including breast and lung cancers. It is particularly noted for its low background uptake in the brain and liver, facilitating the detection of metastases in these regions where standard [18F]FDG PET/CT often has limitations.

Other names
68Ga-DOTA-SA-FAPiGallium-68 DOTA-SA-FAPiGallium68 DOTA-SA-FAPiGallium 68 DOTA-SA-FAPi
02

Targets

FAP (Fibroblast activation protein alpha)

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