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[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.
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