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68Ga-AMTG (also known as [68Ga]Ga-AMTG) is a gallium-68 labeled gastrin-releasing peptide receptor (GRPR) antagonist developed for positron emission tomography (PET) imaging of GRPR-expressing malignancies, such as prostate cancer and breast cancer. It is a structurally modified derivative of the GRPR antagonist RM2, where the metabolically unstable L-tryptophan at position 8 is substituted with α-methyl-L-tryptophan (α-Me-L-Trp8). This modification significantly enhances the peptide's resistance to enzymatic degradation in vivo, resulting in improved metabolic stability and higher tumor-to-background ratios compared to its parent compound. 68Ga-AMTG is utilized as a diagnostic imaging agent in theranostic applications, often paired with therapeutic counterparts like 177Lu-AMTG or 161Tb-AMTG.
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