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[99mTc]Tc-CGGG-rL-A9 is a HER2-targeting radiopharmaceutical designed for the detection and imaging of HER2-positive breast cancer. It consists of the rL-A9 peptide, which binds specifically to the Human Epidermal Growth Factor Receptor 2 (HER2), conjugated to a CGGG (Cysteine-Glycine-Glycine-Glycine) peptide-based chelator that facilitates stable labeling with the radioisotope Technetium-99m (99mTc). In preclinical studies, the radiopeptide demonstrated high binding affinity (Kd: 5.82 ± 0.92 nM) and specificity for HER2-expressing SKBR3 cells, as well as favorable tumor uptake and retention in xenograft models. The incorporation of the CGGG chelator sequence provides superior stability compared to other variants such as CSSG or CEEG, making it a promising candidate for diagnostic imaging of HER2-positive malignancies.
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