Evaluation of Met-Val-Lys as a Renal Brush Border Enzyme-Cleavable Linker to Reduce Kidney Uptake of 68Ga-Labeled DOTA-Conjugated Peptides and Peptidomimetics

Shreya Bendre, Zhengxing Zhang, Hsiou-Ting Kuo, Julie Rousseau, Chengcheng Zhang, Helen Merkens, Áron Roxin, François Bénard & Kuo-Shyan Lin
High kidney uptake is a common feature of peptide-based radiopharmaceuticals, leading to reduced detection sensitivity for lesions adjacent to kidneys and lower maximum tolerated therapeutic dose. In this study, we evaluated if the Met-Val-Lys (MVK) linker could be used to lower kidney uptake of ⁶⁸Ga-labeled DOTA-conjugated peptides and peptidomimetics. A model compound, [⁶⁸Ga]Ga-DOTA-AmBz-MVK(Ac)-OH (AmBz: aminomethylbenzoyl), and its derivative, [⁶⁸Ga]Ga-DOTA-AmBz-MVK(HTK01166)-OH, coupled with the PSMA (prostate-specific membrane antigen)-targeting motif of the previously reported HTK01166 were synthesized and...
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