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Galectins are carbohydrate-binding proteins overexpressed in bladder cancer (BCa) cells. Dendritic galactose moieties have a high affinity for galectin-expressing tumor cells. We radiolabeled a dendritic galactose carbohydrate with 18 F ( 18 F-labeled galactodendritic unit 4 ) and examined its potential in imaging urothelial malignancies. Methods: The 18 F-labeled first-generation galactodendritic unit 4 was obtained from its tosylate precursor. We conducted in vivo studies in a galectin-expressing UMUC3 orthotopic BCa model to determine the ability of 18 F-labeled galactodendritic unit 4 to image BCa. Results: Intravesical administration of 18 F-labeled galactodendritic unit 4 allowed specific accumulation of the carbohydrate radiotracer in galectin-1-overexpressing UMUC3 orthotopic tumors when imaged with PET. The 18 F-labeled galactodendritic unit 4 was not found to accumulate in nontumor murine bladders. Conclusion: The 18 F-labeled galactodendritic unit 4 and similar analogs may be clinically relevant and exploitable for PET imaging of galectin-1-overexpressing bladder tumors.

PET/CT Imaging with an 18F-Labeled Galactodendritic Unit in a Galectin-1–Overexpressing Orthotopic Bladder Cancer Model

PET/CT Imaging with an ¹⁸F-Labeled Galactodendritic Unit in a Galectin-1–Overexpressing Orthotopic Bladder Cancer Model