[68Ga]Ga-DO2A-(OBu-l-tyr)2: Synthesis, 68Ga-radiolabeling and in vitro studies of a novel 68Ga-DO2A-tyrosine conjugate as potential tumor tracer for PET

The synthesis, 68Ga-labeling and in vitro study of the novel tyrosine chelate derivative [68Ga]Ga-1,4,7,10-tetraazacyclododecane-1,7-diacetic acid-4,10-di-(O-butyl)-l-tyrosine ([68Ga]Ga-DO2A-(OBu-l-tyr)2) as a potential tracer for imaging tumor metabolism by positron emission tomography (PET) is presented. This approach combines the biological amino acid transporter targeting properties of l-tyrosine with the outstanding availability of 68GaIII via the 68Ge/68Ga generator. In vitro studies utilizing the F98-glioblastoma cell line revealed specific uptake of [68Ga]Ga-DO2A-(OBu-l-tyr)2 that was comparable to that of the reference O-(2-[18F]fluoroethyl)-l-tyrosine (FET). These promising results indicate a high potential of [68Ga]Ga-DO2A-(OBu-l-tyr)2 for molecular imaging of tumor-driven amino acid uptake by PET.

Graphical abstractThe novel 68Ga-DO2A-tyrosine derivative 10 shows specific uptake in F98-glioblastoma cells indicating high potential for imaging tumor metabolism by positron emission tomography (PET).Figure optionsDownload full-size imageDownload as PowerPoint slide