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Establishing Radiolanthanum Chemistry for Targeted Nuclear Medicine Applications.

We report the first targeted nuclear medicine application of the lanthanum radionuclides  132/135La. These isotopes represent a matched pair for diagnosis via the positron emissions of  132La and therapy mediated by the Auger electron emissions of 135La. We identify two effective chelators, known as DO3Apic and macropa, for these radionuclides. The 18-membered macrocycle, macropa, rapidly binds 132/135La at room temperature with high apparent molar activity, whereas DO3Apic labels with poorer molar activity under similar conditions. These chelators were conjugated to the prostate-specific membrane antigen (PSMA)-targeting agent DUP A to assess the use of radiolanthanum for in vivo imaging. The 132/135La-labeled targeted constructs showed high uptake in tumor xenografts expressing PSMA. This study validates the use of these radioactive lanthanum isotopes for imaging applications and motivates future work to assess the therapeutic effects of the Auger electron emissions of 135La.