Synthesis, radiolabelling and in vitro characterization of the gallium-68-, yttrium-90- and lutetium-177-labelled PSMA Ligand, CHX-A"-DTPA-DUPA-Pep

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Abstract

Since prostate-specific membrane antigen (PSMA) has been identified as a diagnostic target for prostate cancer, many urea-based small PSMA-targeting molecules were developed. First, the clinical application of these Ga-68 labelled compounds in positron emission tomography (PET) showed their diagnostic potential. Besides, the therapy of prostate cancer is a demanding field, and the use of radiometals with PSMA bearing ligands is a valid approach. In this work, we describe the synthesis of a new PSMA ligand, CHX-A"-DTPA-DUPA-Pep, the subsequent labelling with Ga-68, Lu-177 and Y-90 and the first in vitro characterization. In cell investigations with PSMA-positive LNCaP C4-2 cells, KD values of ≤14.67 ± 1.95 nM were determined, indicating high biological activities towards PSMA. Radiosyntheses with Ga-68, Lu-177 and Y-90 were developed under mild reaction conditions (room temperature, moderate pH of 5.5 and 7.4, respectively) and resulted in nearly quantitative radiochemical yields within 5 min. © 2014 by the authors; licensee MDPI, Basel, Switzerland.

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Baur, B., Solbach, C., Andreolli, E., Winter, G., Machulla, H. J., & Reske, S. N. (2014). Synthesis, radiolabelling and in vitro characterization of the gallium-68-, yttrium-90- and lutetium-177-labelled PSMA Ligand, CHX-A"-DTPA-DUPA-Pep. Pharmaceuticals, 7(5), 517–529. https://doi.org/10.3390/ph7050517

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