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Pharmaceuticals 2014, 7(5), 517-529; https://doi.org/10.3390/ph7050517

Synthesis, Radiolabelling and In Vitro Characterization of the Gallium-68-, Yttrium-90- and Lutetium-177-Labelled PSMA Ligand, CHX-A''-DTPA-DUPA-Pep

1
Clinic for Nuclear Medicine, University of Ulm, Albert-Einstein-Allee, 89081 Ulm, Germany
2
Department of Health Sciences, University of Milano-Bicocca, Milan 20900, Italy
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 16 December 2013 / Revised: 27 March 2014 / Accepted: 14 April 2014 / Published: 29 April 2014
(This article belongs to the Special Issue Radiopharmaceutical Chemistry between Imaging and Radioendotherapy)
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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. View Full-Text
Keywords: PSMA; prostate-specific membrane antigen; PET; positron emission tomography; prostate cancer; DUPA; Ga-68; Y-90; Lu-177; radionuclide therapy PSMA; prostate-specific membrane antigen; PET; positron emission tomography; prostate cancer; DUPA; Ga-68; Y-90; Lu-177; radionuclide therapy
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Baur, B.; Solbach, C.; Andreolli, E.; Winter, G.; Machulla, H.-J.; Reske, S.N. Synthesis, Radiolabelling and In Vitro Characterization of the Gallium-68-, Yttrium-90- and Lutetium-177-Labelled PSMA Ligand, CHX-A''-DTPA-DUPA-Pep. Pharmaceuticals 2014, 7, 517-529.

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