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Open AccessArticle

Development of a Single Vial Kit Solution for Radiolabeling of 68Ga-DKFZ-PSMA-11 and Its Performance in Prostate Cancer Patients

University of Pretoria & Steve Biko Academic Hospital, Crn Malherbe and Steve Biko Rd, Pretoria 0001, South Africa
School of Health Sciences, Catalysis and Peptide Research Unit, E-Block 6th Floor, Westville Campus, University Road, Westville, Durban 3630, South Africa
The South African Nuclear Energy Corporation (Necsa), Building P1600, Radiochemistry, Pelindaba, Brits 0240, South Africa
Department of Science and Technology, Preclinical Drug Development Platform, North West University, 11 Hoffman St, Potchefstroom 2520, South Africa
Author to whom correspondence should be addressed.
Academic Editor: Svend Borup Jensen
Molecules 2015, 20(8), 14860-14878;
Received: 31 May 2015 / Revised: 31 July 2015 / Accepted: 3 August 2015 / Published: 14 August 2015
(This article belongs to the Special Issue Preparation of Radiopharmaceuticals and Their Use in Drug Development)
Prostate-specific membrane antigen (PSMA), a type II glycoprotein, is highly expressed in almost all prostate cancers. By playing such a universal role in the disease, PSMA provides a target for diagnostic imaging of prostate cancer using positron emission tomography/computed tomography (PET/CT). The PSMA-targeting ligand Glu-NH-CO-NH-Lys-(Ahx)-HBED-CC (DKFZ-PSMA-11) has superior imaging properties and allows for highly-specific complexation of the generator-based radioisotope Gallium-68 (68Ga). However, only module-based radiolabeling procedures are currently available. This study intended to develop a single vial kit solution to radiolabel buffered DKFZ-PSMA-11 with 68Ga. A 68Ge/68Ga-generator was utilized to yield 68GaCl3 and major aspects of the kit development were assessed, such as radiolabeling performance, quality assurance, and stability. The final product was injected into patients with prostate cancer for PET/CT imaging and the kit performance was evaluated on the basis of the expected biodistribution, lesion detection, and dose optimization. Kits containing 5 nmol DKFZ-PSMA-11 showed rapid, quantitative 68Ga-complexation and all quality measurements met the release criteria for human application. The increased precursor content did not compromise the ability of 68Ga-DKFZ-PSMA-11 PET/CT to detect primary prostate cancer and its advanced lymphatic- and metastatic lesions. The 68Ga-DKFZ-PSMA-11 kit is a robust, ready-to-use diagnostic agent in prostate cancer with high diagnostic performance. View Full-Text
Keywords: PSMA; prostate cancer; PET/CT; 68Ga-HBED-CC-(Ahx)Lys-NH-CO-NH-Glu; 68Ga-DKFZ-PSMA-11; 68Ga-PSMAHBED PSMA; prostate cancer; PET/CT; 68Ga-HBED-CC-(Ahx)Lys-NH-CO-NH-Glu; 68Ga-DKFZ-PSMA-11; 68Ga-PSMAHBED
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Ebenhan, T.; Vorster, M.; Marjanovic-Painter, B.; Wagener, J.; Suthiram, J.; Modiselle, M.; Mokaleng, B.; Zeevaart, J.R.; Sathekge, M. Development of a Single Vial Kit Solution for Radiolabeling of 68Ga-DKFZ-PSMA-11 and Its Performance in Prostate Cancer Patients. Molecules 2015, 20, 14860-14878.

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