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

Molecules

Thomas Ebenhan²  Mariza Vorster²  Biljana Marjanovic-Painter³  Judith Wagener³  Janine Suthiram²  Moshe Modiselle²  Brenda Mokaleng²  Jan Rijn Zeevaart¹  Mike Sathekge² 

[1] Department of Science and Technology, Preclinical Drug Development Platform, North West University, 11 Hoffman St, Potchefstroom 2520, South Africa; E-Mail:;University of Pretoria & Steve Biko Academic Hospital, Crn Malherbe and Steve Biko Rd, Pretoria 0001, South Africa; E-Mails:;The South African Nuclear Energy Corporation (Necsa), Building P1600, Radiochemistry, Pelindaba, Brits 0240, South Africa; E-Mails:

关键词: PSMA;    prostate cancer;    PET/CT;    ⁶⁸Ga-HBED-CC-(Ahx)Lys-NH-CO-NH-Glu;    ⁶⁸Ga-DKFZ-PSMA-11;    ⁶⁸Ga-PSMA^HBED;   

DOI  :  10.3390/molecules200814860

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.