Preparation and Biodistribution Assessment of 68Ga-Dkfz-Psma-617 for Pet Prostate Cancer Imaging Publisher



Sharifi M¹ ; Yousefnia H¹ ; Zolghadri S¹ ; Bahramisamani A¹ ; Naderi M² ; Jalilian AR¹ ; Geramifar P³ ; Beiki D³
Source: Nuclear Science and Techniques Published:2016

Abstract

Prostate-specific membrane antigen (PSMA) is a useful target for diagnostic and therapeutic applications, and it is demonstrated that 68Ga in conjugation with DKFZ-PSMA-617 is better than 68Ga-PSMA-1 in biodistribution data after 1 h, but more preclinical data are still required. In this paper, we presented the additional preclinical data for 68Ga-DKFZ-PSMA-617 and relevant aspects of its production. 68Ga was obtained from the SnO2-based 68Ge/68Ga generator. Optimum conditions (pH, temperature, time and ligand concentration) for 68Ga-DKFZ-PSMA-617 preparation were studied. Radiochemical purity of the radiolabeled compound was determined by HPLC and RTLC. After stability assessments, the complex was intravenously injected into rats. HPLC and ITLC characterizations indicated that the radiopharmaceutical could be prepared with radiochemical purity of >96 % and specific activity of 308.3 TBq/mmol at the optimized conditions (pH of 3.5-4, ligand amount of 2.4 nmol, temperature of 90-95 °C and reaction time of 10 min). Also, the biodistribution data showed no undesirable uptake in nontarget organs at any interval after injection. In fact, the activity is cleaned from blood and excreted rapidly via the kidneys. Generally, this compound can be considered as a well-established PET imaging agent. © 2016 Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Chinese Nuclear Society, Science Press China and Springer Science+Business Media Singapore.