Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2016, Vol. 27 ›› Issue (6): 142 doi: 10.1007/s41365-016-0134-2

• NUCLEAR CHEMISTRY,RADIOCHEMISTRY,RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

Preparation and biodistribution assessment of 68Ga-DKFZ-PSMA-617 for PET prostate cancer imaging

Mehdi Sharifi 1, Hassan Yousefnia  1, Samaneh Zolghadri  1, Ali Bahrami-Samani  1, Mojdeh Naderi  2, Amir Reza Jalilian  1, Parham Geramifar  3, Davood Beiki 3   

  1. 1 Nuclear Science and Technology Research Institute (NSTRI), Tehran 14395-836, Iran
    2 Department of Chemistry, University of Zanjan, Zanjan 4537138791, Iran
    3 Research Center for Nuclear Medicine, Shariati Hospital, Tehran University of Medical Sciences, Tehran 1411713135, Iran
  • Contact: Hassan Yousefnia E-mail:hyousefnia@aeoi.org.ir
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Mehdi Sharifi, Hassan Yousefnia, Samaneh Zolghadri, Ali Bahrami-Samani, Mojdeh Naderi, Amir Reza Jalilian, Parham Geramifar, Davood Beiki. Preparation and biodistribution assessment of 68Ga-DKFZ-PSMA-617 for PET prostate cancer imaging.Nuclear Science and Techniques, 2016, 27(6): 142     doi: 10.1007/s41365-016-0134-2
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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.

Key words: 68Ga, PSMA, Biodistribution, Imaging