• Journal of Radiopharmaceuticals and Molecular Probes
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• v.10 no.1
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• pp.3-11
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• 2024

[⁶⁸Ga]Ga-PSMA-11 is a prostate-specific membrane antigen (PSMA)-targeting radiopharmaceutical based on lysine-urea-glutamic acid derivatives. This study aimed to identify the cause of the irregular decrease in the radiosynthesis yield of [⁶⁸Ga]Ga-PSMA-11 and to suggest a solution. An irregular decrease in production yield occurred during the synthesis of [⁶⁸Ga]Ga-PSMA-11 using a cassette-based automatic synthesizer. Although the reagents used in synthesizing [⁶⁸Ga]Ga-PSMA-11 were replaced with new products, the irregular decrease in radiosynthesis yield continued. In addition, cassettes, equipment, and operating programs used in the cassette-based automatic synthesizer operated normally. On the other hand, when eluting with 0.6 N hydrochloric acid(HCl), leakage was found at the outlet line connection site of the ⁶⁸Ge/⁶⁸Ga generator. The ⁶⁸Ge/⁶⁸Ga generator was eluted with 0.6 N HCl two to four hours before synthesis to remove impurities and improve the synthetic yield reduction. No further irregular yield reduction occurred after using this method. In the event of an irregular decrease in the radiolabeling yield, the pretreatment method developed in this study would help produce [⁶⁸Ga]Ga-PSMA-11 injections with a stable labeling yield.

• Korean Journal of Clinical Laboratory Science
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• v.56 no.2
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• pp.147-155
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• 2024

Gallium-68-prostate-specific membrane antigen-11 (⁶⁸Ga-PSMA-11) is a positron emission tomography radiopharmaceutical that labels a Glu-urea-Lys-based ligand with ⁶⁸Ga, binding specifically to the PSMA. It is used widely for imaging recurrent prostate cancer and metastases. On the other hand, the preparation and quality control testing of ⁶⁸Ga-PSMA-11 in medical institutions takes over 60 minutes, limiting the daily capacity of ⁶⁸Ge/⁶⁸Ga generators. While the generator provides 1,110 MBq (30 mCi) nominally, its activity decreases over time, and the labeling yield declines irregularly. Consequently, additional preparations are needed, increasing radiation exposure for medical technicians, prolonging patient wait times, and necessitating production schedule adjustments. This study aimed to reduce the ⁶⁸Ga-PSMA-11 preparation time and optimize the automated synthesis system. By shortening the reaction time between ⁶⁸Ga and the PSMA-11 precursor and adjusting the number of purification steps, a faster and more cost-effective method was tested while maintaining quality. The final synthesis time was reduced from 30 to 20 minutes, meeting the standards for the HEPES content, residual solvent EtOH content, and radiochemical purity. This optimized procedure minimizes radiation exposure for medical technicians, reduces patient wait times, and maintains consistent production schedules, making it suitable for clinical application.

• The Korean Journal of Nuclear Medicine Technology
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• v.26 no.2
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• pp.15-19
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• 2022

Purpose [⁶⁸Ga]PSMA-11 is needed the high reproducibility, excellent radiochemical yield and purity. In term of radiation safety, the radiation exposure of operator for its production also should be considered. In this work, we performed a comparative study for the fully automated synthesis of [⁶⁸Ga]PSMA-11 between non-cassette type and cassette type. Materials and Methods Two different type of modules (TRACERlab FX N pro for non-cassette type and BIKBox for cassette type) were used for the automated production of [⁶⁸Ga]PSMA-11. According to the previously identified elution profile, Only 2.5 ml with high radioactivity was used for the reaction. After adjusting the pH of the reaction solution with HEPES buffer solution, the precursor was added and reacted with at 95 ℃ for 15 minutes. The reaction mixture was separated and purified using a C18 light cartridge. The product was eluted with 50% EtOH/saline solution and diluted with saline. It was completed by sterilizing filter. In the non-cassette type, the aforementioned process must be prepared directly. However, in the cassette method, synthesis was possible simply by installing a kit that was already completed. Results Both total [⁶⁸Ga]PSMA-11 production time were 25±3(non-cassette type) and 23±3 minutes(cassette type). The radiochemical yield of the non-cassette type(65.5±5.7%) was higher than that of the cassette type(61.6±4.8%) after sterilization filter. The non-cassette type took about 120 minutes of preparation time before synthesis due to washing of synthesizer and reagent preparation. However, since the cassette type does not require washing and reagent preparation, it took about 20 minutes to prepare before synthesis. Both type of synthesizer had a radiochemical high purity(>99%). Conclusion The non-cassette type production of [⁶⁸Ga]PSMA-11 showed higher radiochemical yield and lower cost than the cassette type. However, The cassette type has an advantage in terms of preparation time, convenience, and equipment maintenance.

• Korean Journal of Radiology
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• v.23 no.3
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• pp.293-294
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• 2022

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.9 no.1
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• pp.23-33
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• 2023

Prostate cancer ranks as the world's second most frequently diagnosed cancer among men, and is responsible for the fifth highest number of cancer-related deaths in this population. The development of effective diagnostic and therapeutic approaches for prostate cancer remains a major challenge in the field of oncology. Over the past few years, the prostate-specific membrane antigen (PSMA) has raised as a hopeful tracer for the diagnosis and treatment of prostate cancer.Various radioisotopes, such as ¹³¹I, ^99mTc, ⁶⁸Ga, and ¹⁷⁷Lu, have been used to label PSMA analogues, with varying degrees of success. Among these, ⁶⁸Ga-PSMA-11 and ¹⁷⁷Lu-PSMA-617 have emerged as the most promising radioligands for clinical use. Recently, researchers have been exploring the use of other radioisotopes, such as ²¹¹At, ⁸⁹Zr, ^64/67Cu, and ^203/212Pb, for the labeling of PSMA-targeted radioligands. These radioisotopes have unique properties that may offer advantages over existing radioligands, such as longer half-lives, higher specific activities, and different emission profiles. Efforts are currently underway to develop these radiopharmaceuticals and make them more widely available for clinical use. These exciting developments highlight the potential of PSMA-targeted radioligands for the diagnosis and treatment of prostate cancer, and provided significant implications for the management of this disease in the future. The current study aims to provide a comprehensive summary of the latest research and clinical applications of radiolabeled PSMA inhibitors for diagnoses and therapy of prostate cancer, emphasizing the exciting developments in the field and their potential impact on clinical practice.