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      Study on the Solution for the Reduced [68Ga]Ga-PSMA-11 Synthesis Yield

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      https://www.riss.kr/link?id=A109907474

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      다국어 초록 (Multilingual Abstract) kakao i 다국어 번역

      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.
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      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-...

      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.

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      참고문헌 (Reference)

      1 Hennrich U, "[68Ga]Ga-PSMA-11 : The first FDAapproved 68Ga-radiopharmaceutical for PET imaging of prostate cancer" 14 (14): 713-, 2021

      2 Hennrich U, "[68Ga]Ga-DOTA-TOC : The first FDA-Approved 68Ga-radiopharmaceutical for PET imaging" 13 (13): 38-, 2020

      3 Kumar K, "Total chemical synthesis of PSMA-11 : API for 68Ga-PSMA-11 used for prostate cancer diagnosis" 3 : 100014-, 2021

      4 Shahrokhi P, "The utility of radiolabeled PSMA ligands for tumor imaging" 99 (99): 136-161, 2022

      5 Cusnir R, "The effects of trace metal impurities on Ga-68-radiolabelling with a tris(3-hydroxy-1, 6-dimethylpyridin-4-one)(THP)chelator" 9 (9): 37214-37221, 2019

      6 Kumar K, "The current status of the production and supply of gallium-68" 35 (35): 163-166, 2020

      7 Kim GG, "Study on synthesis of 68GeO2 and behavior of 68Ga3+ for generator column" 10 (10): 189-192, 2016

      8 Padhani AR, "Rationale for Modernising Imaging in Advanced Prostate Cancer" 3 (3): 223-239, 2017

      9 Kahn D, "Radioimmunoscintigraphy with 111Indium labeled CYT-356 for the detection of occult prostate cancer recurrence" 152 : 1490-1495, 1994

      10 Tateishi U, "Prostate-specific membrane antigen(PSMA)-ligand positron emission tomography and radioligand therapy(RLT)of prostate cancer" 50 (50): 349-356, 2020

      1 Hennrich U, "[68Ga]Ga-PSMA-11 : The first FDAapproved 68Ga-radiopharmaceutical for PET imaging of prostate cancer" 14 (14): 713-, 2021

      2 Hennrich U, "[68Ga]Ga-DOTA-TOC : The first FDA-Approved 68Ga-radiopharmaceutical for PET imaging" 13 (13): 38-, 2020

      3 Kumar K, "Total chemical synthesis of PSMA-11 : API for 68Ga-PSMA-11 used for prostate cancer diagnosis" 3 : 100014-, 2021

      4 Shahrokhi P, "The utility of radiolabeled PSMA ligands for tumor imaging" 99 (99): 136-161, 2022

      5 Cusnir R, "The effects of trace metal impurities on Ga-68-radiolabelling with a tris(3-hydroxy-1, 6-dimethylpyridin-4-one)(THP)chelator" 9 (9): 37214-37221, 2019

      6 Kumar K, "The current status of the production and supply of gallium-68" 35 (35): 163-166, 2020

      7 Kim GG, "Study on synthesis of 68GeO2 and behavior of 68Ga3+ for generator column" 10 (10): 189-192, 2016

      8 Padhani AR, "Rationale for Modernising Imaging in Advanced Prostate Cancer" 3 (3): 223-239, 2017

      9 Kahn D, "Radioimmunoscintigraphy with 111Indium labeled CYT-356 for the detection of occult prostate cancer recurrence" 152 : 1490-1495, 1994

      10 Tateishi U, "Prostate-specific membrane antigen(PSMA)-ligand positron emission tomography and radioligand therapy(RLT)of prostate cancer" 50 (50): 349-356, 2020

      11 Hofman MS, "Prostate-specific membrane antigen PET-CT in patients with high-risk prostate cancer before curativeintent surgery or radiotherapy(proPSMA) : a prospective, randomised, multicentre study" 395 : 1208-1216, 2020

      12 Lawhn-Heath C, "Prostate-specific membrane antigen PET in prostate cancer" 299 (299): 248-260, 2021

      13 Barrio M, "Prostate specific membrane antigen(PSMA)ligands for diagnosis and therapy of prostate cancer" 16 (16): 1177-1188, 2016

      14 Debnath S, "PSMA-targeting imaging and theranostic agents-current status and future perspective" 23 (23): 1158-, 2022

      15 Adnan A, "PSMA Receptor-based PET-CT : The basics and current status in clinical and research applications" 13 (13): 158-, 2023

      16 Ghafoor S, "Multimodality imaging of prostate cancer" 60 (60): 1350-1358, 2019

      17 Liu H, "Monoclonal antibodies to the extracellular domain of prostate-specific membrane antigen also react with tumor vascular endothelium" 57 : 3629-3634, 1997

      18 Horoszewicz JS, "Monoclonal antibodies to a new antigenic marker in epithelial prostatic cells and serum of prostatic cancer patients" 7 : 927-935, 1987

      19 Roesch F, "Maturat ion of a key resource-the germanium-68/gallium-68 generator : development and new insights" 5 (5): 202-211, 2012

      20 Oehlke E, "Influence of metal ions on the ⁶⁸Galabeling of DOTATATE" 82 : 232-238, 2013

      21 Zhang X, "High-Yielding Radiosynthesis of [68Ga]Ga-PSMA-11 using a low-cost microfluidic device" 22 (22): 1370-1379, 2020

      22 Kopka K, "Glu-Ureido-based inhibitors of prostate-specific membrane antigen : lessons learned during the development of a novel class of low-molecular-weight. Theranostic Radiotracers" 58 (58): 17S-26S, 2017

      23 Lin M, "Fully automated preparation of 68Ga-PSMA-11 at curie level quantity using cyclotron-produced 68Ga for clinical applications" 155 : 108936-, 2020

      24 Yoo KH, "Early prostate cancer in old-aged patients" 8 (8): 97-101, 2010

      25 Park JY, "Development of an automated synthesizer for the routine production of Ga-68 radiopharmaceuticals" 55 (55): 253-260, 2023

      26 Choi Kim WT, "Current update in basic research in Korea : prostate cancer" 11 (11): 63-70, 2013

      27 Sudbrock F, "Characterization of SnO2-based 68Ge/68Ga generators and 68Ga-DOTATATE preparations : radionuclide purity, radiochemical yield and long-term constancy" 4 (4): 36-, 2014

      28 Kang MJ, "Cancer statistics in Korea : incidence, mortality, survival, and prevalence in 2019" 54 : 330-344, 2022

      29 Wichmann CW, "Automated radiosynthesis of [68Ga]Ga-PSMA-11 and [177Lu]Lu-PSMA-617 on the iPHASE MultiSyn module for clinical applications" 64 (64): 140-146, 2021

      30 Hong JH, "An update of prostate-specific membrane antigen theranostics in prostate cancer" 20 (20): 207-222, 2022

      31 Capasso G, "A systematic review on the current status of PSMA-targeted imaging and radioligand therapy" 263 : 115966-, 2024

      32 Ha YS, "A survey on the quality of life of prostate cancer patients in Korean prostate cancer patients association" 20 (20): 265-272, 2022

      33 Gleason GI, "A positron cow" 8 : 90-94, 1960

      34 Loc'h C, "A new generator for ionic gallium-68" 21 (21): 171-173, 1980

      35 Shetty D, "68Ga-labeled radiopharmaceuticals for positron emission tomography" 44 : 233-240, 2010

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