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Evaluation of [18F]AlF-ND-GUL for Imaging Prostate Cancer

  • Hye Yeon Seo (Department of Biomedical Sciences, Seoul National University Graduate School) ;
  • Nadeem Ahmed Lodhi (Isotope Production Division Pakistan Institute of Nuclear Science & Technology (PINSTECH)) ;
  • Jung Woo Byun (Department of Biomedical Sciences, Seoul National University Graduate School) ;
  • Ran Ji Yoo (Department of Nuclear Medicine, Seoul National University Hospital) ;
  • Jae Min Jeong (CellBion Co., Ltd) ;
  • Yun-Sang Lee (Department of Nuclear Medicine, Seoul National University Hospital)
  • 투고 : 2024.06.20
  • 심사 : 2024.06.28
  • 발행 : 2024.06.30

초록

Prostate cancer (PCa) is the second most frequent cancer. Prostate specific membrane antigen (PSMA) is an effective target for the detection, staging and monitor the response of therapy in the management of PCa. In this study, we aimed to develop a 18F-labeled PSMA-PET tracer ([18F]AlF-ND-GUL) and test its feasibility for targeting PCa. A variety of labeling conditions was tested for optimization to achieve maximum radiolabeling efficiency. To test the imaging capacity of [18F]AlF-ND-GUL, in vivo PET/MR images were performed in 22Rv1 tumor bearing BALB/c nude mice after injection of radiotracer. Optimized labeling condition was to dissolve 300 nmol of precursor (ND-GUL) in buffer (pH 4, 0.1 M, NaOAc-HOAc) and react with [18F]AlF at 110℃ for 30 min. The [18F]AlF-ND-GUL maintained stability of >85% over 4 h. In-vivo molecular PET/MR imaging study results clearly showed high tumor uptake of [18F]AlF-ND-GUL over time. In conclusion, we optimized [18F]AlF-ND-GUL labeling conditions for PCa diagnosis and confirmed PSMA specific binding in vivo.

키워드

과제정보

이 성과는 정부(과학기술정보통신부)의 재원으로 한국연구재단의 지원을 받아 수행된 연구임(No. 2021R1C1C2004706).

참고문헌

  1. Wang L, Lu B, He MJ, Wang YQ, Wang ZP, Du LB. Prostate Cancer Incidence and Mortality: Global Status and Temporal Trends in 89 Countries From 2000 to 2019. Front Public Health 2022;10: 811044.
  2. Mohseninia N, Zamani-Siahkali N, Harsini S, Divband G, Pirich C, Beheshti M. Bone Metastasis in Prostate Cancer: Bone Scan Versus PET Imaging. Semin Nucl Med 2024;54(1):97-118.
  3. Maurer T, Eiber M, Schwaiger M, Gschwend JE. Current use of PSMA - PET in prostate cancer management. Nat Rev Urol 2016;13(4):226-35.
  4. Zhang ZC, Tian AM, Che JZ, Miao YD, Liu YY, Liu YY, Xu YK. Application and optimization of prostate-specific antigen screening strategy in the diagnosis of prostate cancer: a systematic review. Front Oncol 2024;13:1320681.
  5. Lin K, Lipsitz R, Miller T, Janakiraman S. Benefits and harms of Prostate-Specific Antigen Screening for Prostate Cancer: An Evidence Update for the U.S. Preventive Services Task Force. Ann Intern Med 2008;149(3):192-9.
  6. Santoni M, Scarpelli M, Mazzucchelli R, Lopez-Beltran A, Cheng L, Cascinu S, Montironi R. Targeting Prostate-Specific Membrane Antigen for Personalized Therapies in Prostate Cancer: Morphologic and Molecular Backgrounds and Future Promises. J Biol Reg Homeos Ag 2014;28(4):555-63.
  7. Garnuszek P, Karczmarczyk U, Maurin M, Sikora A, Zaborniak J, Pijarowska-Kruszyna J, Jaron A, Wyczolkowska M, Wojdowska W, Pawlak D, Lipinski P, Mikolajczak R. PSMA-D4 Radioligand for Targeted Therapy of Prostate Cancer: Synthesis, Characteristics and Preliminary Assessment of Biological Properties. Int J Mol Sci 2021;22(5):2731.
  8. Xu XP, Zhang JP, Hu SL, He SM, Bao X, Ma G, Luo J, Cheng J, Zhang Y. 99mTc-labeling and evaluation of a HYNIC modified small-molecular inhibitor of prostate-specific membrane antigen. Nucl Med Biol 2017;48:69-75.
  9. Hillier SM, Maresca KP, Lu GL, Merkin RD, Marquis JC, Zimmerman CN, Eckelman WC, Joyal JL, Babich JW. 99mTc-Labeled Small-Molecule Inhibitors of Prostate-Specific Membrane Antigen for Molecular Imaging of Prostate Cancer. J Nucl Med 2013;54(8):1369-76.
  10. Wang GC, Zhou MJ, Zang J, Jiang YY, Chen XH, Zhu ZH, Chen XY. A pilot study of 68Ga-PSMA-617 PET/CT imaging and 177Lu-EB-PSMA-617 radioligand therapy in patients with adenoid cystic carcinoma. Ejnmmi Res 2022;12(1):52.
  11. Peters SMB, Hofferber R, Prive BM, de Bakker M, Gotthardt M, Janssen M, Lange F, Muselaers CHJ, Mehra N, Witjes JA, Costa PF, Nagarajah J, Konijnenberg MW, Jentzen W. [68Ga]Ga-PSMA-11 PET imaging as a predictor for absorbed doses in organs at risk and small lesions in[177Lu]Lu-PSMA-617 treatment. Eur J Nucl Med Mol Imaging 2022;49(4):1101-12.
  12. Jussing E, Milton S, Samen E, Moein MM, Bylund L, Axelsson R, Siikanen J, Tran TA. Clinically Applicable Cyclotron-Produced Gallium-68 Gives High-Yield Radiolabeling of DOTA-Based Tracers. Biomolecules 2021;11(8):1118.
  13. Pandey MK, Byrne JF, Jiang H, Packard AB, DeGrado TR. Cyclotron production of 68Ga via the 68Zn(p,n)68Ga reaction in aqueous solution. Am J Nucl Med Mol Imaging 2014;4(4):303-10.
  14. Lawal IO, Ankrah AO, Mokgoro NP, Vorster M, Maes A, Sathekge MM. Diagnostic sensitivity of Tc-99m HYNIC PSMA SPECT/CT in prostate carcinoma: A comparative analysis with Ga-68 PSMA PET/CT. Prostate 2017;77(11):1205-12.
  15. Kim SB, Song IH, Kim SY, Ko HY, Kil HS, Chi DY, Giesel FL, Kopka K, Hoepping A, Chun JH, Park HS, Yun MJ, Kim SE. Preclinical Evaluation of a Companion Diagnostic Radiopharmaceutical, [18F]PSMA-1007, in a Subcutaneous Prostate Cancer Xenograft Mouse Model. Mol Pharm 2023;20(2):1050-60.
  16. Zlatopolskiy BD, Endepols H, Krapf P, Guliyev M, Urusova EA, Richarz R, Hohberg M, M Dietlein, Drzezga A, Neumaier B. Discovery of 18F-JK-PSMA-7, a PET Probe for the Detection of Small PSMA-Positive Lesions. J Nucl Med 2019;60(6):817-23.
  17. Werner RA, Derlin T, Lapa C, Sheikbahaei S, Higuchi T, Giesel FL, Behr S, Drzezga A, H Kimura, Buck AK, Bengel FM, Pompe MG, Gorin MA, Rowe SP. 18F-Labeled, PSMA-Targeted Radiotracers: Leveraging the Advantages of Radiofluorination for Prostate Cancer Molecular Imaging. Theranostics 2020;10(1):1-16.
  18. McBride WJ, D'Souza CA, Sharkey RM, Karacay H, Rossi EA, Chang CH, Goldenberg DM. Improved 18F labeling of peptides with a fluoride-aluminum-chelate complex. Bioconjug Chem 2010;21(7):1331-40.
  19. McBride WJ, Sharkey RM, Karacay H, D'Souza CA, Rossi EA, Laverman P, Chang CH, Boerman OC, Goldenberg DM. A novel method of 18F radiolabeling for PET. J Nucl Med 2009;50(6):991-8.
  20. Archibald SJ, Allott L. The aluminium-[18F]fluoride revolution: simple radiochemistry with a big impact for radiolabelled biomolecules. Ejnmmi Radiopharm Chem 2021;6(1):30.
  21. Li L, Zhao W, Sun XR, Liu N, Zhou Y, Luan XH, Gao S, Zhao S, Yu J, Yuan S. 18F-RGD PET/CT imaging reveals characteristics of angiogenesis in non-small cell lung cancer. Transl Lung Cancer Res 2020;9(4):1324-32.
  22. Pauwels E, Cleeren F, Tshibangu T, Koole M, Serdons K, Dekervel J, Cutsem EV, Verslype C, Laere KV, Bormans G, Deroose CM. [18F]AlF-NOTA-octreotide PET imaging: biodistribution, dosimetry and first comparison with [68Ga] Ga-DOTATATE in neuroendocrine tumour patients. Eur J Nucl Med Mol Imaging. 2020;47(13):3033-46.
  23. Moon SH, Hong MK, Kim YJ, Lee YS, Lee DS, Chung JK, Jeong JM. Development of a Ga-68 labeled PET tracer with short linker for prostate-specific membrane antigen (PSMA) targeting. Bioorg Med Chem 2018;26(9):2501-7.
  24. Shetty D, Jeong JM, Kim YJ, Lee JY, Hoigebazar L, Lee YS, Lee DS, Chung JK. Development of a bifunctional chelating agent containing isothiocyanate residue for one step F-18 labeling of peptides and application for RGD labeling. Bioorgan Med Chem 2012;20(19):5941-7.
  25. Machulkin AE, Petrov SA, Bodenko V, Larkina MS, Plotnikov E, Yuldasheva F, Tretyakova M, Bexverkhniaia E, Zyk NY, Stasyu K, Zelchan R, Majouga AG, Tolmachev V, Orlova A, Beloglaxkina EK, Yusubov MS. Synthesis and Preclinical Evaluation of Urea-Based Prostate-Specific Membrane Antigen-Targeted Conjugates Labeled with 177Lu. Acs Pharmacol Transl 2024;7(5):1457-73.
  26. Fersing C, Bouhlel A, Cantelli C, Garrigue P, Lisowski V, Guillet B. A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [18F] fluoride: Will [18F]AlF Replace 68Ga for Metal Chelate Labeling? Molecules 2019;24(16):2866.