Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
권호 표지
DOI QR코드

DOI QR Code

Consideration and factors for developing new radiopharmaceuticals

  • Kim, Dong Wook (Department of Chemistry and Chemical Engineering, Inha University)
  • Received : 2020.06.19
  • Accepted : 2020.06.26
  • Published : 2020.06.30
Download PDF
⟨ Previous Next ⟩

Abstract

Radiopharmaceuticals that can be consumed in specific disease site play a key role In order to diagnose and treat the diseases. In addition, radiopharmaceuticals can be used for diagnostic or therapeutic purposes depending on the type of the labeled radioactive isotope. Recently, theragnostic radiopharmaceuticals that can simultaneously diagnose and treat are developed. Therefore, the development of target-specific radiopharmaceuticals is a very important research topic in the field of molecular imaging and therapy. This review paper summarizes the basic considerations for the development of radiopharmaceuticals. For new researchers or students who are now beginning in the field of radiopharmaceuticals, we intend to assist in the development of radiopharmaceuticals by describing the definition of radiopharmaceuticals, the ideal radiopharmaceutical conditions, the considerations for developing new radiopharmaceuticals, the factors affecting the design of radiopharmaceuticals, the requirements of radioisotope labeling reactions, and finally the definition and importance of molar activity in radiopharmaceuticals.

Keywords

References

  1. Boros E, Packard AB. Radioactive transition metals for imaging and therapy. Chem Rev 2018;119:870-901. https://doi.org/10.1021/acs.chemrev.8b00281
  2. Bolton R. Radiohalogen incorporation into organic systems. J Labelled Compd Radiopharm 2002;45:485528. https://doi.org/10.1002/jlcr.575
  3. Ametamey SM, Honer M, Schubiger PA. Molecular imaging with PET. Chem Rev 2008;108:1501-1516. https://doi.org/10.1021/cr0782426
  4. Gambhir SS. Molecular imaging of cancer with positron emission tomography. Nat Rev Cancer 2002;2:683-693. https://doi.org/10.1038/nrc882
  5. Phelps ME. Positron emission tomography provides molecular imaging of biological processes. Proc Natl Acad Sci USA 2000;97:9226-9233. https://doi.org/10.1073/pnas.97.16.9226
  6. Campbell MG, Ritter T. Modern carbon-fluorine bond forming reactions for aryl fluoride synthesis. Chem Rev 2015;115:612-633. https://doi.org/10.1021/cr500366b
  7. Vallabhajosula S. Molecular Imaging; Radiopharmaceutical for PET and SPECT. 1st ed. New York: Springer; 2009.
  8. Oh SJ, Chi DY, Mosdzianowski C, Kim JY, Kil HS, Kang SH et al. Fully automated synthesis of [$^{18}F$]fluoromisonidazole using a conventional [$^{18}F$]FDG module. Nucl Med Biol 2005;32:899-905. https://doi.org/10.1016/j.nucmedbio.2005.06.003
  9. Imperiale A, Sebag F, Vix M, Castinetti F, Kessler L, Moreau F, Bachellier P, Guillet B, Namer IJ, Mundler O, Taieb D. 18F-FDOPA PET/CT imaging of insulinoma revisited. Eur J Nucl Med Mol Imaging 2015;42:409-418. https://doi.org/10.1007/s00259-014-2943-z
  10. Owunwanne A, Patel M, Sadek S. The Handbook of Radiopharmaceuticals. 1st ed. New York: Springer; 1995.
  11. Schirrmacher R, Wangler C, Schirrmacher E. Recent developments and trends in $^{18}F$-radiochemistry: syntheses and applications. Mini-Rev Org Chem 2007;4:317-329. https://doi.org/10.2174/157019307782411699
  12. Kim DW, Ahn DS, Oh YH, Lee S, Oh SJ, Lee SJ, Kim JS, Ryu JS, Moon DH, Chi DY. A new class of SN2 reactions catalyzed by protic solvents; facile fluorination for isotopic labeling of diagnostic molecules. J Am Chem Soc 2006;128:16394-16397. https://doi.org/10.1021/ja0646895
  13. Wadas TJ, Wong EH, Weisman GR, Anderson CJ. Coordinating radiometals of copper, gallium, Indium, yttrium, and zirconium for PET and SPECT imaging of disease. Chem Rev 2010;110:2858-2902. https://doi.org/10.1021/cr900325h
  14. Mascaretti OA. Modern methods for the monofluorination of aliphatic organic compounds. Aldrichimica Acta 1993:26;47-58.
  15. Ross TL, Ermert J, Hocke C, Coenen HH. Nucleophilic 18F-fluorination of heteroaromatic iodonium salts with no-carrier-added [$^{18}F$]fluoride. J Am Chem Soc 2007;129:8018-8025. https://doi.org/10.1021/ja066850h
  16. Lee J-W, Oliveira MT, Jang HB, Lee S, Chi DY, Kim DW, Song CE. Hydrogen-bond promoted nucleophilic fluorination: concept, mechanism and applications in positron emission tomography. Chem Soc Rev 2016;45:4638-4650. https://doi.org/10.1039/c6cs00286b
  17. Chi DY. The development of radiopharmaceuticals for human body imaging. J Korean Ind Eng Chem 2003;14:253-262.
  18. Coenen HH, Gee AD, Adam M, Antoni G, Cutler CS, Fujibayashi Y, Jeong JM, Mach RH, Mindt TL, Pike VW, Windhorst AD. Nucl Med Biol 2019;71:19-22. https://doi.org/10.1016/j.nucmedbio.2019.05.001
  19. Sachin K, Jadhav VH, Kim EM, Kim HL, Lee SB, Jeong HJ, Lim ST, Sohn MH, Kim DW. F-18 Labeling protocol of peptides based on chemically orthogonal strainpromoted cycloaddition under physiologically friendly reaction conditions. Bioconjug Chem 2012;23:1680-1686. https://doi.org/10.1021/bc3002425
  20. Gutfilen B, Souza S, Valentini G. Copper-64: a real theranostic agent. Drug Des. Dev. Ther 2018; 12:3235-3245. https://doi.org/10.2147/DDDT.S170879