Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

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

DOI QR Code

Development of radiolabeled somatostatin derivatives for neuroendocrine tumors

  • Hee-Kwon Kim (Department of Nuclear Medicine, Molecular Imaging & Therapeutic Medicine Research Center, Jeonbuk National University Medical School and Hospital)
  • Received : 2021.12.07
  • Accepted : 2021.12.28
  • Published : 2021.12.30
Download PDF
⟨ Previous Next ⟩

Abstract

Neuroendocrine tumor is one of popular diseases, and somatostatin receptor antagonists have been considered as promising agents for neuroendocrine tumors. Imaging of somatostatin receptor is useful approach on the diagnosis and therapy of neuroendocrine tumors. Thus, several radiolabeled somatostatin derivatives have been developed by scientists, and used for patients with neuroendocrine tumors. In particular, some radiopharmaceuticals for neuroendocrine tumors were approved by FDA. In this highlight review, the development of important radiolabeled somatostatin derivatives is described.

Keywords

Acknowledgement

This research was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (NRF-2021R1A2C1011204).

References

  1. Oberg K. Molecular imaging radiotherapy: theranostics for personalized patient management of neuroendocrine tumors (NETs). Theranostics 2012;2:448 - 458. https://doi.org/10.7150/thno.3931
  2. Lawrence B, Gustafsson BI, Chan A, Svejda B, Kidd M, Modlin IM. The epidemiology of gastroenteropancreatic neuroendocrine tumors. Endocrinol Metab Clin N Am 2011;40:1-18. https://doi.org/10.1016/j.ecl.2010.12.005
  3. Yao JC, Hassan M, Phan A, Dagohoy C, Leary C, Mares JE, Abdalla EK, Fleming JB, Vauthey J, Rashid A, Evans DB. One hundred years after "carcinoid": epidemiology of and prognostic factors for neuroendocrine tumors in 35,825 cases in the United States. J Clin Oncol 2008;26:3063 - 3072. https://doi.org/10.1200/JCO.2007.15.4377
  4. Johnbeck CB, Knigge U, Kjaer A. PET tracers for somatostatin receptor imaging of neuroendocrine tumors: current status and review of the literature. Future Oncol 2014;10:2259 - 2277. https://doi.org/10.2217/fon.14.139
  5. Hoyer D, Bell GI, Berelowitz M, Epelbaum J, Feniuk W, Humphrey PA, O'Carroll A-M., Patel YC, Schonbrunn A, Taylor JE, Reisine T. Classification and nomenclature of somatostatin receptors. 1995;16:86 - 88.
  6. Reubi JC. Somatostatin and other peptide receptors as tools for tumor diagnosis and treatment. Neuroendocrinology 2004;80(suppl 1):51 - 56. https://doi.org/10.1159/000080742
  7. Binderup T, Knigge U, Mellon Mogensen A, Palnaes Hansen C, Kjaer A. Quantitative gene expression of somatostatin receptors and noradrenaline transporter underlying scintigraphic results in patients with neuroendocrine tumors. Neuroendocrinology 2008;87:223 - 232. https://doi.org/10.1159/000113128
  8. Reubi JC, Waser B, Schaer JC, Laissue JA. Somatostatin receptor sst1-sst5 expression in normal and neoplastic human tissues using receptor autoradiography with subtype-selective ligands. Eur J Nucl Med 2001;28:836 - 846. https://doi.org/10.1007/s002590100541
  9. Krenning EP, Kwekkeboom DJ, Bakker WH, Kooij PP, Oei HY, van Hagen M, Postema PT, de Jong M, Reubi JC, Visser TJ, Reijs aeM, Hofland LJ, Koper JW, Lamberts SWJ. Somatostatin receptor scintigraphy with [111In-DTPA-D-Phe1]- and [123I-Tyr3]-octreotide: the Rotterdam experience with more than 1000 patients. Eur J Nucl Med 1993;20:716 - 731. https://doi.org/10.1007/BF00181765
  10. Levine R, Krenning EP. Clinical history of the theranostic radionuclide approach to neuroendocrine tumors and other types of cancer: historical review based on an interview of Eric P. Krenning by Rachel Levine. J Nucl Med 2017;58:3S - 9S. https://doi.org/10.2967/jnumed.116.186502
  11. Velikyan I. 68Ga-Based Radiopharmaceuticals: production and application relationship. Molecules 2015;20:12913-12943. https://doi.org/10.3390/molecules200712913
  12. Walker RC, Smith GT, Liu E, Moore B, Clanton J, Stabin M. Measured human dosimetry of 68Ga-DOTATATE. J Nucl Med.2013;54:855 - 860. https://doi.org/10.2967/jnumed.112.114165
  13. https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecu-lar-entities-and-new-therapeutic-biological-products/novel-drug-appro-vals-2016
  14. Poeppel TD, Binse I, Petersenn S, Lahner H, Schott M, Antoch G, Brandau W, Bockisch A, Boy C. 68Ga-DOTATOC versus 68Ga-DOTATATE PET/CT in functional imaging of neuroendocrine tumors. J Nucl Med 2011;52:1864 - 1870. https://doi.org/10.2967/jnumed.111.091165
  15. Sandstrom M, Velikyan I, Garske-Roman U, Sorensen J, Eriksson B, Granberg D, Lundqvist H, Sundin A, Lubberink M. Comparative biodistribution and radiation dosimetry of 68Ga-DOTATOC and 68Ga-DOTATATE in patients with neuroendocrine tumors. J Nucl Med 2013;54:1755 - 1759. https://doi.org/10.2967/jnumed.113.120600
  16. Velikyan I, Sundin A, Sorensen J, Lubberink M, Sandstrom M, Garske-Roman U, Lundqvist H, Granberg D, Eriksson B. Quantitative and qualitative intrapatient comparison of 68Ga-DOTATOC and 68Ga-DOTATATE: net uptake rate for accurate quantification. J Nucl Med 2014;55:204- 210. https://doi.org/10.2967/jnumed.113.126177
  17. Johnbeck CB, Knigge U, Loft A, Berthelsen AK, Mortensen J, Oturai P, Langer SW, Elema DR, Kjaer A. Head-to-head comparison of 64Cu-DOTATATE and 68Ga-DOTATOC PET/CT: a prospective study of 59 patients with neuroendocrine tumors. J Nucl Med 2017;58:451- 457. https://doi.org/10.2967/jnumed.116.180430
  18. https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecu-lar-entities-and-new-therapeutic-biological-products/novel-drug-approvals-2020
  19. Fani M, Braun F, Waser B, Beetschen K, Cescato R, Erchegyi J, Rivier JE, WWeber WA, Maecke HR, Reubi JC. Unexpected sensitivity of sst2 antagonists to N-terminal radiometal modifications. J Nucl Med 2012;53:1481 - 1489. https://doi.org/10.2967/jnumed.112.102764
  20. Krebs S, Pandit-Taskar N, Reidy D, Beattie BJ, Lyashchenko SK, Lewis JS, Bodei L, Weber WA, O'Donoghue JA. Biodistribution and radiation dose estimates for 68Ga-DOTA-JR11 in patients with metastatic neuroendocrine tumors. Eur J Nucl Med Mol Imaging 2019; 46:677 - 685. https://doi.org/10.1007/s00259-018-4193-y
  21. Nicolas GP, Beykan S, Bouterfa H, Kaufmann J, Bauman A, Lassmann M, Reubi JC, Rivier JEF, Maecke HR, Fani M, Wild D. Safety, biodistribution, and radiation dosimetry of 68Ga-OPS202 in patients with gastroenteropancreatic neuroendocrine tumors: a prospective phase I imaging study. J Nucl Med 2018;9:909 - 914.
  22. Nicolas GP, Schreiter N, Kaul F, Uiters J, Bouterfa H, Kaufmann J, Erlanger TE, Cathomas R, Christ E, Fani M, Wild D. Sensitivity comparison of 68Ga-OPS202 and 68Ga-DOTATOC PET/CT in patients with gastroenteropancreatic neuroendocrine tumors: a prospective phase II imaging study. J Nucl Med 2018;59:915 - 921. https://doi.org/10.2967/jnumed.117.199760
  23. Hirams N, Jadaan R, Al-Ibraheem A. Peptide receptor radionuclide therapy and the treatment of gastroentero-pancreatic neuroendocrine tumors: current findings and future perspectives. Nucl Med Mol Imaging 2018;52:190 - 199. https://doi.org/10.1007/s13139-018-0517-x
  24. Jamar F, Barone R, Mathieu I, Walrand S, Labar D, Carlier P, de Camps J, Schran H, Chen T, Smith MC, Bouterfa H, Valkema R, Krenning EP, Kvols LK, Pauwels S. 86Y-DOTA0-D-Phe1-Tyr3-octreotide (SMT487): a phase 1 clinical study-pharmacokinetics, biodistribution and renal protective effect of different regimens of amino acid co-infusion. Eur J Nucl Med Mol Imaging 2003;30:510 - 518. https://doi.org/10.1007/s00259-003-1117-1
  25. Barone R, Borson-Chazot F, Valkema R, Walrand S, Chauvin F, Gogou L, Kvols LK, Krenning EP, Jamar F, Pauwels S. Patient-specific dosimetry in predicting renal toxicity with 90Y-DOTATOC: relevance of kidney volume and dose rate in finding a dose-effect relationship. J Nucl Med 2005;46(suppl 1): 99S - 106S.
  26. Pauwels S, Barone R, Walrand S, Borson-Chazot F, Valkema R, Kvols LK, Krenning EP, Jamar F. Practical dosimetry of peptide receptor radionuclide therapy with 90Y-labeled somatostatin analogs. J Nucl Med 2005; 46(suppl 1):92S - 98S.
  27. https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecu-lar-entities-and-new-therapeutic-biological-products/novel-drug-approvals-2018