Radiolabelled peptides in nuclear medicine

  • Marko Krošelj Department of Nuclear Medicine, University Medical Centre Ljubljana, Ljubljana, Slovenia
  • Petra Kolenc Peitl Department of Nuclear Medicine, University Medical Centre Ljubljana
  • Aljaž Sočan Department of Nuclear Medicine, University Medical Centre Ljubljana
  • Marijana Leskovec Department of Nuclear Medicine, University Medical Centre Ljubljana
  • Irena Mlinarič-Raščan Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia
  • Tanja Gmeiner Faculty of Pharmacy, University of Ljubljana
Keywords: radiolabelled peptides, theranostics, radiopharmaceuticals, somatostatin, minigastrin

Abstract

Nuclear medicine plays an important role in the management of oncology patients. It enables visualization and localization of tumours, targeted radionuclide therapy and monitoring patient response to therapy. Highly specific peptide molecules can target tumour cells with overexpressed receptors for regulatory peptides and their analogues. When these peptides are radiolabelled we can use them either for diagnosis or therapy, depending on the radionuclide used. These theranostic pairs enable nuclear medicine a personalized approach to patient management. Classical example of theranostic pairs are radiolabelled somatostatin analogues that are routinely used in diagnosis and targeted radionuclide therapy of neuroendocrine neoplasms (NEN). On the other hand, radiolabelled minigastrin analogues can be used for diagnosis of metastatic medullary thyroid carcinoma (MTC) and have a potential to be used also in targeted radionuclide therapy. The purpose of this review is to describe the overview of radiolabelled peptides and to present two theranostic systems used in nuclear medicine.   

Downloads

Download data is not yet available.

References

Fani M, Maecke HR. Radiopharmaceutical development of radiolabelled peptides. Eur J Nucl Med Mol Imaging. 2012;39(1):11-30.

Aloj L, Panico MR, Caraco C, Zannetti A, Del Vecchio S, Di Nuzzo C, et al. Radiolabeling approaches for cholecystokinin B receptor imaging. Biopolymers. 2002;66(6):370-80.

Dash A, Chakraborty S, Pillai MRA, Knapp Jr FF. Peptide receptor radionuclide therapy: an overview. Cancer Biotherapy and Radiopharmaceuticals. 2015;30(2):47-71.

Baum RP. Therapeutic Nuclear Medicine: Springer; 2014.

Baum RP, Kulkarni HR. Theranostics: from molecular imaging using Ga-68 labeled tracers and PET/CT to personalized radionuclide therapy-the Bad Berka experience. Theranostics. 2012;2(5):437-47.

Ležaić L, Fettich J. Zlivanje nuklearnomedicinskih in radioloških preiskav: PET/CT in SPECT/CT Zbornik prispevkov 53Tavčarjevi dnevi; Portorož. 2011:329-37.

Bailey D, Humm J, Todd-Pokropek A, Aswegen Av. Nuclear Medicine Physics: A Handbook for Teachers and Students. Endorsed by: American Association of Physicists in Medicine (AAPM), Asia–Oceania Federation of Organizations for Medical Physics (AFOMP), Australasian College of Physical Scientists and Engineers in Medicine (ACPSEM), European Federation of Organisations for Medical Physics (EFOMP), Federation of African Medical Physics Organisations (FAMPO), World Federation of Nuclear Medicine and Biology (WFNMB). 2014.

Appetecchia M, Baldelli R. Somatostatin analogues in the treatment of gastroenteropancreatic neuroendocrine tumours, current aspects and new perspectives. Journal of Experimental & Clinical Cancer Research. 2010;29(1):19.

Moltara ME, Ocvirk J. Nevroendokrini tumorji prebavil. ONKOLOGIJA/pregledi. 2011(2):88-92.

Reubi JC. Peptide receptors as molecular targets for cancer diagnosis and therapy. Endocr Rev. 2003 Aug;24(4):389-427.

Schottelius M, Wester H-J. Molecular imaging targeting peptide receptors. Methods. 2009;48(2):161-77.

Maecke HR, Reubi JC. Somatostatin receptors as targets for nuclear medicine imaging and radionuclide treatment. Journal of Nuclear Medicine. 2011;52(6):841-4.

Gabriel M, Decristoforo C, Donnemiller E, Ulmer H, Rychlinski CW, Mather SJ, et al. An intrapatient comparison of 99mTc-EDDA/HYNIC-TOC with 111In-DTPA-octreotide for diagnosis of somatostatin receptor-expressing tumors. Journal of Nuclear Medicine. 2003;44(5):708-16.

Owyang C, Logsdon CD. New insights into neurohormonal regulation of pancreatic secretion. Gastroenterology. 2004;127(3):957-69.

Mutt V. Secretin and cholecystokinin. Gastrointestinal hormones. 1988:251-320.

Dufresne M, Seva C, Fourmy D. Cholecystokinin and gastrin receptors. Physiol Rev. 2006 Jul;86(3):805-47.

Reubi JC, Schaer JC, Waser B. Cholecystokinin(CCK)-A and CCK-B/gastrin receptors in human tumors. Cancer Res. 1997 Apr 1;57(7):1377-86.

Charron C, Hickey J, Nsiama T, Cruickshank D, Turnbull W, Luyt L. Molecular imaging probes derived from natural peptides. Natural product reports. 2016.

Matsumori Y, Katakami N, Ito M, Taniguchi T, Iwata N, Takaishi T, et al. Cholecystokinin-B/gastrin receptor: a novel molecular probe for human small cell lung cancer. Cancer research. 1995;55(2):276-9.

Salavati A, Puranik A, Kulkarni HR, Budiawan H, Baum RP, editors. Peptide Receptor Radionuclide Therapy (PRRT) of Medullary and Nonmedullary Thyroid Cancer Using Radiolabeled Somatostatin Analogues. Seminars in Nuclear Medicine; 2016: Elsevier.

Saad MF, Ordonez NG, Rashid RK, Guido JJ, Hill CS, Jr., Hickey RC, et al. Medullary carcinoma of the thyroid. A study of the clinical features and prognostic factors in 161 patients. Medicine (Baltimore). 1984 Nov;63(6):319-42.

Šabani M, Jelovac DB, Petrović MB, Gavrić M. Management of Advanced Medullary Thyroid Carcinoma. Journal of Tumor. 2014;2(8):202-7.

Wells SA, Robinson BG, Gagel RF, Dralle H, Fagin JA, Santoro M, et al. Vandetanib in patients with locally advanced or metastatic medullary thyroid cancer: a randomized, double-blind phase III trial. Journal of clinical oncology. 2012;30(2):134-41.

Behr TM, Jenner N, Radetzky S, Behe M, Gratz S, Yucekent S, et al. Targeting of cholecystokinin-B/gastrin receptors in vivo: preclinical and initial clinical evaluation of the diagnostic and therapeutic potential of radiolabelled gastrin. Eur J Nucl Med. 1998 Apr;25(4):424-30.

Gotthardt M, Boermann O, Behr T, Behe M, Oyen W. Development and clinical application of peptide-based radiopharmaceuticals. Curr Pharm Des. 2004;10(24):2951-63.

Behe M, Becker W, Gotthardt M, Angerstein C, Behr TM. Improved kinetic stability of DTPA- dGlu as compared with conventional monofunctional DTPA in chelating indium and yttrium: preclinical and initial clinical evaluation of radiometal labelled minigastrin derivatives. Eur J Nucl Med Mol Imaging. 2003 Aug;30(8):1140-6.

Nock BA, Maina T, Behe M, Nikolopoulou A, Gotthardt M, Schmitt JS, et al. CCK-2/gastrin receptor-targeted tumor imaging with (99m)Tc-labeled minigastrin analogs. J Nucl Med. 2005 Oct;46(10):1727-36.

von Guggenberg E, Sallegger W, Helbok A, Ocak M, King R, Mather SJ, et al. Cyclic minigastrin analogues for gastrin receptor scintigraphy with technetium-99m: preclinical evaluation. J Med Chem. 2009 Aug 13;52(15):4786-93.

Kolenc-Peitl P, Mansi R, Tamma M, Gmeiner-Stopar T, Sollner-Dolenc M, Waser B, et al. Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor. J Med Chem. 2011 Apr 28;54(8):2602-9.

Aloj L, Aurilio M, Rinaldi V, D'Ambrosio L, Tesauro D, Peitl PK, et al. Comparison of the binding and internalization properties of 12 DOTA-coupled and (1)(1)(1)In-labelled CCK2/gastrin receptor binding peptides: a collaborative project under COST Action BM0607. Eur J Nucl Med Mol Imaging. 2011 Aug;38(8):1417-25.

Laverman P, Joosten L, Eek A, Roosenburg S, Peitl PK, Maina T, et al. Comparative biodistribution of 12 (1)(1)(1)In-labelled gastrin/CCK2 receptor-targeting peptides. Eur J Nucl Med Mol Imaging. 2011 Aug;38(8):1410-6.

Ocak M, Helbok A, Rangger C, Peitl PK, Nock BA, Morelli G, et al. Comparison of biological stability and metabolism of CCK2 receptor targeting peptides, a collaborative project under COST BM0607. Eur J Nucl Med Mol Imaging. 2011 Aug;38(8):1426-35.

Published
2018-10-28
How to Cite
1.
Krošelj M, Kolenc Peitl P, Sočan A, Leskovec M, Mlinarič-Raščan I, Gmeiner T. Radiolabelled peptides in nuclear medicine. TEST ZdravVestn [Internet]. 28Oct.2018 [cited 24Apr.2024];87(9-10):439–452. Available from: http://vestnik-dev.szd.si/index.php/ZdravVest/article/view/2634
Section
Professional Article