[89Zr]Zr-DFO-TOC: a novel radiopharmaceutical for PET imaging of somatostatin receptor positive neuroendocrine tumors

Sanwick, Alexis M.; Haugh, Katherine N.; Williams, Evan J.; Perry, Kala A.; Thiele, Nikki A.; Chaple, Ivis F.

doi:10.1186/s41181-024-00320-9

[⁸⁹Zr]Zr-DFO-TOC: a novel radiopharmaceutical for PET imaging of somatostatin receptor positive neuroendocrine tumors

Journal Article · Wed Dec 18 00:00:00 EST 2024 · EJNMMI Radiopharmacy and Chemistry

DOI:https://doi.org/10.1186/s41181-024-00320-9· OSTI ID:2538177

Sanwick, Alexis M. ^[1]; Haugh, Katherine N. ^[1]; Williams, Evan J. ^[1]; Perry, Kala A. ^[1]; Thiele, Nikki A. ^[2]; ^[1]

University of Tennessee, Knoxville, TN (United States)
Oak Ridge National Laboratory (ORNL), Oak Ridge, TN (United States)

Neuroendocrine tumors (NETs) are clinically diverse types of tumors that can arise anywhere in the body. Previous studies have shown that somatostatin receptors (SSTRs) are overexpressed on NET cell membranes relative to healthy tissue, allowing for tumor targeting through radiolabeled somatostatin analogs (SSAs). This work aims to develop a novel ⁸⁹Zr-labeled tracer incorporating the SSA, octreotide (TOC), for positron emission tomography (PET) imaging of SSTR + NETs and predictive dosimetry calculations, leveraging the excellent nuclear (t_½ = 3.27 days, β+ = 22.3%, β⁺_avg = 395.5 keV) and chemical characteristics (+ 4 oxidation state, preferential coordination number of 7/8, favorable aqueous chemistry) of ⁸⁹Zr. In combination with ⁸⁹Zr, the known radiochemistry with the chelator deferoxamine (DFO) gives reason to believe that this radiopharmaceutical incorporating an octreotide conjugate will be successful in studying the suitability of detecting SSTR + NETs.

View Accepted Manuscript (DOE)

Research Organization:: Oak Ridge National Laboratory (ORNL), Oak Ridge, TN (United States)

Sponsoring Organization:: USDOE

Grant/Contract Number:: AC05-00OR22725

OSTI ID:: 2538177

Journal Information:: EJNMMI Radiopharmacy and Chemistry, Journal Name: EJNMMI Radiopharmacy and Chemistry Journal Issue: 1 Vol. 9; ISSN 2365-421X

Publisher:: BioMed CentralCopyright Statement

Country of Publication:: United States

Language:: English

References (23)

Neuroendocrine Tumors—Less Well Known, Often Misunderstood, and Rapidly Growing in Incidence Chauhan, Aman; Kohn, Elise; Del Rivero, Jaydira JAMA Oncology, Vol. 6, Issue 1 https://doi.org/10.1001/jamaoncol.2019.4568	journal	January 2020
Somatostatin receptors in prostate tissues and derived cell cultures, and the in vitro growth inhibitory effect of BIM-23014 analog Tatoud, Roger; Degeorges, Armelle; Prévost, Grégoire Molecular and Cellular Endocrinology, Vol. 113, Issue 2 https://doi.org/10.1016/0303-7207(95)03630-P	journal	September 1995
PET imaging with 89Zr: From radiochemistry to the clinic Deri, Melissa A.; Zeglis, Brian M.; Francesconi, Lynn C. Nuclear Medicine and Biology, Vol. 40, Issue 1 https://doi.org/10.1016/j.nucmedbio.2012.08.004	journal	January 2013
Production of Zr-89 using sputtered yttrium coin targets Queern, Stacy Lee; Aweda, Tolulope Aramide; Massicano, Adriana Vidal Fernandes Nuclear Medicine and Biology, Vol. 50 https://doi.org/10.1016/j.nucmedbio.2017.03.004	journal	July 2017
Somatostatin receptors: From signaling to clinical practice Theodoropoulou, Marily; Stalla, Günter K. Frontiers in Neuroendocrinology, Vol. 34, Issue 3 https://doi.org/10.1016/j.yfrne.2013.07.005	journal	August 2013
Imaging Somatostatin Positive Tumors with Tyr³-Octreotate/Octreotide Conjugated to Desferrioxamine B Squaramide Radiolabeled with either Zirconium-89 or Gallium-68 Noor, Asif; Van Zuylekom, Jessica K.; Rudd, Stacey E. Bioconjugate Chemistry, Vol. 32, Issue 7 https://doi.org/10.1021/acs.bioconjchem.1c00109	journal	March 2021
Internalization of [DOTAo,125I-Tyr3]Octreotide by Somatostatin Receptor-Positive Cells In Vitro and In Vivo: Implications for Somatostatin Receptor-Targeted Radio-guided Surgery Hof land, Leo J.; Breeman, Wout A. P.; Krenning, Eric P. Proceedings of the Association of American Physicians, Vol. 111, Issue 1 https://doi.org/10.1046/j.1525-1381.1999.09110.x	journal	January 1999
Octreotide Lamberts, Steven W. J.; van der Lely, Aart-Jan; de Herder, Wouter W. New England Journal of Medicine, Vol. 334, Issue 4 https://doi.org/10.1056/NEJM199601253340408	journal	January 1996
Stimulation of tyrosine phosphatase and inhibition of cell proliferation by somatostatin analogues: mediation by human somatostatin receptor subtypes SSTR1 and SSTR2. Buscail, L.; Delesque, N.; Estève, J. P. Proceedings of the National Academy of Sciences, Vol. 91, Issue 6 https://doi.org/10.1073/pnas.91.6.2315	journal	March 1994
Radiolabeling and quality control of therapeutic radiopharmaceuticals: optimization, clinical implementation and comparison of radio-TLC/HPLC analysis, demonstrated by [177Lu]Lu-PSMA Hooijman, Eline L.; Ntihabose, Carolline M.; Reuvers, Thom G. A. EJNMMI Radiopharmacy and Chemistry, Vol. 7, Issue 1 https://doi.org/10.1186/s41181-022-00181-0	journal	November 2022
One Hundred Years After “Carcinoid”: Epidemiology of and Prognostic Factors for Neuroendocrine Tumors in 35,825 Cases in the United States Yao, James C.; Hassan, Manal; Phan, Alexandria Journal of Clinical Oncology, Vol. 26, Issue 18 https://doi.org/10.1200/JCO.2007.15.4377	journal	June 2008
In Vivo Molecular Imaging of Somatostatin Receptors in Pancreatic Islet Cells and Neuroendocrine Tumors by Miniaturized Confocal Laser-Scanning Fluorescence Microscopy Fottner, C.; Mettler, E.; Goetz, M. Endocrinology, Vol. 151, Issue 5 https://doi.org/10.1210/en.2009-1313	journal	March 2010
Expression of Somatostatin Receptor (SSTR) Subtypes (SSTR-1, 2A, 3, 4 and 5) in Neuroendocrine Tumors Using Real-time RT-PCR Method and Immunohistochemistry Mizutani, Gou; Nakanishi, Yoko; Watanabe, Noriko ACTA HISTOCHEMICA ET CYTOCHEMICA, Vol. 45, Issue 3 https://doi.org/10.1267/ahc.12006	journal	January 2012
Alpha-, Delta- and PP-cells Brereton, Melissa F.; Vergari, Elisa; Zhang, Quan Journal of Histochemistry & Cytochemistry, Vol. 63, Issue 8 https://doi.org/10.1369/0022155415583535	journal	July 2015
Prognosis of patients with neuroendocrine tumor: a SEER database analysis Man, Da; Wu, Jingjing; Shen, Zhan Cancer Management and Research, Vol. Volume 10 https://doi.org/10.2147/CMAR.S174907	journal	November 2018
89Zr-DFO-J591 for ImmunoPET of Prostate-Specific Membrane Antigen Expression In Vivo Holland, J. P.; Divilov, V.; Bander, N. H. Journal of Nuclear Medicine, Vol. 51, Issue 8 https://doi.org/10.2967/jnumed.110.076174	journal	July 2010
Investigation of cancer cell lines for peptide receptor-targeted drug development Sun, Lichun; Luo, Jing; Mackey, L. Vienna Journal of Drug Targeting, Vol. 19, Issue 8 https://doi.org/10.3109/1061186X.2011.558089	journal	August 2011
Correlations between [68Ga]Ga-DOTA-TOC Uptake and Absorbed Dose from [177Lu]Lu-DOTA-TATE Bruvoll, Ragnar; Blakkisrud, Johan; Mikalsen, Lars Tore Cancers, Vol. 15, Issue 4 https://doi.org/10.3390/cancers15041134	journal	February 2023
Somatostatin Analogs in Clinical Practice: A Review Gomes-Porras, Mariana; Cárdenas-Salas, Jersy; Álvarez-Escolá, Cristina International Journal of Molecular Sciences, Vol. 21, Issue 5 https://doi.org/10.3390/ijms21051682	journal	February 2020
Regulatory Mechanisms of Somatostatin Expression Ampofo, Emmanuel; Nalbach, Lisa; Menger, Michael D. International Journal of Molecular Sciences, Vol. 21, Issue 11 https://doi.org/10.3390/ijms21114170	journal	June 2020
Re-Evaluations of Zr-DFO Complex Coordination Chemistry for the Estimation of Radiochemical Yields and Chelator-to-Antibody Ratios of 89Zr Immune-PET Tracers Imura, Ryota; Ida, Hiroyuki; Sasaki, Ichiro Molecules, Vol. 26, Issue 16 https://doi.org/10.3390/molecules26164977	journal	August 2021
Lutathera®: The First FDA- and EMA-Approved Radiopharmaceutical for Peptide Receptor Radionuclide Therapy Hennrich, Ute; Kopka, Klaus Pharmaceuticals, Vol. 12, Issue 3 https://doi.org/10.3390/ph12030114	journal	July 2019
[68Ga]Ga-DOTA-TOC: The First FDA-Approved 68Ga-Radiopharmaceutical for PET Imaging Hennrich, Ute; Benešová, Martina Pharmaceuticals, Vol. 13, Issue 3 https://doi.org/10.3390/ph13030038	journal	March 2020

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[⁸⁹Zr]Zr-DFO-TOC: a novel radiopharmaceutical for PET imaging of somatostatin receptor positive neuroendocrine tumors