| Article | |
| Title | Exploring the Potential of High-Molar-Activity Samarium-153 for Targeted Radionuclide Therapy with [$^{153}$Sm]Sm-DOTA-TATE |
| Author(s) | Vermeulen, Koen (SCK-CEN, Mol) ; Van de Voorde, Michiel (SCK-CEN, Mol) ; Segers, Charlotte (SCK-CEN, Mol) ; Coolkens, Amelie (SCK-CEN, Mol) ; Pérez, Sunay Rodriguez (SCK-CEN, Mol) ; Daems, Noami (SCK-CEN, Mol) ; Duchemin, Charlotte (Leuven U. ; CERN) ; Crabbé, Melissa (SCK-CEN, Mol) ; Opsomer, Tomas (SCK-CEN, Mol) ; Vargas, Clarita Saldarriaga (SCK-CEN, Mol) ; Heinke, Reinhard (Leuven U. ; CERN) ; Lambert, Laura (CERN) ; Bernerd, Cyril (Leuven U. ; CERN) ; Burgoyne, Andrew R (SCK-CEN, Mol) ; Cocolios, Thomas Elias (Leuven U.) ; Stora, Thierry (CERN) ; Ooms, Maarten (SCK-CEN, Mol) |
| Publication | 2022 |
| Number of pages | 15 |
| In: | Pharmaceutics 14 (2022) 2566 |
| DOI | 10.3390/pharmaceutics14122566 |
| Subject category | Health Physics and Radiation Effects |
| Accelerator/Facility, Experiment | CERN MEDICIS |
| Abstract | Samarium-153 is a promising theranostic radionuclide, but low molar activities (Am) resulting from its current production route render it unsuitable for targeted radionuclide therapy (TRNT). Recent efforts combining neutron activation of $^{152}$Sm in the SCK CEN BR2 reactor with mass separation at CERN/MEDICIS yielded high-Am $^{153}$Sm. In this proof-of-concept study, we further evaluated the potential of high-Am $^{153}$Sm for TRNT by radiolabeling to DOTA-TATE, a well-established carrier molecule binding the somatostatin receptor 2 (SSTR2) that is highly expressed in gastroenteropancreatic neuroendocrine tumors. DOTA-TATE was labeled with $^{153}$Sm and remained stable up to 7 days in relevant media. The binding specificity and high internalization rate were validated on SSTR2-expressing CA20948 cells. In vitro biological evaluation showed that [$^{153}$Sm]Sm-DOTA-TATE was able to reduce CA20948 cell viability and clonogenic potential in an activity-dependent manner. Biodistribution studies in healthy and CA20948 xenografted mice revealed that [$^{153}$Sm]Sm-DOTA-TATE was rapidly cleared and profound tumor uptake and retention was observed whilst these were limited in normal tissues. This proof-of-concept study showed the potential of mass-separated $^{153}$Sm for TRNT and could open doors towards wider applications of mass separation in medical isotope production. |
| Copyright/License | © 2022-2024 The authors (License: CC-BY-4.0) |
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Journalen skapades 2023-02-15, och modifierades senast 2023-02-23
