Exploring the potential of high-molar activity Samarium-153 for targeted radionuclide therapy with [153Sm]Sm-DOTA-TATE

Koen Vermeulen, Michiel Van de Voorde, Charlotte Segers, Amelie Coolkens, Sunay Rodriguez Perez, Charlotte Duchemin, Melissa Crabbé, Tomas Opsomer, Clarita Saldarriaga Vargas, Heinke Reinhard, Laura Lambert, Cyril Bernerd, Andrew Burgoyne, Thomas Elias Cocolios, Thierry Stora, Maarten Ooms

Research outputpeer-review


Samarium-153 is a promising theranostic radionuclide but low molar activities (Am) resulting from its current production route renders it unsuitable for targeted radionu-clide therapy (TRNT). Recent efforts combining neutron activation of 152Sm in the SCK CEN BR2 reactor with mass separation at CERN/MEDICIS yielded high Am 153Sm. In this proof-of-concept study we further evaluated the potential of high Am 153Sm 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 153Sm 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 [153Sm]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 [153Sm]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 153Sm for TRNT and could open doors towards wider applications of mass separation in medical isotope production.
Original languageEnglish
Article number2566
Pages (from-to)1-15
Number of pages15
StatePublished - 18 Nov 2022

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