@article{vermeulen_exploring_2022,
	title = {Exploring the {Potential} of {High}-{Molar}-{Activity} {Samarium}-153 for {Targeted} {Radionuclide} {Therapy} with [{153Sm}]{Sm}-{DOTA}-{TATE}},
	volume = {14},
	issn = {1999-4923},
	url = {https://www.mdpi.com/1999-4923/14/12/2566},
	doi = {10.3390/pharmaceutics14122566},
	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 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.},
	language = {en},
	number = {12},
	urldate = {2022-11-30},
	journal = {Pharmaceutics},
	author = {Vermeulen, Koen and Van de Voorde, Michiel and Segers, Charlotte and Coolkens, Amelie and Rodriguez Pérez, Sunay and Daems, Noami and Duchemin, Charlotte and Crabbé, Melissa and Opsomer, Tomas and Saldarriaga Vargas, Clarita and Heinke, Reinhard and Lambert, Laura and Bernerd, Cyril and Burgoyne, Andrew R. and Cocolios, Thomas Elias and Stora, Thierry and Ooms, Maarten},
	month = nov,
	year = {2022},
	keywords = {scientific-publication},
	pages = {2566},
}