Preparation and Preliminary Biological Evaluation of [153Sm] Samarium Amd3100; Towards a Possible Therapeutic Chemokine Receptor Cxcr4 Targeting Complex



Aghanejad A^{1, 3} ; Jalilian AR² ; Bahramisamani A² ; Beiki D^{1, 3} ; Maus S⁴ ; Khalaj A³ Show Affiliations
Source: Iranian Journal of Nuclear Medicine Published:2015

Abstract

Introduction: In continuation of recent development of possible C-X-C chemokine receptor type 4 (CXCR4) imaging agents, we report the development of a possible CXCR4 targeted therapy agent.; Methods: [153 Sm]labeled 1,1′¬-[1,4-phenylenebis(methylene)] bis-1,4,8,11-tetraazacyclo- tetradecane ([153Sm]-AMD3100) was prepared using [153Sm]SmCl3 and AMD-3100 for 24h at 50.,aC in acetate buffer. Stability tests, partition coefficient determination, toxicity tests and biodistribution studies of the complex in wild-type rats were determined.; Results: The radiolabeled complex was prepared in high radiochemical purity (<95%; RTLC and <99% HPLC) and specific activity of 278 GBq/mmol and demonstrated significant stability up to 48h at 37 .,aC (in presence of human serum). Partition coefficient determination was calculated Log P= -1.09. Hepatotoxicity experiments demonstrated no distinguishable effect on hepatic enzymes in 10 days post injection. Initial complex biodistribution data showed significant liver and kidney accumulation in wild-type rats.; Conclusion: Since lung and spleen are considered as CXCR4 rich organs, the best lung/blood and spleen/blood ratios were achieved 12 and 7 at 24 h post injection. Further investigations are needed especially on therapeutic properties of this agent. K.