Development of [64Cu]-DOTA-anti-CD20 for targeted therapy

A. R. Jalilian, L. Mirsadeghi, Y. Yari-Kamrani, P. Rowshanfarzad, M. Kamali-Dehghan, M. Sabet

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

Copper-64 was produced as a by-product of 55Co via 64Ni(p,n)64Cu by 15 MeV proton bombardment of natNi resulting in a thick target yield of 5.31 MBq/μAh (143.5 μCi/μAh) and a radiochemical separation yield of 95% (radionuclide purity >97% after 25 hours of bombardment). Rituximab was successively labeled with [64Cu]-CuCl2. N-succinimidyl-1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA-NHS) was prepared at 25°C using DOTA and N-hydroxy succinimide (NHS) in CH2Cl 2 followed by the addition of 1 ml of a Rituximab pharmaceutical solution. Radiolabeling was performed at 37°C in 3 hours. Radio thin-layer chromatography showed an overall radiochemical purity of 90-95% at optimized conditions (specific activity=30 GBq/mg, labeling efficacy; 82%) using various chromatography systems. The final isotonic 64Cu-DOTA-Rituximab complex was passed through a 0.22 μm filter and checked by gel electrophoresis for radiolysis control. Stability of the final product was checked in the formulation and in presence of human serum at 37°C.

Original languageEnglish
Pages (from-to)563-568
Number of pages6
JournalJournal of Radioanalytical and Nuclear Chemistry
Volume274
Issue number3
DOIs
Publication statusPublished - 1 Dec 2007

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