Fully Automated Production and Characterization of 64Cu and Proof‐of‐Principle Small‐Animal PET Imaging Using 64Cu‐Labelled CA XII Targeting 6A10 Fab. (23rd May 2018)

• Record Type: Journal Article
• Authors: Fiedler, Luise; Kellner, Markus; Oos, Rosel; Böning, Guido; Ziegler, Sibylle; Bartenstein, Peter; Zeidler, Reinhard; Gildehaus, Franz Josef; Lindner, Simon
• Is Part Of: ChemMedChem. Volume 13:Number 12(2018)
• Page Start: 1230
• Page End: 1237
• Publication Date: 2018-05-23
• Subjects: 64Cu -- 6A10 Fab -- Comecer Alceo -- positron emission tomography -- solid targets; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201800130
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract: 64 Cu is a cyclotron‐produced radionuclide which offers, thanks to its characteristic decay scheme, the possibility of combining positron emission tomography (PET) investigations with radiotherapy. We evaluated the Alceo system from Comecer SpA to automatically produce 64 Cu for radiolabelling purposes. We established a 64 Cu production routine with high yields and radionuclide purity in combination with excellent operator radiation protection. The carbonic anhydrase XII targeting 6A10 antibody Fab fragment was successfully radiolabelled with the produced 64 Cu, and proof‐of‐principle small‐animal PET experiments on mice bearing glioma xenografts were performed. We obtained a high tumor‐to‐contralateral muscle ratio, which encourages further in vivo investigations of the radioconjugate regarding a possible application in diagnostic tumor imaging. Abstract : Ideal decay : An automated 64 Cu production system using the first‐generation Alceo setup was established and evaluated. Volume, pH, radionuclide purity, non‐radioactive metal impurities, and molar activity of the product were determined. The carbonic anhydrase XII targeting 6A10 Fab fragment was radiolabelled with the produced 64 Cu, and proof‐of‐principle small‐animal PET imaging was performed.