Salvé Mallory, Avohou Hermane T, Monbaliu Jean-Christophe M, Lebrun Pierre, Lemaire Christian, Damblon Christian, de Tullio Pascal, Hubert Philippe, Hustinx Roland, Luxen André
GIGA-CRC In VIVO Imaging, University of Liège, Liège, Belgium.
Nuclear Medicine and Oncological Imaging Division, CHU of Liege, Liège, Belgium.
J Labelled Comp Radiopharm. 2018 May 30;61(6):487-500. doi: 10.1002/jlcr.3613. Epub 2018 Apr 25.
This work reports on the development of amide bond bioconjugation for the production of -NOTA and -NODAGA PRGD using batch strategy and microfluidic reactor technology. The final radiolabelling step was fully optimized using Design of Experiments and Design Space approaches, hence targeting robust labelling yields in routine. Optimal labelling conditions were defined in sodium acetate buffer as 168 μg/mL peptide concentration, 4.9 pH, 47.5°C temperature, and 12.5-minute reaction time. Upon optimization, the Gallium-68 radiolabelling was fully automated. All the work was designed to be compliant to the GMP environment and to support the pharmaceutical scale-up.
