Automated radiosynthesis of pharmaceutical grade [68Ga]Ga-NODAGA-Lys40-Exendin-4 and demonstration of its efficacy for use in patients

The radiosynthesis of pharmaceutical grade [ 68 Ga]Ga-NODAGA-Lys 40 -Exendin-4 was accomplished in a fixed tubing-based module, EZ Modular-Lab Standard. Purification of the product via hydrophilic-lipophilic balance cartridge, yielded satisfactory results with radiochemical purity > 98%. The decay-corrected radiochemical yield (RCY) with 50 µg of Exendin-4[Lys 40 (NODAGA)] was (78.7 ± 0.8)%, which, by far, to the best of our knowledge, is the highest RCY reported till date, using an automated synthesizer. The quality control parameters were in accordance with that of gallium ( 68 Ga) Edotreotide ® Injections, featuring in the European Pharmacopoeia. Pre-clinical dosimetry studies in animal models, with co-administration of kidney protectant, demonstrates promising potential of the product towards clinical translation to insulinoma patients.