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

• Published in: Journal of radioanalytical and nuclear chemistry Vol. 333; no. 8; pp. 3873 - 3891
• Main Authors: Menon, Sreeja Raj, Mitra, Arpit, Chakraborty, Avik, Kamaldeep, Sahu, Sudeep, Tawate, Megha, Lad, Sangita, Rakshit, Sutapa, Upadhye, Trupti, Ray, Mukti Kanta, Banerjee, Sharmila
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01-08-2024; Springer Nature B.V
• Subjects: Automatic control; Chemistry; Chemistry and Materials Science; Diagnostic Radiology; Gallium; Hadrons; Heavy Ions; Inorganic Chemistry; Nuclear Chemistry; Nuclear Physics; Pharmaceuticals; Physical Chemistry; Quality control; Radiochemistry; Pancreatic neuroendocrine tumors; (NODAGA); Exendin-4[Lys; Insulinoma; PET/CT; Glucagon-like peptide-1 receptor
• ISSN: 0236-5731; 1588-2780
• DOI: 10.1007/s10967-024-09535-1

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.
Graphical abstract