Abstract
AbstractThe radiosynthesis of pharmaceutical grade [68Ga]Ga-NODAGA-Lys40-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[Lys40(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 (68Ga) 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
Funder
Advanced Centre for Treatment, Research and Education in Cancer (ACTREC) - Khargar
Publisher
Springer Science and Business Media LLC
Reference43 articles.
1. Mehrabi A, Fischer L, Hafezi M et al (2014) A systematic review of localization, surgical treatment options, and outcome of insulinoma. Pancreas 43(5):675–686
2. Jansen TJP, van Lith SAM, Boss M et al (2019) Exendin-4 analogs in insulinoma theranostics. J Label Comp Radiopharm 62(10):656–672
3. Wild D, Wicki A, Mansi R et al (2010) Exendin-4-based radiopharmaceuticals for glucagonlike peptide-1 receptor PET/CT and SPECT/CT. J Nucl Med 51(7):1059–1067
4. Velikyan I, Bulenga TN, Selvaraju R et al (2015) Dosimetry of [177Lu]-DO3A-VS-Cys 40-Exendin-4-impact on the feasibility of insulinoma internal radiotherapy. Am J Nucl Med Mol Imaging 5(2):109–126
5. Nock BA, Kanellopoulos P, Joosten L et al (2023) Peptide radioligands in cancer theranostics: agonists and antagonists. Pharmaceuticals 16(5):674