177 Lu-DOTA-coupled minigastrin peptides: promising theranostic agents in neuroendocrine cancers

Molecular Biology Reports
Syed Faheem Askari RizviRashid Rasheed

Abstract

Treatment with radionuclide labeled regulatory peptides is a promising tool in the management of patients with inoperable receptor positive neuroendocrine tumors. Peptide receptor lutetium-177 radionuclide therapy currently has gained ample attention due to high specific accumulation of regulatory peptides at tumor cell surface and promising characteristics of β- and γ-energy photons of lutetium-177 radionuclide. In this study gastrin peptides analogues were labeled with lutetium-177 by subsequent mixing of 177LuCl3 (~ 185 MBq), ammonium acetate buffer of 5 pH, gentistic acid, aqueous solution of gastrin peptide analogues (1 mg/mL) and heating the reaction mixture at 98 °C which resulted in high radiochemical yield (> 96%). Chromatographic analysis was carried out to analyze the radiochemical purity. The shelf life and serum stability results showed the labeled peptides are sufficiently stable up to 4-h. Glomerular filtration rate study results showed moderate filtration through kidneys. The GFR values of 177Lu-MGCL2 and 177Lu-MGCL4 was noted 48 mL/min and 45 mL/min, respectively. Biodistribution and scintigraphy study using rat and rabbit models showed minimal non-target accumulation, moderate uptake by liver and kidneys. The ...Continue Reading

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Citations

Feb 8, 2020·Dalton Transactions : an International Journal of Inorganic Chemistry·Claudine Herlan, Stefan Bräse
Feb 26, 2021·Dose-response : a Publication of International Hormesis Society·Samina RoohiSyed Ali Raza Naqvi
Mar 7, 2019·Chemical Reviews·Heather D AgnewJames R Heath

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