Importantly, the tumour uptake in the biodistribution study was not significantly affected with 2.9, 2.5, 3.2 and 1.5% iA/g for radiolabelled Ex4, MVK-Ex4, MV-MVK-Ex4 and MVK-MVK-Ex4, respectively.
Renal uptake of 68Ga-exendin-4 can be effectively reduced by pretreatment with Gelofusine. Introduction. Glucagon-like peptide-1 receptor (GLP-1R) imaging, using radiolabeled exendin-4, is recently established for detecting insulinomas in patients with hyperinsulinemic...
The aim of the present study was to investigate, whether the co-injection of gelofusine - the strategy known for somatostatin analogues, might reduce kidney uptake of 99mTc-labelled [Lys40-(Ahx-HYNIC)NH2]exendin-4.
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Results: Gelofusine reduced the renal accumulation of 111 In-exendin-4 by 18.1%, whereas the pancreatic uptake remained unchanged. In 3 of 10 subjects, the kidney uptake was reduced to such an extent that the pancreatic tail could be better discriminated from the kidney signal.
As we hypothesized, the kidney uptake of the directly iodinated [Nle14,125I-Tyr40-NH2]Ex-4.32. Singh G, Eng J, Raufman JP. Use of 125I-[Y39]exendin-4 to characterize exendin receptors on dis-persed pancreatic acini and gastric chief cells from guinea pig.
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High kidney uptake also limits the use of radiolabeled exendin for therapeutic applications.The use of [68Ga]Ga-NOTA-MI-exendin-4 reduced the estimated ab-sorbed kidney dose in both mice and humans by 12%.
Lu-DOTA-MI-exendin-4. The new exendin analogues with a Met-Ile linker showed 23-fold reduced renal retention and improved tumor-to-kidney ratios compared with their reference without the Met-Ile linker.
Reducing kidney uptake of radiolabelled exendin-4 using variants of the renally cleavable linker MVK.Results: Three exendin-4 derivatives, carrying either one MVK, a MV-MVK or a MVK-MVK linker were synthesized and compared to a reference compound lacking a cleavable linker.
