2023
DOI: 10.1186/s41181-023-00206-2
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Reducing kidney uptake of radiolabelled exendin-4 using variants of the renally cleavable linker MVK

Belinda Trachsel,
Giulia Valpreda,
Alexandra Lutz
et al.

Abstract: Background Peptidic radiotracers are preferentially excreted through the kidneys, which often results in high persistent renal retention of radioactivity, limiting or even preventing therapeutic clinical translation of these radiotracers. Exendin-4, which targets the glucagon-like-peptide 1 receptor (GLP-1R) overexpressed in insulinomas and in congenital hyperinsulinism, is an example thereof. The use of the tripeptide MVK, which is readily cleaved between methionine and valine by neprilysin at… Show more

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Cited by 3 publications
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“…Furthermore, the replacement of Lys by Arg was shown to effectively lead to reduced kidney uptake of radiolabeled peptides or metabolites thereof [ 50 , 51 ]. Finally, the use of cleavable linkers specific for enzymes present at the renal brush border membrane of kidneys have shown promising results [ 52 , 53 ]. Such approaches will be investigated in the future in order to improve the pharmacokinetic properties of our lead compound [ 111 In]In-XG1.…”
Section: Resultsmentioning
confidence: 99%
“…Furthermore, the replacement of Lys by Arg was shown to effectively lead to reduced kidney uptake of radiolabeled peptides or metabolites thereof [ 50 , 51 ]. Finally, the use of cleavable linkers specific for enzymes present at the renal brush border membrane of kidneys have shown promising results [ 52 , 53 ]. Such approaches will be investigated in the future in order to improve the pharmacokinetic properties of our lead compound [ 111 In]In-XG1.…”
Section: Resultsmentioning
confidence: 99%