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- W2100647824 abstract "The translation of radiolabeled tumor-targeting peptides into clinical routine is often hampered by an enhanced accumulation into the excreting organs. It has recently been reported that the (EH)<sub>3</sub> purification tag is able to improve the biodistribution of Affibody molecules. Therefore, the aim of this study was to prove the positive influence of (EH)<sub>3</sub> on the biodistribution of 2 peptidic radiopharmaceuticals, Glu-urea-Lys(Ahx)-HBED-CC and TATE-PEG<sub>2</sub>-HBED-CC (HBED-CC is <i>N,N</i>′-bis [2-hydroxy-5(carboxyethyl)benzyl] ethylenediamine-<i>N,N</i>′- diacetic acid, TATE is octreotate, and PEG<sub>2</sub> is 8-amino-3,6-dioxaoctanoic acid spacer). <b>Methods:</b> Both compounds were compared with their respective (EH)<sub>3</sub>-conjugated variants in cell-based in vitro assays and organ distribution. <b>Results:</b> The introduction of (EH)<sub>3</sub> to HBED-CC significantly changed the biodistribution profiles. In both cases, the uptake in several organs was reduced whereas tumor uptake was not affected. Most importantly, (EH)<sub>3</sub> lowered the kidney and liver uptake of the prostate-specific membrane antigen inhibitor each by a factor of 2.8 and, in the case of octreotate, the liver accumulation by a factor of 51. <b>Conclusion:</b> The biodistribution data suggest that (EH)<sub>3</sub> is able to improve the pharmacokinetic properties of peptidic radiopharmaceuticals, leading to reduced uptake in organs such as the liver, an important site of metastatic disease." @default.
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- W2100647824 date "2013-06-26" @default.
- W2100647824 modified "2023-10-14" @default.
- W2100647824 title "Pharmacokinetic Properties of Peptidic Radiopharmaceuticals: Reduced Uptake of (EH)<sub>3</sub>-Conjugates in Important Organs" @default.
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- W2100647824 doi "https://doi.org/10.2967/jnumed.112.114512" @default.
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