{"id":10225,"date":"2026-01-15T20:36:13","date_gmt":"2026-01-15T19:36:13","guid":{"rendered":"https:\/\/www.m2olie.de\/?post_type=publications&#038;p=10225"},"modified":"2026-06-28T20:41:09","modified_gmt":"2026-06-28T18:41:09","slug":"comparison-of-two-18f-fluorinated-glycopeptides-for-pet-imaging-of-the-functional-liver-mass","status":"publish","type":"publications","link":"https:\/\/www.m2olie.de\/en\/publications\/comparison-of-two-18f-fluorinated-glycopeptides-for-pet-imaging-of-the-functional-liver-mass\/","title":{"rendered":"Comparison of two\u00a018F-fluorinated glycopeptides for PET imaging of the functional liver mass"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">Zierke MA, Hofer K, Samadikhah K, Rangger C, W\u00e4ngler C, W\u00e4ngler B, Junker A, Schmid AM, Haubner R (2026) Comparison of two <sup>18<\/sup>F-Fluorinated Glycopeptides for PET Imaging of the Functional Liver Mass. <em>EJNMMI Radiopharmacy and Chemistry, 11(1)<\/em>, 35.<br><strong>DOI<\/strong>:\u00a0<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/41934561\/\" target=\"_blank\" rel=\"noreferrer noopener\">10.1186\/s41181-026-00445-z.<\/a><\/p>\n\n\n\n<h2 class=\"wp-block-heading\">Abstract<\/h2>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Background:\u00a0<\/strong>The non-invasive determination of the asialoglycoprotein receptor (ASGR) expression on liver tissue might be a predictive parameter helping to prevent severe liver diseases as well as liver failure after surgery and transplantation. Recently, we introduced [<sup>68<\/sup>Ga]Ga-NODAGA-NonaLysan, which showed even a higher liver uptake as the gold standard [<sup>99m<\/sup>Tc]Tc-Galactosyl Serum Albumin. Here we describe the synthesis and evaluation of two\u00a0<sup>18<\/sup>F-labeled analogues, prepared using either a SiFA- or an AlF-labeling approach.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Results:\u00a0<\/strong>The two precursors could be produced in high purity (> 97%). Both labeling strategies allowed production of the radiopharmaceuticals in high radiochemical purity. The radiochemical yield was up to 58% d.c. for [<sup>18<\/sup>F]SiFA-NonaLysan and up to 71% d.c. for Al[<sup>18<\/sup>F]F-NOTA-6-Ahx-NonaLysan. In vitro evaluation showed high stability in PBS and human serum. Both compounds possessed nanomolar affinity for the ASGR (IC<sub>50<\/sub>\u00a0= 0.9 \u00b1 1.1 nM and 3.0 \u00b1 2.1 nM, respectively). However, based on the design differences, Al[<sup>18<\/sup>F]F-NOTA-6-Ahx-NonaLysan showed a 100-fold lower logD as found for [<sup>18<\/sup>F]SiFA-NonaLysan. In consequence, the protein binding effect was higher for [<sup>18<\/sup>F]SiFA-NonaLysan, and the lipophilic character drastically affected the pharmacokinetic pattern. Initial liver uptake was higher for [<sup>18<\/sup>F]SiFA-NonaLysan (100% ID\/g vs. 70% ID\/g 10 min p.i.), but was accompanied by a quick organ washout and activity accumulation in the intestines. A much better activity retention was observed for Al[<sup>18<\/sup>F]F-NOTA-6-Ahx-NonaLysan. PET\/MR imaging confirmed the differences in liver uptake, with a higher retention found for the latter. Based on the receptor function, both compounds are internalized and subsequently degraded. For Al[<sup>18<\/sup>F]F-NOTA-6-Ahx-NonaLysan, all radioactive liver metabolites found were more hydrophilic than the intact compound. For [<sup>18<\/sup>F]SiFA-NonaLysan, the contrary is the case, and almost all liver metabolites were more lipophilic. The hepatobiliary excretion of these metabolites prevents a stable activity retention in the hepatic tissue.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Conclusion:\u00a0<\/strong>In this study, we successfully synthesized two new\u00a0<sup>18<\/sup>F-labeled radiopharmaceuticals targeting the ASGR. The in vivo evaluation revealed two different pharmacokinetic profiles. Extremely high uptake was found for [<sup>18<\/sup>F]SiFA-NonaLysan in the initial phase, followed by a quick organ washout. Al[<sup>18<\/sup>F]F-NOTA-6-Ahx-NonaLysan showed a lower but more stable activity retention in the liver, indicating advantageous imaging properties.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Keywords<\/strong>:\u00a0<br>Aluminum fluoride; Asialoglycoprotein receptor; Fluorine-18; Positron emission tomography; Silicon-fluoride acceptor.<\/p>\n","protected":false},"featured_media":0,"comment_status":"open","ping_status":"closed","template":"","meta":{"footnotes":""},"categories":[],"class_list":["post-10225","publications","type-publications","status-publish","hentry"],"_links":{"self":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/10225","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications"}],"about":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/types\/publications"}],"replies":[{"embeddable":true,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/comments?post=10225"}],"version-history":[{"count":1,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/10225\/revisions"}],"predecessor-version":[{"id":10226,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/10225\/revisions\/10226"}],"wp:attachment":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/media?parent=10225"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/categories?post=10225"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}