{"id":6471,"date":"2025-05-09T09:29:00","date_gmt":"2025-05-09T07:29:00","guid":{"rendered":"https:\/\/www.m2olie.de\/?post_type=publications&#038;p=6471"},"modified":"2025-10-09T09:59:17","modified_gmt":"2025-10-09T07:59:17","slug":"development-and-clinical-potential-of-18f-psima-for-prostate-cancer-pet-imaging-rsc-medicinal-chemistry","status":"publish","type":"publications","link":"https:\/\/www.m2olie.de\/en\/publications\/development-and-clinical-potential-of-18f-psima-for-prostate-cancer-pet-imaging-rsc-medicinal-chemistry\/","title":{"rendered":"Development and Clinical Potential of 18F-PSiMA for Prostate Cancer PET Imaging."},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">Gower-Fry L, Bailey JJ, Wuest M, Pike S, Kostikov A, Dorian A, W\u00e4ngler C, Wuest F, Schirrmacher R (<strong>2025<\/strong>) Development and Clinical Potential of <sup>18<\/sup>F-PSiMA for Prostate Cancer PET Imaging. <em>RSC Medicinal Chemistry, 16(8)<\/em>, 3633\u20133644. <br><strong>DOI<\/strong>: <a href=\"https:\/\/pubs.rsc.org\/en\/content\/articlehtml\/2025\/md\/d5md00275c\" target=\"_blank\" rel=\"noreferrer noopener\">10.1039\/d5md00275c.<\/a><\/p>\n\n\n\n<h2 class=\"wp-block-heading\">Abstract<\/h2>\n\n\n\n<p class=\"wp-block-paragraph\">Prostate-specific membrane antigen (PSMA) is a key target for diagnosing prostate cancer through positron emission tomography (PET). While\u00a0<sup>68<\/sup>Ga-labeled PSMA compounds are widely used,\u00a0<sup>18<\/sup>F-labeled PSMA inhibitors have gained traction for clinical tumor imaging. We previously investigated PSMA-targeting compounds based on the Lys-urea-Glu motif, incorporating a silicon fluoride-acceptor (SiFA) and chemical auxiliaries to enhance\u00a0<em>in vivo<\/em>\u00a0biodistribution. This led to the development of\u00a0<sup>18<\/sup>F-PSiMA, a SiFA-based radiotracer with an optimized linker exhibiting favorable PSMA potency (IC<sub>50<\/sub>\u00a0= 154 \u00b1 47 nM in LNCaP cells).\u00a0<sup>18<\/sup>F-PSiMA radiosynthesis with low to high concentrations of\u00a0<sup>18<\/sup>F and precursor achieved molar activities (<em>A<\/em><sub>m<\/sub>) of 10.9\u201382.5 GBq \u03bcmol<sup>\u22121<\/sup>\u00a0and showed a 24\u201338% increase in tumor uptake in LNCaP tumors (SUV<sub>60min<\/sub>\u00a01.56 \u00b1 0.18; 7.23 \u00b1 0.75% ID per g at lower\u00a0<em>A<\/em><sub>m<\/sub>\u00a0and SUV<sub>60min<\/sub>\u00a01.90 \u00b1 0.29; 9.62 \u00b1 1.29% ID per g at higher\u00a0<em>A<\/em><sub>m<\/sub>) compared to our previous lead,\u00a0<sup>18<\/sup>F-SiFA-Asp<sub>2<\/sub>-PEG<sub>3<\/sub>-PSMA. PSMA specificity was confirmed by a 20 \u00b1 10% reduction in SUV<sub>60min<\/sub>\u00a0upon co-injection with DCFPyl. These promising\u00a0<em>in vitro<\/em>\u00a0and\u00a0<em>in vivo<\/em>\u00a0results support further clinical translation of\u00a0<sup>18<\/sup>F-PSiMA for prostate cancer PET imaging.<\/p>\n","protected":false},"featured_media":0,"comment_status":"open","ping_status":"closed","template":"","meta":{"footnotes":""},"categories":[],"class_list":["post-6471","publications","type-publications","status-publish","hentry"],"_links":{"self":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/6471","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=6471"}],"version-history":[{"count":4,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/6471\/revisions"}],"predecessor-version":[{"id":6917,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/publications\/6471\/revisions\/6917"}],"wp:attachment":[{"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/media?parent=6471"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.m2olie.de\/en\/wp-json\/wp\/v2\/categories?post=6471"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}