[18F]ZCDD083: a PFKFB3-targeted PET tracer for atherosclerotic plaque imaging

Carlo De Dominicis, Paola Perrotta, Sergio Dall'angelo, Leonie Wyffels, Steven Staelens* (Corresponding Author), G. R. Y. de Meyer* (Corresponding Author), Matteo Zanda* (Corresponding Author)

*Corresponding author for this work

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PFKFB3, a glycolysis-related enzyme upregulated in inflammatory conditions and angiogenesis, is an emerging target for diagnosis and therapy of atherosclerosis. The fluorinated phenoxindazole [18F]ZCDD083 was synthesized, radiolabeled in 17 ± 5% radiochemical yield and >99% radiochemical purity, and formulated for preclinical PET/CT imaging in mice. In vivo stability analysis showed no significant metabolite formation. Biodistribution studies showed high blood pool activity and slow hepatobiliary clearance. Significant activity was detected in the lung 2 h postinjection (pi) (11.0 ± 1.5%ID/g), while at 6 h pi no pulmonary background was observed. Ex vivo autoradiography at 6 h pi showed significant high uptake of [18F]ZCDD083 in the arch region and brachiocephalic artery of atherosclerotic mice, and no uptake in control mice, matching plaques distribution seen by lipid staining along with PFKFB3 expression seen by immunofluorescent staining. In vivo PET scans showed higher aortic region uptake of [18F]ZCDD083 in atherosclerotic ApoE-/-Fbn1C1039G+/- than in control mice (0.78 ± 0.05 vs 0.44 ± 0.09%ID/g). [18F]ZCDD083 was detected in aortic arch and brachiocephalic artery of ApoE-/- (with moderate atherosclerosis) and ApoE-/-Fbn1C1039G+/- (with severe, advanced atherosclerosis) mice, suggesting this tracer may be useful for the noninvasive detection of atherosclerotic plaques in vivo.

Original languageEnglish
Pages (from-to)933-939
Number of pages7
JournalACS Medicinal Chemistry Letters
Issue number5
Early online date19 Feb 2020
Publication statusPublished - 14 May 2020

Bibliographical note

Copyright © 2020 American Chemical Society.

We thank the European Union’s Horizon 2020 research and
innovation program under the Marie Sklodowska-Curie ITNEuropean Joint Doctorate MOGLYNET (grant agreement No.


  • Atherosclerosis
  • plaque
  • fluorine
  • PET imaging
  • glycolysis
  • preclinical


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