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Article

Automated Radiosynthesis, Preliminary In Vitro/In Vivo Characterization of OncoFAP-Based Radiopharmaceuticals for Cancer Imaging and Therapy

1
Nuclear Medicine, Department of Translational Research and Advanced Technologies in Medicine and Surgery, University of Pisa and Azienda Ospedaliero Universitaria Pisana, 56126 Pisa, Italy
2
Medical Imaging Center, University Medical Center Groningen, University of Groningen, 9712 CP Groningen, The Netherlands
3
Philochem AG, R&D Department, Libernstrasse 3, CH-8112 Otelfingen, Switzerland
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Department of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology, CH-8093 Zurich, Switzerland
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Philogen S.p.A., 53100 Siena, Italy
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Biomedical Photonic Imaging Group, Faculty of Science and Technology, University of Twente, 7522 NB Enschede, The Netherlands
*
Author to whom correspondence should be addressed.
Academic Editors: Aurélie Maisonial-Besset and Fabien Caillé
Pharmaceuticals 2022, 15(8), 958; https://doi.org/10.3390/ph15080958
Received: 23 June 2022 / Revised: 29 July 2022 / Accepted: 29 July 2022 / Published: 2 August 2022
FAP-targeted radiopharmaceuticals represent a breakthrough in cancer imaging and a viable option for therapeutic applications. OncoFAP is an ultra-high-affinity ligand of FAP with a dissociation constant of 680 pM. OncoFAP has been recently discovered and clinically validated for PET imaging procedures in patients with solid malignancies. While more and more clinical validation is becoming available, the need for scalable and robust procedures for the preparation of this new class of radiopharmaceuticals continues to increase. In this article, we present the development of automated radiolabeling procedures for the preparation of OncoFAP-based radiopharmaceuticals for cancer imaging and therapy. A new series of [68Ga]Ga-OncoFAP, [177Lu]Lu-OncoFAP and [18F]AlF-OncoFAP was produced with high radiochemical yields. Chemical and biochemical characterization after radiolabeling confirmed its excellent stability, retention of high affinity for FAP and absence of radiolysis by-products. The in vivo biodistribution of [18F]AlF-NOTA-OncoFAP, a candidate for PET imaging procedures in patients, was assessed in mice bearing FAP-positive solid tumors. The product showed rapid accumulation in solid tumors, with an average of 6.6% ID/g one hour after systemic administration and excellent tumor-to-healthy organs ratio. We have developed simple, quick, safe and robust synthetic procedures for the preparation of theranostic OncoFAP-compounds based on Gallium-68, Lutetium-177 and Fluorine-18 using the commercially available FASTlab synthesis module. View Full-Text
Keywords: 68Ga-labeled; 177Lu-labeled; Al[18F]F-labeled; OncoFAP; automated radiosynthesis; positron emission tomography; radiopharmaceuticals; tumors imaging; theranostics 68Ga-labeled; 177Lu-labeled; Al[18F]F-labeled; OncoFAP; automated radiosynthesis; positron emission tomography; radiopharmaceuticals; tumors imaging; theranostics
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MDPI and ACS Style

Bartoli, F.; Elsinga, P.; Nazario, L.R.; Zana, A.; Galbiati, A.; Millul, J.; Migliorini, F.; Cazzamalli, S.; Neri, D.; Slart, R.H.J.A.; Erba, P.A. Automated Radiosynthesis, Preliminary In Vitro/In Vivo Characterization of OncoFAP-Based Radiopharmaceuticals for Cancer Imaging and Therapy. Pharmaceuticals 2022, 15, 958. https://doi.org/10.3390/ph15080958

AMA Style

Bartoli F, Elsinga P, Nazario LR, Zana A, Galbiati A, Millul J, Migliorini F, Cazzamalli S, Neri D, Slart RHJA, Erba PA. Automated Radiosynthesis, Preliminary In Vitro/In Vivo Characterization of OncoFAP-Based Radiopharmaceuticals for Cancer Imaging and Therapy. Pharmaceuticals. 2022; 15(8):958. https://doi.org/10.3390/ph15080958

Chicago/Turabian Style

Bartoli, Francesco, Philip Elsinga, Luiza Reali Nazario, Aureliano Zana, Andrea Galbiati, Jacopo Millul, Francesca Migliorini, Samuele Cazzamalli, Dario Neri, Riemer H. J. A. Slart, and Paola Anna Erba. 2022. "Automated Radiosynthesis, Preliminary In Vitro/In Vivo Characterization of OncoFAP-Based Radiopharmaceuticals for Cancer Imaging and Therapy" Pharmaceuticals 15, no. 8: 958. https://doi.org/10.3390/ph15080958

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