Abstract
Abstract
Background
[68Ga]Ga-FAPI-46 is a promising radiopharmaceutical for in vivo detection of the fibroblast activation protein by positron emission tomography. Until now, the synthesis of [68Ga]Ga-FAPI-46 has been only performed manually. Our aim was to evaluate the automated synthesis of this radiopharmaceutical on two different commercially available synthesis modules in order to make the tracer readily available for clinical application.
Results
The synthesis of [68Ga]Ga-FAPI-46 with different amounts of precursor (10–50 μg) on the Modular Lab PharmTracer (MLPT) and Modular Lab eazy (ML eazy) from Eckert & Ziegler with a customized synthesis template and a customized single-use cassette yielded best results with 50 μg FAPI-46 for clinical multi-dose application. All relevant quality control parameters tested (e.g. sterility, stability and radiochemical purity) were in accordance with the European Pharmacopoeia.
Conclusions
[68Ga]Ga-FAPI-46 was successfully synthesized fully-automated on the synthesis modules Modular Lab PharmTracer and ML eazy and is, thus, available for multi-dose application in clinical settings.
Publisher
Springer Science and Business Media LLC
Subject
Pharmacology (medical),Pharmacology,Radiology Nuclear Medicine and imaging,Analytical Chemistry
Reference9 articles.
1. Boschi S, Lodi F, Malizia C, Cicoria G, Marengo M. Automation synthesis modules review. Appl Radiat Isot. 2013;76:38–45.
2. Brennen WN, Isaacs JT, Denmeade SR. Rationale behind targeting fibroblast activation protein-expressing carcinoma-associated fibroblasts as a novel chemotherapeutic strategy. Mol Cancer Ther. 2012;11(2):257–66.
3. Giesel F, Adeberg S, Syed M, Lindner T, Jimenez LD, Mavriopoulou E, Staudinger F, Tonndorf-Martini E, Regnery S, Rieken S, ElShafie R, Rohrich M, Flechsig P, Kluge A, Altmann A, Debus J, Haberkorn UA, Kratochwil C. FAPI-74 PET/CT using either (18)F-AlF or cold-kit (68)Ga-labeling: biodistribution, radiation Dosimetry and tumor delineation in lung Cancer patients. J Nucl Med. 2020;59(9):1415-22.
4. Jansen K, Heirbaut L, Cheng JD, Joossens J, Ryabtsova O, Cos P, Maes L, Lambeir AM, De Meester I, Augustyns K, Van der Veken P. Selective inhibitors of fibroblast activation protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine scaffold. ACS Med Chem Lett. 2013;4(5):491–6.
5. Lindner T, Loktev A, Altmann A, Giesel F, Kratochwil C, Debus J, Jager D, Mier W, Haberkorn U. Development of Quinoline-based Theranostic ligands for the targeting of fibroblast activation protein. J Nucl Med. 2018;59(9):1415–22.
Cited by
24 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献