| Report number | MED-035 |
| Title | 153SM-FAPI-46 RADIOLIGAND THERAPY WITH HIGH-MOLAR ACTIVITY 153SM |
| Author(s) | Prior, John (CHUV) ; Kratochwill, Clemens (Heidelberg University Hospital) ; Ooms, Marteen (SCK CEN) ; Cocolios, Thomas Elias (KU Leuven (BE)) ; Decristoforo, Clemens (INMUL) |
| Publication | 2023 |
| Imprint | 2023-03-21 |
| Number of pages | 3 |
| Keywords | MEDICIS; isotope mass separation; Samarium-153; high molar activity; high specific activity;theranostics;clinical translation |
| Abstract | New radiobioconjugates targeting fibroblast overexpressed in certain forms of cancers have recently been developed by the dept of nuclear medicine in Heidelberg and have shown important results in a range of different preclinical and clinical investigations. It demonstrates the potential of a new generation of radiopharmaceuticals targeting the Fibroblast Activation Protein (FAP), quinolone-based FAP inhibitors (FAPI) with a DOTA-chelator moiety and have shown potential benefits in both diagnosis and treatment, including patients presenting disseminated metastasis in lungs. As already investigated with FAPI-04, rapid tumor-targeting and kidney clearance but also a relatively short residency time in tumor is observed and therefore needs to find better suited radionuclides than 90Y or 177Lu, with shorter physical half-life, beta and photon emitting properties for theranostic investigations. A first pilot study was performed in Heidelberg with Low Molar Activity (LMA) Samarium-153 FAPI-46. Samarium-153 has a half-life of 46.8h, beta particles (Eave 225keV, Emax 806keV), and has a photon (103keV) making it an ideal radionuclide for theranostics investigations with FAPI . Further investigations to identify its potential in imaging contrast, biokinetics and ultimately therapeutics benefits with a High Molar Activity (HMA) grade 153Sm-FAPI46 are required, because according to preliminary data presented at the “Nuklearmedizin-2022” (nuclear-medicine convention of the D-A-CH states), receptor-saturation due to poor specific activity of the radiopharmaceutical likely presents a relevant limitation for this kind of treatment. Indeed, the low molar activity form of Samarium-153 has long been known for pain palliation, marketed as Quadramet ® in the form of 153Sm-EDTMP for patients suffering of an advanced staged cancers with bone metastasis. Until recently it was not possible to target other tumors because of the mode of production by target activation in a nuclear reactor and its production in LMA form. Recently the synthesis of high molar activity (HMA) 153Sm-DOTATATE obtained from an activated target in a nuclear reactor and subsequent mass separation produced HMA 153Sm within MED-025 project has shown its suitability for imaging and therapeutic benefits in animal models to target NET tumors. |
| Submitted by | thierry.stora@cern.ch |
Record created 2023-03-21, last modified 2023-05-17
