an-automated-radiosynthesis-of-68gaga-fapi-46-for-routine-clinical-use

An Automated Radiosynthesis of [<sup>68</sup>Ga]Ga-FAPI-46 for Routine Clinical Use

[68Ga]Ga-FAPI-46 is a promising new tracer for the imaging of fibroblast activation protein (FAP) by positron emission tomography (PET). Labeled FAP ...

Sir Charles Gairdner Hospital

University of Western Australia

The aim of this preclinical study was to directly compare [F]PSMA-1007 with both [Ga]Ga-PSMA-11 and [F]AlF-PSMA-11 in mice bearing PSMA-positive tumor xenografts. Uptake was assessed by PET/CT at 1, 2 and 4 h post-injection, and by ex vivo measurement after 4 h. [F]PSMA-1007 demonstrated the highest tumor uptake of the three tracers. The high uptake in bone for mice injected with [F]AlF-PSMA-11 suggested rapid in vivo decomposition. This was confirmed by an in vitro plasma stability study.

Direct in vivo comparison of [F]PSMA-1007 with [Ga]Ga-PSMA-11 and [F]AlF-PSMA-11 in mice bearing PSMA-expressing xenografts.

Since first becoming commercially available in 2018, the PET radiopharmaceutical [ F]PSMA-1007 has been used widely for the diagnosis and staging of prostate cancer. A pharmacopoeia monograph first became available in 2021, prescribing a radiochemical purity specification of >91%, based on analytical results from both TLC (for [ F]fluoride impurity alone) and HPLC (for all other  F-impurities). Though this monograph has provided clarity for the quality control testing of [ F]PSMA-1007, it prescribes a HPLC method using phosphate buffer mobile phase that may present a risk of precipitation of phosphate salts in the HPLC system. The method also requires specialised hardware not immediately available to all laboratories. This work describes the development of a simple, rapid reversed-phase HPLC method utilising 0.1 M ammonium formate mobile phase for the accurate assessment of both [ F]fluoride impurity and overall radiochemical purity in a single test. This method is especially useful for assessment of product stability over time. A more accurate TLC method for [ F]fluoride impurity is also described.

Development of a high-performance liquid chromatography method for rapid radiochemical purity measurement of [ F]PSMA-1007, a PET radiopharmaceutical for detection of prostate cancer.

Article	Year
Direct in vivo comparison of [F]PSMA-1007 with [Ga]Ga-PSMA-11 and [F]AlF-PSMA-11 in mice bearing PSMA-expressing xenografts. Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine\| PubMed ID: 32321698	2020
Development of a high-performance liquid chromatography method for rapid radiochemical purity measurement of [ F]PSMA-1007, a PET radiopharmaceutical for detection of prostate cancer. Journal of labelled compounds & radiopharmaceuticals\| PubMed ID: 36649714	2023

Joseph A. Ioppolo

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