Optimization of 177Lu-labelling of DOTA-TOC, PSMA-I&T and FAPI-46 for clinical application

Aylin Cankaya; Matthias Balzer; Holger Amthauer; Winfried Brenner; Sarah Spreckelmeyer

doi:10.1186/s41181-023-00196-1

Optimization of ¹⁷⁷Lu-labelling of DOTA-TOC, PSMA-I&T and FAPI-46 for clinical application

EJNMMI Radiopharm Chem. 2023 May 26;8(1):10. doi: 10.1186/s41181-023-00196-1.

Authors

Aylin Cankaya¹, Matthias Balzer¹, Holger Amthauer¹, Winfried Brenner¹, Sarah Spreckelmeyer²

Affiliations

¹ Charité - Universitätsmedizin Berlin, corporate member of Freie Universität Berlin, Humboldt-Universität zu Berlin, and Berlin Institute of Health, Department of Nuclear Medicine, Augustenburger Platz 1, 13353, Berlin, Germany.
² Charité - Universitätsmedizin Berlin, corporate member of Freie Universität Berlin, Humboldt-Universität zu Berlin, and Berlin Institute of Health, Department of Nuclear Medicine, Augustenburger Platz 1, 13353, Berlin, Germany. sarah.spreckelmeyer@charite.de.

Abstract

Background: ¹⁷⁷Lu-radiopharmaceuticals are routinely used for the treatment of various tumor entities. The productions of radiopharmaceuticals follow strict good-manufacturing practice guidelines and synthesis optimizations thereof have a strong impact on e.g. the quality of the product, radiation safety and costs. The purpose of this study is to optimize the precursor load of three radiopharmaceuticals. For that, different precursor loads were evaluated and compared to previously reported findings.

Results: All three radiopharmaceuticals were successfully synthesized in high radiochemical purities and yields on the ML Eazy. The precursor load was optimized for [¹⁷⁷Lu]Lu-FAPI-46 from 27.0 to 9.7 µg/GBq, for [¹⁷⁷Lu]Lu-DOTATOC from 11 to 10 µg/GBq and for [¹⁷⁷Lu]Lu-PSMA-I&T from 16.3 to 11.6 µg/GBq.

Conclusions: We successfully reduced the precursor load for all three radiopharmaceuticals while maintaining their quality.

Keywords: Automatization; Lutetium-177; Precursor load; Radiopharmaceuticals.