[F]PARPi的全自动高剂量放射性合成

Pacelli Anna, Zarrad Fadi, Fendler Wolfgang P, Herrmann Ken, Nader Michael

Klinik für Nuklearmedizin, Universitätsklinikum Essen (AöR), Hufelandstraße 55, D-45147 Essen, Germany.

Pharmaceuticals (Basel). 2022 Jul 14;15(7):865. doi: 10.3390/ph15070865.

[F]PARPi is currently undergoing clinical trials as a PET tracer for many applications. However, only manual radiosynthesis was reported; this has several drawbacks, including an increased risk of contamination from the operator, and the need to limit the starting activity. The automation of the previously reported protocol for [F]PARPi synthesis is challenging, as it requires transferring microvolumes of reagents, which many platforms cannot accommodate. We report a revised, high yield, and automated protocol for the radiosynthesis of [F]PARPi, with final doses of over 20 GBq.

[F]PARPi目前正在作为一种PET示踪剂进行多种应用的临床试验。然而，此前仅报道了手动放射性合成方法；这种方法存在几个缺点，包括操作人员污染风险增加以及需要限制起始活度。对先前报道的[F]PARPi合成方案进行自动化具有挑战性，因为它需要转移微升体积的试剂，而许多平台无法做到这一点。我们报告了一种经修订的、高产率且自动化的[F]PARPi放射性合成方案，最终剂量超过20GBq。