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[F]PARPi的全自动高剂量放射性合成

Fully Automated, High-Dose Radiosynthesis of [F]PARPi.

作者信息

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

机构信息

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

出版信息

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

DOI:10.3390/ph15070865
PMID:35890164
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9317788/
Abstract

[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.

摘要

[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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/cb50f4f24ee9/pharmaceuticals-15-00865-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/35f6ff8b54e5/pharmaceuticals-15-00865-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/7be2d55f58e6/pharmaceuticals-15-00865-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/bf7c3015b771/pharmaceuticals-15-00865-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/2e2e5cd7997d/pharmaceuticals-15-00865-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/0e470901c4b8/pharmaceuticals-15-00865-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/486615d1cdb0/pharmaceuticals-15-00865-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/6ebfc503ea14/pharmaceuticals-15-00865-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/cb50f4f24ee9/pharmaceuticals-15-00865-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/35f6ff8b54e5/pharmaceuticals-15-00865-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/7be2d55f58e6/pharmaceuticals-15-00865-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/bf7c3015b771/pharmaceuticals-15-00865-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/2e2e5cd7997d/pharmaceuticals-15-00865-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/0e470901c4b8/pharmaceuticals-15-00865-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/486615d1cdb0/pharmaceuticals-15-00865-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/6ebfc503ea14/pharmaceuticals-15-00865-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7519/9317788/cb50f4f24ee9/pharmaceuticals-15-00865-g006.jpg

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