用于临床应用的DOTA-TOC、PSMA-I&T和FAPI-46的镥标记优化

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

作者信息

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

机构信息

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.

出版信息

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

DOI:10.1186/s41181-023-00196-1

PMID:37233924

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10219910/

Abstract

BACKGROUND

Lu-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 [Lu]Lu-FAPI-46 from 27.0 to 9.7 µg/GBq, for [Lu]Lu-DOTATOC from 11 to 10 µg/GBq and for [Lu]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.

摘要

背景

镥放射性药物通常用于治疗各种肿瘤实体。放射性药物的生产遵循严格的药品生产质量管理规范指南，其合成优化对例如产品质量、辐射安全性和成本有很大影响。本研究的目的是优化三种放射性药物的前体负载量。为此，评估了不同的前体负载量，并与先前报道的结果进行了比较。

结果

所有三种放射性药物均在ML Eazy上以高放射化学纯度和产率成功合成。[镥]镥-FAPI-46的前体负载量从27.0微克/吉贝可优化至9.7微克/吉贝可，[镥]镥-DOTATOC的前体负载量从11微克/吉贝可优化至10微克/吉贝可，[镥]镥-PSMA-I&T的前体负载量从16.3微克/吉贝可优化至11.6微克/吉贝可。