Radiolabelling an 18F biologic via facile IEDDA “click” chemistry on the GE FASTLab™ platform,Reaction Chemistry & Engineering

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Radiolabelling an 18F biologic via facile IEDDA “click” chemistry on the GE FASTLab™ platform
Reaction Chemistry & Engineering ( IF 3.4 ) Pub Date : 2021-4-15 , DOI: 10.1039/d1re00117e
Louis Allott _{1,

2,

3} , Ala Amgheib _{1,

4} , Chris Barnes ₁ , Marta Braga ₁ , Diana Brickute ₁ , Ning Wang ₁ , Ruisi Fu ₁ , Sadaf Ghaem-Maghami _{1,

4} , Eric O Aboagye ₁

Affiliation

The use of biologics in positron emission tomography (PET) imaging is an important area of radiopharmaceutical development and new automated methods are required to facilitate their production. We report an automated radiosynthesis method to produce a radiolabelled biologic via facile inverse electron demand Diels–Alder (IEDDA) “click” chemistry on a single GE FASTLab™ cassette. We exemplified the method by producing a fluorine-18 radiolabelled interleukin-2 (IL2) radioconjugate from a trans-cyclooctene (TCO) modified IL2 precursor. The radioconjugate was produced using a fully automated radiosynthesis on a single FASTLab™ cassette in a decay-corrected radiochemical yield (RCY, d.c.) of 19.8 ± 2.6% in 110 min (from start of synthesis); the molar activity was 132.3 ± 14.6 GBq μmol⁻¹. The in vitro uptake of [¹⁸F]TTCO-IL2 correlated with the differential receptor expression (CD25, CD122, CD132) in PC3, NK-92 and activated human PBMCs. The automated method may be adapted for the radiosynthesis of any TCO-modified protein via IEDDA chemistry.

中文翻译：

在 GE FASTLab™ 平台上通过简单的 IEDDA“点击”化学对 18F 生物制品进行放射性标记

生物制剂在正电子发射断层扫描 (PET) 成像中的使用是放射性药物开发的一个重要领域，需要新的自动化方法来促进其生产。我们报告了一种自动放射合成方法，通过在单个 GE FASTLab™ 盒上简便的逆电子需求 Diels-Alder (IEDDA)“点击”化学来生产放射性标记的生物制品。我们通过从反式环辛烯 (TCO) 修饰的 IL2 前体生产氟 18 放射性标记的白细胞介素 2 (IL2) 放射性缀合物来举例说明该方法。放射性结合物是在单个 FASTLab™ 盒上使用全自动放射合成生产的，110 分钟内（从合成开始）衰减校正放射化学产率（RCY，dc）为 19.8 ± 2.6%；摩尔活度为132.3±14.6 GBq μmol ^-1。[ ¹⁸ F]TTCO-IL2 的体外摄取与 PC3、NK-92 和活化的人 PBMC 中的差异受体表达（CD25、CD122、CD132）相关。自动化方法可适用于通过IEDDA 化学放射合成任何 TCO 修饰的蛋白质。

更新日期：2021-04-23

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