Issue 6, 2021

Radiolabelling an 18F biologic via facile IEDDA “click” chemistry on the GE FASTLab™ platform

Abstract

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.

Graphical abstract: Radiolabelling an 18F biologic via facile IEDDA “click” chemistry on the GE FASTLab™ platform

Supplementary files

Article information

Article type
Paper
Submitted
25 3 2021
Accepted
14 4 2021
First published
15 4 2021
This article is Open Access
Creative Commons BY license

React. Chem. Eng., 2021,6, 1070-1078

Radiolabelling an 18F biologic via facile IEDDA “click” chemistry on the GE FASTLab™ platform

L. Allott, A. Amgheib, C. Barnes, M. Braga, D. Brickute, N. Wang, R. Fu, S. Ghaem-Maghami and E. O. Aboagye, React. Chem. Eng., 2021, 6, 1070 DOI: 10.1039/D1RE00117E

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