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

Allott, Louis; Amgheib, Ala; Barnes, Chris; Braga, Marta; Brickute, Diana; Wang, Ning; Fu, Ruisi; Ghaem-Maghami, Sadaf; Aboagye, Eric O.


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Dr Louis Allott
Lecturer in Translational Radiopharmaceutics

Ala Amgheib

Chris Barnes

Marta Braga

Diana Brickute

Ning Wang

Ruisi Fu

Sadaf Ghaem-Maghami

Eric O. Aboagye


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 radiochemical yield (RCY) of 19.8 ± 2.6% in 110 min (from start of synthesis); the molar activity was 132.3 ± 14.6 GBq/μmol. 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.


Allott, L., Amgheib, A., Barnes, C., Braga, M., Brickute, D., Wang, N., …Aboagye, E. O. (in press). Radiolabelling an 18F biologic via facile IEDDA “click” chemistry on the GE FASTLab™ platform. Reaction Chemistry and Engineering,

Journal Article Type Article
Acceptance Date Apr 14, 2021
Online Publication Date Apr 15, 2021
Deposit Date Apr 19, 2021
Publicly Available Date Oct 27, 2022
Journal Reaction Chemistry & Engineering
Print ISSN 2058-9883
Publisher Royal Society of Chemistry
Peer Reviewed Peer Reviewed
Public URL


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