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.

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 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.

Citation

Allott, L., Amgheib, A., Barnes, C., Braga, M., Brickute, D., Wang, N., Fu, R., Ghaem-Maghami, S., & Aboagye, E. O. (in press). Radiolabelling an 18F biologic via facile IEDDA “click” chemistry on the GE FASTLab™ platform. Reaction Chemistry and Engineering, https://doi.org/10.1039/d1re00117e

• Journal Article Type: Article
• Acceptance Date: Apr 14, 2021
• Online Publication Date: Apr 15, 2021
• Deposit Date: Apr 19, 2021
• Publicly Available Date: May 26, 2021
• Journal: Reaction Chemistry & Engineering
• Print ISSN: 2058-9883
• Publisher: Royal Society of Chemistry
• Peer Reviewed: Peer Reviewed
• DOI: https://doi.org/10.1039/d1re00117e
• Public URL: https://hull-repository.worktribe.com/output/3757315