Radiolabelling an F-18 biologic via facile IEDDA "click" chemistry on the GE FASTLab (TM) platform
File(s)
Published version
Author(s)
Type
Journal Article
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.
Date Issued
2021-04-15
Date Acceptance
2021-04-14
Citation
Reaction Chemistry and Engineering, 2021, 6 (6), pp.1070-1078
ISSN
2058-9883
Publisher
Royal Society of Chemistry
Start Page
1070
End Page
1078
Journal / Book Title
Reaction Chemistry and Engineering
Volume
6
Issue
6
Copyright Statement
© The Royal Society of Chemistry 2021. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
License URL
Sponsor
Imperial College Healthcare NHS Trust- BRC Funding
Imperial College Healthcare NHS Trust
Identifier
http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000642563400001&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
Grant Number
RDC04
RDB22 79560
Subjects
Science & Technology
Physical Sciences
Technology
Chemistry, Multidisciplinary
Engineering, Chemical
Chemistry
Engineering
Publication Status
Published
Date Publish Online
2021-04-15