[18F]FET-βAG-TOCA: the design, evaluation and clinical translation of a fluorinated octreotide
File(s)cancers-12-00865.pdf (2.69 MB)
Published version
Author(s)
Allott, Louis
Dubash, Suraiya
Aboagye, Eric O
Type
Journal Article
Abstract
The success of Lutathera™ ([177Lu]Lu-DOTA-TATE) in the NETTER-1 clinical trial as a peptide receptor radionuclide therapy (PRRT) for somatostatin receptor expressing (SSTR) neuroendocrine tumours (NET) is likely to increase the demand for patient stratification by positron emission tomography (PET). The current gold standard of gallium-68 radiolabelled somatostatin analogues (e.g., [68Ga]Ga-DOTA-TATE) works effectively, but access is constrained by the limited availability and scalability of gallium-68 radiopharmaceutical production. The aim of this review is three-fold: firstly, we discuss the peptide library design, biological evaluation and clinical translation of [18F]fluoroethyltriazole-βAG-TOCA ([18F]FET-βAG-TOCA), our fluorine-18 radiolabelled octreotide; secondly, to exemplify the potential of the 2-[18F]fluoroethylazide prosthetic group and copper-catalysed azide-alkyne cycloaddition (CuAAC) chemistry in accessing good manufacturing practice (GMP) compatible radiopharmaceuticals; thirdly, we aim to illustrate a framework for the translation of similarly radiolabelled peptides, in which in vivo pharmacokinetics drives candidate selection, supported by robust radiochemistry methodology and a route to GMP production. It is hoped that this review will continue to inspire the development and translation of fluorine-18 radiolabelled peptides into clinical studies for the benefit of patients.
Date Issued
2020-04-02
Date Acceptance
2020-03-31
Citation
Cancers, 2020, 12 (4)
ISSN
2072-6694
Publisher
MDPI AG
Journal / Book Title
Cancers
Volume
12
Issue
4
Copyright Statement
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access
article distributed under the terms and conditions of the Creative Commons Attribution
(CC BY) license (http://creativecommons.org/licenses/by/4.0/).
article distributed under the terms and conditions of the Creative Commons Attribution
(CC BY) license (http://creativecommons.org/licenses/by/4.0/).
Sponsor
Medical Research Council (MRC)
Identifier
https://www.ncbi.nlm.nih.gov/pubmed/32252406
PII: cancers12040865
Grant Number
MR/J007986/1
Subjects
2-[18F]fluoroethylazide
Lutathera
clinical translation
fluorine-18
octreotide
positron emission tomography
radiopharmaceuticals
Publication Status
Published
Coverage Spatial
Switzerland
Article Number
ARTN 865