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[18F]FET-βAG-TOCA: the design, evaluation and clinical translation of a fluorinated octreotide

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Title: [18F]FET-βAG-TOCA: the design, evaluation and clinical translation of a fluorinated octreotide
Authors: Allott, L
Dubash, S
Aboagye, EO
Item 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.
Issue Date: 2-Apr-2020
Date of Acceptance: 31-Mar-2020
URI: http://hdl.handle.net/10044/1/79096
DOI: 10.3390/cancers12040865
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/).
Sponsor/Funder: Medical Research Council (MRC)
Funder's Grant Number: MR/J007986/1
Keywords: 2-[18F]fluoroethylazide
Lutathera
clinical translation
fluorine-18
octreotide
positron emission tomography
radiopharmaceuticals
2-[18F]fluoroethylazide
Lutathera
clinical translation
fluorine-18
octreotide
positron emission tomography
radiopharmaceuticals
1112 Oncology and Carcinogenesis
Publication Status: Published
Conference Place: Switzerland
Article Number: ARTN 865
Appears in Collections:Department of Surgery and Cancer