Biodistribution and first clinical results of 18F-SiFAlin-TATE PET: a novel 18F-labeled somatostatin analog for imaging of neuroendocrine tumors

Ilhan, Harun; Lindner, Simon; Todica, Andrei; Cyran, Clemens C.; Tiling, Reinhold; Auernhammer, Christoph J.; Spitzweg, Christine; Boeck, Stefan; Unterrainer, Marcus; Gildehaus, Franz Josef; Böning, Guido; Jurkschat, Klaus; Wängler, Carmen; Wängler, Björn; Schirrmacher, Ralf; Bartenstein, Peter

doi:10.1007/s00259-019-04501-6

Cited by 75 publications

(87 citation statements)

References 24 publications

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“…A set of alternative labelling strategies including the introduction of aluminium mono-[ 18 F]fluoride cations ([ 18 F]AlF 2+ ), labelling of SiFA by 19 F- 18 F isotopic exchange reactions (IEX), and 1-step 19 F- 18 F IEX on trifluoroborates such as trialkylammoniomethyl-BF 3 are currently being evaluated (for a review, see [138]). Initial clinical trials with 18 F-AlF-NOTA-octreotide [48] and 18 F-SiFAlin-TATE [139] most recently published indicate promising data. Further studies will demonstrate if these compounds might replace the established 68 Ga-labelled octreotide derivatives.…”

Section: Somatostatin Receptormentioning

confidence: 99%

Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology

Rangger

Haubner

2020

Pharmaceuticals

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This review deals with the development of peptide-based radiopharmaceuticals for the use with positron emission tomography and peptide receptor radiotherapy. It discusses the pros and cons of this class of radiopharmaceuticals as well as the different labelling strategies, and summarises approaches to optimise metabolic stability. Additionally, it presents different target structures and addresses corresponding tracers, which are already used in clinical routine or are being investigated in clinical trials.

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Section: Somatostatin Receptormentioning

confidence: 99%

Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology

Rangger

Haubner

2020

Pharmaceuticals

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“…Another elegant method to label somatostatin analogs is the use of [ 18 F]-aluminum fluoride with radiotracers previously developed for radiometals, such as NOTATOC [ 153 ]. These new generation analogs demonstrated general properties (affinity for the targeted receptors, metabolic stability, biodistribution and clearance) which are much more interesting, and some of them have been investigated in patients, where they gave results comparable to [ 68 Ga]-DOTATOC [ 154 , 155 ]. In addition, [ 18 F]F-FET-βAG-TOCA and [ 18 F]-IMP466 ([Al 18 F]-NOTATOC) are currently being evaluated in phase I clinical trials (EudraCT number 2013-003152-20 and NCT03511768, respectively).…”

Section: Targeting Of Somatostatin Receptors With Radiopharmaceutimentioning

confidence: 99%

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

et al. 2020

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Identified in 1973, somatostatin (SST) is a cyclic hormone peptide with a short biological half-life. Somatostatin receptors (SSTRs) are widely expressed in the whole body, with five subtypes described. The interaction between SST and its receptors leads to the internalization of the ligand–receptor complex and triggers different cellular signaling pathways. Interestingly, the expression of SSTRs is significantly enhanced in many solid tumors, especially gastro-entero-pancreatic neuroendocrine tumors (GEP-NET). Thus, somatostatin analogs (SSAs) have been developed to improve the stability of the endogenous ligand and so extend its half-life. Radiolabeled analogs have been developed with several radioelements such as indium-111, technetium-99 m, and recently gallium-68, fluorine-18, and copper-64, to visualize the distribution of receptor overexpression in tumors. Internal metabolic radiotherapy is also used as a therapeutic strategy (e.g., using yttrium-90, lutetium-177, and actinium-225). With some radiopharmaceuticals now used in clinical practice, somatostatin analogs developed for imaging and therapy are an example of the concept of personalized medicine with a theranostic approach. Here, we review the development of these analogs, from the well-established and authorized ones to the most recently developed radiotracers, which have better pharmacokinetic properties and demonstrate increased efficacy and safety, as well as the search for new clinical indications.

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“…Single-step radiolabelling protocols to produce 4 and 5 are attractive and result in excellent RCY, however only manual radiosynthesis methods have been described. The radiosynthesis of 4 requires precise manipulation of small reaction volumes and would benefit from the development of an automated procedure to produce the radioconjugate on scale [56]. [ 18 F]FP-Gluc-TOCA (1) is the most complex radioconjugate to produce with a total of five radiosynthetic steps and two HPLC purifications, which is not compatible with routine production to satisfy the growing demand for SSTR2 stratification, despite excellent preclinical and clinical performance.…”

Section: Comparison Of 18 F-radiolabelled Octreotide Analoguesmentioning

confidence: 99%

[18F]FET-βAG-TOCA: The Design, Evaluation and Clinical Translation of a Fluorinated Octreotide

Allott

Dubash

Aboagye

2020

Cancers

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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.

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Biodistribution and first clinical results of 18F-SiFAlin-TATE PET: a novel 18F-labeled somatostatin analog for imaging of neuroendocrine tumors

Cited by 75 publications

References 24 publications

Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology

Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

[18F]FET-βAG-TOCA: The Design, Evaluation and Clinical Translation of a Fluorinated Octreotide

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