A kit-based aluminium-[<sup>18</sup>F]fluoride approach to radiolabelled microbubbles

Teh, Jin Hui; Braga, Marta; Allott, Louis; Barnes, Clifford A.; Hernández-Gil, Javier; Tang, Meng-Xing; Aboagye, Eric O.; Long, Nicholas J.

doi:10.1039/d1cc04790f

Cited by 4 publications

(1 citation statement)

References 31 publications

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“…Thus, we aim to develop a facile method to access an 18 F-labelled analogue of EMI-137. We hypothesize that this could be achieved using the aluminium-[ 18 F]fluoride ([ 18 F]AlF) method reported by McBride et al, which combines the convenience of radiometal-based labelling, the favourable decay characteristics of fluorine-18 [ 36 , 37 ], and has the potential to be formulated into a kit [ 38 ]. With a recent study showing that [ 18 F]AlF-NOTA-Octreotide outperforms its 68 Ga counterpart for imaging SSTR2 [ 39 ], the results from this study could offer a valuable alternative to [ 68 Ga]Ga-EMP-100 for imaging c-Met.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of [18F]AlF-EMP-105 for Molecular Imaging of C-Met

Teh,

Amgheib,

et al. 2023

Pharmaceutics

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C-Met is a receptor tyrosine kinase that is overexpressed in a range of different cancer types, and has been identified as a potential biomarker for cancer imaging and therapy. Previously, a 68Ga-labelled peptide, [68Ga]Ga-EMP-100, has shown promise for imaging c-Met in renal cell carcinoma in humans. Herein, we report the synthesis and preliminary biological evaluation of an [18F]AlF-labelled analogue, [18F]AlF-EMP-105, for c-Met imaging by positron emission tomography. EMP-105 was radiolabelled using the aluminium-[18F]fluoride method with 46 ± 2% RCY and >95% RCP in 35–40 min. In vitro evaluation showed that [18F]AlF-EMP-105 has a high specificity for c-Met-expressing cells. Radioactive metabolite analysis at 5 and 30 min post-injection revealed that [18F]AlF-EMP-105 has good blood stability, but undergoes transformation—transchelation, defluorination or demetallation—in the liver and kidneys. PET imaging in non-tumour-bearing mice showed high radioactive accumulation in the kidneys, bladder and urine, demonstrating that the tracer is cleared predominantly as [18F]fluoride by the renal system. With its high specificity for c-Met expressing cells, [18F]AlF-EMP-105 shows promise as a potential diagnostic tool for imaging cancer.

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Section: Introductionmentioning

confidence: 99%

Evaluation of [18F]AlF-EMP-105 for Molecular Imaging of C-Met

Teh,

Amgheib,

et al. 2023

Pharmaceutics

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Bifunctional Hexadentate Pyclen–Based Chelating Agent for Mild Radiofluorination in Aqueous Solution at Room Temperature with a Ga‐¹⁸F Ternary Complex

Dioury,

San,

Gnanalingam

et al. 2024

Chemistry A European J

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Positron Emission Tomography (PET) is used in oncology for tumor diagnosis, commonly relying on fluorine‐18 (18F) emission detection. The conventional method of 18F incorporation on to probes by covalent bonding is harsh for sensitive biomolecules, which are nonetheless compounds of choice for the development of targeted probes. This study explores gallium‐18F (Ga18F) coordination, a milder alternative method occurring in aqueous media at the final stage of radiosyntheses. Pyclen‐based chelating agents were proposed to capture (GaF) species at room temperature and pH ≥ 5 making the radiofluorination process compatible with heat‐ and acid‐sensitive biomolecules. Highly promising results were obtained with the PC2A‐based chelating agent LH2 derived from the new bifunctional PC2A‐OAE‐NCS compound. The solid‐state structure of GaF(L) was elucidated by X‐ray diffraction and revealed an unconventional heptacoordination of Ga(III). A high radiochemical conversion (RCC) of 86% was achieved at room temperature, in water at pH 5 within 20 minutes. Stability studies showed the robustness of the GaF(L) complex in aqueous media for at least one day and at least one hour for the radiolabeled analog Ga18F(L). These findings demonstrated that PC2A‐based compounds are chelating agents of choice for (Ga18F) species, suggesting a real technological breakthrough for PET imaging and precision medicine.

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Radiochemistry with {Al18F}2+: Current status and optimization perspectives for efficient radiofluorination by complexation

Schmitt

Moreau

2023

Coordination Chemistry Reviews

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A kit-based aluminium-[¹⁸F]fluoride approach to radiolabelled microbubbles

Cited by 4 publications

References 31 publications

Evaluation of [18F]AlF-EMP-105 for Molecular Imaging of C-Met

Evaluation of [18F]AlF-EMP-105 for Molecular Imaging of C-Met

Bifunctional Hexadentate Pyclen–Based Chelating Agent for Mild Radiofluorination in Aqueous Solution at Room Temperature with a Ga‐¹⁸F Ternary Complex

Radiochemistry with {Al18F}2+: Current status and optimization perspectives for efficient radiofluorination by complexation

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A kit-based aluminium-[18F]fluoride approach to radiolabelled microbubbles

Cited by 4 publications

References 31 publications

Evaluation of [18F]AlF-EMP-105 for Molecular Imaging of C-Met

Evaluation of [18F]AlF-EMP-105 for Molecular Imaging of C-Met

Bifunctional Hexadentate Pyclen–Based Chelating Agent for Mild Radiofluorination in Aqueous Solution at Room Temperature with a Ga‐18F Ternary Complex

Radiochemistry with {Al18F}2+: Current status and optimization perspectives for efficient radiofluorination by complexation

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Resources

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A kit-based aluminium-[¹⁸F]fluoride approach to radiolabelled microbubbles

Bifunctional Hexadentate Pyclen–Based Chelating Agent for Mild Radiofluorination in Aqueous Solution at Room Temperature with a Ga‐¹⁸F Ternary Complex