[ 18 F]MEL050 as a melanin-targeted PET tracer: Fully automated radiosynthesis and comparison to  18 F-FDG for the detection of pigmented melanoma in mice primary subcutaneous tumors and pulmonary metastases

Rizzo-Padoin, N.; Chaussard, Michael; Vignal, N.; Kotula, Ewa; Tsoupko-Sitnikov, Vadim; Vaz, Sofia; Hontonnou, Fortune; Liu, Wang‐Qing; Poyet, Jean-Luc; Vidal, Michel; Merlet, Pascal; Hosten, Benoît; Sarda‐Mantel, Laure

doi:10.1016/j.nucmedbio.2016.08.010

Cited by 15 publications

(46 citation statements)

References 25 publications

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“…The tissue distribution studies showed a modest uptake of radioactivity in the mouse brain (2.55 ± 0.61%IA/g at 1 h) demonstrating the ability of this compound to cross the blood-brain barrier. In comparison, the uptake of MEL050 in mouse brain as determined from microPET imaging studies was 1.38 ± 0.40%IA/g at 60–70 min [ 38 ]. More importantly, the levels in the brain were significantly lower than those in the tumor.…”

Section: Discussionmentioning

confidence: 99%

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

Garg

Nazih

et al. 2017

EJNMMI Res

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BackgroundThe purpose of this study was to develop a positron emission tomography (PET) imaging probe that is easy to synthesize and selectively targets melanoma in vivo. Herein, we report the synthesis and preclinical evaluation of N-(2-diethylaminoethyl) 4-[18F]Fluoroethoxy benzamide (4-[18F]FEBZA).A one-step synthesis was developed to prepare 4-[18F]FEBZA in high radiochemical yields and specific activity. The binding affinity, the in vitro binding, and internalization studies were performed using B16F1 melanoma cell line. The biodistribution studies were performed in C57BL/6 normal mice, C57BL/6 mice bearing B16F1 melanoma tumor xenografts, and nu/nu athymic mice bearing HT-29 human adenocarcinoma tumor and C-32 amelanotic melanoma tumor xenografts. MicroPET studies were performed in mice bearing B16F1 and HT-29 tumor xenografts.Results4-[18F]FEBZA was prepared in 53 ± 14% radiochemical yields and a specific activity of 8.7 ± 1.1 Ci/μmol. The overall synthesis time for 4-[18F]FEBZA was 54 ± 7 min. The in vitro binding to B16F1 cells was 60.03 ± 0.48% after 1 h incubation at 37 °C. The in vivo biodistribution studies show a rapid and high uptake of F-18 in B16F1 tumor with 8.66 ± 1.02%IA/g in this tumor at 1 h. In contrast, the uptake at 1 h in HT-29 colorectal adenocarcinoma and C-32 amelanotic melanoma tumors was significantly lower with 3.68 ± 0.47%IA/g and 3.91 ± 0.23%IA/g in HT-29 and C-32 tumors, respectively. On microPET images, the melanoma tumor was clearly visible by 10 min post-injection and the intensity in the tumor continued to increase with time. In contrast, the HT-29 tumor was not visible on the microPET scans.ConclusionsA rapid and facile synthesis of 4-[18F]FEBZA is developed. This method offers a reliable production of 4-[18F]FEBZA in high radiochemical yields and specific activity. A high binding affinity to melanoma cells and high uptake in tumor was noted. The microPET scan clearly delineates the melanoma tumor by 10 min post-injection. The results from these preclinical studies support the potential of 4-[18F]FEBZA as an effective probe to image melanoma.

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Section: Discussionmentioning

confidence: 99%

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

Garg

Nazih

et al. 2017

EJNMMI Res

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“…18 F-MEL050 showed a clear delineation of melanoma lesions with rapid background washout and higher tumor-to-background than 18 F-FDG. Rizzo-Padoin et al [192] confirmed this data and reported that 18 F-MEL050 PET/CT could detect sub-millimeter pulmonary metastases not found on 18 F-FDG PET/CT. Additionally, Denoyer et al [193] reported that lymph node metastases could be identified with perilesional 18 F-MEL050 administration.…”

Section: New Radiolabeled Radiotracers In Petmentioning

confidence: 63%

New Perspectives in Imaging of Uveal Melanoma

Solnik¹,

Paduszynska²,

Czarnecka³

et al. 2021

Preprint

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Uveal melanoma is the most common primary intraocular malignancy in adults characterized by insidious onset and poor prognosis strongly associated with tumor size and the presence of distant metastases, most commonly in the liver. Contrary to most tumor identification, biopsy followed by pathological exam is not recommended in ophthalmic oncology. Therefore, early and non-invasive diagnosis is essential to enhance patients’ chances for early treatment possibilities. We reviewed imaging modalities currently used in the diagnosis of uveal melanoma, i.e., fundus imaging, ultrasonography (US), optical coherence tomography (OCT), single-photon emission computed tomography (SPECT), positron emission tomography/computed tomography (PET/CT), magnetic resonance imaging (MRI), fundus fluorescein angiography (FFA), indocyanine green angiography (ICGA), fundus autofluorescence (FAF). The principle of imaging techniques was briefly explained, along with their role in the diagnostic process and a summary of their advantages and limitations. Further, the experimental data and the advancements in imaging modalities were searched. We described their innovations, showed current usage and research, and explained the possibilities of utilizing them to diagnose uveal melanoma and their potential application in personalized medicine such as theranostics.

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“…18 F-MEL050 clearly delineated melanoma lesions with rapid background washout and a higher tumor-to-background ratio than 18 F-FDG. Rizzo-Padoin et al [207] confirmed these data and reported that 18 F-MEL050 PET/CT could detect submillimeter pulmonary metastases not found on 18 F-FDG PET/CT. Denoyer et al [208] reported that lymph node metastases could be identified with perilesional 18 F-MEL050 administration.…”

Section: New Radiolabeled Radiotracers In Petmentioning

confidence: 75%

Imaging of Uveal Melanoma—Current Standard and Methods in Development

Solnik

Paduszyńska

Czarnecka

et al. 2022

Cancers

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Uveal melanoma is the most common primary intraocular malignancy in adults, characterized by an insidious onset and poor prognosis strongly associated with tumor size and the presence of distant metastases, most commonly in the liver. Contrary to most tumor identification, a biopsy followed by a pathological exam is used only in certain cases. Therefore, an early and noninvasive diagnosis is essential to enhance patients’ chances for early treatment. We reviewed imaging modalities currently used in the diagnostics of uveal melanoma, including fundus imaging, ultrasonography (US), optical coherence tomography (OCT), single-photon emission computed tomography (SPECT), fundus fluorescein angiography (FFA), indocyanine green angiography (ICGA), fundus autofluorescence (FAF), as well as positron emission tomography/computed tomography (PET/CT) or magnetic resonance imaging (MRI). The principle of imaging techniques is briefly explained, along with their role in the diagnostic process and a summary of their advantages and limitations. Further, the experimental data and the advancements in imaging modalities are explained. We describe UM imaging innovations, show their current usage and development, and explain the possibilities of utilizing such modalities to diagnose uveal melanoma in the future.

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[ 18 F]MEL050 as a melanin-targeted PET tracer: Fully automated radiosynthesis and comparison to 18 F-FDG for the detection of pigmented melanoma in mice primary subcutaneous tumors and pulmonary metastases

Cited by 15 publications

References 25 publications

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

Selective targeting of melanoma using N-(2-diethylaminoethyl) 4-[18F]fluoroethoxy benzamide (4-[18F]FEBZA): a novel PET imaging probe

New Perspectives in Imaging of Uveal Melanoma

Imaging of Uveal Melanoma—Current Standard and Methods in Development

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