Synthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma

Billaud, Emilie; Maisonial-Besset, Aurélie; Rbah-Vidal, Latifa; Vidal, Aurélien; Besse, Sophie; Béquignat, Jean-Baptiste; Decombat, Caroline; Degoul, Françoise; Audin, Laurent; Deloye, Jean‐Bernard; Dollé, Frédéric; Kühnast, Bertrand; Madelmont, Jean‐Claude; Tarrit, Sébastien; Galmier, Marie-Josèphe; Borel, Michèle; Auzeloux, Philippe; Miot-Noirault, Élisabeth; Chezal, Jean‐Michel

doi:10.1016/j.ejmech.2015.01.034

Cited by 9 publications

(2 citation statements)

References 46 publications

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“…Other groups have been also investigating benzamide compounds as possible therapeutic agents for melanoma [ 58 , 59 , 60 , 61 ]. A recent review described the pre-clinical use of benzamides as imaging agents including multi-modality and therapeutic agents [ 62 ].…”

Section: Targeting Melanin With Small Moleculesmentioning

confidence: 99%

Targeting Melanin in Melanoma with Radionuclide Therapy

Allen

Malo

Jiao

et al. 2022

IJMS

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Nearly 100,000 individuals are expected to be diagnosed with melanoma in the United States in 2022. Treatment options for late-stage metastatic disease up until the 2010s were few and offered only slight improvement to the overall survival. The introduction of B-RAF inhibitors and anti-CTLA4 and anti-PD-1/PD-L1 immunotherapies into standard of care brought measurable increases in the overall survival across all stages of melanoma. Despite the improvement in the survival statistics, patients treated with targeted therapies and immunotherapies are subject to very serious side effects, the development of drug resistance, and the high costs of treatment. This leaves room for the development of novel approaches as well as for the exploration of novel combination therapies for the treatment of metastatic melanoma. One such approach is targeting melanin pigment with radionuclide therapy. Advances in melanin-targeting radionuclide therapy of melanoma can be viewed from two spheres: (1) radioimmunotherapy (RIT) and (2) radiolabeled small molecules. The investigation of mechanisms of the action and efficacy of targeting melanin in melanoma treatment by RIT points to the involvement of the immune system such as complement dependent cytotoxicity. The combination of RIT with immunotherapy presents synergistic killing in mouse melanoma models. The field of radiolabeled small molecules is focused on radioiodinated compounds that have the ability to cross the cellular membranes to access intracellular melanin and can be applied in both therapy and imaging as theranostics. Clinical applications of targeting melanin with radionuclide therapies have produced encouraging results and clinical work is on-going. Continued work on targeting melanin with radionuclide therapy as a monotherapy, or possibly in combination with standard of care agents, has the potential to strengthen the current treatment options for melanoma patients.

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Section: Targeting Melanin With Small Moleculesmentioning

confidence: 99%

Targeting Melanin in Melanoma with Radionuclide Therapy

Allen

Malo

Jiao

et al. 2022

IJMS

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“…The experimental procedure followed for the synthesis of 2a using methyl 2-amino benzoate (1.10 g, 7.24 mmol) substrate produced 1.94 g (96% yield, 99.2% purity) as a white to light brown crystalline solid: mp 81−84 °C (lit. 41 mp 82−84 °C); 1 H NMR (400 MHz, DMSO-d 6 ) δ 7.93 (d, J = 2.1 Hz, 1H), 7.49 (d, J = 8.8 Hz, 1H), 6.79 (s, 2H), 6.65 (d, J = 8.8 Hz, 1H), 3.79 (s, 3H).…”

Section: ■ Experimental Sectionmentioning

confidence: 99%

NCBSI/KI: A Reagent System for Iodination of Aromatics through In Situ Generation of I-Cl

2021

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PET and SPECT imaging of melanoma: the state of the art

Wei

Ehlerding

Lan

et al. 2017

Eur J Nucl Med Mol Imaging

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Melanoma represents the most aggressive form of skin cancer, and its incidence continues to rise worldwide. F-FDG PET imaging has transformed diagnostic nuclear medicine and has become an essential component in the management of melanoma, but still has its drawbacks. With the rapid growth in the field of nuclear medicine and molecular imaging, a variety of promising probes that enable early diagnosis and detection of melanoma have been developed. The substantial preclinical success of melanin- and peptide-based probes has recently resulted in the translation of several radiotracers to clinical settings for noninvasive imaging and treatment of melanoma in humans. In this review, we focus on the latest developments in radiolabeled molecular imaging probes for melanoma in preclinical and clinical settings, and discuss the challenges and opportunities for future development.

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Synthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma

Cited by 9 publications

References 46 publications

Targeting Melanin in Melanoma with Radionuclide Therapy

Targeting Melanin in Melanoma with Radionuclide Therapy

NCBSI/KI: A Reagent System for Iodination of Aromatics through In Situ Generation of I-Cl

PET and SPECT imaging of melanoma: the state of the art

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