Efficacy of Targeted Radionuclide Therapy Using [131I]ICF01012 in 3D Pigmented BRAF- and NRAS-Mutant Melanoma Models and In Vivo NRAS-Mutant Melanoma

Akil, Hussein; Quintana, Mercedes; Raymond, J.; Billoux, Tommy; Benboubker, Valentin; Besse, Sophie; Auzeloux, Philippe; Delmas, Véronique; Petit, Valérie; Larue, Lionel; D’Incan, M.; Degoul, Françoise; Rouanet, Jacques

doi:10.3390/cancers13061421

Cited by 6 publications

(5 citation statements)

References 54 publications

(84 reference statements)

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“…Furthermore, 3D models can be used to design targeted nuclear medicine therapy (e.g., effects of α or β labelled radiopharmaceuticals). Table 4 lists the recently developed radiopharmaceuticals using 3D models of various tumor types [54][55][56][57][58][59][60][61][62][63].…”

Section: Nuclear Medicine Therapymentioning

confidence: 99%

Three-Dimensional In Vitro Tumor Spheroid Models for Evaluation of Anticancer Therapy: Recent Updates

Nayak,

Bentivoglio,

Varani

et al. 2023

Cancers

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Advanced tissue engineering processes and regenerative medicine provide modern strategies for fabricating 3D spheroids. Several different 3D cancer models are being developed to study a variety of cancers. Three-dimensional spheroids can correctly replicate some features of solid tumors (such as the secretion of soluble mediators, drug resistance mechanisms, gene expression patterns and physiological responses) better than 2D cell cultures or animal models. Tumor spheroids are also helpful for precisely reproducing the three-dimensional organization and microenvironmental factors of tumors. Because of these unique properties, the potential of 3D cell aggregates has been emphasized, and they have been utilized in in vitro models for the detection of novel anticancer drugs. This review discusses applications of 3D spheroid models in nuclear medicine for diagnosis and therapy, immunotherapy, and stem cell and photodynamic therapy and also discusses the establishment of the anticancer activity of nanocarriers.

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Section: Nuclear Medicine Therapymentioning

confidence: 99%

Three-Dimensional In Vitro Tumor Spheroid Models for Evaluation of Anticancer Therapy: Recent Updates

Nayak,

Bentivoglio,

Varani

et al. 2023

Cancers

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“…The radioactivity is delivered to a specific tumor by means of a systemic injection. For melanoma treatment, targeted treatment can be achieved by labeling small molecules, such as melanin ligands, peptides that recognize a specific receptor (MC1R), or antibodies (anti-melanin, anti-GD3) [365,366]. The efficacy of targeted radiotherapy depends on the dose delivered, which in turn depends on the radionuclide used and the time that the labeled compound remains associated with the target.…”

Section: Novel Structures and Drug Design Approachesmentioning

confidence: 99%

Targeting GPCRs and Their Signaling as a Therapeutic Option in Melanoma

Raymond

Aktary

Larue

et al. 2022

Cancers

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G-protein-coupled receptors (GPCRs) serve prominent roles in melanocyte lineage physiology, with an impact at all stages of development, as well as on mature melanocyte functions. GPCR ligands are present in the skin and regulate melanocyte homeostasis, including pigmentation. The role of GPCRs in the regulation of pigmentation and, consequently, protection against external aggression, such as ultraviolet radiation, has long been established. However, evidence of new functions of GPCRs directly in melanomagenesis has been highlighted in recent years. GPCRs are coupled, through their intracellular domains, to heterotrimeric G-proteins, which induce cellular signaling through various pathways. Such signaling modulates numerous essential cellular processes that occur during melanomagenesis, including proliferation and migration. GPCR-associated signaling in melanoma can be activated by the binding of paracrine factors to their receptors or directly by activating mutations. In this review, we present melanoma-associated alterations of GPCRs and their downstream signaling and discuss the various preclinical models used to evaluate new therapeutic approaches against GPCR activity in melanoma. Recent striking advances in our understanding of the structure, function, and regulation of GPCRs will undoubtedly broaden melanoma treatment options in the future.

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“…The mechanistic experiments revealed that the tolerance was a dominant immune escape mechanism while exhaustion was not detected after treatment with [ 131 I]ICF01012. Finally, the same researchers studied therapy with [ 131 I]ICF01012 alone or in combination with MEK inhibitors (MEKi) [ 69 ]. They utilized spheroidal and in vivo melanoma models that harbor constitutive MAPK/ERK activation thought to be responsible for tumor radioresistance.…”

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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Efficacy of Targeted Radionuclide Therapy Using [131I]ICF01012 in 3D Pigmented BRAF- and NRAS-Mutant Melanoma Models and In Vivo NRAS-Mutant Melanoma

Cited by 6 publications

References 54 publications

Three-Dimensional In Vitro Tumor Spheroid Models for Evaluation of Anticancer Therapy: Recent Updates

Three-Dimensional In Vitro Tumor Spheroid Models for Evaluation of Anticancer Therapy: Recent Updates

Targeting GPCRs and Their Signaling as a Therapeutic Option in Melanoma

Targeting Melanin in Melanoma with Radionuclide Therapy

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