N-(2-diethylaminoethyl)-6-iodoquinoxaline-2-carbamide (ICF 01012) is a new melanoma imaging agent showing promising properties for application in internal radionuclide therapy. We developed an analytical protocol for detection of ICF 01012 in biological samples using HPLC. The proposed method was first validated using standard of ICF 01012 and four potent metabolites of this compound and then applied to follow the metabolic fate of [(125)I]ICF 01012 after injection in melanoma-bearing mice. The results demonstrate that this method exhibits a good linearity (r(2)=0.9947), specificity and acceptable accuracy. This simple method appears convenient and sufficient for pharmacokinetic studies on [(125)I]ICF 01012.
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http://dx.doi.org/10.1016/j.jchromb.2008.09.021 | DOI Listing |
BMC Cancer
April 2022
INSERM U1240 IMoST, Université Clermont Auvergne, F-63000, Clermont-Ferrand, France.
Background: Benzamide-based radioligands targeting melanin were first developed for imaging melanoma and then for therapeutic purpose with targeted radionuclide therapy (TRT). [I]ICF01012 presents a highly favorable pharmacokinetics profile in vivo for therapy. Tumour growth reduction and increase survival have been established in preclinical models of melanoma.
View Article and Find Full Text PDFMed Phys
November 2018
Université Clermont Auvergne, CNRS/IN2P3, Laboratoire de Physique de Clermont, UMR6533, 4 Avenue Blaise Pascal TSA 60026, CS 60026 63178, Aubière Cedex, France.
Purpose: Dosimetry for melanoma-targeted radionuclide therapy (TRT) with [ I]ICF01012, a melanin ligand, has been previously evaluated in mice bearing melanomas. In this study, activity distribution and dosimetry are performed on healthy rabbits (Fauve de Bourgogne) using SPECT-CT imaging and ex vivo measurements.
Material And Methods: Ex vivo biodistribution (i.
Oncotarget
March 2016
Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
Radiolabelled melanin ligands offer an interesting strategy for the treatment of disseminated pigmented melanoma. One of these molecules, ICF01012 labelled with iodine 131, induced a significant slowing of melanoma growth. Here, we have explored the combination of [131I]ICF01012 with coDbait, a DNA repair inhibitor, to overcome melanoma radioresistance and increase targeted radionuclide therapy (TRT) efficacy.
View Article and Find Full Text PDFEur J Med Chem
March 2015
Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France; Inserm, U 990, F-63000 Clermont-Ferrand, France; Centre Jean Perrin, F-63011 Clermont-Ferrand, France. Electronic address:
Melanin pigment represents an attractive target to address specific treatment to melanoma cells, such as cytotoxic radionuclides. However, less than half of the patients have pigmented metastases. Hence, specific marker is required to stratify this patient population before proceeding with melanin-targeted radionuclide therapy.
View Article and Find Full Text PDFEur J Dermatol
January 2016
Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, Inserm, U 990, F-63000 Clermont-Ferrand, France.
Background: Melanin-targeting radiotracers are interesting tools for imaging and treatment of pigmented melanoma metastases. However, variation of the pigment concentration may alter the efficiency of such targeting.
Objectives: A clear assessment of both tumor melanin status and dosimetry are therefore prerequisites for internal radiotherapy of disseminated melanoma.
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