Preparation and biologic evaluation of a novel radioiodinated benzylpiperazine, 123I-MEL037, for malignant melanoma

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dc.contributor.authorPham, TQen_AU
dc.contributor.authorBerghofer, PJen_AU
dc.contributor.authorLiu, Xen_AU
dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorDikic, Ben_AU
dc.contributor.authorBallantyne, Pen_AU
dc.contributor.authorMattner, Fen_AU
dc.contributor.authorNguyen, VHen_AU
dc.contributor.authorLoc'h, Cen_AU
dc.contributor.authorKatsifis, Aen_AU
dc.date.accessioned2020-03-23T22:59:44Zen_AU
dc.date.available2020-03-23T22:59:44Zen_AU
dc.date.issued2007-07-13en_AU
dc.description.abstractRadiopharmaceuticals that can target the random metastatic dissemination of melanoma tumors may present opportunities for imaging and staging the disease as well as potential radiotherapeutic applications. A novel molecule, 2-(2-(4-(4-123I-iodobenzyl)piperazin-1-yl)-2-oxoethyl)isoindoline-1,3-dione (MEL037), was synthesized, labeled with 123I, and evaluated for application in melanoma tumor scintigraphy and radiotherapy. Methods: The tumor imaging potential of 123I-MEL037 was studied in vivo in C57BL/6J female mice bearing the B16F0 murine melanoma tumor and in BALB/c nude mice bearing the A375 human amelanotic melanoma tumor by biodistribution, competition studies, and SPECT. Results: 123I-MEL037 exhibited high and rapid uptake in the B16F0 melanoma tumor at 1 h (13 %ID/g [percentage injected dose per gram]), increasing with time to reach 25 %ID/g at 6 h. A significant uptake was also observed in the eyes (2 %ID, at 3–6 h after injection) of black mice. No uptake was observed in the tumor or in the eyes of nude mice bearing the A375 tumor. Because of high uptake and long retention in the tumor and rapid body clearance, the mean contrast ratios (MCR) of 123I-MEL037 were 30 and 60, at 24 and 48 h after injection, respectively. At 24 h after injection of mice bearing the B16 melanoma, SPECT indicated that the radioactivity was located predominately in the tumor followed by the eyes, whereas no specific localization of the radioactivity was noted in mice bearing the A375 human amelanotic tumor. In competition experiments, uptake of 123I-MEL037 in brain, lung, heart, and kidney—organs known to contain σ-receptors—was not significantly different in haloperidol-treated animals compared with control animals. Therefore, reduction of uptake in tumor and eyes of the pigmented mice bearing the B16F0 tumor suggested that the mechanism of tumor uptake was likely due to an interaction with melanin. Conclusion: These findings suggested that 123I-MEL037, which displays a rapid and very high tumor uptake, appeared to be a promising imaging agent for detection of most melanoma tumors with the potential for development as a therapeutic agent in melanoma tumor proliferation. © 2007 by the Society of Nuclear Medicine, Inc.en_AU
dc.identifier.citationPham, T. Q., Berghofer, P., Liu, X., Greguric, I., Dikic, B., Ballantyne, P., Mattner, F Nguyen, V. H., Loc'h, C., & Katsifis, A. (2007). Preparation and biologic evaluation of a novel radioiodinated benzylpiperazine, 123I-MEL037, for malignant melanoma. Journal of Nuclear Medicine, 48(8), 1348-1356. doi:10.2967/jnumed.107.041673en_AU
dc.identifier.govdoc8862en_AU
dc.identifier.issn0161-5505en_AU
dc.identifier.issue8en_AU
dc.identifier.journaltitleJournal of Nuclear Medicineen_AU
dc.identifier.pagination1348-1356en_AU
dc.identifier.urihttps://doi.org/10.2967/jnumed.107.041673en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9197en_AU
dc.identifier.volume48en_AU
dc.language.isoenen_AU
dc.publisherSociety of Nuclear Medicine and Molecular Imagingen_AU
dc.subjectMelanomasen_AU
dc.subjectNeoplasmsen_AU
dc.subjectSingle photon emission computed tomographyen_AU
dc.subjectIodine 123en_AU
dc.subjectScintiscanningen_AU
dc.subjectRadiotherapyen_AU
dc.subjectReceptorsen_AU
dc.subjectRadiopharmaceuticalsen_AU
dc.titlePreparation and biologic evaluation of a novel radioiodinated benzylpiperazine, 123I-MEL037, for malignant melanomaen_AU
dc.typeJournal Articleen_AU
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