61Cu-Labelled radiodiagnostics of melanoma with NAPamide-targeted radiopharmaceutical

Kálmán-Szabó, Ibolya and Bunda, Szilvia and Lihi, Norbert and Szaniszló, Zsófia and Szikra, Dezső and Szabó Péliné, Judit and Fekete, Anikó and Gyuricza, Barbara and Szücs, Dániel and Papp, Gábor and Trencsényi, György and Kálmán, Ferenc K. (2023) 61Cu-Labelled radiodiagnostics of melanoma with NAPamide-targeted radiopharmaceutical. International Journal of Pharmaceutics, 632. p. 122527. ISSN 03785173

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Abstract

Malignant melanoma is a major public health problem with an increasing incidence and mortality in the Caucasian population due to its significant metastatic potential. The early detection of this cancer type by imaging techniques like positron emission tomography acts as an important contributor to the long-term survival. Based on literature data, the radio labelled alpha-MSH analog NAPamide molecule is an appropriate diagnostictool for the detection of melanoma tumors. Inspired by these facts, a new radiotracer, the [61Cu]Cu-KFTGNAPamide has been synthesized to exploit the beneficial features of the positron emitter 61Cu and the melanoma specificity of the NAPamide molecule. In this work, we report a new member of the CB-15aneN5 ligand family (KFTG) as the chelator for 61Cu(II) complexation. On the basis of the thorough physico-chemical characterization, the rigid [Cu(KFTG)]+ complex exhibits fast complex formation (t1/2 = 155 s at pH 5.0 and 25 ◦C) and high inertness (t1/2 = 2.0 h in 5.0 M HCl at 50 ◦C) as well as moderate superoxide dismutase activity (IC50 = 2.3 μM). Furthermore, the [61Cu]Cu-KFTG-NAPamide possesses outstanding features in the diagnostics of B16-F10 melanoma tumors by PET imaging: (T/M(SUVs) (in vivo): appr. 14, %ID/g: 7 ± 1 and T/M (ex vivo): 315 ± 24 at 180 min).

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