Diagnosis of Melanoma with 61Cu-Labeled PET Tracer

Bunda, Szilvia and Kálmán-Szabó, Ibolya and Lihi, Norbert and Képes, Zita and Szikra, Dezső and Péliné Szabó, Judit and Timári, István and Szücs, Dániel and May, Nóra V. and Papp, Gábor Csaba and Trencsényi, György and Kálmán, Ferenc K. (2024) Diagnosis of Melanoma with 61Cu-Labeled PET Tracer. JOURNAL OF MEDICINAL CHEMISTRY, 67 (11). pp. 9342-9354. ISSN 0022-2623 (In Press)

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Abstract

Until the recent years, substances containing radioactive 61Cu were strongly considered as potential positron-emitting radiopharmaceuticals for use in positron emission tomography (PET) applications; however, due to their suitably long half-life, and generator-independent and cost-effective production, they seem to be economically viable for human imaging. Since malignant melanoma (MM) is a major public health problem, its early diagnosis is a crucial contributor to long-term survival, which can be achieved using radiolabeled α-melanocyte-stimulating hormone analog NAPamide derivatives. Here, we report on the physicochemical features of a new CB-15aneN5-based Cu(II) complex ([Cu(KFTGdiac)]−) and the ex vivo and in vivo characterization of its NAPamide conjugate. The rigid chelate possesses prompt complex formation and suitable inertness (t1/2 = 18.4 min in 5.0 M HCl at 50 °C), as well as excellent features in the diagnosis of B16–F10 melanoma tumors (T/M(SUVs) (in vivo): 12.7, %ID/g: 6.6 ± 0.3, T/M (ex vivo): 22).

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