Diagnosis of Melanoma with 61Cu-Labeled PET Tracer

Szilvia Bunda; Ibolya Kálmán-Szabó; Norbert Lihi; Zita Képes; Dezső Szikra; Judit Peline Szabo; István Timári; Dániel Szücs; Nóra V May; Gábor Papp; György Trencsényi; Ferenc K Kálmán

doi:10.1021/acs.jmedchem.4c00479

Diagnosis of Melanoma with ⁶¹Cu-Labeled PET Tracer

J Med Chem. 2024 May 16. doi: 10.1021/acs.jmedchem.4c00479. Online ahead of print.

Authors

Szilvia Bunda¹, Ibolya Kálmán-Szabó^{2

3}, Norbert Lihi⁴, Zita Képes², Dezső Szikra², Judit Peline Szabo², István Timári^{5

6}, Dániel Szücs², Nóra V May⁷, Gábor Papp¹, György Trencsényi^{2

3}, Ferenc K Kálmán¹

Affiliations

¹ Department of Physical Chemistry, University of Debrecen, Egyetem tér 1., H-4032 Debrecen, Hungary.
² Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary.
³ Gyula Petrányi Doctoral School of Clinical Immunology and Allergology, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.
⁴ HUN-REN-UD Mechanisms of Complex Homogeneous and Heterogeneous Chemical Reactions Research Group, Department of Inorganic and Analytical Chemistry, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary.
⁵ Department of Organic Chemistry, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary.
⁶ HUN-REN-UD Molecular Recognition and Interaction Research Group, University of Debrecen, Egyetem tér 1, H-4032 Debrecen, Hungary.
⁷ Centre for Structural Science, Research Centre for Natural Sciences, Hungarian Research Network (HUN-REN), Magyar tudósok körútja 2, H-1117 Budapest, Hungary.

PMID: 38753457
DOI: 10.1021/acs.jmedchem.4c00479

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 (t_1/2 = 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).