Diagnosis of Melanoma with 61 Cu-Labeled PET Tracer

• Published in: Journal of medicinal chemistry Vol. 67; no. 11; p. 9342
• Main Authors: Bunda, Szilvia, Kálmán-Szabó, Ibolya, Lihi, Norbert, Képes, Zita, Szikra, Dezső, Peline Szabo, Judit, Timári, István, Szücs, Dániel, May, Nóra V, Papp, Gábor, Trencsényi, György, Kálmán, Ferenc K
• Format: Journal Article
• Language: English
• Published: United States 13.06.2024
• Subjects: Animals; Cell Line, Tumor; Coordination Complexes - chemical synthesis; Coordination Complexes - chemistry; Copper Radioisotopes - chemistry; Humans; Melanoma - diagnostic imaging; Melanoma, Experimental - diagnostic imaging; Mice; Mice, Inbred C57BL; Positron-Emission Tomography - methods; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - chemistry; Tissue Distribution
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/acs.jmedchem.4c00479

Until the recent years, substances containing radioactive Cu 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-15aneN -based Cu(II) complex ([Cu(KFTGdiac)] ) and the and characterization of its NAPamide conjugate. The rigid chelate possesses prompt complex formation and suitable inertness ( = 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) ( ): 12.7, %ID/g: 6.6 ± 0.3, T/M ( ): 22).