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Diagnosis of Melanoma with 61 Cu-Labeled PET Tracer.

Authors :
Bunda S
Kálmán-Szabó I
Lihi N
Képes Z
Szikra D
Peline Szabo J
Timári I
Szücs D
May NV
Papp G
Trencsényi G
Kálmán FK
Source :
Journal of medicinal chemistry [J Med Chem] 2024 Jun 13; Vol. 67 (11), pp. 9342-9354. Date of Electronic Publication: 2024 May 16.
Publication Year :
2024

Abstract

Until the recent years, substances containing radioactive <superscript>61</superscript> 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 <subscript>5</subscript> -based Cu(II) complex ([Cu(KFTGdiac)] <superscript>-</superscript> ) and the ex vivo and in vivo characterization of its NAPamide conjugate. The rigid chelate possesses prompt complex formation and suitable inertness ( t <subscript>1/2</subscript> = 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).

Details

Language :
English
ISSN :
1520-4804
Volume :
67
Issue :
11
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
38753457
Full Text :
https://doi.org/10.1021/acs.jmedchem.4c00479