Kálmán-Szabó, Ibolya and Bunda, Szilvia and Lihi, Norbert and Szaniszló, Zsófia and Szikra, Dezső and Péliné Szabó, Judit and Fekete, Anikó and Gyuricza, Barbara and Szücs, Dániel and Papp, Gábor Csaba and Trencsényi, György and Kálmán, Ferenc Krisztián (2023) 61Cu-Labelled radiodiagnostics of melanoma with NAPamide-targeted radiopharmaceutical. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 632. ISSN 0378-5173
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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 diagnostic tool for the detection of melanoma tumors. Inspired by these facts, a new radiotracer, the [61Cu]Cu-KFTG-NAPamide 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). © 2022 Elsevier B.V.
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| Additional Information: | Funding details: Magyar Tudományos Akadémia, MTA, KDP-2021 Funding details: Nemzeti Kutatási Fejlesztési és Innovációs Hivatal, NKFIH, FK-134551, ÚNKP-21-5, ÚNKP-22-5 Funding details: Nemzeti Kutatási, Fejlesztési és Innovaciós Alap, NKFIA Funding text 1: The research was funded by the Hungarian National Research, Development and Innovation Office (FK-134551) project, the New National Excellence Program ÚNKP-21-5 and ÚNKP-22-5 (F. K. K.). F. K. K. acknowledges financial support of the János Bolyai Research Scholarship of the Hungarian Academy of Sciences. The authors are indebted to KIFÜ for awarding access to resource based in Hungary. The research was supported by the KDP-2021 program of the Ministry for Innovation and Technology from the source of the National Research, Development and Innovation Fund (Gy.T. and I. K-SZ.). Funding text 2: The research was funded by the Hungarian National Research, Development and Innovation Office (FK-134551) project, the New National Excellence Program ÚNKP-21-5 and ÚNKP-22-5 (F. K. K.). F. K. K. acknowledges financial support of the János Bolyai Research Scholarship of the Hungarian Academy of Sciences. The authors are indebted to KIFÜ for awarding access to resource based in Hungary. The research was supported by the KDP-2021 program of the Ministry for Innovation and Technology from the source of the National Research, Development and Innovation Fund (Gy.T. and I. K-SZ.). |
| Uncontrolled Keywords: | RADIOTHERAPY; Melanoma; Cu-61; Positron emission tomography (PET); NAPamide; |
| Subjects: | R Medicine / orvostudomány > RM Therapeutics. Pharmacology / terápia, gyógyszertan |
| SWORD Depositor: | MTMT SWORD |
| Depositing User: | MTMT SWORD |
| Date Deposited: | 03 Mar 2023 11:26 |
| Last Modified: | 03 Mar 2023 11:26 |
| URI: | http://real.mtak.hu/id/eprint/161324 |
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