Copper and Copper Complexes in Tumor Therapy

ChemMedChem, Journal Year: 2024, Volume and Issue: 19(11)

Published: March 6, 2024

Copper (Cu), a crucial trace element in physiological processes, has garnered significant interest for its involvement cancer progression and potential therapeutic applications. The regulation of cellular copper levels is essential maintaining homeostasis, as imbalances can lead to toxicity cell death. development drugs that target homeostasis emerged promising strategy anticancer treatment, with particular focus on chelators, ionophores, novel complexes. Recent research also investigated the complexes therapy.

Language: Английский

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Advances in Radioligand Theranostics in Oncology

Molecular Diagnosis & Therapy, Journal Year: 2024, Volume and Issue: 28(3), P. 265 - 289

Published: March 31, 2024

Language: Английский

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Advancements in the development of radiopharmaceuticals for nuclear medicine applications in the treatment of bone metastases

Nuclear Medicine and Biology, Journal Year: 2024, Volume and Issue: 130-131, P. 108879 - 108879

Published: Feb. 3, 2024

Language: Английский

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Comparison of 64Cu-DOTA-PSMA-3Q and 64Cu-NOTA-PSMA-3Q utilizing NOTA and DOTA as bifunctional chelators in prostate cancer: preclinical assessment and preliminary clinical PET/CT imaging

European Journal of Nuclear Medicine and Molecular Imaging, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 15, 2025

This study aims to investigate the efficacy and safety of prostate-specific membrane antigen (PSMA) radiolabeled with copper-64 (64Cu) using bifunctional chelating agents (BFCAs) NOTA (1,4,7-triazacyclononane-1,4,7-triacetic acid) DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid). As widely utilized BFCAs in development radiopharmaceuticals, play a critical role ensuring stable chelation 64Cu. evaluates stability, bioavailability, therapeutic potential these compounds preclinical models initial clinical trials. 64Cu-DOTA-PSMA-3Q 64Cu-NOTA-PSMA-3Q were synthesized by manual labeling. The radiochemical purity, specificity biological distribution product evaluated studies. In 23 patients suspected prostate cancer, PET/CT imaging was used evaluate differences diagnosis. purities are more than 98% have good stability vitro. Biodistribution studies healthy mice revealed that both tracers primarily underwent renal excretion post-injection. Liver uptake significantly higher at 1 h after injection (P<0.05). Micro-PET/CT 22Rv1 tumor-bearing demonstrated similar tumor for (P>0.05). However, 24 h, exhibited better retention compared involving no adverse reactions or significant changes vital signs observed, underscoring tracers. Notably, lacrimal glands (17.73 vs. 10.84), parotid (20.98 16.30), submandibular (20.26 17.28) 64Cu-DOTA-PSMA-3Q. Conversely, sublingual lower (7.10 7.49). Of particular relevance, liver (4.04 8.18), highlighting key difference their biodistribution profiles. Both suitable chelators 64Cu-labeled PSMA-3Q imaging. showed injection, while liver, addition, salivary glands, tissues. Overall, findings highlight importance selecting right agent optimize outcomes. Chinese Clinical Trial Registry ChiCTR2300072655, Registered 20 June 2023.

Language: Английский

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64Cu production via the 68Zn(p,nα)64Cu nuclear reaction: An untapped, cost-effective and high energy production route

Nuclear Medicine and Biology, Journal Year: 2024, Volume and Issue: 128-129, P. 108875 - 108875

Published: Jan. 1, 2024

Language: Английский

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⁶⁴Cu tumor labeling with hexadentate picolinic acid‐based bispidine immunoconjugates

Chemistry - A European Journal, Journal Year: 2024, Volume and Issue: 30(32)

Published: March 20, 2024

Discussed are two picolinate appended bispidine ligands (3,7-diazabicyclo[3.3.1]nonane derivatives) in comparison with an earlier described bis-pyridine derivative, which all known to strongly bind Cu

Language: Английский

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Comparison of a Series of ⁶⁸Ga-Labeled DOTA-LLP2A Conjugates for Positron Emission Tomography Imaging of Very Late Antigen-4 in Melanoma

Molecular Pharmaceutics, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 3, 2025

Melanoma, with its steadily rising global incidence, is characterized by high invasiveness, leading to poor prognosis in advanced stages. There remains an unmet clinical need for the development of radiolabeled PET imaging probes early diagnosis melanoma. Integrin VLA-4, a key factor melanoma metastasis, presents promising protein target address specificity shortcomings existing imaging. This study evaluates

Language: Английский

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Estado del arte y perspectivas futuras de nuevos radionúclidos en Medicina Nuclear. Parte I

Revista Española de Medicina Nuclear e Imagen Molecular, Journal Year: 2025, Volume and Issue: unknown, P. 500082 - 500082

Published: Jan. 1, 2025

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Radiotheranostic landscape: A review of clinical and preclinical development

European Journal of Nuclear Medicine and Molecular Imaging, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 1, 2025

Language: Английский

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Synthesis of Bispidine-Based Prostate-Specific Membrane Antigen-Targeted Conjugate and Initial Investigations

Organics, Journal Year: 2025, Volume and Issue: 6(1), P. 7 - 7

Published: Feb. 10, 2025

Nowadays, PSMA ligands are widely used for radiotheragnostic purposes in prostate cancer. The synthesis of a PSMA-Bisp conjugate was developed and realized with good yield (overall ~58% the last two steps). All newly synthesized compounds were characterized by physicochemical methods: 1H 13C NMR, HRMS, LCMS (for biologically tested samples). Subsequently, Bisp1 (diacetate bispidine ligand), Bisp-alkyne (bifunctional derivative Bisp1), its labeled 64Cu mild conditions. In vitro studies [64Cu]Cu-PSMA-Bisp have shown great stability model solutions. Finally, compared to well-known PSMA-617 they showed similar excess bovine serum (BVS), at same time, labeling is extremely high kinetics conditions, while requires heating (90 °C). Thus, this can be incredibly promising nuclear medicine.

Language: Английский

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