Specific oncology diagnostics requires new types of the selective radiopharmaceuticals, particularly those suitable for the molecular PET imaging. The aim of this work is to present a new, specific PET-immunodiagnostic radiopharmaceutical based on the monoclonal antibody IgG M75 targeting human carbonic anhydrase IX labelled with 64Cu (T½ = 12.70h) and its in vitro and in vivo evaluation. The antibody IgG M75 was conjugated with a non-commercial copper-specific chelator "phosphinate" and then labelled with the positron emitter 64Cu. Stability of the labelled conjugated was tested in human serum. The immunoreactivity of the labelled conjugate was evaluated in vitro on a suitable cell cultures of the colorectal carcinoma (HT-29) and its imaging properties were estimated in vivo on a mouse model with inoculated colorectal carcinoma HT-29 imaged on a µPET/CT. The tested radioimmunoconjugate was obtained in a specific activity of 0.25-0.5 MBq/µg. In vitro uptake experiments revealed specific binding to the HT-29 cells (45 ± 2.8% of the total added activity) and the measured KD value was found to be 9.2nM. Imaging clearly demonstrated significant uptake of the labelled monoclonal antibody in the tumour at 18h post administration. The radioimmunoconjugate 64Cu-PS-IgG M75 seems to be a suitable candidate for PET diagnostics of hypoxic tumours expressing human carbonic anhydrase IX.

• MeSH
• aktivní transport MeSH
• antigeny nádorové imunologie   MeSH
• buňky HT-29 MeSH
• buňky NIH 3T3 MeSH
• imunokonjugáty farmakokinetika   farmakologie   MeSH
• inhibitory enzymů farmakokinetika   farmakologie   MeSH
• karboanhydrasa IX antagonisté a inhibitory   imunologie   MeSH
• kyseliny fosfinové MeSH
• lidé MeSH
• monoklonální protilátky farmakokinetika   farmakologie   MeSH
• myši nahé MeSH
• myši MeSH
• nádory diagnostické zobrazování   enzymologie   MeSH
• PET/CT MeSH
• protinádorové látky imunologicky aktivní farmakokinetika   farmakologie   MeSH
• radiofarmaka farmakokinetika   farmakologie   MeSH
• radioizotopy mědi farmakokinetika   farmakologie   MeSH
• techniky in vitro MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• hodnotící studie MeSH