Anti-HER2 antibody DOTA-pertuzumab conjugation and labelling studies with Ac-225

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68407700%3A21340%2F22%3A00361724" target="_blank" >RIV/68407700:21340/22:00361724 - isvavai.cz</a>

Výsledek na webu

<a href="https://link.springer.com/article/10.1007/s00259-022-05924-4" target="_blank" >https://link.springer.com/article/10.1007/s00259-022-05924-4</a>

DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Anti-HER2 antibody DOTA-pertuzumab conjugation and labelling studies with Ac-225

Popis výsledku v původním jazyce

The overexpression of human epidermal growth factor receptor type 2 (HER2) is observed in various tumours. It serves as a prognostic and predictive biomarker. Targeting of HER2 receptors by monoclonal antibodies such as trastuzumab or pertuzumab is used in immunotherapy of these diseases]. The similar targeting concept can and has been applied in radioimmunotherapy. In recent years the most focus is placed on use of alpha-emitting radionuclides which makes radioimmunotherapy a part of targeted alpha-particle therapy. The most studied radionuclides are therefore At-211, Pb-212 or Ac-225. The use of Ac-225 can be especially benefcial thanks to the enormous energy released per one decay. Even though, this radionuclide has already been studied in labelling of various monoclonal antibodies and nanobodies, labelling of pertuzumab monoclonal antibody has been neglected. In this study the conjugation of pertuzumab with DOTA-NHS bifunctional chelator and radiolabelling of prepared conjugates by Ac-225 was performed. The concentration of conjugate was confrmed by UV spectrometry and the conjugate was characterized by MALDI-TOF-MS. The radiolabeling was carried out for various conjugate:radionuclide molar ratios and reaction volumes and pH. The kinetics of radiolabelling was tested by TLC.

Název v anglickém jazyce

Anti-HER2 antibody DOTA-pertuzumab conjugation and labelling studies with Ac-225

Popis výsledku anglicky

The overexpression of human epidermal growth factor receptor type 2 (HER2) is observed in various tumours. It serves as a prognostic and predictive biomarker. Targeting of HER2 receptors by monoclonal antibodies such as trastuzumab or pertuzumab is used in immunotherapy of these diseases]. The similar targeting concept can and has been applied in radioimmunotherapy. In recent years the most focus is placed on use of alpha-emitting radionuclides which makes radioimmunotherapy a part of targeted alpha-particle therapy. The most studied radionuclides are therefore At-211, Pb-212 or Ac-225. The use of Ac-225 can be especially benefcial thanks to the enormous energy released per one decay. Even though, this radionuclide has already been studied in labelling of various monoclonal antibodies and nanobodies, labelling of pertuzumab monoclonal antibody has been neglected. In this study the conjugation of pertuzumab with DOTA-NHS bifunctional chelator and radiolabelling of prepared conjugates by Ac-225 was performed. The concentration of conjugate was confrmed by UV spectrometry and the conjugate was characterized by MALDI-TOF-MS. The radiolabeling was carried out for various conjugate:radionuclide molar ratios and reaction volumes and pH. The kinetics of radiolabelling was tested by TLC.

Druh

O - Ostatní výsledky

CEP obor

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OECD FORD obor

10402 - Inorganic and nuclear chemistry

Projekt

<a href="/cs/project/TJ04000129" target="_blank" >TJ04000129: Separace radionuklidů pro cílenou alfa částicovou terapii</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2022

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů