Does the Number of Bifunctional Chelators Conjugated to a mAb Affect the Biological Activity of Its Radio-Labeled Counterpart? Discussion Using the Example of mAb against CD-20 Labeled with


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
12 05 2022
Historique:
pubmed: 21 4 2022
medline: 18 5 2022
entrez: 20 4 2022
Statut: ppublish

Résumé

There has been considerable interest in developing a monoclonal antibody (mAb) against-CD-20 (for example, Rituximab) modified by bifunctional chelating agents (BCA) for non-Hodgkin's lymphoma radioimmunotherapy. Therefore, many researchers have modified this monoclonal antibody by attaching different BCA moieties and evaluated their biological activities in terms of in vitro study and in vivo study in healthy and tumor xenografted rodents. This mini-perspective reviews the in vitro studies, the immunoreactivity and physiological distribution studies: organ-to-blood and the tumor-to-organ ratio of conjugates with different numbers of chelators per mAb. We set up a null hypothesis that states there is no statistical significance between the biological activity of monoclonal antibody (Rituximab) and the number of conjugated bifunctional chelators. Overall, we have concluded that there is no strong evidence for this hypothesis. However, the literature data should be questioned due to the potential lack of uniform study methodology.

Identifiants

pubmed: 35442675
doi: 10.1021/acs.jmedchem.1c02044
pmc: PMC9109692
doi:

Substances chimiques

Antibodies, Monoclonal 0
Chelating Agents 0
Radioisotopes 0
Rituximab 4F4X42SYQ6
Lutetium 5H0DOZ21UJ

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

6419-6430

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Auteurs

Urszula Karczmarczyk (U)

National Centre for Nuclear Research, Radioisotope Centre POLATOM, Otwock 05-400, Poland.

Agnieszka Sawicka (A)

National Centre for Nuclear Research, Radioisotope Centre POLATOM, Otwock 05-400, Poland.

Piotr Garnuszek (P)

National Centre for Nuclear Research, Radioisotope Centre POLATOM, Otwock 05-400, Poland.

Michał Maurin (M)

National Centre for Nuclear Research, Radioisotope Centre POLATOM, Otwock 05-400, Poland.

Wioletta Wojdowska (W)

National Centre for Nuclear Research, Radioisotope Centre POLATOM, Otwock 05-400, Poland.

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Classifications MeSH