Characteristics of Ibritumomab as Radionuclide Therapy Agent

  • Hidekazu KawashimaEmail author
Part of the Resistance to Targeted Anti-Cancer Therapeutics book series (RTACT, volume 18)


Ibritumomab tiuxetan was approved by the FDA as the first radiolabeled monoclonal antibody (mAb) for radioimmunotherapy (RIT: a selective internal radiation therapy using radioisotopes conjugated to tumor-directed antibodies or those fragments) in early 2002 and is now widely used for the treatment of B-cell non-Hodgkin’s lymphoma (NHL). This pharmaceutical agent consists of the murine anti-CD20 chimeric IgG1 mAb, ibritumomab, which is covalently conjugated with the chelator tiuxetan, permitting stable binding to metal cations. In the clinic, two kinds of radioisotopes can be coupled to ibritumomab tiuxetan, namely 111In for cancer imaging and 90Y for the targeted cytotoxic therapy. Dual-label protocols (confirmation of the appropriate mAb distribution using 111In-ibritumomab tiuxetan, followed by radiotherapy by 90Y-ibritumomab tiuxetan) can lead to the effective RIT. To better understand how these radiopharmaceuticals achieve “theranostics” (a combination of diagnosis and therapy) against B-cell NHL, the pharmaceutical characteristics of 90Y-/111In-conjugated ibritumomab tiuxetan are outlined in this chapter.


Antigen-antibody reaction Radioimmunotherapy β-particle Cytotoxic radiation γ ray In vivo imaging Theranostics 



% injected dose per gram of tissue






Antibody-dependent cellular cytotoxicity


Complement-dependent cytotoxicity


Diethylenetriaminepentaacetic acid


Human antimurine antibody


Dissociation constant


Monoclonal antibody


Medical Internal Radiation Dose


Non-Hodgkin’s lymphoma


Positron emission tomography




Single-photon emission computed tomography


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Copyright information

© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Radioisotope Research CenterKyoto Pharmaceutical UniversityYamashina-ku, KyotoJapan

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