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99mTc-Labeled rituximab, a chimeric murine/human anti-CD20 monoclonal antibody.

Authors

Chopra A.

Source

Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2012 Sep 20 [updated 2012 Oct 25].

Excerpt

Rituximab is a chimeric murine/human monoclonal antibody (mAb) that targets the CD20 antigen (also known as membrane-spanning 4-domains, subfamily A, member 1; or MS4A1), which is expressed on 95% of the transformed B-cells that participate in the pathogenesis of non-Hodgkin lymphomas (NHL; diffused large-B cell, low-grade, or the follicular types), a hematological malignancy, and autoimmune diseases such as rheumatoid arthritis (RA), granulomatosis with polyangiitis (Wegener's granulomatosis), and microscopic polyangiitis. The CD20 antigen is not expressed on any other hematopoietic cells and is not shed for circulation into the plasma or internalized by the cells (1). Therefore, the CD20 antigen is considered to be an excellent target for the treatment of the various B-lymphocyte, cell-based diseases such as those mentioned above. The United States Food and Drug Administration has approved the use of rituximab for the treatment of NHL and the other diseases mentioned above. The exact mechanism of action of rituximab has been discussed by Maloney (2). Although much is known about the pathogenesis of the different forms of NHL at the molecular level, the prognosis for an individual suffering from this disease is based on the morphological and histological information obtained with invasive methods used on the patients (3). As an alternative to the invasive methods, noninvasive procedures, such as imaging with radiolabeled agents using single-photon emission computed tomography (SPECT) or positron emission tomography, are attractive options to screen for patients who can benefit the most from an anti-cancer treatment, and the same imaging technique(s) can be used to monitor and assess the efficacy of a treatment (4). Rituximab was labeled with 99mTc ([99mTc]rituximab) and used with SPECT for the imaging of NHL (1) and several inflammatory autoimmune diseases such as RA, Behcet’s disease, sarcoidosis, and others, in humans (5).

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