Rituximab (Rituxan), a monoclonal antibody (mAb) against CD-20, and trastuzumab (Herceptin), a mAb against HER2, have shown efficacy in clinical trials and have gained approval for therapeutic use from the Food and Drug Administration (FDA). Mylotarg, an anti-CD33 mAb conjugated with the exceedingly cytotoxic antibiotic calicheamicin, has also proven effective for treating patients with acute myeloid leukemia (AML) and it has also received FDA approval. A major area of development in mAb therapeutics involves the use of radionuclides to augment the inherent mAb activity and to exploit specific targeting properties. Zevalin, an anti-CD20 mAb armed with 90Y, and Bexxar, an anti-CD20 mAb armed with 131I, are two radionuclide-bearing mAbs that have recently been approved by the FDA. This chapter presents the background and strategies pertaining to radiolabeled monoclonal antibody therapy.
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