Abstract
Antibody–drug conjugate (ADC) development started about three decades ago with the hypothesis that toxins conjugated to antibodies would enhance antitumor activity and reduce toxicity by delivering toxins to specific tumor sites. Since then, the field has evolved to include potent small molecule drugs (SMD) and radiolabeled drugs conjugated to antibodies targeting both solid tumors and hematologic malignancies. Improved ADC technology has paved the way for increased drug delivery to the target tumors and decreased normal tissue exposure to cytotoxic agents. Radio-immunoconjugates (RICs) present a different set of challenges leading to unique development pathways. Several factors need to be taken into consideration when developing RICs, such as decay of radioactivity, potentially higher exposure to normal tissue caused by lower specificity, and dehalogenation leading to a loss of signal. This chapter focuses on antibodies conjugated to SMDs.
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Khandelwal, A., Saber, H., Shapiro, M.A., Zhao, H. (2013). Antibody–Drug Conjugate Development. In: Phillips, G. (eds) Antibody-Drug Conjugates and Immunotoxins. Cancer Drug Discovery and Development. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-5456-4_2
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DOI: https://doi.org/10.1007/978-1-4614-5456-4_2
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