Monoclonal antibodies (mAbs) have played a major role in cancer medicine, with active drugs such as trastuzumab (Herceptin), cetuximab (Erbitux), bevacizumab (Avastin) and rituximab (Rituxan) in a wide range of therapeutic applications. The mechanisms of these agents involve such activities as direct signaling, interactions with Fcg receptors on effector cells, and complement fixation. Several approaches have been explored to improve antibody-based therapies for cancer treatment by optimizing such activities and by conscripting their selectivity profiles for the delivery of high potency cytotoxic drugs. The field has advanced significantly in the past few years, with the approval of brentuximab vedotin (ADCETRIS) for the treatment of relapsed Hodgkin and anaplastic large cell lymphomas. The antibody-drug conjugate (ADC) is comprised of a potent antimitotic agent, monomethyl auristatin E (MMAE), conjugated to an anti-CD30 mAb through a lysosomally cleavable dipeptide linker. This presentation will describe the discovery and development of this drug and will overview advancements in the field of ADCs for cancer therapy, with particular emphasis on parameters that impact activity, tolerability, and potency.<br/>

Potent antibody-based conjugates for cancer therapy: From early stage research to a clinically approved drug

254th National Meeting (2017)

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