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Biomedicines 2014, 2(1), 1-13;

Conjugates of Small Molecule Drugs with Antibodies and Other Proteins

Protein Interactions Group, Cancer and Inflammation Program, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, USA
Basic Science Program, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, MD 21702, USA
Genentech., San Francisco, CA 94080, USA
Author to whom correspondence should be addressed.
Received: 19 November 2013 / Revised: 17 January 2014 / Accepted: 17 January 2014 / Published: 24 January 2014
(This article belongs to the Special Issue Feature Papers)
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Conjugates of small molecule drugs with antibodies (ADCs) and with other proteins (protein-drug conjugates, PDC) are used as a new class of targeted therapeutics combining the specificity of monoclonal antibodies (mAbs) and other proteins with potent cytotoxic activity of small molecule drugs for the treatment of cancer and other diseases. A(P)DCs have three major components, antibody (targeting protein), linker and payload, the cytotoxic drug. Recently, advances in identifying targets, selecting highly specific mAbs of preferred isotypes, optimizing linker technology and improving chemical methods for conjugation have led to the approval of two ADCs by Food and Drug Administration (FDA) and more than 30 ADCs in advanced clinical development. However, the complex and heterogeneous nature of A(P)DCs often cause poor solubility, instability, aggregation and eventually unwanted toxicity. This article reviews the main components of A(P)DCs, and discusses the choices for drugs, linkers and conjugation methods currently used. Future work will need to focus on developments and strategies for overcoming such major problems associated with the A(P)DCs. View Full-Text
Keywords: antibody-drug conjugates; ADC; biotherapeutics; drugs; biologics antibody-drug conjugates; ADC; biotherapeutics; drugs; biologics

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Feng, Y.; Zhu, Z.; Chen, W.; Prabakaran, P.; Lin, K.; Dimitrov, D.S. Conjugates of Small Molecule Drugs with Antibodies and Other Proteins. Biomedicines 2014, 2, 1-13.

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