Antibody-drug conjugates or  are an emerging area of study within medicinal chemistry research. Due to their specificity to disease-targeted antigens, they are generally thought of as sophisticated drug delivery systems.

Over the last decade, antibody-drug conjugates have been actively utilized as therapeutics for hematological and solid tumor cancers due to their capability to deliver a cytotoxic compound to a specific cancer cell with only limited affecting normal or healthy cells.

An antibody drug conjugate has three major constituents: a monoclonal antibody (mAb), a chemical linker, and a potent cytotoxic payload. Researchers and scientists have been working on optimizing antibody-drug conjugates.  Their primary focus is, in many cases, the design and development of either the antibody or the chemical linker. So far, little effort devoted to the optimization of payload compounds.

After reviewing more than 114 ongoing or recently completed clinical trials, Samantha M. Gromek and Marcy J. Balunas at the Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs, CT, USA, noted that there is generally a lack of diversity in the cytotoxic payloads that are utilized.

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The researchers noted that in payload selection, only that seven payload compounds were reported (a number of additional trials are ongoing with structures that have not been reported). Six of these seven payload compounds were derived from natural product sources, with the exception of one synthetic payload, highlighting the importance of natural products as cytotoxic payloads for ADC.

The conclusions are published in the online first edition of volume 15, 2014 of Current Topics in Medicinal Chemistry published by Betham Science.

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