Advances in Anticancer Antibody-Drug Conjugates and Immunotoxins
Franco Dosio, Barbara Stella, Sofia Cerioni, Daniela Gastaldi and Silvia Arpicco
Affiliation: Dipartimento di Scienza e Tecnologia del Farmaco, University of Torino, v. P. Giuria 9, I-10125 Torino, Italy.
Antibody-delivered drugs and toxins are poised to become important classes of cancer therapeutics. These biopharmaceuticals
have potential in this field, as they can selectively direct highly potent cytotoxic agents to cancer cells
that present tumor-associated surface markers, thereby minimizing systemic toxicity. The activity of some conjugates is of
particular interest receiving increasing attention, thanks to very promising clinical trial results in hematologic cancers.
Over twenty antibody-drug conjugates and eight immunotoxins in clinical trials as well as some recently approved drugs,
support the maturity of this approach. This review focuses on recent advances in the development of these two classes of
biopharmaceuticals: conventional toxins and anticancer drugs, together with their mechanisms of action. The processes of
conjugation and purification, as reported in the literature and in several patents, are discussed and the most relevant results
in clinical trials are listed. Innovative technologies and preliminary results on novel drugs and toxins, as reported in the
literature and in recently-published patents (up to February 2013) are lastly examined.
Keywords: Antibody drug conjugate, anticancer agents, auristatins immunotoxin, calicheamicins, cross-linkers, duocarmycins,
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