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Targeted Tumor Therapies at a Glance

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Conventional tumor therapy is usually based on surgery, radiation and chemotherapy. Treatment with chemotherapeutics is often impeded by dose-limiting toxicities. Therefore, medical scientists sought for tools to improve chemotherapy by directly coupling targeting molecules to cytotoxic substances. This review provides a general overview on the development of targeted drugs designed for tumor therapy. Further carrier-based delivery systems of antitumorigenic drugs will not be described here. The targeting moiety is usually an antibody or a fragment thereof. Growth factors, cytokines and ligands are also used as targeting moiety. The targeting moiety is coupled to the toxic moiety either chemically or both components were combined as fusion proteins. In addition to those targeted molecules containing conventional chemotherapeutics, more sophisticated targeted drugs were developed containing protein toxins, such as diphtheria toxin or Pseudomonas exotoxin. Only a small number of these protein toxins inside tumor cells results in efficient killing of the target cell. Several of these targeted toxins are currently in clinical trials. Another targeting mechanism utilizes the activation of formerly harmless substances in the vicinity of tumor cells. This mechanism is referred to as directed enzyme prodrug therapy.

Keywords: Tumor therapy; cancer; prodrug; targeted toxins

Document Type: Research Article


Publication date: 2009-02-01

More about this publication?
  • Current Drug Targets aims to cover the latest and most outstanding developments on the medicinal chemistry and pharmacology of molecular drug targets e.g. disease specific proteins, receptors, enzymes, genes. Each issue of the journal will be devoted to a single timely topic, with series of in-depth reviews, written by leaders in the field, covering a range of current topics on drug targets. These issues will be organized and led by a guest editor who is a recognized expert in the overall topic. As the discovery, identification, characterisation and validation of novel human drug targets for drug discovery continues to grow; this journal will be essential reading for all pharmaceutical scientists involved in drug discovery and development.
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