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Kinase Inhibitor Conjugates

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In the last decade kinase inhibitors have emerged as a new class of very potent and relatively safe anticancer drugs. However, despite their success, off-target toxicities and induction of rapid resistance are major drawbacks that highly compromise successful longterm administration. In the current review, we provide an overview of the approaches that have been undertaken to overcome these issues by conjugation of these agents to carriers that enable their cellular and/or intracellular targeted delivery. Eventually, targeting kinase inhibitors will provide powerful treatment options not only for cancer, but also for other less-life threatening diseases that involve deregulated kinase signaling pathways.

Keywords: CML patients; Drug targeting; anticancer drugs; conjugation; drug resistance; intracellular targeted delivery; kinase inhibitors; kinase signaling pathways; long-term administration; off-organ toxicity

Document Type: Research Article

Affiliations: Department of Pharmaceutics, Utrecht Institute of Pharmaceutical Sciences, Utrecht University, Utrecht, the Netherlands.

Publication date: 01 July 2012

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