Abstract
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: Drug targeting, kinase inhibitors, conjugation, drug resistance, off-organ toxicity, anticancer drugs, long-term administration, intracellular targeted delivery, kinase signaling pathways, CML patients
Current Pharmaceutical Design
Title:Kinase Inhibitor Conjugates
Volume: 18 Issue: 20
Author(s): Stefan Harmsen and Robbert Jan Kok
Affiliation:
Keywords: Drug targeting, kinase inhibitors, conjugation, drug resistance, off-organ toxicity, anticancer drugs, long-term administration, intracellular targeted delivery, kinase signaling pathways, CML patients
Abstract: 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.
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Cite this article as:
Harmsen Stefan and Jan Kok Robbert, Kinase Inhibitor Conjugates, Current Pharmaceutical Design 2012; 18 (20) . https://dx.doi.org/10.2174/138161212800672778
DOI https://dx.doi.org/10.2174/138161212800672778 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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