Title:Kinase Inhibitor Conjugates
VOLUME: 18 ISSUE: 20
Author(s):Stefan Harmsen and Robbert Jan Kok
Affiliation:Department of Pharmaceutics, Utrecht Institute of Pharmaceutical Sciences, Utrecht University, Utrecht, the Netherlands.
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.
