Document Detail


Why do kinase inhibitors cause cardiotoxicity and what can be done about it?
MedLine Citation:
PMID:  20728698     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Cancer growth and metastasis are often driven by activating mutations in, or gene amplications of, specific tyrosine or serine/threonine kinases. Kinase inhibitors (KIs) promised to provide targeted therapy-specifically inhibiting the causal or contributory kinases driving tumor progression while leaving function of other kinases intact. These inhibitors are of 2 general classes: (1) monoclonal antibodies that are typically directed against receptor tyrosine kinases or their ligands and (2) small molecules targeting specific kinases. The latter will be the focus of this review. This class of therapeutics has had some remarkable successes, including revolutionizing the treatment of some malignancies (eg, imatinib [Gleevec] in the management of chronic myeloid leukemia) and adding significantly to the management of other difficult to treat cancers (eg, sunitinib [Sutent] and sorafenib [Nexavar] in the management of renal cell carcinoma). But in some instances, cardiotoxicity, often manifest as left ventricular dysfunction and/or heart failure, has ensued after the use of KIs in patients. Herein we will explore the mechanisms underlying the cardiotoxicity of small-molecule KIs, hoping to explain how and why this happens, and will further examine strategies to deal with the problem.
Authors:
Hui Cheng; Thomas Force
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Progress in cardiovascular diseases     Volume:  53     ISSN:  1873-1740     ISO Abbreviation:  Prog Cardiovasc Dis     Publication Date:    2010 Sep-Oct
Date Detail:
Created Date:  2010-08-23     Completed Date:  2010-09-27     Revised Date:  2013-05-02    
Medline Journal Info:
Nlm Unique ID:  0376442     Medline TA:  Prog Cardiovasc Dis     Country:  United States    
Other Details:
Languages:  eng     Pagination:  114-20     Citation Subset:  AIM; IM    
Copyright Information:
Copyright 2010 Elsevier Inc. All rights reserved.
Affiliation:
Center for Translational Medicine and Cardiology Division, Thomas Jefferson University, Philadelphia, PA 19107, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antineoplastic Agents / adverse effects*,  chemistry
Drug Design
Heart Failure / chemically induced*,  pathology,  prevention & control
Humans
Myocytes, Cardiac / drug effects*,  pathology
Neoplasms / drug therapy*,  enzymology
Protein Kinase Inhibitors / adverse effects*,  chemistry
Risk Assessment
Structure-Activity Relationship
Ventricular Dysfunction, Left / chemically induced*,  pathology,  prevention & control
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Protein Kinase Inhibitors

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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