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Updated: Sep 30, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Cardiotoxicity Induced by Protein Kinase Inhibitors in Patients with Cancer
Aleksandra Grela-Wojewoda1, Renata Pacholczak-Madej1,2, Agnieszka Adamczyk3
1Department of Clinical Oncology, Maria Sklodowska-Curie National Research Institute of Oncology, Kraków Branch, Garncarska 11, 31-115 Kraków, Poland.
Abstract:
Kinase inhibitors (KIs) represent a growing class of drugs directed at various protein kinases and used in the treatment of both solid tumors and hematologic malignancies. It is a heterogeneous group of compounds that are widely applied not only in different types of tumors but also in tumors that are positive for a specific predictive factor. This review summarizes common cardiotoxic effects of KIs, including hypertension, arrhythmias with bradycardia and QTc prolongation, and cardiomyopathy that can lead to heart failure, as well as less common effects such as fluid retention, ischemic heart disease, and elevated risk of thromboembolic events. The guidelines for cardiac monitoring and management of the most common cardiotoxic effects of protein KIs are discussed. Potential signaling pathways affected by KIs and likely contributing to cardiac damage are also described. Finally, the need for further research into the molecular mechanisms underlying the cardiovascular toxicity of these drugs is indicated.
Insights
Kinase inhibitors (KIs) combat cancer but can cause heart problems like hypertension and cardiomyopathy. This review details KI cardiotoxicity, monitoring, and management strategies.
Area of Science:
- Oncology
- Cardiology
- Pharmacology
Background:
- Kinase inhibitors (KIs) are crucial in treating solid tumors and hematologic malignancies.
- These drugs target various protein kinases and are used in tumors with specific predictive factors.
Purpose of the Study:
- To review the common and less common cardiotoxic effects of kinase inhibitors.
- To discuss guidelines for cardiac monitoring and management of KI-induced cardiotoxicity.
- To explore potential signaling pathways involved in KI cardiovascular damage.
Main Methods:
- Literature review of kinase inhibitors and their cardiovascular effects.
- Analysis of reported cardiotoxic events associated with KIs.
- Discussion of current cardiac monitoring and management guidelines.
Main Results:
- Common cardiotoxic effects include hypertension, arrhythmias (bradycardia, QTc prolongation), and cardiomyopathy leading to heart failure.
- Less common effects encompass fluid retention, ischemic heart disease, and thromboembolic events.
- Potential signaling pathways contributing to cardiac damage are identified.
Conclusions:
- Kinase inhibitors present significant cardiovascular risks that require careful monitoring and management.
- Further research into the molecular mechanisms of KI cardiotoxicity is essential for improved patient outcomes.
- Understanding these mechanisms can lead to safer and more effective cancer therapies.
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