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Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
Published on: July 17, 2019
Cardiotoxicity of BRAF/MEK inhibitors
Katharina Seuthe1, Valerie Lohner2, Kevin Terre3
1Faculty of Medicine and University Hospital Cologne, Clinic III for Internal Medicine, University of Cologne, Cologne, Germany.
Abstract:
Rapidly accelerated fibrosarcoma type B/B-Raf proto-oncogene, serine/threonine kinase (BRAF) and mitogen-activated protein kinase (MEK) inhibitors have transformed outcomes in cancer therapy, particularly in melanoma. However, cardiovascular toxicities are increasingly recognized in real-world clinical practice. Reported events include asymptomatic left ventricular ejection fraction decline and heart failure, hypertension, venous and arterial thromboembolism, QT prolongation or arrhythmias. The underlying mechanisms are multifactorial, involving on-target disturbances of extracellular signal-regulated kinase signalling in cardiomyocytes and endothelium, off-target mitochondrial and metabolic effects, microvascular dysfunction and inflammation, with risk patterns differing between combination therapy and monotherapy. This review synthesizes the biological rationale of BRAF and MEK inhibitors, summarizes incidence and phenotype of cardiotoxicity across pivotal trials and observational cohorts, outlines baseline risk assessment and surveillance strategies and proposes pragmatic management algorithms aligned with contemporary cardio-oncology guidance. Understanding, detecting, and managing cardiotoxicity proactively enables safe delivery of highly effective BRAF/MEK-directed therapy while preserving cardiovascular health.
Insights
BRAF and MEK inhibitors improve cancer therapy but can cause heart problems like heart failure and arrhythmias. Early detection and management are key to safe treatment and preserving heart health.
Area of Science:
- Cardio-oncology
- Molecular oncology
- Pharmacology
Background:
- BRAF and MEK inhibitors have revolutionized cancer treatment, especially for melanoma.
- Cardiovascular toxicities associated with these inhibitors are a growing concern in clinical practice.
Purpose of the Study:
- To review the mechanisms and clinical implications of BRAF and MEK inhibitor-induced cardiotoxicity.
- To provide guidance on risk assessment, surveillance, and management of cardiotoxicity.
Main Methods:
- Literature review synthesizing biological rationale, clinical trial data, and observational cohort studies.
- Analysis of reported cardiovascular events, including heart failure, hypertension, thromboembolism, and arrhythmias.
- Development of management algorithms based on current cardio-oncology guidelines.
Main Results:
- Cardiotoxicity manifests as left ventricular dysfunction, heart failure, hypertension, thromboembolism, and arrhythmias.
- Mechanisms are multifactorial, involving on-target and off-target effects on cardiomyocytes and endothelium.
- Risk profiles differ between combination and monotherapy.
Conclusions:
- Proactive understanding, detection, and management of cardiotoxicity are crucial.
- These strategies enable safe administration of BRAF/MEK inhibitor therapy.
- Preserving cardiovascular health is paramount during cancer treatment.
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