Phase 1 study to evaluate the effect of the MEK inhibitor trametinib on cardiac repolarization in patients with solid tumours

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• 作者：Amita Patnaik ; Anthony Tolcher…
• 关键词：Trametinib ; MEK inhibitor ; Cancer ; Cardiac repolarization ; QT interval
• 刊名：Cancer Chemotherapy and Pharmacology
• 出版年：2016
• 出版时间：September 2016
• 年：2016
• 卷：78
• 期：3
• 页码：491-500
• 全文大小：522 KB
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Biomedicine
  Cancer Research
  Pharmacology and Toxicology
  Oncology
  
• 出版者：Springer Berlin / Heidelberg
• ISSN：1432-0843
• 卷排序：78

文摘

PurposeTrametinib is a reversible, selective inhibitor of the mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and 2 (MEK2). Cardiotoxicity (congestive heart failure, decreased heart rate, left ventricular dysfunction, and hypertension) related to trametinib is an infrequent, but serious, adverse event (AE). Prolongation of the QT interval increases the risk of life-threatening cardiac arrhythmia. Thus, the risk of trametinib inducing QT prolongation at putative supratherapeutic exposure was evaluated.