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Title
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Entrectinib : a potent new TRK, ROS1, and ALK inhibitor
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Author
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Abstract
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| Introduction: Receptor tyrosine kinases (RTKs) and their signaling pathways, control normal cellular processes; however, their deregulation play important roles in malignant transformation. In advanced non-small cell lung cancer (NSCLC), the recognition of oncogenic activation of specific RTKs, has led to the development of molecularly targeted agents that only benefit roughly 20% of patients. Entrectinib is a pan-TRK, ROS1 and ALK inhibitor that has shown potent anti-neoplastic activity and tolerability in various neoplastic conditions, particularly NSCLC. Areas covered: This review outlines the pharmacokinetics, pharmacodynamics, mechanism of action, safety, tolerability, pre-clinical studies and clinical trials of entrectinib, a promising novel agent for the treatment of advanced solid tumors with molecular alterations of Trk-A, B and C, ROS1 or ALK. Expert opinion: Among the several experimental drugs under clinical development, entrectinib is emerging as an innovative and promising targeted agent. The encouraging antitumor activity reported in the Phase 1 studies, together with the acceptable toxicity profile, suggest that entrectinib, thanks to its peculiar mechanism of action, could play an important role in the treatment-strategies of multiple TRK-A, B, C, ROS1, and ALK-dependent solid tumors, including NSCLC and colorectal cancer. That being said, further evidence for its clinical use is still needed. |
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Language
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English
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Source (journal)
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Expert opinion on investigational drugs. - London
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Publication
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London
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2015
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ISSN
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1354-3784
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DOI
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10.1517/13543784.2015.1096344
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Volume/pages
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24
:11
(2015)
, p. 1493-1500
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ISI
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000369914100009
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Pubmed ID
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26457764
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Full text (Publisher's DOI)
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Full text (publisher's version - intranet only)
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