Receptor Tyrosine Kinase Fusions and BRAF Kinase Fusions are Rare but Actionable Resistance Mechanisms to EGFR Tyrosine Kinase Inhibitors
نویسندگان
چکیده
منابع مشابه
Mechanisms of resistance to EGFR tyrosine kinase inhibitors
Since the discovery that non-small cell lung cancer (NSCLC) is driven by epidermal growth factor receptor (EGFR) mutations, the EGFR tyrosine kinase inhibitors (EGFR-TKIs, e.g., gefitinib and elrotinib) have been effectively used for clinical treatment. However, patients eventually develop drug resistance. Resistance to EGFR-TKIs is inevitable due to various mechanisms, such as the secondary mu...
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The tyrosine kinase inhibitors (TKI) of the epidermal growth factor receptor (EGFR) are becoming the first line of therapy for advanced non-small cell lung cancer (NSCLC). Acquired mutations in EGFR account for one of the major mechanisms of resistance to the TKIs. Three generations of EGFR TKIs have been used in clinical applications. AZD9291 (osimertinib; Tagrisso) is the first and only FDA a...
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Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have shown dramatic effects against that tumors harboring EGFR activating mutations in the EGFR intracytoplasmic tyrosine kinase domain and resulted in cell apoptosis. Unfortunately, a number of patients ultimately developed resistance by multiple mechanisms. Thus, elucidation of the mechanism of resistance to EGFR-TKIs c...
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Infl ammatory myofi broblastic tumor (IMT) is a neoplasm that typically occurs in children. The genetic landscape of this tumor is incompletely understood and therapeutic options are limited. Although 50% of IMTs harbor anaplastic lymphoma kinase ( ALK) rearrangements, no therapeutic targets have been identifi ed in ALK-negative tumors. We report for the fi rst time that IMTs harbor other actio...
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Aim of present review is to provide an evidence-based update of mechanisms responsible for the onset of resistance to drug therapy by EGFR inhibitors, particularly with regards to TKIs. Among ABC transporters involved in MDR, P-glycoprotein and BCRP have been considered the pumps responsible for TKIs treatment failure. Moreover, two subtypes of EGFR mutations have been described: mutations of t...
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ژورنال
عنوان ژورنال: Journal of Thoracic Oncology
سال: 2018
ISSN: 1556-0864
DOI: 10.1016/j.jtho.2018.05.027