Leslie G. Oesterich, Jonathan W. Riess

Research output: Chapter in Book/Report/Conference proceedingChapter


ROS1 is a receptor tyrosine kinase with ROS1 gene fusions identified in 0.9–2.1% of non-small cell lung cancers (NSCLC), as well as a number of other malignancies. These fusions are constitutively activated, leading to significant changes in cell differentiation, proliferation, growth, and survival. The fusions can be identified by a number of methods including fluorescent in situ hybridization, immunohistochemistry, real-time PCR, and next-generation sequencing. The tyrosine kinase inhibitor crizotinib is a potent inhibitor of ROS1 and was approved by the FDA for treatment of metastatic non-small cell lung cancer (NSCLC) with ROS1 rearrangement in March 2016. However, as with other oncogenes, patients treated with crizotinib eventually develop resistance and progressive disease. A number of different resistance mutations have been discovered, the mechanisms of which can be broken down into two major categories: mutations within the ROS1 kinase domain and bypass signaling pathways. Several additional tyrosine kinase inhibitors are under development with varying degrees of CNS penetration and efficacy against resistance mutations.

Original languageEnglish (US)
Title of host publicationCurrent Cancer Research
PublisherSpringer Nature
Number of pages24
StatePublished - 2019

Publication series

NameCurrent Cancer Research
ISSN (Print)2199-2584
ISSN (Electronic)2199-2592


  • Ceritinib
  • Crizotinib
  • Lung cancer
  • Non-small cell lung cancer
  • Oncogene
  • ROS1 inhibitor
  • ROS1 rearrangement
  • Targeted therapy
  • Tyrosine kinase inhibitor (TKI) resistance
  • Tyrosine kinase inhibitors

ASJC Scopus subject areas

  • Cancer Research
  • Oncology


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