ROS1 Targeted Therapies: Current Status

Curr Oncol Rep. 2021 Jun 14;23(8):94. doi: 10.1007/s11912-021-01078-y.


Purpose of review: Molecular drivers are increasingly identified as therapeutic targets for non-small cell lung cancer (NSCLC). This review focuses on the role of ROS1 inhibitors in treating relapsed/metastatic ROS-1 altered (ROS1+) NSCLC.

Recent findings: Four FDA-approved drugs have significant activity against ROS1+ NSCLC: crizotinib, ciritinib, lorlatinib, and entrectinib. Each drug yields an overall response rates exceeding 60% with ciritinib, lorlatinib, and entrectinib possessing intracranial activity. The drugs have manageable toxicity profiles. ROS1 alterations are rare molecular drivers of NSCLC that can be effectively treated with a variety of ROS1-targetd drugs. New agents are being identified that may treat resistance mutations.

Keywords: Molecular drivers; Non-small cell lung cancer; ROS1; Targeted therapy.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Drug Resistance, Neoplasm / drug effects
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / pathology
  • Molecular Targeted Therapy / methods*
  • Mutation / drug effects
  • Protein-Tyrosine Kinases / therapeutic use*
  • Proto-Oncogene Proteins / therapeutic use*


  • Antineoplastic Agents
  • Proto-Oncogene Proteins
  • Protein-Tyrosine Kinases
  • ROS1 protein, human