Evaluating entrectinib as a treatment option for non-small cell lung cancer

Expert Opin Pharmacother. 2020 Nov;21(16):1935-1942. doi: 10.1080/14656566.2020.1798932. Epub 2020 Jul 31.


Introduction: Entrectinib, an oral pan-TRK, ALK, and ROS1 inhibitor is approved as a first-line treatment for NTRK-rearranged solid tumors and ROS1-rearranged non-small cell lung cancer (NSCLC). It has demonstrated clinical efficacy for patients harboring the relevant gene rearrangement in both systemic and intracranial disease, regardless of the tumor type.

Areas covered: In this review, the authors analyzed data from preclinical and clinical studies, the characteristics of entrectinib compared to those of other relevant inhibitors (currently available and/or under investigation), and the emerging resistance mechanisms. The authors then provide the readers with their future perspectives.

Expert opinion: Entrectinib has been well studied across many tumor types, including NSCLC with ALK, ROS1, and NTRK rearrangements. The drug has demonstrated favorable properties with oral administration, prolonged response duration, high intracranial efficacy, and a favorable toxicity profile. However, with acquisition of resistance and the development of newer generation TKIs, the optimal place for entrectinib in the landscape of targeted therapies for NSCLC warrants further validation.

Keywords: ALK; NTRK; ROS1; entrectinib; non-small cell lung cancer.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Benzamides / administration & dosage
  • Benzamides / adverse effects
  • Benzamides / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / enzymology
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Clinical Trials as Topic
  • Humans
  • Indazoles / administration & dosage
  • Indazoles / adverse effects
  • Indazoles / therapeutic use*
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / enzymology
  • Lung Neoplasms / pathology
  • Protein Kinase Inhibitors / administration & dosage
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein-Tyrosine Kinases / metabolism*
  • Treatment Outcome


  • Benzamides
  • Indazoles
  • Protein Kinase Inhibitors
  • Protein-Tyrosine Kinases
  • entrectinib