期刊
EXPERT REVIEW OF ANTICANCER THERAPY
卷 20, 期 5, 页码 333-341出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14737140.2020.1747439
关键词
Entrectinib; lung cancer; NSCLC; NTRK; ROS1; Rozlytrek; targeted therapy
类别
资金
- Fondazione Oncologia Niguarda Onlus
Introduction: Gene fusions are strong driver alterations in various cancers, increasingly diagnosed with multiple testing techniques. ROS1 fusions can be found in 1-2% of non-small cell lung cancer (NSCLC) and several tyrosine kinase inhibitors (TKIs) have been tested in this oncogene-driven disease. NTRK fusions are characteristic of a few rare types of cancer, also infrequently seen in some common cancers including NSCLC. Entrectinib is a newer ROS1 and NTRK inhibitor developed across different tumor types harboring rearrangements in these genes. Entrectinib was granted FDA accelerated approval in August 2019 for the treatment of ROS1+ NSCLC and NTRK-driven solid tumors. Areas covered: This review covers the mechanism of action, safety, and efficacy of entrectinib in patients with metastatic NSCLC. Expert opinion: Entrectinib is an orally bioavailable TKI of TrkA, TrkB, TrkC, and ROS1, with the ability to cross the blood-brain barrier. Entrectinib was effective and well-tolerated in patients harboring ROS1- or NTRK-rearranged NSCLC treated within phase I and II studies. Entrectinib appears to be the most appropriate treatment choice for TKIs-naive patients, especially in those presenting brain metastasis. Conversely, in case of systemic progression with the evidence of acquired resistance mutations in ROS1 or Trk proteins, a sequential therapy with entrectinib could not be successful.
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