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-naïve 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.
Entrectinib for the treatment of metastatic NSCLC: safety and efficacy / A. Sartore Bianchi, E.G. Pizzutilo, G. Marrapese, F. Tosi, G. Cerea, S. Siena. - In: EXPERT REVIEW OF ANTICANCER THERAPY. - ISSN 1473-7140. - 20:5(2020 May 03), pp. 333-341.
|Titolo:||Entrectinib for the treatment of metastatic NSCLC: safety and efficacy|
SARTORE BIANCHI, ANDREA (Primo) (Corresponding)
PIZZUTILO, ELIO GREGORY (Secondo)
CEREA, GIULIO (Penultimo)
SIENA, SALVATORE (Ultimo)
|Parole Chiave:||Entrectinib; lung cancer; NSCLC; NTRK; ROS1; Rozlytrek; targeted therapy|
|Settore Scientifico Disciplinare:||Settore MED/06 - Oncologia Medica|
|Data di pubblicazione:||3-mag-2020|
|Data ahead of print / Data di stampa:||apr-2020|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1080/14737140.2020.1747439|
|Appare nelle tipologie:||01 - Articolo su periodico|