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Profile of entrectinib and its potential in the treatment of ROS1-positive NSCLC: evidence to date

Authors Facchinetti F, Friboulet L

Received 15 June 2019

Accepted for publication 30 August 2019

Published 9 September 2019 Volume 2019:10 Pages 87—94

DOI https://doi.org/10.2147/LCTT.S190786

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Melinda Thomas

Peer reviewer comments 4

Editor who approved publication: Dr Sai-Hong Ignatius Ou


Francesco Facchinetti, Luc Friboulet

INSERM U981, Gustave Roussy Cancer Campus, Université Paris Saclay, Villejuif, France

Correspondence: Francesco Facchinetti
INSERM U981, Gustave Roussy Cancer Campus, 114 Rue Edouard, Villejuif 94800, France
Tel + 33 14 211 5662
Email Francesco.Facchinetti@gustaveroussy.fr

Abstract: ROS1 inhibition provides impressive survival benefits in ROS1-rearranged non-small cell lung cancer (NSCLC) patients. Crizotinib is the only tyrosine kinase inhibitor (TKI) approved by both FDA and EMA for the treatment of ROS1-positive lung cancer. In addition, several TKI have been tested with preliminary proofs of success in this oncogene-driven disease, either in the post-crizotinib setting or as first-line targeted agents. Here we present the evidence concerning entrectinib, an ALK/ROS1/NTRK inhibitor developed across different tumor types harboring rearrangements in these genes, in the context of ROS1-driven NSCLC. Of interest, in August 2019 entrectinib was granted by FDA accelerated approval for the treatment of ROS1-rearranged NSCLC, as well as of NTRK-driven solid tumors.

Keywords: lung cancer, ROS1, tyrosine kinase inhibitors, entrectinib

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