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

Francesco Facchinetti, Luc Friboulet INSERM U981, Gustave Roussy Cancer Campus, Université Paris Saclay, Villejuif, FranceCorrespondence: Francesco FacchinettiINSERM U981, Gustave Roussy Cancer Campus, 114 Rue Edouard, Villejuif 94800, FranceTel + 33 14 211 5662Email Francesco.Facchinetti...

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Autores principales: Facchinetti F, Friboulet L
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2019
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Acceso en línea:https://doaj.org/article/86eac883de4548c38cf524c882715cd7
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Sumario:Francesco Facchinetti, Luc Friboulet INSERM U981, Gustave Roussy Cancer Campus, Université Paris Saclay, Villejuif, FranceCorrespondence: Francesco FacchinettiINSERM U981, Gustave Roussy Cancer Campus, 114 Rue Edouard, Villejuif 94800, FranceTel + 33 14 211 5662Email Francesco.Facchinetti@gustaveroussy.frAbstract: 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