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Entrectinib (ROZLYTREK™)

Entrectinib (Rozlytrek) is a selective inhibitor of the tyrosine kinases TRK A/B/C, ROS1 and ALK, whose activating gene rearrangements drive proliferation in small subsets of different tumor types. Entrectinib was invented and developed into Phase I by NMS, then licensed to Ignyta (San Diego, USA) and subsequently acquired by Roche. Entrectinib was recently approved in USA, Japan and Canada and is in preregistration Phase in Europe for the treatment of adults with ROS1-positive, metastatic non-small cell lung cancer (NSCLC), as well as adult and paediatric patients with relapsed/refractory tumors harbouring NTRK gene fusions. Entrectinib was specifically designed to efficiently penetrate the blood brain barrier and it is efficacious also in patients with brain metastases, with a good tolerability profile.