+353-1-416-8900REST OF WORLD
+44-20-3973-8888REST OF WORLD
1-917-300-0470EAST COAST U.S
1-800-526-8630U.S. (TOLL FREE)


  • PDF Icon


  • 15 Pages
  • August 2018
  • Region: Global
  • Citeline
  • ID: 4775206
Drug Overview
Entrectinib (Roche/Chugai/Nerviano) is a selective tyrosine kinase inhibitor (TKI) of the tropomyosin receptor kinases (Trk) A, B, and C; ROS1; and anaplastic lymphoma kinase (ALK) proteins. Under normal conditions, these oncogenes regulate the flow of cellular growth signaling. However, mutations or molecular alterations can result in overactivity, setting off a signal cascade that drives uncontrolled proliferation. Entrectinib binds to and inhibits TrkA, TrkB, TrkC, ROS1, and ALK, disrupting signaling and thereby leading to an induction of apoptosis and an inhibition of tumor cell proliferation in tumor cells that express these kinases. In vivo models of entrectinib in TrkB expressing neuroblastoma cells suggest that the drug may enhance the efficacy of conventional chemotherapy.

Table of Contents

Drug Overview
Product Profiles
entrectinib : Non-small cell lung cancer (NSCLC)
Figure 24: The authors drug assessment summary for Cyramza in non-small cell lung cancer
Figure 84: The authors drug assessment summary for entrectinib in non-small cell lung cancer
Figure 94: Entrectinib sales for NSCLC across the US, Japan, and five major EU markets, by country, 2017–26
Table 1: Entrectinib pivotal trial data in non-small cell lung cancer