Entrectinib

Entrectinib

  • August 2018 •
  • 15 pages •
  • Report ID: 5780213 •
  • Format: PDF
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.