Article
Cabozantinib overcomes crizotinib resistance in ROS1 fusion-positive cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research - 1 Jan 2015
Katayama Ryohei, Kobayashi Yuka, Friboulet Luc, Lockerman Elizabeth L, Koike Sumie, Shaw Alice T, Engelman Jeffrey A, Fujita Naoya
Abstract excerpt
PURPOSE: ROS1 rearrangement leads to constitutive ROS1 activation with potent transforming activity. In an ongoing phase I trial, the ALK tyrosine kinase inhibitor (TKI) crizotinib shows remarkable initial responses in patients with non-small cell lung cancer (NSCLC) harboring ROS1 fusions; however, cancers eventually develop crizotinib resistance due to acquired mutations such as G2032R in ROS1. Thus,...
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