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RXDX-101

National Institutes of Health

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entrectinib

Papers overview

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2018
2018
Phase 1 study of entrectinib (RXDX-101), a TRK, ROS1, and ALK inhibitor, in children, adolescents, and young adults with recurrent or refractory solid tumors.
10536Background: Entrectinib (RXDX-101) inhibits TRKA/B/C, ROS1, and ALK tyrosine kinases with IC50 < 2 nM. In vivo, entrectinib… 
Review
2018
Review
2018
LC–MS/MS reveals the formation of iminium and quinone methide reactive intermediates in entrectinib metabolism: In vivo and in vitro metabolic investigation
2016
2016
Abstract 2136: Entrectinib is effective against the gatekeeper and other emerging resistance mutations in NTRK-, ROS1- and ALK- rearranged cancers
Gene rearrangements involving NTRK1, NTRK2, NTRK3, ROS1 and ALK result in oncogenic fusion proteins that have been identified in… 
2015
2015
29LBA Entrectinib (RXDX-101), an oral pan-Trk, ROS1, and ALK inhibitor in patients with advanced solid tumors harboring gene rearrangements
2015
2015
Abstract 5390: The TRK inhibitor RXDX-101 enhances the efficacy of temozolomide and irinotecan in a xenograft model of neuroblastoma
Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA Purpose: Neuroblastoma (NB) is one of the most… 
2014
2014
437 PIM kinase inhibitor AZD1208 sensitises SCLC to BH3 mimetic AZD4320
2014
2014
436 Monitoring activity of RXDX-101 in Phase 1/2 patients using a pharmacodynamic assay for TrkA activation
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