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entrectinib

Known as: N-(5-(3,5-Difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide 
An orally bioavailable inhibitor of the tyrosine kinases tropomyosin receptor kinases (Trk) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic… 
National Institutes of Health

Related topics

Related topics

5 relations

Broader (2)

BenzamidesIndazoles
NCIt Antineoplastic Agent TerminologyReceptor Tyrosine Kinase Inhibition

Narrower (1)

RXDX-101

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
2019
2019
On the right TRK: from oncogene discovery to cancer therapeutics
Circa 1983, transfection of mouse NIH3T3 cells with genomic DNA isolated from human tumours had already yielded the first three… 
2019
2019
Digging into lorlatinib resistance in ALK-positive lung cancer: an editorial.
Non-small cell lung cancers (NSCLC) harboring molecular oncogenic activations (e.g., EGFR, MET, BRAF mutations, ALK, ROS1 fusions… 
2018
2018
Foretinib Overcomes Entrectinib Resistance Associated with the NTRK1 G667C Mutation in NTRK1 Fusion–Positive Tumor Cells in a Brain Metastasis Model
Purpose: Rearrangement of the neurotrophic tropomyosin receptor kinase 1 (NTRK1) gene, which encodes tyrosine receptor kinase A… 
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
2018
2018
Entrectinib Effective across NTRK Fusion-Positive Cancers.
Entrectinib may be an effective therapy for patients with NTRK fusion-positive solid tumors, regardless of tumor type. In a… 
2017
2017
A Kinome-Wide Selective Radiolabeled TrkB/C Inhibitor for in Vitro and in Vivo Neuroimaging: Synthesis, Preclinical Evaluation, and First-in-Human.
The proto-oncogenes NTRK1/2/3 encode the tropomyosin receptor kinases TrkA/B/C which play pivotal roles in neurobiology and… 
2017
2017
Abstract CT030: STARTRK-NG: A phase 1/1b study of entrectinib in children and adolescents with advanced solid tumors and primary CNS tumors, with or without TRK, ROS1, or ALK fusions
Background: The STARTRK-NG (Studies of Tumor Alterations Responsive to Targeting Receptor Kinases - Next Generation) trial is a… 
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
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