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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.
Review
2020
Review
2020
Tropomyosin receptor kinase inhibitors in the management of sarcomas.
PURPOSE OF REVIEW Genetic aberrations resulting in tropomyosin receptor kinase (TRK) fusion proteins can drive oncogenesis and… 
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… 
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
Time-to-treatment discontinuation (TTD) and real-world progression-free survival (rwPFS) as endpoints for comparative efficacy analysis between entrectinib trial and crizotinib real-world ROS1 fusion…
9070 Background: Entrectinib is an oral tyrosine kinase inhibitor for ROS1+ NSCLC. Three phase 1/2 single-arm studies showed… 
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… 
2018
2018
EAPH-10. SUCCESSFUL TREATMENT OF A SECONDARY PEDIATRIC HIGH GRADE GLIOMA WITH A NOVEL BEND4-NTRK2 FUSION WITH ENTRECTINIB, A TRK INHIBITOR
A 2 month old child with a large hemispheric tumor; after subtotal resection, pathology showed pilomyxoid astrocytoma with… 
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… 
2017
2017
Detecting NTRK, ROS1, and ALK gene fusions in gastrointestinal tumor patients.
619Background: The STARTRK-2 trial is a potentially registration-enabling Phase 2 global basket trial of the tyrosine kinase… 
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… 
2016
2016
Patients with NTRK Fusions Respond to Targeted Therapies.
LOXO-101, which targets proteins encoded by gene fusions involving NTRK1, NTRK2, and NTRK3, and entrectinib, which targets fusion… 
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