NTRK fusions in lung cancer: From biology to therapy.
Sign Up to like & getrecommendations! Published in 2021 at "Lung cancer"
DOI: 10.1016/j.lungcan.2021.09.005
Abstract: Fusions involving TRK protein tyrosine kinases are oncogenic drivers in a variety of tumors in children and adults, with a prevalence of ∼0.2% in non-small cell lung cancer. Diagnosis can be challenging due to structural… read more here.
Keywords: ntrk fusions; trk; biology; lung cancer ... See more keywords
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00308
Abstract: Tropomyosin receptor kinase (TRK) secondary mutations mediating acquired resistance, especially at the solvent-front (SF) and the DFG motif, represent an unmet clinical need. Small-molecule macrocyclic kinase inhibitors have displayed significant advantages in overcoming clinical resistance… read more here.
Keywords: acquired resistance; trk; resistance; trk inhibitors ... See more keywords
Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01607
Abstract: Changes in expression and dysfunctional signaling of TrkA/B/C receptors and oncogenic Trk fusion proteins are found in neurological diseases and cancers. Here, we describe the development of a first 18F-labeled optimized lead suitable for in… read more here.
Keywords: trk; fluorine labeled; identification 18f; 18f track ... See more keywords
Comment on: “Tumour-agnostic drugs in paediatric cancers”, Chisholm et al., BJC 2020
Sign Up to like & getrecommendations! Published in 2020 at "British Journal of Cancer"
DOI: 10.1038/s41416-020-01103-0
Abstract: We agree in principle with our colleagues’ endorsement in this journal of the use of the tropomyosin receptor kinase (TRK) inhibitor LOXO-101 (larotrectinib) in children. Our enthusiasm for the accelerated deployment of LOXO-101 has been… read more here.
Keywords: comment tumour; tumour agnostic; trk; loxo 101 ... See more keywords
NTRK fusion-positive cancers and TRK inhibitor therapy
Sign Up to like & getrecommendations! Published in 2018 at "Nature Reviews Clinical Oncology"
DOI: 10.1038/s41571-018-0113-0
Abstract: NTRK gene fusions involving either NTRK1, NTRK2 or NTRK3 (encoding the neurotrophin receptors TRKA, TRKB and TRKC, respectively) are oncogenic drivers of various adult and paediatric tumour types. These fusions can be detected in the… read more here.
Keywords: ntrk fusion; trk inhibitors; trk; fusion ... See more keywords
Tumour response to TRK inhibition in a patient with pancreatic adenocarcinoma harbouring an NTRK gene fusion
Sign Up to like & getrecommendations! Published in 2019 at "Annals of Oncology"
DOI: 10.1093/annonc/mdz385
Abstract: Abstract Background Although rare, NTRK gene fusions are known to be oncogenic drivers in pancreatic ductal adenocarcinoma (PDAC). We report the response of a metastatic CTRC-NTRK1 gene fusion-positive PDAC to targeted treatment with the oral… read more here.
Keywords: response; gene fusion; trk; gene ... See more keywords
TRK Fusions Are Enriched in Cancers with Uncommon Histologies and the Absence of Canonical Driver Mutations
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DOI: 10.1158/1078-0432.ccr-19-3165
Abstract: Purpose: TRK inhibitors achieve marked tumor-agnostic efficacy in TRK fusion–positive cancers and consequently are now an established standard of care. Little is known, however, about the demographics, outcomes, response to alternative standard therapies, or genomic… read more here.
Keywords: trk inhibitors; trk fusions; trk fusion; trk ... See more keywords
Abstract B184: TPX-0005, a highly potent TRK inhibitor, effectively overcomes clinical-resistance TRK mutations including solvent front mutants TRKA G595R, TRKB G639R, and TRKC G623R
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.targ-17-b184
Abstract: The tropomyosin receptor kinases (TRKs), including TRKA/B/C encoded by NTRK1/2/3 genes, are high-affinity receptors for neurotrophins. Oncogenic rearrangement of NTRK1, NTRK2, and NTRK3 have been identified in many solid malignancies. The use of TRK inhibitors… read more here.
Keywords: inhibitor; trk; trka g595r; tpx 0005 ... See more keywords
Abstract 4179: Potent and selective TRK inhibitor CH7057288
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DOI: 10.1158/1538-7445.am2017-4179
Abstract: TRK receptor tyrosine kinases are expressed as fusion proteins encoded by various fusion genes across a wide variety of cancer types, including lung and colorectal cancer. These fusion proteins have potent oncogenic activity and are… read more here.
Keywords: trk inhibitor; potent selective; inhibitor; trk ... See more keywords
Abstract CT127: Phase I and expanded access experience of LOXO-195 (BAY 2731954), a selective next-generation TRK inhibitor (TRKi)
Sign Up to like & getrecommendations! Published in 2019 at "Clinical Trials"
DOI: 10.1158/1538-7445.am2019-ct127
Abstract: Background: Larotrectinib, a selective TRKi, is now FDA approved for pediatric and adult TRK-fusion solid tumors, regardless of tumor origin. Emergent TRK kinase mutations are a common mechanism of resistance to TRKis. LOXO-195, a selective… read more here.
Keywords: trk kinase; trk; expanded access; loxo 195 ... See more keywords
Abstract PR01: Blocking Colony Stimulating Factor 1 Receptor (CSF-1R) and Tropomyosin Receptor Kinase (Trk) improves antitumor efficacy of immunotherapy
Sign Up to like & getrecommendations! Published in 2017 at "Cancer immunology research"
DOI: 10.1158/2326-6074.tumimm16-pr01
Abstract: The tumor microenvironment can provide a strong limitation to the antitumor activity of immunotherapy. Established tumors can escape immune responses by creating an inflammatory milieu that supports and recruits tumor-infiltrating myeloid cells (TIMs) with immune… read more here.
Keywords: immunotherapy; trk; csf; cancer ... See more keywords