TRK Inhibitors: Tissue-Agnostic Anti-Cancer Drugs [PDF]
Pharmaceuticals, 2021 Recently, two tropomycin receptor kinase (Trk) inhibitors, larotrectinib and entrectinib, have been approved for Trk fusion-positive cancer patients. Clinical trials for larotrectinib and entrectinib were performed with patients selected based on the ...
Sun-Young Han
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Selective type II TRK inhibitors overcome xDFG mutation mediated acquired resistance to the second-generation inhibitors selitrectinib and repotrectinib [PDF]
Acta Pharmaceutica Sinica BNeurotrophic receptor kinase (NTRK) fusions are actionable oncogenic drivers of multiple pediatric and adult solid tumors, and tropomyosin receptor kinase (TRK) has been considered as an attractive therapeutic target for “pan-cancer” harboring these ...
Xiaoyun Lu, Shuang Xiang
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Pyrazolo[1,5-a]pyrimidine as a Prominent Framework for Tropomyosin Receptor Kinase (Trk) Inhibitors—Synthetic Strategies and SAR Insights [PDF]
MoleculesTropomyosin receptor kinases (Trks) are transmembrane receptor tyrosine kinases named TrkA, TrkB, and TrkC and encoded by the NTRK1, NTRK2, and NTRK3 genes, respectively.
Amol T. Mahajan +5 more
doaj +3 more sources
Basket trial of TRK inhibitors demonstrates efficacy in TRK fusion-positive cancers [PDF]
Journal of Hematology & Oncology, 2018 Unlike many conventional cancers with preferential patterns of oncogenic genetic alterations, TRK fusions resulting from NTRK1/2/3 genetic alterations drive oncogenic transformations in more than 20 different malignancies over diverse tissue/cell ...
Yu Chen, Ping Chi
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Entrectinib and other ALK/TRK inhibitors for the treatment of neuroblastoma [PDF]
Drug Design, Development and Therapy, 2018 Holly L Pacenta, Margaret E Macy Department of Pediatrics, University of Colorado Anschutz Medical Campus and Children’s Hospital Colorado, Aurora, CO, USA Abstract: RTK plays important roles in many cellular signaling processes involved in ...
Pacenta HL, Macy ME
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Development of small-molecule tropomyosin receptor kinase (TRK) inhibitors for NTRK fusion cancers [PDF]
Acta Pharmaceutica Sinica B, 2021 Tropomyosin receptor kinase A, B and C (TRKA, TRKB and TRKC), which are well-known members of the cell surface receptor tyrosine kinase (RTK) family, are encoded by the neurotrophic receptor tyrosine kinase 1, 2 and 3 (NTRK1, NTRK2 and NTRK3) genes ...
Tingting Jiang +7 more
doaj +2 more sources
NTRK Fusions and TRK Inhibitors: Potential Targeted Therapies for Adult Glioblastoma [PDF]
Frontiers in Oncology, 2020 IntroductionGlioblastoma multiforme (GBM) is the most common primary central nervous (CNS) system malignancy with a poor prognosis. The standard treatment for GBM is neurosurgical resection, followed by radiochemotherapy and adjuvant temozolomide ...
Yuekun Wang +3 more
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NTRK-fused central nervous system tumours: clinicopathological and genetic insights and response to TRK inhibitors [PDF]
Acta Neuropathologica CommunicationsBackground Neurotrophic tropomyosin receptor kinase (NTRK) gene fusions are found in 1% of gliomas across children and adults. TRK inhibitors are promising therapeutic agents for NTRK-fused gliomas because they are tissue agnostic and cross the blood ...
Eric Eunshik Kim +10 more
doaj +2 more sources
Not all NTRK fusions in mesenchymal neoplasia are driver events: implications on classification and targeted therapy. [PDF]
J Pathol Clin ResAbstract NTRK fusions drive the pathogenesis of a distinctive group of mesenchymal neoplasms with significant impact on classification and targeted therapy. However, unexpected NTRK fusions have been reported in other sarcoma entities, raising uncertainty over their specificity and clinical management.
Yakoub MA +4 more
europepmc +2 more sources
TRK immunohistochemistry in pediatric rhabdomyosarcomas: diagnostic and prognostic utility and limitations [PDF]
Pathology and Oncology ResearchRhabdomyosarcoma is the third most common extracranial solid tumor in childhood. Treatment of patients is multimodal, based on systemic chemotherapy and local therapy by surgery and/or radiotherapy.
Renáta Lajti +8 more
doaj +2 more sources