NTRK fusion-positive cancers and TRK inhibitor therapy [PDF]
Nature Reviews Clinical Oncology, 2018 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 clinic using a variety of methods, including tumour DNA and RNA sequencing and plasma cell-free DNA profiling.
Emiliano Cocco +2 more
exaly +5 more sources
NTRK Fusion in Non-Small Cell Lung Cancer: Diagnosis, Therapy, and TRK Inhibitor Resistance [PDF]
Frontiers in Oncology, 2022 Neurotrophic tropomyosin receptor kinase (NTRK) gene fusion has been identified as an oncogenic driver of various solid tumors, and it is rare in non-smalll cell lung cancer (NSCLC) with a frequency of approximately less than 1%.
Fangfang Liu +5 more
doaj +3 more sources
JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo [PDF]
Molecules, 2022 The tropomyosin receptor kinases (TRKs) have been validated as effective targets in anticancer drug discovery. Two first-generation TRK inhibitors have been approved into market and displayed an encouraging therapeutic response in cancer patients ...
Jie Wang +11 more
doaj +3 more sources
TRK inhibitor activity and resistance in TRK fusion-positive cancers in adults [PDF]
Cancer Genetics, 2022 NTRK fusions drive oncogenesis in a variety of adult cancers. The approval of the first-generation TRK inhibitors, larotrectinib and entrectinib, for any cancer with an NTRK fusion represented a focal point in tumor-agnostic drug development. These agents achieve high response rates and durable disease control, and display intracranial activity.
Guilherme Harada, Alexander Drilon
semanticscholar +4 more sources
A novel c-Met/TRK inhibitor 1D228 efficiently inhibits tumor growth by targeting angiogenesis and tumor cell proliferation [PDF]
Cell Death and Disease, 2023 Multiple tumors are synergistically promoted by c-Met and TRK, and blocking their cross-signalling pathway may give better effects. In this study, we developed a tyrosine kinase inhibitor 1D228, which exhibited excellent anti-tumor activity by targeting ...
Baijiao An +16 more
doaj +3 more sources
TRK inhibitor in a patient with metastatic triple-negative breast cancer and fusions identified cell-free DNA analysis [PDF]
Therapeutic Advances in Medical Oncology, 2023 Tissue-agnostic indications for targeted therapies have expanded options for patients with advanced solid tumors. The Food and Drug Administration approvals of the programmed death-ligand 1 inhibitor pembrolizumab and the TRK inhibitors larotrectinib and
Arielle J. Medford +15 more
doaj +3 more sources
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
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
doaj +3 more sources
Selective TRK Inhibitor CH7057288 against TRK Fusion-Driven Cancer [PDF]
Molecular Cancer Therapeutics, 2018 Abstract Members of the tropomyosin receptor kinase (TRK) family are expressed in their constitutively activated forms as a result of a gene fusion that occurs across a wide variety of cancer types. We have identified CH7057288 as a potent and selective TRK inhibitor that belongs to a novel chemical class.
Hiroshi, Tanaka +14 more
openaire +3 more sources
TRK fusion positive cancers: From first clinical data of a TRK inhibitor to future directions [PDF]
Critical Reviews in Oncology/Hematology, 2020 Genetic alterations of neurotrophic tropomyosin or tyrosine receptor kinase (NTRK) 1/2/3 genes generate TRK fusion proteins have been reported in a variety of adult and child cancers from diverse cell/tissue lineages. Larotrectinib, a tumour-agnostic TRK inhibitor, has shown remarkable efficacy in a novel "basket" study which has enrolled patients from
Roviello G. +6 more
openaire +4 more sources