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Crizotinib

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https://www.readbyqxmd.com/read/29032042/a-reliable-and-stable-method-for-determination-of-brigatinib-in-rat-plasma-by-uplc-ms-ms-application-to-a-pharmacokinetic-study
#1
Jian Wen, Susu Bao, Yaoyao Cai, Bowen Zhang, Rongrong Wang, Chenchen Wang, Guoxin Hu
Brigatinib is the second-generation anaplastic lymphoma kinase - inhibitor in non-small cell lung cancer and it can overcome the crizotinib-resistance. Chromatographic separation was carried out on an Acquity Ultra Performance Liquid Chromatography (UPLC) unit with a BEH C18 column (2.1mm×50mm, 1.7μm). The mobile phase was composed of acetonitrile and 0.1% formic acid in water. No endogenous interfering compounds was discovered at retention time of brigatinib (0.56min) and imatinib (IS, 1.41min). MS/MS detection was performed in positive mode...
October 5, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29024938/expression-and-role-of-tyro3-and-axl-as-potential-therapeutical-targets-in-leiomyosarcoma
#2
Carmela Dantas-Barbosa, Tom Lesluyes, François Le Loarer, Fréderic Chibon, Isabelle Treilleux, Jean-Michel Coindre, Pierre Meeus, Mehdi Brahmi, Olivia Bally, Isabelle Ray-Coquard, Marie-Pierre Sunyach, Axel Le Cesne, Olivier Mir, Sylvie Bonvalot, Maud Toulmonde, Antoine Italiano, Pierre Saintigny, Myriam Jean-Denis, Francoise Ducimetiere, Dominique Ranchere, Hiba El Sayadi, Laurent Alberti, Jean-Yves Blay
BACKGROUND: Leiomyosarcoma (LMS) are 15% of adult sarcomas and remain seldom curable in metastatic phase. The TAM receptors and their ligands are overexpressed or activated in multiple malignancies, including LMS. METHODS: The TAM receptor and ligand expression was evaluated in LMS cell lines and 358 sarcoma samples by either gene expression or immunohistochemistry. TYRO3 and AXL were knocked down. Crizotinib and foretinib were investigated in vitro. RESULTS: High expression of TYRO3 and AXL was detected in LMS cell lines...
October 12, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/29021430/crizotinib-induced-rectal-perforation-with-abscess
#3
Asako Yanagisawa, Noriko Hayama, Hiroyuki Amano, Makoto Nakamura, Satoshi Hirano, Sukeyuki Nakamura, Hiroshi Tabeta
An 86-year-old Japanese man was diagnosed with stage IV lung adenocarcinoma. The patient was treated with crizotinib after EML4-ALK rearrangement was detected from his pleural effusion. He subsequently developed abdominal pain and rebound tenderness in the right lower abdomen. Contrast-enhanced abdominal CT showed a low-density area in the abdominal cavity. The size of the abscess was decreased by drainage and the administration of antibiotics. Fistulography revealed a fistula from the rectum to the abscess, and a diagnosis of lower intestinal tract perforation with abscess formation was made...
October 11, 2017: Internal Medicine
https://www.readbyqxmd.com/read/28979145/anaplastic-lymphoma-kinase-inhibition-in-metastatic-non-small-cell-lung-cancer-clinical-impact-of-alectinib
#4
REVIEW
Ittai B Muller, Adrianus J de Langen, Elisa Giovannetti, Godefridus J Peters
A subset of non-small cell lung cancer (NSCLC) tumors (5%) harbors an anaplastic lymphoma kinase (ALK) translocation that drives tumorigenesis. The clinically approved first-line treatment crizotinib specifically inhibits ALK and improves progression-free survival (PFS) in treated and untreated patients by 4 months compared to standard chemotherapy. While some patients relapse after crizotinib treatment due to resistance mutations in ALK, second-generation ALK inhibitors effectively induce tumor response and prolong PFS...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28978110/increased-pd-l1-expression-in-erlotinib-resistant-nsclc-cells-with-met-gene-amplification-is-reversed-upon-met-tki-treatment
#5
Christina Demuth, Morten Nørgaard Andersen, Kristine Raaby Jakobsen, Anne Tranberg Madsen, Boe Sandahl Sørensen
INTRODUCTION: Cancer cells can achieve immune evasion by expressing the programmed death receptor 1 ligand (PD-L1) on the cell surface. Blockade of the receptor (PD-1) can avert this evasion. Here we aim at investigating PD-L1 expression in erlotinib-resistant lung cancer cells with MET proto-oncogene (MET) gene amplification. MATERIALS AND METHODS: We employed an erlotinib-resistant NSCLC cell line with MET gene amplification. PD-L1 mRNA (qPCR) and protein (flow cytometry) expression was investigated after treatment with MET and mitogen-activated protein kinase (MAPK) targeting drugs (crizotinib and SCH772984, respectively)...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28971587/concurrent-ros1-gene-rearrangement-and-kras-mutation-in-lung-adenocarcinoma-a-case-report-and-literature-review
#6
You-Cai Zhu, Xue-Ping Lin, Xiao-Feng Li, Li-Xin Wu, Hua-Fei Chen, Wen-Xian Wang, Chun-Wei Xu, Jian-Fa Shen, Jian-Guo Wei, Kai-Qi Du
Lung adenocarcinomas with gene rearrangement in the receptor tyrosine kinase ROS1 have emerged as a rare molecular subtype. Although these lung adenocarcinomas respond to ROS1tyrosine kinase inhibitors, many patients ultimately acquire resistance. ROS1gene rearrangement is generally mutually exclusive with other driver genomic alterations, such as those in EGFR, KRAS, or ALK, thus multiple genomic alterations are extremely rare. Herein, we report a case of a 42-year-old man diagnosed with lung adenocarcinoma positive for a SDC4-ROS1 fusion, who was treated with crizotinib followed by three cycles of chemotherapy...
October 3, 2017: Thoracic Cancer
https://www.readbyqxmd.com/read/28970558/detection-of-known-and-novel-alk-fusion-transcripts-in-lung-cancer-patients-using-next-generation-sequencing-approaches
#7
Julie A Vendrell, Sylvie Taviaux, Benoît Béganton, Sylvain Godreuil, Patricia Audran, David Grand, Estelle Clermont, Isabelle Serre, Vanessa Szablewski, Peter Coopman, Julien Mazières, Valérie Costes, Jean-Louis Pujol, Pierre Brousset, Isabelle Rouquette, Jérôme Solassol
Rearrangements of the anaplastic lymphoma kinase (ALK) gene in non-small cell lung cancer (NSCLC) represent a novel molecular target in a small subset of tumors. Although ALK rearrangements are usually assessed by immunohistochemistry (IHC) and fluorescence in situ hybridization (FISH), molecular approaches have recently emerged as relevant alternatives in routine laboratories. Here, we evaluated the use of two different amplicon-based next-generation sequencing (NGS) methods (AmpliSeq and Archer(®)FusionPlex(®)) to detect ALK rearrangements, and compared these with IHC and FISH...
October 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28966724/correlation-between-c-met-and-aldh1-contributes-to-the-survival-and-tumor-sphere-formation-of-aldh1-positive-breast-cancer-stem-cells-and-predicts-poor-clinical-outcome-in-breast-cancer
#8
Yuka Nozaki, Shoma Tamori, Masahiro Inada, Reika Katayama, Hiromi Nakane, Osamu Minamishima, Yuka Onodera, Makoto Abe, Shota Shiina, Kei Tamura, Daichi Kodama, Keiko Sato, Yasushi Hara, Ryo Abe, Ryoko Takasawa, Atsushi Yoshimori, Nariyoshi Shinomiya, Sei-Ichi Tanuma, Kazunori Akimoto
c-Met is a receptor-type tyrosine kinase, which is involved in a wide range of cellular responses such as proliferation, motility, migration and invasion. It has been reported to be overexpressed in various cancers. However, the role of c-Met in breast cancer stem cells (CSCs) still remains unclear. We herein, show that c-Met expression is significantly elevated in Basal-like type of breast cancer in comparison with other subtypes. High expression of c-Met strongly correlated with the expression of two CSC markers, ALDH1A3 and CD133 in breast cancers...
July 2017: Genes & Cancer
https://www.readbyqxmd.com/read/28961830/combination-therapy-of-erlotinib-crizotinib-in-a-lung-adenocarcinoma-patient-with-primary-egfr-mutation-plus-secondary-met-amplification-and-a-novel-acquired-crizotinib-resistant-mutation-met-g1108c
#9
Y Q Li, S S Song, S H Jiang, X Y Zhang
No abstract text is available yet for this article.
October 1, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/28960893/crizotinib-targets-in-glioblastoma-stem-cells
#10
Audelaure Junca, Claire Villalva, Gaëlle Tachon, Pierre Rivet, Ulrich Cortes, Karline Guilloteau, Anaïs Balbous, Julie Godet, Michel Wager, Lucie Karayan-Tapon
Glioblastoma stem cells (GSCs) are believed to be involved in the mechanisms of tumor resistance, therapeutic failures, and recurrences after conventional glioblastoma therapy. Therefore, elimination of GSCs might be a prerequisite for the development of successful therapeutic strategies. ALK, ROS1, and MET are targeted by Crizotinib, a tyrosine kinase inhibitor which has been approved for treatment of ALK-rearranged non-small-cell lung cancer. In this study we investigated ALK, ROS1, and MET status in nine glioblastoma stem cell lines and tumors from which they arise...
September 27, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28950372/activity-and-safety-of-crizotinib-in-patients-with-advanced-clear-cell-sarcoma-with-met-alterations-european-organization-for-research-and-treatment-of-cancer-phase-2-trial-90101-create
#11
P Schöffski, A Wozniak, P G Casali, P Rutkowski, J-Y Blay, L H Lindner, S J Strauss, A Anthoney, F Duffaud, S Richter, V Grünwald, M G Leahy, P Reichardt, J Sufliarsky, W T van der Graaf, R Sciot, M Debiec-Rychter, T van Cann, S Marréaud, M Lia, T Raveloarivahy, L Collette, S Bauer
Background: Clear cell sarcoma (CCSA) is an orphan malignancy, characterised by a specific t(12;22) translocation, leading to rearrangement of the EWSR1 gene and overexpression of MET. We prospectively investigated the efficacy and safety of the tyrosine kinase inhibitor (TKI) crizotinib in patients with advanced or metastatic CCSA. Patients and methods: Patients with CCSA received oral crizotinib 250 mg twice daily. Primary endpoint was objective response rate (ORR), secondary endpoints included duration of response, disease control rate (DCR), progression-free survival (PFS), progression-free rate (PFR), overall survival (OS), overall survival rate (OSR) and safety...
September 18, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/28938595/multiple-receptor-tyrosine-kinase-activation-related-to-alk-inhibitor-resistance-in-lung-cancer-cells-with-alk-rearrangement
#12
Se Hoon Choi, Dong Ha Kim, Yun Jung Choi, Seon Ye Kim, Jung-Eun Lee, Ki Jung Sung, Woo Sung Kim, Chang-Min Choi, Jin Kyung Rho, Jae Cheol Lee
The activation of alternative receptor tyrosine kinases (RTKs) is known to mediate resistance to ALK inhibitors. However, the role of multiple RTK activation in resistance has yet to be determined. Two crizotinib-resistant (H3122/CR-1 and H3122/CR-2) and one TAE684-resistant (H2228/TR) cell lines were established. Multi-RTK arrays and Western blots were performed to detect the activation of bypass signals. There were no secondary mutations in the sequencing. EGFR and MET were activated in H3122/CR-1 cells whereas EGFR and IGF1R were activated in H3122/CR-2 cells...
August 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28926892/-effect-and-mechanism-of-silibinin-on-the-inhibition-of-alk-positive-nsclc-cells-by-sensitizing-crizotinib
#13
C C Lin, C H Lu, Y H Pan, L Jiao, H Y Chen, L Li, Y He
Objective: To explore the synergistic effect of silibinin combined with crizotinib on anaplastic lymphoma kinase positive (ALK+ ) non-small cell lung cancer (NSCLC) cells and its mechanism. Methods: H2228 and H3122 cells were treated with silibinin, crizotinib alone or in combination. Cell proliferation was measured by 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay and colony formation assay. Migration or invasion ability was tested by wound healing assay or transwell assay, respectively...
September 23, 2017: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
https://www.readbyqxmd.com/read/28911956/alk-and-ros1-double-rearranged-lung-squamous-cell-carcinoma-responding-to-crizotinib-treatment-a-case-report
#14
Qiong Li, Jian Wu, Li-Xu Yan, Jun-Wei Huang, Zhou Zhang, Jin-E Zhang, Xing-Lin Gao, Ze-Ru Luo, Jing Liu, Shi-Fang Yang, Yan-Hui Liu
No abstract text is available yet for this article.
September 11, 2017: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/28903995/ros1-1
#15
REVIEW
Prodipto Pal, Zanobia Khan
ROS1 is a receptor tyrosine kinase that has recently been shown to undergo gene rearrangements in~1%-2% of non-small cell lung carcinoma (NSCLC) and in a variety of other tumours including cholangiocarcinoma, gastric carcinoma, colorectal carcinoma and in spitzoid neoplasms, glioblastoma and inflammatory myofibroblastic tumours. The ROS1 gene fusion undergoes constitutive activation, regulates cellular proliferation and is implicated in carcinogenesis. ROS1 fusions can be detected by fluorescence in situ hybridisation, real-time PCR, sequencing-based techniques and immunohistochemistry-based methods in clinical laboratories...
September 13, 2017: Journal of Clinical Pathology
https://www.readbyqxmd.com/read/28893136/investigation-on-the-binding-mechanism-of-loratinib-with-the-c-ros-oncogene-1-ros1-receptor-tyrosine-kinase-via-molecular-dynamics-simulation-and-binding-free-energy-calculations
#16
Xiaoyun Wu, Yuanyuan Wang, Shanhe Wan, Jiajie Zhang
The c-ros oncogene 1 (ROS1) has proven to be an important cancer target for the treatment of various human cancers. The anaplastic lymphoma kinase inhibitor crizotinib has been granted approval for the treatment of patients with ROS1 positive metastatic non-small-cell lung cancer by the Food and Drug Administration on 2016. However, serious resistance due to the secondary mutation of glycine 2032 to arginine (G2032R) was developed in clinical studies. Loratinib (PF-06463922), a macrocyclic analog of crizotinib, showed significantly improved inhibitory activity against wild-type (WT) ROS1 and ROS1(G2032R) mutant...
September 25, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28891712/molecular-and-clinical-features-of-second-generation-anaplastic-lymphoma-kinase-inhibitors-ceritinib
#17
Tommaso De Pas, Laura Pala, Chiara Catania, Fabio Conforti
The discovery of ALK rearrangement in non-small-cell lung cancer (NSCLC) triggered rapid clinical development of a family of specific drugs targeting this alteration, called ALK inhibitors. Despite high rate of responses, the vast majority of patients treated with first-generation ALK inhibitor crizotinib will ultimately develop disease progression. The second-generation ALK inhibitor, ceritinib, is an oral, small-molecule that inhibits the ALK kinase activity with a potency 20-fold greater than crizotinib, being able to tackle some of the principal mechanisms of resistance to crizotinib...
September 11, 2017: Future Oncology
https://www.readbyqxmd.com/read/28886275/preclinical-rationale-for-combination-of-crizotinib-with-mitomycin-c-for-the-treatment-of-advanced-colorectal-cancer
#18
Avital Lev, Safoora Deihimi, Elena Shagisultanova, Joanne Xiu, Amriti R Lulla, David T Dicker, Wafik S El-Deiry
Colorectal cancer (CRC) is a leading cause of cancer-related deaths in the United States. We analyzed 26 MSI-High and 558 non-MSI-High CRC tumors. BRCA2 mutations were highly enriched (50%) in MSI-High CRC. Immunohistochemistry showed that BRCA2-mutated MSI-High CRC had high c-MET (64%) expression compared to BRCA-WT (17%). We hypothesized a mechanistic link between BRCA2-deficiency and c-MET overexpression and synergistic interaction between drugs that treat BRCA-deficient tumors (mitomycin C (MMC) or PARP inhibitors) and c-MET inhibitors (crizotinib)...
September 8, 2017: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/28882182/-s-crizotinib-induces-apoptosis-in-human-non-small-cell-lung-cancer-cells-by-activating-ros-independent-of-mth1
#19
Xuanxuan Dai, Guilong Guo, Peng Zou, Ri Cui, Weiqian Chen, Xi Chen, Changtian Yin, Wei He, Rajamanickam Vinothkumar, Fan Yang, Xiaohua Zhang, Guang Liang
BACKGROUND: Non-small cell lung cancer (NSCLC) accounts for approximately 80-85% of all lung cancers and is usually diagnosed at an advanced stage with poor prognosis. Targeted therapy has produced unprecedented outcomes in patients with NSCLC as a number of oncogenic drivers have been found. Crizotinib, a selective small-molecule inhibitor, has been widely used for the treatment of NSCLC patients with ALK gene rearrangements. A recent study has also shown that (S)-enantiomer of crizotinib exhibits anticancer activity by targeting the protein mutT homologue (MTH1)...
September 7, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28881678/autophagy-is-required-for-crizotinib-induced-apoptosis-in-met-amplified-gastric-cancer-cells
#20
Rebecca D Schroeder, Woonyoung Choi, David S Hong, David J McConkey
MET amplification has been clinically credentialed as a therapeutic target in gastric cancer, but the molecular mechanisms underlying sensitivity and resistance to MET inhibitors are still not well understood. Using whole-genome mRNA expression profiling, we identified autophagy as a top molecular pathway that was activated by the MET inhibitor crizotinib in drug-sensitive human gastric cancer cells, and functional studies confirmed that crizotinib increased autophagy levels in the drug-sensitive cells in a concentration-dependent manner...
August 1, 2017: Oncotarget
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