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Crizotinib

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https://www.readbyqxmd.com/read/29220734/high-throughput-routine-determination-of-17-tyrosine-kinase-inhibitors-by-lc-ms-ms
#1
Camille Merienne, Marine Rousset, Dominique Ducint, Nadège Castaing, Karine Titier, Mathieu Molimard, Stéphane Bouchet
Several studies have shown that therapeutic drug monitoring of tyrosine kinase inhibitors (TKI) can improve their benefit in cancer. An analytical tool has been developed in order to quantify 17 tyrosine kinase inhibitors and 2 metabolites in human plasma (afatinib, axitinib, bosutinib, crizotinib, dabrafenib, dasatinib, erlotinib, gefitinib, imatinib, lapatinib, nilotinib, ponatinib, regorafenib, regorafenib M2, regorafenib M5, ruxolitinib, sorafenib, sunitinib, vandetanib). Drugs were arranged in four groups, according to their plasma concentration range: 0...
November 28, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29216400/activity-and-safety-of-crizotinib-in-patients-with-alveolar-soft-part-sarcoma-with-rearrangement-of-tfe3-european-organization-for-research-and-treatment-of-cancer-eortc-phase-2-trial-90101-create
#2
P Schöffski, A Wozniak, B Kasper, S Aamdal, M G Leahy, P Rutkowski, S Bauer, H Gelderblom, A Italiano, L H Lindner, I Hennig, S Strauss, B Zakotnik, A Anthoney, L Albiges, J-Y Blay, P Reichardt, J Sufliarsky, W T A van der Graaf, M Debiec-Rychter, R Sciot, T Van Cann, S Marréaud, T Raveloarivahy, S Collette, S Stacchiotti
Background: Alveolar soft part sarcoma(ASPS) is an orphan malignancy associated with a rearrangement of transcription factor E3(TFE3), leading to abnormal MET gene expression. We prospectively assessed the efficacy and safety of the tyrosine kinase inhibitor(TKI) crizotinib in patients with advanced or metastatic ASPS. Patients and methods: Eligible patients with reference pathology-confirmed ASPS received oral crizotinib 250 mg twice daily. By assessing the presence or absence of a TFE3 rearrangement, patients were attributed to MET+ and MET- sub-cohorts...
December 5, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29209525/final-results-of-the-large-scale-multinational-trial-profile-1005-efficacy-and-safety-of-crizotinib-in-previously-treated-patients-with-advanced-metastatic-alk-positive-non-small-cell-lung-cancer
#3
Fiona Blackhall, D Ross Camidge, Alice T Shaw, Jean-Charles Soria, Benjamin J Solomon, Tony Mok, Vera Hirsh, Pasi A Jänne, Yuankai Shi, Pan-Chyr Yang, Tommaso De Pas, Toyoaki Hida, Javier De Castro Carpeño, Silvana Lanzalone, Anna Polli, Shrividya Iyer, Arlene Reisman, Keith D Wilner, Dong-Wan Kim
Purpose: Crizotinib is a potent, orally administered tyrosine kinase inhibitor approved for the treatment of anaplastic lymphoma kinase (ALK)-positive advanced non-small-cell lung cancer (NSCLC). We report final results from PROFILE 1005, the largest clinical trial to date for an ALK inhibitor in ALK-positive NSCLC. Patients and methods: PROFILE 1005 (NCT00932451) was a multicenter, single-arm phase 2 trial of the efficacy, safety and tolerability of crizotinib (250 mg twice daily; 3 week continuous treatment cycles) in patients with ALK-positive NSCLC after failure of ≥1 lines of systemic treatment for locally advanced/metastatic disease...
2017: ESMO Open
https://www.readbyqxmd.com/read/29206031/chemoselective-installation-of-amine-bonds-on-proteins-through-aza-michael-ligation
#4
Allyson M Freedy, Maria J Matos, Omar Boutureira, Francisco Corzana, Ana Guerreiro, Padma Akkapeddi, Víctor J Somovilla, Tiago Rodrigues, Karl Nicholls, Bangwen Xie, Gonzalo Jiménez-Osés, Kevin M Brindle, André A Neves, Gonçalo J L Bernardes
Chemical modification of proteins is essential for a variety of important diagnostic and therapeutic applications. Many strategies developed to date lack chemo- and regioselectivity as well as result in non-native linkages that may suffer from instability in vivo and adversely affect the protein's structure and function. We describe here the reaction of N-nucleophiles with the amino acid dehydroalanine (Dha) in a protein context. When Dha is chemically installed in proteins, the addition of a wide-range N-nucleophiles enables the rapid formation of amine linkages (secondary and tertiary) in a chemoselective manner under mild, biocompatible conditions...
December 5, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29203817/high-expression-of-%C3%AE-catenin-contributes-to-the-crizotinib-resistant-phenotype-in-the-stem-like-cell-population-in-neuroblastoma
#5
Abdulraheem Alshareef, Nidhi Gupta, Hai-Feng Zhang, Chengsheng Wu, Moinul Haque, Raymond Lai
ALK has been identified as a novel therapeutic target in neuroblastoma (NB), but resistance to ALK inhibitors (such as crizotinib) is well recognized. We recently published that the crizotinib sensitivity in NB cells strongly correlates with the crizotinib-ALK binding, and β-catenin effectively hinders this interaction and confers crizotinib resistance. Here, we asked if these observations hold true for the stem-like cells in NB cells, which were purified based on their responsiveness to a Sox2 reporter. Compared to bulk, reporter unresponsive (RU) cells, reporter responsive (RR) cells had significantly higher neurosphere formation ability, expression of CD133/nestin and chemo-resistance...
December 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29202231/identification-of-novel-aurora-kinase-a-aurka-inhibitors-via-hierarchical-ligand-based-virtual-screening
#6
Yue Kong, Andreas Bender, Aixia Yan
Aurora kinases are essential for cell mitosis, amplified and overexpressed in various human malignancies. Therefore, Aurora kinases have been promising targets for anticancer therapies, which has prompted an intensive search for their small-molecule inhibitors. In this work, we performed a hierarchical and time-efficient virtual screening cascade for scaffold hopping, aiming to obtain structurally novel and highly potent hit compounds targeting Aurora kinases. The cascade consisted of a shape- and an electrostatic-based protocol, combined with a QSAR-based selection protocol...
December 4, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29202023/combating-drug-resistant-mutants-of-anaplastic-lymphoma-kinase-with-potent-and-selective-type-i1-2-inhibitors-by-stabilizing-unique-dfg-shifted-loop-conformation
#7
Peichen Pan, Huidong Yu, Qinglan Liu, Xiaotian Kong, Hu Chen, Jiean Chen, Qi Liu, Dan Li, Yu Kang, Huiyong Sun, Wenfang Zhou, Sheng Tian, Sunliang Cui, Feng Zhu, Youyong Li, Yong Huang, Tingjun Hou
Targeted inhibition of anaplastic lymphoma kinase (ALK) dramatically improved therapeutic outcomes in the treatment of ALK-positive cancers, but unfortunately patients invariably progressed due to acquired resistance mutations in ALK. Currently available drugs are all type-I inhibitors bound to the ATP-binding pocket and are most likely to be resistant in patients harboring genetic mutations surrounding the ATP pocket. To overcome drug resistance, we rationally designed a novel kind of "bridge" inhibitor, which specially bind into an extended hydrophobic back pocket adjacent to the ATP-binding site of ALK...
November 22, 2017: ACS Central Science
https://www.readbyqxmd.com/read/29201885/alectinib-can-replace-crizotinib-as-standard-first-line-therapy-for-alk-positive-lung-cancer
#8
EDITORIAL
Takehiro Uemura, Toyoaki Hida
No abstract text is available yet for this article.
November 2017: Annals of Translational Medicine
https://www.readbyqxmd.com/read/29199697/anaplastic-lymphoma-kinase-status-in-lung-cancers-an-immunohistochemistry-and-fluorescence-in-situ-hybridization-study-from-a-tertiary-cancer-center-in-india
#9
S S Murthy, S J Rajappa, S D Gundimeda, K M Mallavarapu, S Ayyagari, P Yalavarthi, D Fonseca, P Paliwal, Hgr Nair, V Koppula, Kvvn Raju, S T Rao
BACKGROUND AND OBJECTIVES: Fluorescence in situ hybridization (FISH) and immunohistochemistry (IHC) have shown good concordance for the detection of echinoderm microtubule-associated protein-like 4 and anaplastic lymphoma kinase (ALK) rearrangement. Since studies reporting FISH/IHC concordance, clinicopathological features, and clinical outcomes of ALK-positive patients from India are lacking, this study was undertaken. MATERIALS AND METHODS: This is a retrospective, observational study of patients with adenocarcinoma of the lung on whom ALK test was performed between March 2013 and December 2015...
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29199691/new-insights-into-anaplastic-lymphoma-kinase-positive-nonsmall-cell-lung-cancer
#10
A P Dubey, N Pathi, S Viswanath, A Rathore, A Pathak, R Sud
BACKGROUND: A novel fusion gene of echinoderm microtubule-associated protein-like 4 (EML4) and anaplastic lymphoma kinase (ALK) has been identified in a subset of non-small-cell lung cancers (NSCLCs). Patients with the ALK-EML4 fusion gene demonstrate unique clinicopathological and physiological characteristics. Here we present an analysis of clinicopathological profile of patients of metastatic adenocarcinoma harboring the ALK-EML4 fusion gene and their response to targeted therapy in the form of crizotinib...
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29199685/role-of-crizotinib-in-c-mesenchymal-epidermal-transition-positive-nonsmall-cell-lung-cancer-patients
#11
U Batra, A Jain, M Sharma, R Bajaj, M Suryavanshis
The increasing cases of NSCLC and improved understanding of its molecular biology has lead to identification of its varied driver mutations. cMET amplification has an important role as resistance mechanism for EGFR TKIs. Crizotinib is a drug which shows its anti-tumoral effect in cMET positive cases. Here we present a case series of three such patients who achieved were cMET amplified and showed partial response on Crizotinib.
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29199678/ceritinib-in-anaplastic-lymphoma-kinase-positive-nonsmall-cell-lung-cancer-among-patients-who-were-previously-exposed-to-crizotinib-experience-from-the-indian-subcontinent
#12
A P Joshi, M V Chandrakanth, V Noronha, V Patil, A Chougule, A Mahajan, A K Janu, R Chanana, K Prabhash
Ceritinib is a novel ALK inhibitor approved for advanced stage NSCLC with ALK gene rearrangement, progressed and/or intolerant to crizotinib. 13 patients were included in our study who received ceritinib. Majority of them were women and never smokers with a median age of 47 yrs. Nearly half of them had a compromised performance status and received ceritinib in third line and beyond. Ceritinib showed nearly 50% response rates. With a median follow up of 9 months for the entire cohort, median PFS and OS were not reached...
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29187012/targeted-therapies-in-non-small-cell-lung-cancer-a-focus-on-alk-ros1-tyrosine-kinase-inhibitors
#13
Assunta Sgambato, Francesca Casaluce, Paolo Maione, Cesare Gridelli
Anaplastic lymphoma kinase (ALK) and ROS1 rearrangements define important molecular subgroups of advanced non-small cell lung cancer (NSCLC). The identification of these genetic driver alterations created new potential for highly active therapeutic interventions. After discovery of ALK rearrangements in NSCLC, it was recognized that these confer sensitivity to ALK inhibition. Areas covered: Crizotinib, the first-in-class ALK/ROS1/MET inhibitor, was initially approved as second-line treatment of ALK-positive advanced NSCLC but after this, it was firmly established as the standard first-line therapy for advanced ALK-positive NSCLC...
November 29, 2017: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/29184678/liquid-biopsy-for-monitoring-anaplastic-lymphoma-kinase-inhibitors-in-non-small-cell-lung-cancer-two-cases-compared
#14
REVIEW
Mariangela Manicone, Maria Chiara Scaini, Maria Grazia Rodriquenz, Antonella Facchinetti, Alfredo Tartarone, Michele Aieta, Rita Zamarchi, Elisabetta Rossi
Three to seven percent of non-small cell lung cancer (NSCLC) patients show anaplastic lymphoma kinase (ALK)-translocation and could be treated with ALK-inhibitors. However, under crizotinib, a first-generation ALK-inhibitor, patients develop drug resistance after a median of 12 months. To overcome crizotinib resistance, several next-generation ALK inhibitors have been developed. In NSCLC, liquid biopsy allowed important improvements in the detection of the epidermal growth factor receptor (EGFR) mutation. The ability of liquid biopsy to detect oncogenic gene/protein fusions is a newly investigated field, and is not routinely applied yet...
October 2017: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/29174814/design-synthesis-biological-evaluation-and-molecular-modeling-of-novel-2-amino-4-1-phenylethoxy-pyridine-derivatives-as-potential-ros1-inhibitors
#15
Yuanxin Tian, Tingting Zhang, Lifan Long, Zhonghuang Li, Shanhe Wan, Guangfa Wang, Yonghuan Yu, Ju Hou, Xiaoyun Wu, Jiajie Zhang
With the aim of discovering potential and selective inhibitors targeting ROS1 kinase, we rationally designed, synthesized and evaluated two series of novel 2-amino-pyridine derivatives with 1-phenylethoxy at C-3 and C-4 position. The enzymic assays results indicated that six of the new compounds 13b-13d and 14a-14c showed remarkably higher inhibitory activities against ROS1 kinase. The most promising compounds, 13d and 14c displayed the most desired ROS1 inhibitory activity with IC50 values of 440 nM and 370 nM respectively...
November 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29174809/discovery-of-novel-2-4-diarylaminopyrimidine-analogues-as-alk-and-ros1-dual-inhibitors-to-overcome-crizotinib-resistant-mutants-including-g1202r
#16
Yu Wang, Shaowei Chen, Gang Hu, Jiao Wang, Wenfeng Gou, Daiying Zuo, Yucheng Gu, Ping Gong, Xin Zhai
Aiming to explore novel anaplastic lymphoma kinase (ALK) and proto-oncogene tyrosine-protein kinase ROS (ROS1) dual inhibitors to overcome crizotinib-resistant mutants, two series of 2,4-diarylaminopyrimidine (DAAP) analogues bearing thiazole or 1,2,3-triazole moieties were designed and synthesized based upon the cocrystal structure of ceritinib with ALKWT (PDB 4MKC) as well as the binding model of ceritinib with ALKG1202R. The cellular and enzymatic assays validated 34c (WY-135) as a promising ALK (IC50 = 1...
November 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29174542/quantitative-wide-spectrum-kinase-profiling-in-live-cells-for-assessing-the-effect-of-cellular-atp-on-target-engagement
#17
James D Vasta, Cesear R Corona, Jennifer Wilkinson, Chad A Zimprich, James R Hartnett, Morgan R Ingold, Kristopher Zimmerman, Thomas Machleidt, Thomas A Kirkland, Kristin G Huwiler, Rachel Friedman Ohana, Michael Slater, Paul Otto, Mei Cong, Carrow I Wells, Benedict-Tilman Berger, Thomas Hanke, Carina Glas, Ke Ding, David H Drewry, Kilian V M Huber, Timothy M Willson, Stefan Knapp, Susanne Müller, Poncho L Meisenheimer, Frank Fan, Keith V Wood, Matthew B Robers
For kinase inhibitors, intracellular target selectivity is fundamental to pharmacological mechanism. Although a number of acellular techniques have been developed to measure kinase binding or enzymatic inhibition, such approaches can fail to accurately predict engagement in cells. Here we report the application of an energy transfer technique that enabled the first broad-spectrum, equilibrium-based approach to quantitatively profile target occupancy and compound affinity in live cells. Using this method, we performed a selectivity profiling for clinically relevant kinase inhibitors against 178 full-length kinases, and a mechanistic interrogation of the potency offsets observed between cellular and biochemical analysis...
November 13, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/29174221/lung-toxicity-in-non-small-cell-lung-cancer-patients-exposed-to-alk-inhibitors-report-of-a-peculiar-case-and-systematic-review-of-the-literature
#18
REVIEW
Benedetta Pellegrino, Francesco Facchinetti, Paola Bordi, Mario Silva, Letizia Gnetti, Marcello Tiseo
Lung toxicity is a potential fatal effect involving non-small-cell lung cancer (NSCLC) patients exposed to tyrosine kinase inhibitors (TKIs). Moving from our experience regarding a patient who developed lung toxicity while receiving 2 different anaplastic lymphoma kinase (ALK)-TKIs, we performed a systematic review to assess the epidemiologic magnitude and the clinical significance of such toxicity in NSCLC patients treated with ALK-TKIs. Studies were identified using MEDLINE and additional sources (European Society for Medical Oncology, American Society of Clinical Oncology, and World Conference on Lung Cancer abstracts) in agreement with Preferred Reporting Items for Systematic Reviews and Meta-Analyses and Cochrane guidelines...
October 28, 2017: Clinical Lung Cancer
https://www.readbyqxmd.com/read/29167003/-prognostic-analysis-of-patients-with-advanced-non-small-cell-lung-cancer-%C3%A2-in-different-genotypes
#19
Ping Liu, Yuhua Wu, Lijuan Zhou, Na Qin, Quan Zhang, Hui Zhang, Xi Li, Xinyong Zhang, Jialin Lv, Xinjie Yang, Jinghui Wang, Shucai Zhang
BACKGROUND: Non-small cell lung cancer (NSCLC) has been transformed from the treatment according to histological type to genotype treatment model. The epidermal growth factor receptor (EGFR) and anaplastic lymphoma kinase (ALK) genes are the most important drivers in lung cancer. The aim of this study is to explore the clinical characteristics and prognostic factors of patients with advanced NSCLC with different genotypes. METHODS: We retrospectively reviewed the clinical data of 553 advanced NSCLC patients with EGFR mutations and ALK positive who were hospitalized in the Beijing Chest Hospital from July 2004 to December 2015, and the independent prognostic factors of patients were analyzed by Cox proportional hazards regression model...
November 20, 2017: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
https://www.readbyqxmd.com/read/29165815/development-and-validation-of-a-liquid-chromatography-tandem-mass-spectrometry-analytical-method-for-the-therapeutic-drug-monitoring-of-eight-novel-anticancer-drugs
#20
M Herbrink, N de Vries, H Rosing, A D R Huitema, B Nuijen, J H M Schellens, J H Beijnen
To support therapeutic drug monitoring (TDM) of patients with cancer, a fast and accurate method for simultaneous quantification of the registered anticancer drugs afatinib, axitinib, ceritinib, crizotinib, dabrafenib, enzalutamide, regorafenib and trametinib in human plasma using liquid chromatography tandem mass spectrometry was developed and validated. Human plasma samples were collected from treated patients and stored at -20 (o) C. Analytes and internal standards (stable isotopically labeled analytes) were extracted with acetonitrile...
November 22, 2017: Biomedical Chromatography: BMC
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