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https://www.readbyqxmd.com/read/28302215/-altered-treg-and-il-1a-expression-in-the-immune-microenvironment-%C3%A2-of-lung-squamous-cell-cancer-after-egfr-blockade
#1
Haiyang He, Luyu Qi, Yiling Hou
BACKGROUND: Targeting the mutations and amplifications in the epidermal growth factor receptor (EGFR) gene has curative effects on cancers of the lung, oral cavity, and gastrointestinal system. However, a systemic immune inflammation is an adverse effect of this therapeutic strategy. In this study, we aimed to identify the possible changes in the tumor microenvironment that contribute to the anti-cancer activity of EGFR inhibition. METHODS: Squamous-cell cancers were induced by the syngeneic transplantation of either EGFR-null or wild-type mouse primary keratinocytes that had been transduced with an oncogenic H-ras retrovirus...
March 20, 2017: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
https://www.readbyqxmd.com/read/28300553/neutrophil-elastase-inhibitor-sivelestat-ameliorates-gefitinib-naphthalene-induced-acute-pneumonitis-in-mice
#2
Hironori Mikumo, Toyoshi Yanagihara, Naoki Hamada, Eiji Harada, Saiko Ogata-Suetsugu, Chika Ikeda-Harada, Masako Arimura-Omori, Kunihiro Suzuki, Testuya Yokoyama, Yoichi Nakanishi
Gefitinib, an epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI), is an effective therapeutic agent for non-small cell lung cancer with EGFR mutations. It can cause severe acute pneumonitis in some patients. We previously demonstrated that mice with naphthalene-induced airway epithelial injury developed severe gefitinib-induced pneumonitis and that neutrophils played important roles in the development of the disease. This study aimed to investigate the effects of the neutrophil elastase inhibitor sivelestat on gefitinib-induced pneumonitis in mice...
March 12, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28296233/sustained-response-to-standard-dose-osimertinib-in-a-patient-with-plasma-t790m-positive-leptomeningeal-metastases-from-primary-lung-adenocarcinoma
#3
Oscar Siu-Hong Chan, Warren Kam-Wing Leung, Rebecca Mei-Wan Yeung
A 44-year-old male, never smoker, suffers from stage IV adenocarcinoma of the right lung with epidermal growth factor receptor (EGFR) exon-21 L858R point mutation on initial presentation. After 23 months of treatment with gefitinib, intercalated with multiple courses of radiotherapy, leptomeningeal metastases (LMs) developed. Acquired T790M mutation was confirmed by the droplet digital polymerase chain reaction plasma EGFR test. After switching to osimertinib at the standard dose, his neurocognitive function improved clinically, coupled with sustained radiological improvement...
March 15, 2017: Asia-Pacific Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28295308/comparison-of-gefitinib-erlotinib-and-afatinib-in-non-small-cell-lung-cancer-a-meta-analysis
#4
Zuyao Yang, Allan Hackshaw, Qi Feng, Xiaohong Fu, Yuelun Zhang, Chen Mao, Jinling Tang
Gefitinib, erlotinib and afatinib are three widely used epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) for treating advanced non-small cell lung cancer (NSCLC) with proven efficacy. We undertook a systematic review and meta-analysis to synthesize existing studies with direct comparisons of EGFR TKIs in NSCLC in terms of both efficacy and safety. Eight randomized trials and 82 cohort studies with a total of 17621 patients were included for analysis. Gefitinib and erlotinib demonstrated comparable effects on progression-free survival (hazard ratio [HR], 1...
March 14, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28291344/first-bispecific-inhibitors-of-the-epidermal-growth-factor-receptor-kinase-and-the-nf-%C3%AE%C2%BAb-activity-as-novel-anti-cancer-agents
#5
Mostafa M Hamed, Sarah S Darwish, Jennifer Herrmann, Ashraf H Abadi, Matthias Engel
The activation of the NF-κB transcription factor is a major adaptive response induced upon treatment with EGFR kinase inhibitors, leading to the emergence of resistance in non-small cell lung cancer and other tumor types. To suppress this survival mechanism, we developed new thiourea quinazoline derivatives that are dual inhibitors of both EGFR kinase and the NF-κB activity. Optimization of the hit compound, identified in a NF-κB reporter gene assay, led to compound 9b, exhibiting a cellular IC50 for NF-κB inhibition of 0...
March 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28290473/phosphoproteomics-reveals-hmga1-a-ck2-substrate-as-a-drug-resistant-target-in-non-small-cell-lung-cancer
#6
Yi-Ting Wang, Szu-Hua Pan, Chia-Feng Tsai, Ting-Chun Kuo, Yuan-Ling Hsu, Hsin-Yung Yen, Wai-Kok Choong, Hsin-Yi Wu, Yen-Chen Liao, Tse-Ming Hong, Ting-Yi Sung, Pan-Chyr Yang, Yu-Ju Chen
Although EGFR tyrosine kinase inhibitors (TKIs) have demonstrated good efficacy in non-small-cell lung cancer (NSCLC) patients harboring EGFR mutations, most patients develop intrinsic and acquired resistance. We quantitatively profiled the phosphoproteome and proteome of drug-sensitive and drug-resistant NSCLC cells under gefitinib treatment. The construction of a dose-dependent responsive kinase-substrate network of 1548 phosphoproteins and 3834 proteins revealed CK2-centric modules as the dominant core network for the potential gefitinib resistance-associated proteins...
March 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28287096/blockade-of-vascular-endothelial-growth-factor-receptors-by-tivozanib-has-potential-anti-tumour-effects-on-human-glioblastoma-cells
#7
Majid Momeny, Farima Moghaddaskho, Narges K Gortany, Hassan Yousefi, Zahra Sabourinejad, Ghazaleh Zarrinrad, Shahab Mirshahvaladi, Haniyeh Eyvani, Farinaz Barghi, Leila Ahmadinia, Mahmoud Ghazi-Khansari, Ahmad R Dehpour, Saeid Amanpour, Seyyed M Tavangar, Leila Dardaei, Amir H Emami, Kamran Alimoghaddam, Ardeshir Ghavamzadeh, Seyed H Ghaffari
Glioblastoma (GBM) remains one of the most fatal human malignancies due to its high angiogenic and infiltrative capacities. Even with optimal therapy including surgery, radiotherapy and temozolomide, it is essentially incurable. GBM is among the most neovascularised neoplasms and its malignant progression associates with striking neovascularisation, evidenced by vasoproliferation and endothelial cell hyperplasia. Targeting the pro-angiogenic pathways is therefore a promising anti-glioma strategy. Here we show that tivozanib, a pan-inhibitor of vascular endothelial growth factor (VEGF) receptors, inhibited proliferation of GBM cells through a G2/M cell cycle arrest via inhibition of polo-like kinase 1 (PLK1) signalling pathway and down-modulation of Aurora kinases A and B, cyclin B1 and CDC25C...
March 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28274536/chronic-myelomonocytic-leukemia-blast-crisis-in-a-patient-with-advanced-non-small-cell-lung-cancer-treated-with-egfr-tyrosine-kinase-inhibitors
#8
Hiroaki Ogata, Isamu Okamoto, Goichi Yoshimoto, Teppei Obara, Kayo Ijichi, Eiji Iwama, Taishi Harada, Koichi Akashi, Yoichi Nakanishi
A 59-year-old woman with epidermal growth factor receptor gene (EGFR) mutation-positive advanced lung adenocarcinoma was treated with afatinib after a diagnosis of chronic myelomonocytic leukemia (CMML). Twenty-one weeks later, she developed agranulocytosis, and CMML subsequently progressed to blast crisis. After complete remission of CMML, gefitinib was initiated; however, agranulocytosis recurred. This is the first reported case of both EGFR mutation-positive advanced non-small cell lung cancer with CMML, and of CMML blast crisis...
March 2017: Respiratory Investigation
https://www.readbyqxmd.com/read/28272214/genetic-characterization-drives-personalized-therapy-for-early-stage-non-small-cell-lung-cancer-nsclc-patients-and-survivors-with-metachronous-second-primary-tumor-mst-a-case-report
#9
Xingchen Ding, Linlin Wang, Xijun Liu, Xindong Sun, Jinming Yu, Xue Meng
RATIONALE: The pathogenesis and progression of lung cancer is a complicated process in which many genes take part. But molecular gene testing is typically only performed in advanced-stage non-squamous non-small-cell lung cancer (NSCLC). The value of tyrosine kinase inhibitors (TKI) administration is not widely recognized with respect to early-stage NSCLC. PATIENT CONCERNS: Here, we present a case of a man, heavy smoker who initially presented with stage IA lung adenocarcinoma (LADC)...
March 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28271729/egfr-tki-combination-with-immunotherapy-in-non-small-cell-lung-cancer
#10
Myung-Ju Ahn, Jong-Mu Sun, Se-Hoon Lee, Jin Seok Ahn, Keunchil Park
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKI) has significantly improved clinical outcomes compared with chemotherapy in non-small cell lung cancer (NSCLC) patients with sensitizing EGFR gene mutation. Areas covered: Almost all patients treated with EGFR TKIs eventually develop acquired resistance. It has been reported that activation of the oncogenic EGFR pathway enhances susceptibility of the lung tumors to PD-1 blockade in mouse model, suggesting combination of PD1 blockade with EGFR TKIs may be a promising therapeutic strategy...
March 8, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28265596/a-fluorescent-light-up-aggregation-induced-emission-probe-for-screening-gefitinib-sensitive-non-small-cell-lung-carcinoma
#11
Yi Hu, Leilei Shi, Yue Su, Chuan Zhang, Xin Jin, Xinyuan Zhu
Fluorescent light-up probes with aggregation-induced emission (AIE) characteristics have been focused on recently. In this report, a new fluorescent probe, namely, DEVD-TPE, which consisted of the substrate peptide Asp-Glu-Val-Asp (DEVD) and the AIE reporter group tetraphenylethene (TPE), was developed for detecting caspase-3 in living cells. In a slightly alkaline solution, the DEVD-TPE probe displayed almost no fluorescence owing to the dynamic rotation of the phenyl rings in solution. However, DEVD-TPE exhibited significant fluorescence when it was cleaved by caspase-3, as well as when the reporter group TPE underwent aggregation...
March 7, 2017: Biomaterials Science
https://www.readbyqxmd.com/read/28260924/impact-of-gefitinib-in-early-stage-treatment-on-circulating-cytokines-and-lymphocytes-for-patients-with-advanced-non-small-cell-lung-cancer
#12
Jin Sheng, Wenfeng Fang, Xia Liu, Shan Xing, Jianhua Zhan, Yuxiang Ma, Yan Huang, Ningning Zhou, Hongyun Zhao, Li Zhang
OBJECTIVES: The impact of epidermal growth factor receptor (EGFR) tyrosine-kinase inhibitors (TKIs) on the human immune system remains undefined. This study illustrates the immunomodulatory effect of gefitinib in patients with advanced non-small cell lung cancer (NSCLC) and its relevant prognostic significance. PATIENTS AND METHODS: Peripheral blood samples were collected from 54 patients at baseline and after 4 weeks of gefitinib treatment. Circulating lymphocyte populations and cytokine levels were measured...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28260629/uplc-esi-ms-ms-study-of-the-effect-of-green-tea-extract-on-the-oral-bioavailability-of-erlotinib-and-lapatinib-in-rats-potential-risk-of-pharmacokinetic-interaction
#13
Hadir M Maher, Nourah Z Alzoman, Shereen M Shehata, Ashwag O Abahussain
Green tea (GT) is one of the most consumed beverages worldwide. Tyrosine kinase inhibitors (TKIs) belong to the oral targeted therapy that gained much interest in oncology practice, among which are erlotinib (ERL) and lapatinib (LAP). Since green tea polyphenols (GTP) are known to be inhibitors of receptor tyrosine kinases, GTE could likely potentiate the anticancer effect of TKIs, but with a possibility of pharmacokinetic (PK) interaction with co-administered TKIs. In this study, the effect of GTE on the PK of ERL/LAP in rats was studied...
April 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28259822/ddx17-nucleocytoplasmic-shuttling-promotes-acquired-gefitinib-resistance-in-non-small-cell-lung-cancer-cells-via-activation-of-%C3%AE-catenin
#14
Kai Li, Chunfen Mo, Di Gong, Yan Chen, Zhao Huang, Yanyan Li, Jie Zhang, Lugang Huang, Yuan Li, Frances V Fuller-Pace, Ping Lin, Yuquan Wei
Although epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) are effective for non-small cell lung cancer (NSCLC) patients with EGFR mutations, almost all these patients will eventually develop acquired resistance to EGFR-TKI. However, the molecular mechanisms responsible for gefitinib resistance remain still not fully understood. Here, we report that elevated DDX17 levels are observed in gefitinib-resistant NSCLC cells than gefitinib-sensitive cells. Upregulation of DDX17 enhances the gefitinib resistance, whereas DDX17-silenced cells partially restore gefitinib sensitivity...
March 1, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28258422/outcome-in-advanced-non-small-cell-lung-cancer-patients-with-successful-rechallenge-after-recovery-from-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitor-induced-interstitial-lung-disease
#15
Kosuke Kashiwabara, Hiroshi Semba, Shinji Fujii, Shinsuke Tsumura
PURPOSE: Several non-small cell lung cancer (NSCLC) cases of successful rechallenge with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) after recovery from gefitinib or erlotinib-induced interstitial lung disease (ILD) have been reported, but it is not clear whether the rechallenge affects the outcome. METHODS: We retrospectively evaluated the difference in the outcome between advanced NCLC patients with active EGFR mutations who received EGFR-TKI rechallenge after recovery from EGFR-TKI-induced ILD and those who did not...
March 3, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28254656/gefitinib-enhances-radiotherapeutic-effects-of-131-i-hegf-targeted-to-egfr-by-increasing-tumor-uptake-of-hegf-in-tumor-xenografts
#16
Lu Xia, He Peng, Luo Zhiqiang, Zhang Xiaoli
Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor which has been proven effective for cancer treatment. In this study, we sought to determine whether gefitinib could increase the in vivo tumor uptake of human (131)I-EGF ((131)I-hEGF), thereby enhancing the potential of hEGF as a vehicle for EGFR-targeted radionuclide therapy. Western blot analysis was conducted to detect the effects of gefitinib on EGFR expression in human head and neck squamous carcinoma cell line UM-SCC-22B...
February 4, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28253240/patient-response-to-use-of-tyrosine-kinase-inhibitors-in-lung-cancer-a-retrospective-audit-during-funding-changes
#17
Anne Fraser
BACKGROUND: The New Zealand Pharmaceutical Management Agency (PHARMAC) approved funding of erlotinib in October 2010 as second line therapy in all non-squamous non-small cell lung cancer after platinum-based chemotherapy with no requirement for epidermal growth factor (EGFR) mutation testing. Funding widened in August 2012 to include gefitinib as first line treatment for patients with a proven EGFR mutation. Then in January 2014, both tyrosine kinase inhibitors (TKIs) were approved for first line treatment, but only for disease with EGFR mutation...
March 3, 2017: New Zealand Medical Journal
https://www.readbyqxmd.com/read/28247504/epigallocatechin-3-gallate-augments-the-therapeutic-effects-of-benzo-a-pyrene-mediated-lung-carcinogenesis
#18
Meghan M Cromie, Zhongwei Liu, Weimin Gao
Our previous study found curcumin and vitamin E to have protective effects against benzo[a]pyrene (BaP) exposure in human normal lung epithelial BEAS-2B cells. The first objective of this study was to determine whether epigallocatechin-3-gallate (EGCG) elicited the same response. Co-treatment with 5 µM BaP and 20 µM EGCG in BEAS-2B promoted a significant reduction in cell viability and greater G2/M cell cycle arrest, induction of ROS, and reductions in BaP-induced CYP1A1/CYP1B1/COMT, EGFR, p-Akt (Ser473), p-p53 (Thr55), and survivin mRNA/protein expression, as well as an increase in p-p53 (Ser15)...
March 1, 2017: BioFactors
https://www.readbyqxmd.com/read/28245116/discovery-of-an-orally-selective-inhibitor-of-signal-transducer-and-activator-of-transcription-3-using-advanced-multiple-ligand-simultaneous-docking
#19
Wenying Yu, Chenglong Li, Wenda Zhang, Yuanzheng Xia, Shanshan Li, Jia-Yuh Lin, Keqin Yu, Mu Liu, Lei Yang, Jianguang Luo, Yijun Chen, Hongbin Sun, Lingyi Kong
Targeting signal transducer and activator of transcription 3 (STAT3) is a potential anticancer strategy. However, STAT3 inhibitors with good selectivity and bioavailability are rare. The aim of this study was to discover selective direct STAT3 inhibitors with good druglikeness. By the advanced multiple ligand simultaneous docking (AMLSD) method, compound 9 was designed as an orally bioavailable STAT3 inhibitor that presented superior druggability and selectivity compared with other representative STAT3 inhibitors...
March 15, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28237165/treatment-of-choice-for-patients-with-egfr-mutation-positive-non-small-cell-lung-carcinoma-presenting-with-choroidal-metastases-radiotherapy-or-tkis
#20
David Maskell, Konstantinos Geropantas, Michael Kouroupis, Andrew Glenn, Thankamma Ajithkumar
INTRODUCTION: It is not uncommon for patients with non-small cell lung cancer (NSCLC) to develop choroidal metastases (CM). External beam radiotherapy (EBRT) has traditionally been considered the treatment of choice for CM as it offers high response rates and quick relief of symptoms. However, new targeted treatments can offer an effective, alternative treatment strategy for patients harbouring specific genetic abnormalities. CASE STUDY: We present the case of a patient presenting with a symptomatic metastasis to the choroid from an epidermal growth factor receptor (EGFR) mutation-positive NSCLC and exhibiting an excellent clinical and radiological response to the tyrosine kinase inhibitor (TKI) gefitinib...
February 2017: Canadian Journal of Ophthalmology. Journal Canadien D'ophtalmologie
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