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https://www.readbyqxmd.com/read/29238696/identification-of-clinically-approved-drugs-indacaterol-and-canagliflozin-for-repurposing-to-treat-epidermal-growth-factor-tyrosine-kinase-inhibitor-resistant-lung-cancer
#1
Hongjian Li, Christy Wing-Sum Tong, Yee Leung, Man-Hon Wong, Kenneth Kin-Wah To, Kwong-Sak Leung
In advanced lung cancer, epidermal growth factor tyrosine kinase inhibitors (EGFR TKIs) have extraordinary clinical efficacy. However, their usefulness is severely compromised by drug resistance mediated by various mechanisms, the most important of which is the secondary EGFR T790M mutation. The mutation blocks the binding of EGFR TKIs to the receptor kinase, thereby abolishing the therapeutic efficacy. In this study, we used our free and open-source protein-ligand docking software idock to screen worldwide approved small-molecule drugs against EGFR T790M...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/29228726/tyrosine-kinase-inhibitors-show-different-anti-brain-metastases-efficacy-in-nsclc-a-direct-comparative-analysis-of-icotinib-gefitinib-and-erlotinib-in-a-nude-mouse-model
#2
Jianlong Tan, Min Li, Wen Zhong, Chengping Hu, Qihua Gu, Yali Xie
Brain metastasis is an increasing problem in non-small cell lung cancer (NSCLC) patients. Tyrosine kinase inhibitors (TKIs), including gefitinib, erlotinib, and icotinib, are reported to be effective in patients with brain metastases. However, direct comparative studies of the pharmacokinetics and efficacy of these three drugs in treating brain metastases are lacking. In the present investigation, we found that gefitinib penetrated the blood-tumor barrier and was distributed to brain metastases more effectively than erlotinib or icotinib in a nude mouse model...
November 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29228636/the-efficacy-of-40-mg-versus-dose-de-escalation-to-less-than-40-mg-of-afatinib-giotrif-as-the-first-line-therapy-for-patients-with-primary-lung-adenocarcinoma-harboring-favorable-epidermal-growth-factor-mutations
#3
Chien-Ying Liu, Chih-Liang Wang, Shih-Hong Li, Ping-Chih Hsu, Chih-Hung Chen, Ting-Yu Lin, Chih-Hsi Kuo, Yueh-Fu Fang, How-Wen Ko, Chih-Teng Yu, Tai-Yun Yang, Cheng-Ta Yang
The choice of a first-line therapy for lung cancer is a crucial decision that can impact the survival as well as the quality of life of a patient. Inhibitors of epidermal growth factor receptor (EGFR) such as afatinib, erlotinib, and gefitinib have previously been used to treat non-small cell lung cancer harboring favorable EGFR mutations. Although afatinib has greater efficacy than other EGFR inhibitors, adverse events related to its use can result in the discontinuation of the therapy. In this study, we compared the therapeutic efficacy in lung cancer patients of a regimen of 40 mg/day of afatinib with that of a lower dose regimen of <40 mg/day resulting either from a lower starting dose of 30 mg/day or dose adjustment...
November 14, 2017: Oncotarget
https://www.readbyqxmd.com/read/29228391/arsenic-attenuates-heparin-binding-egf-like-growth-factor-egfr-signalling-that-promotes-matrix-metalloprotease-9-dependent-astrocyte-damage-in-the-developing-rat-brain
#4
Rajesh Kushwaha, Juhi Mishra, Sachin Tripathi, Waseem Raza, Kapil Mandrah, Somendu Kumar Roy, Sanghamitra Bandyopadhyay
We earlier reported that exposure to arsenic at concentrations in ground water of India attenuated glial fibrillary acidic protein (GFAP) during brain development. Here, we validated the effects and explored mechanism in cultured astrocytes and developing rat brain. We hypothesized participation of epidermal growth factor receptor (EGFR), known to regulate GFAP. We found that arsenic inactivated EGFR, marked by reduced phospho-EGFR in astrocytes. Screening EGFR ligands revealed an arsenic-mediated attenuation in cellular and secreted-Heparin-binding EGF-like growth factor (HB-EGF)...
December 7, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29225473/the-combination-therapy-of-salinomycin-and-gefitinib-using-poly-d-l-lactic-co-glycolic-acid-poly-ethylene-glycol-nanoparticles-for-targeting-both-lung-cancer-stem-cells-and-cancer-cells
#5
Yu Zhang, Qi Zhang, Jing Sun, Huijie Liu, Qingfeng Li
Purpose: Lung cancer (LC) is the leading cause of cancer death worldwide. Evidences suggest that both LC cancer stem cells (CSCs) and cancer cells are supposed to be eliminated to achieve superior treatment effect against LC. Salinomycin could eradiate CSCs in various types of cancers, and gefitinib is a first-line therapy in LC. The purpose of the present study was to develop salinomycin-loaded nanoparticles (salinomycin-NPs) combined with gefitinib-loaded nanoparticles (gefitinib-NPs) to eradicate both LC CSCs and cancer cells...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29224735/a-novel-three-dimensional-cell-culture-method-enhances-antiviral-drug-screening-in-primary-human-cells
#6
Robert Koban, Markus Neumann, Aila Daugs, Oliver Bloch, Andreas Nitsche, Stefan Langhammer, Heinz Ellerbrok
Gefitinib is a specific inhibitor of the epidermal growth factor receptor (EGFR) and FDA approved for treatment of non-small cell lung cancer. In a previous study we could show the in vitro efficacy of gefitinib for treatment of poxvirus infections in monolayer (2D) cultivated cell lines. Permanent cell lines and 2D cultures, however, are known to be rather unphysiological; therefore it is difficult to predict whether determined effective concentrations or the drug efficacy per se are transferable to the in vivo situation...
December 7, 2017: Antiviral Research
https://www.readbyqxmd.com/read/29221264/continuation-of-gefitinib-plus-chemotherapy-prolongs-progression-free-survival-in-advanced-non-small-cell-lung-cancer-patients-who-get-acquired-resistance-to-gefitinib-without-t790m-mutations
#7
Ting Ding, Fei Zhou, Xiaoxia Chen, Shijia Zhang, Yinan Liu, Hui Sun, Shengxiang Ren, Xuefei Li, Chao Zhao, Heyong Wang, Caicun Zhou
Background: Aimed to identify the benefit population from continuation of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), this study investigated the efficacy of continuation of EGFR-TKIs plus chemotherapy beyond the response evaluation criteria in solid tumors-progressive disease (RECIST-PD) according to different progression modes and T790M mutational status. Methods: From November 2009 to July 2015, 630 patients with advanced non-small cell lung cancer (NSCLC) receiving gefitinib as initial EGFR-TKI treatment were screened in Shanghai Pulmonary Hospital...
September 2017: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/29221189/novel-direct-ampk-activator-suppresses-non-small-cell-lung-cancer-through-inhibition-of-lipid-metabolism
#8
Xi Chen, Chun Xie, Xing-Xing Fan, Ze-Bo Jiang, Vincent Kam-Wai Wong, Jia-Hui Xu, Xiao-Jun Yao, Liang Liu, Elaine Lai-Han Leung
Drug resistance is becoming an obstacle in anti-cancer therapies. For target-based therapy of lung cancer, gefitinib, as the first generation of tyrosine kinase inhibitors (TKIs), demonstrated good initial response to the non-small cell lung cancer (NSCLC) patients whom harbors epidermal growth factor receptor (EGFR) mutation. However, within one year, additional EGFR mutation occurred, leading to eventual gefitinib-resistance. Therefore, it is urgently to discover novel effective small molecule inhibitors for those patients...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29220734/high-throughput-routine-determination-of-17-tyrosine-kinase-inhibitors-by-lc-ms-ms
#9
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/29215816/efficacy-of-afatinib-in-a-previously-treated-patient-with-non-small-cell-lung-cancer-harboring-her2-mutation-case-report
#10
Cheol Kyu Park, Jae Young Hur, Chang Min Choi, Tae Ok Kim, Hyun Ju Cho, Hong Joon Shin, Jung Hwan Lim, Yoo Duk Choi, Young Chul Kim, In Jae Oh
Human epidermal growth factor receptor 2 (HER2) mutation in non-small cell lung cancer (NSCLC) is an oncogenic driver that possibly becomes a druggable target to HER2-targeted therapy. The benefit of HER2-targeted therapy is much less defined especially in eastern populations. We provide evidence of clinical benefit of afatinib in a 50-year-old Asian woman with HER2-mutant NSCLC who previously failed cytotoxic chemotherapy and gefitinib treatment. Next-generation sequencing of the tumor tissue revealed a HER2 exon 20 mutation (c...
January 1, 2018: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/29215723/high-cholesterol-in-lipid-rafts-reduces-the-sensitivity-to-egfr-tki-therapy-in-non-small-cell-lung-cancer
#11
Qiufang Chen, Zhenzhen Pan, Min Zhao, Qin Wang, Chen Qiao, Liyun Miao, Xuansheng Ding
Overcoming EGFR-TKI resistant which has the initial enthusiasm over substantial clinical responses is a formidable challenge on nowadays. In this study, we showed that cholesterol level in lipid rafts in gefitinib resistant non-small cell lung cancer (NSCLC) cell lines was remarkably higher than gefitinib sensitive cell line, and depletion of cholesterol increase gefitinib sensitivity. Furthermore, Cholesterol-depleted enhanced gefitinib inhibit phosphorylation of EGFR, Akt-1, MEK1/2 and ERK1/2 and these were reversed in cholesterol add-back experiments...
December 7, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29212192/vorinostat-and-metformin-sensitize-egfr-tki-resistant-nsclc-cells-via-bim-dependent-apoptosis-induction
#12
Hengyi Chen, Yubo Wang, Caiyu Lin, Conghua Lu, Rui Han, Lin Jiao, Li Li, Yong He
There is a close relationship between low expression of BIM and resistance to epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Vorinostat is a pan-histone deacetylase inhibitor (HDACi) that augments BIM expression in various types of tumor cells, however, this effect is attenuated by the high expression of anti-apoptotic proteins in EGFR-TKI resistant non-small cell lung cancer (NSCLC) cells. Vorinostat in combination with metformin - a compound that can inhibit anti-apoptotic proteins expression, might cooperate to activate apoptotic signaling and overcome EGFR-TKI resistance...
November 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/29207668/genetic-or-pharmacologic-inhibition-of-egfr-ameliorates-sepsis-induced-aki
#13
Xuan Xu, Juan Wang, Ruhao Yang, Zheng Dong, Dongshan Zhang
Despite recent studies have demonstrated that the EGF receptor (EGFR) activation provided a renoprotective role during ischemic and folic acid-induced AKI, the role and regulation mechanism of EGFR in septic AKI remains unclear. Here, gefitinib, a highly selective EGFR inhibitor, abrogated LPS-induced phosphorylation of EGFR, ERK1/2, and STAT3 as well as expression of COX, eNOS, and proinflammatory cytokines in HK-2 cells. In addition, c-Src is an upstream of EGFR signaling pathway and mediates LPS-induced EGFR transactivation...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29207630/shp2-regulates-migratory-behavior-and-response-to-egfr-tkis-through-erk1-2-pathway-activation-in-non-small-cell-lung-cancer-cells
#14
Yu-Jing Sun, Zhong-Ling Zhuo, Hai-Peng Xian, Ke-Zhong Chen, Fan Yang, Xiao-Tao Zhao
In the clinical treatment of lung cancer, therapy failure is mainly caused by cancer metastasis and drug resistance. Here, we investigated whether the tyrosine phosphatase Shp2 is involved in the development of metastasis and drug resistance in non-small cell lung cancer (NSCLC). Shp2 was overexpressed in a subset of lung cancer tissues, and Shp2 knockdown in lung cancer cells inhibited cell proliferation and migration, downregulated c-Myc and fibronectin expression, and upregulated E-cadherin expression. In H1975 cells, which carry double mutations (L858R + T790M) in epidermal growth factor receptor (EGFR) that confers resistance toward the tyrosine kinase inhibitor gefitinib, Shp2 knockdown increased cellular sensitivity to gefitinib; conversely, in H292 cells, which express wild-type EGFR and are sensitive to gefitinib, Shp2 overexpression increased cellular resistance to gefitinib...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29201462/efficacy-of-second-line-pemetrexed-carboplatin-in-egfr-activating-mutation-positive-nsclc-does-exon-19-deletion-differ-from-exon-21-mutation
#15
Amit Joshi, Vanita Noronha, Vijay M Patil, Anuradha Chougule, Atanu Bhattacharjee, Rajiv Kumar, Supriya Goud, Sucheta More, Anant Ramaswamy, Ashay Karpe, Nikhil Pande, Arun Chandrasekharan, Alok Goel, Vikas Talreja, Abhishek Mahajan, Amit Janu, Nilendu Purandare, Kumar Prabhash
Background: It is unknown whether the outcomes of second-line pemetrexed-carboplatin chemotherapy administered after progression on gefitinib are dependent on type of EGFR mutation present at baseline. Method: Adult non-small-cell lung cancer patients, with exon 19 deletion or exon 21 L858R mutation, who progressed on gefitinib and received pemetrexed-carboplatin chemotherapy were selected for this analysis. Result: 55 patients received pemetrexed-carboplatin as second-line treatment...
2017: Chemotherapy Research and Practice
https://www.readbyqxmd.com/read/29199705/outcomes-in-lung-cancer-an-experience-from-routine-tertiary-care-setting
#16
R Thippeswamy, S Patil, P Prashanth, C T Sateesh, T Vittal, H P Shashidhara, K M Haridas
BACKGROUND: The aim of this study was to establish characteristics of lung cancer patients diagnosed at a tertiary care hospital in Bangalore. METHODS: The retrospective study was undertaken comprising of 202 patients diagnosed of advanced lung cancer in a tertiary care setting. Data was analyzed to identify patients' characteristics, smoking history, tumor histology, stage of the disease, treatment received, and survival rates. RESULTS: Among the 202 patients diagnosed, 134 were males, and 68 were females...
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29199688/study-of-gefitinib-maintenance-in-unselected-patients-with-metastatic-primary-lung-adenocarcinoma-a-descriptive-study
#17
R Kumar, B Dubashi, S Kayal, S C Lazzar, D Barathi, V Kumar
BACKGROUND: Maintenance treatment of patients with advanced nonsmall cell lung cancer (NSCLC) without disease progression after first-line chemotherapy is a subject of ongoing research. The aim of this study was to investigate the efficacy, safety, and tolerability of the epidermal growth factor receptor (EGFR)-tyrosine-kinase inhibitor, i.e., gefitinib in the maintenance setting irrespective of EGFR status. METHODS: Patients aged 18 years or older of Indian origin, who had a life expectancy of >12 weeks with histologically or cytologically confirmed Stage IV NSCLC, the WHO performance status of 0-2, and who had completed four to six cycles of first-line platinum-based doublet chemotherapy without disease progression or unacceptable toxic effects were included in the study...
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29199650/tuberculosis-in-epidermal-growth-factor-receptor-mutation-in-lung-adenocarcinoma-on-treatment-with-gefitinib-erlotinib
#18
EDITORIAL
D Gothi, S Spalgais
No abstract text is available yet for this article.
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29193123/physiologically-based-pharmacokinetic-modeling-to-evaluate-the-systemic-exposure-of-gefitinib-in-cyp2d6-ultrarapid-metabolizers-and-extensive-metabolizers
#19
Yingxue Chen, Diansong Zhou, Weifeng Tang, Wangda Zhou, Nidal Al-Huniti, Eric Masson
Gefitinib is a selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase and is used for the treatment of non-small-cell lung cancer (NSCLC) with activating EGFR mutations. Gefitinib is metabolized by CYP2D6 and CYP3A4. This analysis compared the systemic exposure of gefitinib after oral administration in CYP2D6 ultrarapid metabolizers (UM) vs extensive metabolizers (EM). Physiologically based pharmacokinetic (PBPK) modeling was conducted using a population-based simulator. The model was calibrated using itraconazole-gefitinib clinical drug-drug interaction data and validated with gefitinib data in CYP2D6 EM vs poor metabolizers (PM)...
November 28, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29192320/combined-sn-38-and-gefitinib-treatment-promotes-cd44-degradation-in-head-and-neck-squamous-cell-carcinoma-cells
#20
Toshiyuki Nanbu, Naoki Umemura, Emika Ohkoshi, Kumi Nanbu, Hiroshi Sakagami, Jun Shimada
The aim of the present study was to search for an effective regimen among existing chemotherapies for head and neck squamous cell carcinoma (HNSCC). Among the tested drugs, we focused on combined SN-38, which is the active metabolite produced from irinotecan hydrochloride - a type I DNA topoisomerase inhibitor - after it is metabolized by carboxylesterase in the liver and gefitinib, an EGFR tyrosine kinase inhibitor treatment, based on the ability of this combination to inhibit HNSCC cell growth. Contrary to our expectation, in vivo, there was no significant difference in tumor growth suppression between gefitinib-only treatment and gefitinib plus SN-38...
January 2018: Oncology Reports
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