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https://www.readbyqxmd.com/read/29674428/optimising-endocrine-therapy-in-postmenopausal-women-with-advanced-breast-cancer
#1
Thomas Ho Lai Yau, Kl Cheung
Hormone receptor-positive breast cancer is commonly treated with endocrine therapy; however, overtime cancer cells can develop endocrine resistance. This review aims to document combination therapy and sequential therapy in the use of endocrine agents and targeted agents. By conducting two systematic searches using 4 databases: Cochrane Library, MEDLINE, EMBASE, and Web of Science. A total of 26 studies that covered combination therapy were obtained and included for the review. 14 were phase III documenting combinations of mechanistic target of rapamycin (mTOR), phosphoinositide-3-kinase (PI3K), vascular endothelial growth factor receptor (VEGFR), human epidermal growth factor receptor 2 (HER2), and cyclin dependent kinase 4/6 (CDK4/6) inhibitors...
April 19, 2018: Endocrine-related Cancer
https://www.readbyqxmd.com/read/29671943/epithelial-to-mesenchymal-transition-in-the-context-of-epidermal-growth-factor-receptor-inhibition-in-non-small-cell-lung-cancer
#2
Giuseppe Bronte, Sara Bravaccini, Enrico Bronte, Marco Angelo Burgio, Christian Rolfo, Angelo Delmonte, Lucio Crinò
The identification of oncogenic driver mutations in non-small-cell lung cancer (NSCLC) has led to the development of targeted drugs. Tyrosine kinase inhibitors (TKIs) directed against the epidermal growth factor receptor (EGFR) target lung tumours bearing EGFR-activating mutations. This new therapeutic strategy has greatly improved tumour response rates. However, drug resistance invariably occurs during TKI-based treatment. Epithelial-to-mesenchymal transition (EMT) is one of the resistance mechanisms identified in EGFR-mutated NSCLC treated with TKIs...
April 19, 2018: Biological Reviews of the Cambridge Philosophical Society
https://www.readbyqxmd.com/read/29662665/molecular-mechanism-of-action-and-potential-biomarkers-of-growth-inhibition-of-synergistic-combination-of-afatinib-and-dasatinib-against-gefitinib-resistant-non-small-cell-lung-cancer-cells
#3
Miao Wang, Alex Yuang-Chi Chang
Epidermal growth factor receptor - tyrosine kinase inhibitor (EGFR-TKI) is the first choice of treatment for advanced non-small cell lung cancer (NSCLC) patients harbouring activating EGFR mutations. However, single agent usually has limited efficacy due to heterogeneous resistant mechanisms of cancer cells. Thus drug combination therapy would offer more benefits by synergistic interactions and avoidance of resistance emergence. In this study, we selected 8 NSCLC cell lines with different genetic characteristics as research models to investigate the efficacy of 4 agents (gefitinib, cetuximab, afatinib and dasatinib) and their combinations...
March 27, 2018: Oncotarget
https://www.readbyqxmd.com/read/29660496/quantitative-targeted-proteomic-analysis-of-potential-markers-of-tyrosine-kinase-inhibitor-tki-sensitivity-in-egfr-mutated-lung-adenocarcinoma
#4
Shivangi Awasthi, Tapan Maity, Benjamin L Oyler, Yue Qi, Xu Zhang, David R Goodlett, Udayan Guha
Lung cancer causes the highest mortality among all cancers. Patients harboring kinase domain mutations in the epidermal growth factor receptor (EGFR) respond to EGFR tyrosine kinase inhibitors (TKIs), however, acquired resistance always develops. Moreover, 30-40% of patients with EGFR mutations exhibit primary resistance. Hence, there is an unmet need for additional biomarkers of TKI sensitivity that complement EGFR mutation testing and predict treatment response. We previously identified phosphopeptides whose phosphorylation is inhibited upon treatment with EGFR TKIs, erlotinib and afatinib in TKI sensitive cells, but not in resistant cells...
April 13, 2018: Journal of Proteomics
https://www.readbyqxmd.com/read/29656750/afatinib-in-heavily-pretreated-advanced-nsclc-patients-who-progressed-following-prior-gefitinib-or-erlotinib-compassionate-use-program-in-korea
#5
Moon Ki Choi, Jin Seok Ahn, Young-Chul Kim, Byoung Chul Cho, In-Jae Oh, Sang-We Kim, Jong Seok Lee, Joo-Hang Kim, Myung-Ju Ahn, Keunchil Park
INTRODUCTION: Afatinib, an irreversible ErbB family blocker, approved for first-line treatment of epidermal growth factor receptor (EGFR) mutated advanced non-small cell lung cancer (NSCLC). This study investigated experience of afatinib within a compassionate use program (CUP). METHODS: The afatinib CUP was an open-label, multicenter, single-arm program in Korea. We enrolled patients with stage IV NSCLC and who had received at least one line of previous cytotoxic chemotherapy and previous EGFR TKI treatment with either an EGFR mutation or documented clinical benefit...
May 2018: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/29650684/epidermal-growth-factor-receptor-tyrosine-kinase-inhibitors-for-central-nervous-system-metastases-from-non-small-cell-lung-cancer
#6
REVIEW
Manmeet S Ahluwalia, Kevin Becker, Benjamin P Levy
Central nervous system (CNS) metastases are a common complication in patients with epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC), resulting in a poor prognosis and limited treatment options. Treatment of CNS metastases requires a multidisciplinary approach, and the optimal treatment options and sequence of therapies are yet to be established. Many systemic therapies have poor efficacy in the CNS due to the challenges of crossing the blood-brain barrier (BBB), creating a major unmet need for the development of agents with good BBB-penetrating biopharmaceutical properties...
April 12, 2018: Oncologist
https://www.readbyqxmd.com/read/29629521/anaplastic-lymphoma-kinase-alk-expressing-lung-adenocarcinoma-with-combined-neuroendocrine-component-or-neuroendocrine-transformation-implications-for-neuroendocrine-transformation-and-response-to-alk-tyrosine-kinase-inhibitors
#7
Jongmin Sim, Hyunjin Kim, Jiyeon Hyeon, Yoon La Choi, Joungho Han
BACKGROUND: Anaplastic lymphoma kinase tyrosine kinase inhibitors (ALK-TKIs) are usually effective in lung adenocarcinoma patients with anaplastic lymphoma kinase (ALK) rearrangement. However, even after a good response to ALK-TKI therapy, most patients acquire resistance to these agents. Histological transformation is one of several suggested mechanisms of acquired resistance to ALK-TKIs. The clinicopathologic features of four patients with ALK-expressing adenocarcinoma and neuroendocrine features were analyzed...
April 9, 2018: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/29627693/in-silico-evidences-for-binding-of-glucokinase-activators-to-egfr-c797s-to-overcome-egfr-resistance-obstacle-with-mutant-selective-allosteric-inhibition
#8
Harun Patel, Rahul Pawara, Sanjay Surana
The tyrosine kinase inhibitors (TKI) against epidermal growth factor receptor (EGFR) are generally utilized as a part of patients with non-small cell lung carcinoma (NSCLC). However, EGFR T790M mutation results in resistance to most clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation has been in active clinical development to triumph the resistance problem; they covalently bind with conserved Cys797 inside the EGFR active site, offering both potency and kinase-selectivity. Third generation drugs target C797, which makes the C797S resistance mutation more subtle...
March 29, 2018: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/29626621/first-in-human-phase-i-study-of-ac0010-a-mutant-selective-egfr-inhibitor-in-non-small-cell-lung-cancer-safety-efficacy-and-potential-mechanism-of-resistance
#9
Yuxiang Ma, Xin Zheng, Hongyun Zhao, Wenfeng Fang, Yang Zhang, Jieying Ge, Lu Wang, Weicong Wang, Ji Jiang, Shaokun Chuai, Zhou Zhang, Wanhong Xu, Xiao Xu, Pei Hu, Li Zhang
INTRODUCTION: AC0010 is a mutation-selective, third-generation EGFR tyrosine kinase inhibitor (TKI). This first-in-human phase I trial determine the maximum tolerated dose (MTD), recommended phase II dose (RP2D), schedule, safety, pharmacokinetics, pharmacodynamics, and antitumor activity of AC0010 in patients with advanced or recurrent NSCLC and acquired resistance to the first-generation EGFR-TKI. METHODS: Patients received escalating daily doses of AC0010 (50 to 600 mg) throughout 28-day cycles...
April 4, 2018: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/29621416/c-met-inhibitors-for-advanced-non-small-cell-lung-cancer
#10
Giulia Pasquini, Giuseppe Giaccone
The role of the c-mesenchymal-epithelial transition factor (c-MET) signaling pathway in tumor progression and invasion has been extensively studied. C-MET inhibitors have shown anti-tumor activity in NSCLC both in preclinical and in clinical trials. However, given the molecular heterogeneity of NSCLC, it is likely that only a specific subset of NSCLC patients will benefit from c-MET inhibitors. Emerging data also suggest that MET inhibitors in combination with EGFR-TKIs (epidermal growth factor receptor tyrosine kinase inhibitors) may have a role in therapy for both EGFR-TKI resistant and EGFR-TKI naïve patients...
April 5, 2018: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/29618075/thoracoscopic-rebiopsy-to-detect-the-t790m-mutation-after-postoperative-recurrence
#11
Masatsugu Hamaji, Hideki Motoyama, Toshi Menju, Toyofumi-Fengshi Chen-Yoshikawa, Makoto Sonobe, Young Hak Kim, Hiroshi Date
After pulmonary resection for non-small-cell lung cancer, some patients with postoperative recurrence and mutated epidermal growth factor receptor (EGFR) subsequently receive EGFR-tyrosine kinase inhibitors (EGFR-TKIs). Osimertinib may be efficacious if those patients become resistant to the 1st-line EGFR-TKI because of the T790M mutation. We recently performed thoracoscopic rebiopsy to detect the T790M mutation in 4 patients who became resistant to the 1st-line EGFR-TKI treatment for postoperative recurrence...
April 2, 2018: Interactive Cardiovascular and Thoracic Surgery
https://www.readbyqxmd.com/read/29616327/whole-exome-sequencing-identifies-key-mutated-genes-in-t790m-wildtype-cmet-unamplified-lung-adenocarcinoma-with-acquired-resistance-to-first-generation-egfr-tyrosine-kinase-inhibitors
#12
Chenguang Li, Hailin Liu, Bin Zhang, Liqun Gong, Yanjun Su, Zhenfa Zhang, Changli Wang
PURPOSE: Lung cancer is the leading cause of cancer-related death worldwide. Lung adenocarcinoma harboring EGFR-activating mutations will inevitably acquire resistance to first-generation EGFR tyrosine kinase inhibitors (TKIs). EGFR T790M mutation and cMET amplification are common mechanisms. Further study is needed to explore unknown genomic alterations contributing to drug resistance. METHODS: Tumor and blood samples from 69 stage IIIB-IV NSCLC patients defined as acquired resistance to first-generation EGFR TKIs (gefitinib, erlotinib or ecotinib) were collected...
April 3, 2018: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/29616128/egfr-tki-resistance-and-map17-are-associated-with-cancer-stem-cell-like-properties
#13
Yi Shao, Hui Lv, Dian-Sheng Zhong, Qing-Hua Zhou
Patients with non-small-cell lung cancer (NSCLC) with sensitive epidermal growth factor receptor (EGFR) mutations generally react well to tyrosine kinase inhibitors (TKIs). However acquired resistance eventually occurs. Several mechanisms contribute to the resistance including T790M mutation, c-Met amplification and PIK3CA mutation. In recent years, cancer stem cells (CSCs) have been suggested to be involved in TKI resistance. MAP17 is aberrantly overexpressed in a number of malignancies. However, the expression pattern and function of MAP17 in CSCs are still unclear...
May 2018: Oncology Letters
https://www.readbyqxmd.com/read/29615847/uncommon-egfr-mutations-in-cytological-specimens-of-1-874-newly-diagnosed-indonesian-lung-cancer-patients
#14
Elisna Syahruddin, Laksmi Wulandari, Nunuk Sri Muktiati, Ana Rima, Noni Soeroso, Sabrina Ermayanti, Michael Levi, Heriawaty Hidajat, Grace Widjajahakim, Ahmad Rusdan Handoyo Utomo
Purpose: We aimed to evaluate the distribution of individual epidermal growth factor receptor ( EGFR ) mutation subtypes found in routine cytological specimens. Patients and methods: A retrospective audit was performed on EGFR testing results of 1,874 consecutive cytological samples of newly diagnosed or treatment-naïve Indonesian lung cancer patients (years 2015-2016). Testing was performed by ISO15189 accredited central laboratory. Results: Overall test failure rate was 5...
2018: Lung Cancer: Targets and Therapy
https://www.readbyqxmd.com/read/29594878/acquired-resistance-to-an-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitor-egfr-tki-in-an-uncommon-g719s-egfr-mutation
#15
Atsushi Osoegawa, Takafumi Hashimoto, Yohei Takumi, Miyuki Abe, Tomonori Yamada, Ryoji Kobayashi, Michiyo Miyawaki, Hideya Takeuchi, Tatsuro Okamoto, Kenji Sugio
Background Acquired resistance (AR) to an epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) is a common event, and several underlying mechanisms, including T790 M, MET amplification and PTEN downregulation, have been reported for the common EGFR mutations. EGFR G719X is an uncommon mutation that has been reported to show sensitivity to EGFR-TKIs. However, no established cell lines harboring the EGFR G719X have been reported in the literature. Materials and Methods G719S-GR cells were established from malignant pleural effusion of a patient whose tumor developed AR from gefitinib treatment...
March 28, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29581983/clinical-characteristics-and-survival-outcomes-for-non-small-cell-lung-cancer-patients-with-epidermal-growth-factor-receptor-double-mutations
#16
Min Peng, Yi Ming Weng, Hua Li Liu, Gui Fang Yang, Yi Yao, Guang Han, Qi Bin Song
Multiple randomized clinical trials have demonstrated that epidermal growth factor receptor (EGFR) exon 19 deletion (19Del) and exon 21 L858R mutation (L858R) are highly correlated with sensitivity to epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) treatment in non-small-cell lung cancer (NSCLC). A mutation in exon 20 (T790M) is reportedly associated with resistance to EGFR-TKIs. However, few studies have focused on patients harboring double mutations in these 3 mutation sites. In this retrospective study, forty-five patients (45/2546, 1...
2018: BioMed Research International
https://www.readbyqxmd.com/read/29581791/usefulness-of-bronchoscopic-rebiopsy-of-non-small-cell-lung-cancer-with-acquired-resistance-to-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitor
#17
Eun Kyong Goag, Jung Mo Lee, Kyung Soo Chung, Song Yee Kim, Ah Young Leem, Joo Han Song, Ji Ye Jung, Moo Suk Park, Yoon Soo Chang, Young Sam Kim, Joon Chang, Eun Young Kim
Background : Approximately 50% of non-small cell lung cancer (NSCLC) patients with acquired resistance to EGFR-TKI harbor the EGFR mutation T790M. The recent development and wide use of third-generation EGFR-TKIs targeting T790M-mutant NSCLCs have increased the importance of rebiopsy after EGFR-TKI failure. We aimed to investigate the advantages of flexible bronchoscopy as a rebiopsy method and the prevalence of and factors affecting the T790M mutation after EGFR-TKI failure. Methods : We investigated 139 patients who had undergone bronchoscopic rebiopsy and endobronchial ultrasound-guided transbronchial needle aspiration (EBUS-TBNA) between Sep 2014 and Jul 2016...
2018: Journal of Cancer
https://www.readbyqxmd.com/read/29575765/combination-therapy-of-apatinib-with-icotinib-for-primary-acquired-icotinib-resistance-in-patients-with-advanced-pulmonary-adenocarcinoma-with-egfr-mutation
#18
Pinghui Xia, Jinlin Cao, Xiayi Lv, Luming Wang, Wang Lv, Jian Hu
Multi-targeted agents represent the next generation of targeted therapies for solid tumors, and patients with acquired resistance to EGFR-tyrosine kinase inhibitors (TKIs) may also benefit from their combination with TKI therapy. Third-generation targeted drugs, such as osimertinib, are very expensive, thus a more economical solution is required. The aim of this study was to explore the use of apatinib combined with icotinib therapy for primary acquired resistance to icotinib in three patients with advanced pulmonary adenocarcinoma with EGFR mutations...
March 24, 2018: Thoracic Cancer
https://www.readbyqxmd.com/read/29573196/efatutazone-and-t0901317-exert-synergistically-therapeutic-effects-in-acquired-gefitinib-resistant-lung-adenocarcinoma-cells
#19
Jie Ni, Lei-Lei Zhou, Li Ding, Xue-Qin Zhang, Xia Zhao, Huizi Li, Haixia Cao, Siwen Liu, Zhuo Wang, Rong Ma, Jianzhong Wu, Jifeng Feng
The development of acquired EGFR-TKI therapeutic resistance is still a serious clinical problem in the management of lung adenocarcinoma. Peroxisome proliferator activated receptor gamma (PPARγ) agonists may exhibit anti-tumor activity by transactivating genes which are closely associated with cell proliferation, apoptosis, and differentiation. However, it remains not clear whether efatutazone has similar roles in lung adenocarcinoma cells of gefitinib resistant such as HCC827-GR and PC9-GR. It has been demonstrated by us that efatutazone prominently increased the mRNA and protein expression of PPARγ, liver X receptor alpha (LXRα),as well as ATP binding cassette subfamily A member 1 (ABCA1)...
March 23, 2018: Cancer Medicine
https://www.readbyqxmd.com/read/29571987/clinical-analysis-by-next-generation-sequencing-for-nsclc-patients-with-met-amplification-resistant-to-osimertinib
#20
Yubo Wang, Li Li, Rui Han, Lin Jiao, Jie Zheng, Yong He
INTRODUCTION: The efficacy of osimertinib was compromised by the development of resistance mechanisms, such as MET amplification. However, cohort studies of osimertinib resistance mechanism, and the correlation of MET and progression-free survival (PFS) after osimertinib resistance have been poorly investigated. OBJECTIVES: This study was carried out to study the acquired MET amplification after osimertinib resistance in advanced lung adenocarcinoma patients, and interrogate the correlation of clinical prognosis and MET amplification...
April 2018: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
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