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https://www.readbyqxmd.com/read/29039585/identification-of-genome-variations-in-patients-with-lung-adenocarcinoma-using-whole-genome-re%C3%A2-sequencing
#1
Guiyuan Li, Yunqing Mei, Fan Yang, Shengming Yi, Lemin Wang
Lung adenocarcinoma is one of the types of non‑small cell lung carcinoma, which tends to be treated with surgical therapy rather than radiation therapy. It occurs in smokers and non‑smokers, and is the most common form of lung cancer among non‑smokers and women. Gene rearrangements, including ALK, ROS1 and RET, and gene mutations, including epidermal growth factor receptor (EGFR), HER2, Kristen rat sarcoma viral oncogene homolog, BRAF, phosphoinositide‑3‑kinase, catalytic, α polypeptide and MET, have been identified in lung adenocarcinoma, which enable targeted therapy in lung adenocarcinoma, for example erlotinib, gefitinib and afatinib, which are EGFR inhibitors...
October 17, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29033690/dual-egfr-and-braf-blockade-overcomes-resistance-to-vemurafenib-in-braf-mutated-thyroid-carcinoma-cells
#2
Tiziana Notarangelo, Lorenza Sisinni, Valentina Condelli, Matteo Landriscina
BACKGROUND: BRAF inhibitors are effective anticancer agents in BRAF-mutated melanomas. By contrast, evidences about sensitivity of thyroid carcinomas to BRAF inhibition are conflicting and it has been proposed that BRAF V600E thyroid carcinoma cells are less sensitive to BRAF inhibitors due to activation of parallel signaling pathways. This study evaluated the hypothesis that feedback activation of EGFR signaling counteracts the cytostatic activity of vemurafenib (PLX4032) in BRAF V600E thyroid carcinoma cells...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/29031981/fabrication-and-characterization-of-gefitinib-releasing-polyurethane-foam-as-a-coating-for-drug-eluting-stent-in-the-treatment-of-bronchotracheal-cancer
#3
Weiluan Chen, Chiara di Carlo, Donal Devery, Donnacha J McGrath, Peter E McHugh, Kathrin Kleinsteinberg, Stefan Jockenhoevel, Wim E Hennink, Robbert J Kok
The purpose of the present study was to develop gefitinib-loaded polymeric foams that can be used as coating of drug-eluting stents for palliative treatment of bronchotracheal cancer. Release of such an anticancer drug from such stent coating can retard tumor regrowth into the bronchial lumen. Gefitinib-loaded polyurethane (PU) foams were prepared by embedding either gefitinib micronized crystals or gefitinib-loaded poly(lactic-co-glycolic acid) microspheres in water-blown films, with up to 10% w/w loading for gefitinib microcrystals and 15% w/w for gefitinib microspheres (corresponding to 1...
October 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29031620/targeting-non-small-cell-lung-cancer-with-small-molecule-egfr-tyrosine-kinase-inhibitors
#4
REVIEW
Mahaveer Singh, Hemant R Jadhav
Epidermal growth factor (EGFR) tyrosine kinase inhibitors (TKIs), such as gefitinib and erlotinib, show excellent clinical efficacy for patients with non-small cell lung cancer (NSCLC) with EGFR mutations, including Exon 19 deletion and single-point substitution, and L858R of exon 21. The reason for the reduction in effectiveness of these EGFR TKIs is the T790M gatekeeper mutation in the ATP-binding pocket of Exon 20, which increases the affinity of EGFR for ATP. Newer EGFR TKIs, such as afatinib, osimertinib, rociletinib, EGF816 and ASP8273, selectively target T790M mutants, sparing wild-type EGFR...
October 12, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/29026574/complete-remission-of-rare-adenocarcinoma-of-the-oropharynx-with-apceden-%C3%A2-dendritic-cell-based-vaccine-a%C3%A2-case-report
#5
Chaitanya Kumar, Sakshi Kohli, Srikanth Chiliveru, Minish Jain, Bandana Sharan
APCEDEN (®) is an autologous monocyte-derived dendritic cell-based immunotherapy. A 58-year-old man with adenocarcinoma of oropharynx shows complete remission after receiving APCEDEN (®) in conjunction with Geftinib validated by reduction in size, whereas Gefitinib alone lead to disease progression.
October 2017: Clinical Case Reports
https://www.readbyqxmd.com/read/29022575/gefitinib-inhibits-m2-like-polarization-of-tumor-associated-macrophages-in-lewis-lung-cancer-by-targeting-the-stat6-signaling-pathway
#6
Muhammad Tariq, Jie-Qiong Zhang, Gui-Kai Liang, Qiao-Jun He, Ling Ding, Bo Yang
M2-like polarized tumor-associated macrophages (TAMs) play a pivotal role in promoting cancer cell growth, invasion, metastasis and angiogenesis. The identification of M2-like TAMs during tumor progression is an attractive approach for cancer therapy. In this study, we investigated the relevance of macrophage polarization and the antitumor effect of gefitinib in Lewis Lung cancer (LLC) in vitro and in vivo. Gefitinib at a concentration below 2.5 μmol/L did not cause significant growth inhibition on LLC and RAW 264...
October 12, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28993193/%C3%AE-lipoic-acid-inhibits-human-lung-cancer-cell-proliferation-through-grb2-mediated-egfr-downregulation
#7
Lan Yang, Ya Wen, Guoqing Lv, Yuntao Lin, Junlong Tang, Jingxiao Lu, Manqiao Zhang, Wen Liu, Xiaojuan Sun
BACKGROUND: Alpha lipoic acid (α -LA) is a naturally occurring antioxidant and metabolic enzyme co-factor. Recently, α -LA has been reported to inhibit the growth of various cancer cells, but the precise signaling pathways that mediate the effects of α -LA on non-small cell lung cancer (NSCLC) development remain unclear. METHODS: The CCK-8 assay was used to assess cell proliferation in NSCLC cell lines after α -LA treatment. The expression of growth factor receptor-bound protein 2 (Grb2), cyclin-dependent kinase (CDK)-2, CDK4, CDK6, Cyclin D3, Cyclin E1, Ras, c-Raf, epidermal growth factor receptor (EGFR), ERK1/2 and activated EGFR and ERK1/2 was evaluated by western blotting...
October 6, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28987609/structure-based-design-and-synthesis-of-2-4-diaminopyrimidines-as-egfr-l858r-t790m-selective-inhibitors-for-nsclc
#8
Lingfeng Chen, Weitao Fu, Chen Feng, Rong Qu, Linjiang Tong, Lulu Zheng, Bo Fang, Yinda Qiu, Jie Hu, Yuepiao Cai, Jianpeng Feng, Hua Xie, Jian Ding, Zhiguo Liu, Guang Liang
Mutated epidermal growth factor receptor (EGFR) is a major driver of non-small cell lung cancer (NSCLC). The EGFR(T790M) secondary mutation has become a leading cause of clinically-acquired resistance to gefitinib and erlotinib. Herein, we present a structure-based design approach to increase the potency and selectivity of the previously reported reversible EGFR inhibitor 7, at the kinase and cellular levels. Three-step structure-activity relationship exploration led to promising compounds 19e and 19h with unique chemical structure and binding mode from the other third-generation tyrosine kinase inhibitors...
September 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28982345/development-and-characterization-of-gefitinib-loaded-polymeric-nanoparticles-by-ionic-gelation-method
#9
Minakshi Gupta, Harish Dureja, Rakesh Kumar Marwaha
BACKGROUND: There is rapidly growing interest in the development of nanoparticle drug delivery mainly for anticancer drugs as it promises to solve several problems related to anticancer drugs like poor water solubility, low therapeutic index, nonspecific distribution and higher systemic toxicity, etc. OBJECTIVE: The objective of the study was to investigate the effect of various critical variables like, concentration of chitosan, concentration of sodium tripolyphosphate (STPP) and volume of STPP on various characteristics of gefitinib loaded nanoparticles...
October 4, 2017: Pharmaceutical Nanotechnology
https://www.readbyqxmd.com/read/28981161/effects-of-concomitant-medication-use-on-gefitinib-induced-hepatotoxicity
#10
Soyeon Cho, Jeong Yee, Jae Youn Kim, Sandy Jeong Rhie, Hye Sun Gwak
Gefitinib is a drug used for the treatment of non-small cell lung cancer (NSCLC) patients. Severe hepatotoxicity was observed, but only a few cases have been reported on the hepatotoxicity of gefitinib. This study aimed to investigate the association between gefitinib-induced hepatotoxicity and various factors including concomitant medications in lung cancer patients. From January 2013 to December 2014, a retrospective study was performed with NSCLC patients who were treated with gefitinib. Associations between hepatotoxicity and various factors including concomitant drugs were analyzed...
October 5, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28979811/a-novel-multi-target-inhibitor-harboring-selectivity-of-inhibiting-egfr-t790m-sparing-wild-type-egfr
#11
Xiaoping Song, Xin Qi, Qiang Wang, Weiming Zhu, Jing Li
Non-Small Cell Lung Cancer (NSCLC) is driven by a variety of deregulated kinases and the development of multi-target inhibitor for multiple signaling pathways or multiple steps is required. Here, we reported that ZWM026, an indolocarbazoles analogue, derived from mangrove in coastal marine wetland, exhibited selectivity and reversibility against T790M mutant over wild-type EGFR in naturally occurring NSCLC cells and constructed NIH-3T3 cells. It simultaneously inhibited activities of HER2, HER3, HER4 and RET but was different from current multi-target kinase inhibitors...
2017: American Journal of Cancer Research
https://www.readbyqxmd.com/read/28978341/mab-mdr1-modified-chitosan-nanoparticles-overcome-acquired-egfr-tki-resistance-through-two-potential-therapeutic-targets-modulation-of-mdr1-and-autophagy
#12
Yan Zheng, Chang Su, Liang Zhao, Yijie Shi
BACKGROUND: Tyrosine kinase inhibitors (TKIs) that act against the epithelial growth factor receptor (EGFR) were once widely used in chemotherapy for many human cancers. However, acquired chemoresistance occurred in almost all patients, limiting the clinical application of EGFR-TKI. Thus far, no effective methods existing can resolve this problem. Designing a therapeutic treatment with a specific multi-target profile has been regarded as a possible strategy to overcome acquired EGFR-TKI resistance...
October 4, 2017: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/28978102/acquisition-of-the-t790m-resistance-mutation-during-afatinib-treatment-in-egfr-tyrosine-kinase-inhibitor-na%C3%A3-ve-patients-with-non-small-cell-lung-cancer-harboring-egfr-mutations
#13
Kentaro Tanaka, Kaname Nosaki, Kohei Otsubo, Koichi Azuma, Shinya Sakata, Hiroshi Ouchi, Ryotaro Morinaga, Hiroshi Wataya, Akiko Fujii, Noriaki Nakagaki, Nobuko Tsuruta, Masafumi Takeshita, Eiji Iwama, Taishi Harada, Yoichi Nakanishi, Isamu Okamoto
The T790M secondary mutation of the epidermal growth factor receptor (EGFR) gene accounts for 50% to 60% of cases of resistance to the first-generation EGFR tyrosine kinase inhibitors (TKIs) gefitinib and erlotinib. The prevalence of T790M in EGFR mutation-positive patients who acquire resistance to the irreversible, second-generation EGFR-TKI afatinib has remained unclear, however. We here determined the frequency of T790M acquisition at diagnosis of progressive disease in patients with EGFR-mutated non-small cell lung cancer (NSCLC) treated with afatinib as first-line EGFR-TKI...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28968167/gefitinib-plus-chemotherapy-versus-chemotherapy-in-epidermal-growth-factor-receptor-mutation-positive-non-small-cell-lung-cancer-resistant-to-first-line-gefitinib-impress-overall-survival-and-biomarker-analyses
#14
Tony S K Mok, Sang-We Kim, Yi-Long Wu, Kazuhiko Nakagawa, Jin-Ji Yang, Myung-Ju Ahn, Jie Wang, James Chih-Hsin Yang, You Lu, Shinji Atagi, Santiago Ponce, Xiaojin Shi, Yuri Rukazenkov, Vincent Haddad, Kenneth S Thress, Jean-Charles Soria
Purpose The Iressa Mutation-Positive Multicentre Treatment Beyond ProgRESsion Study (IMPRESS) compared the continuation of gefitinib plus chemotherapy with placebo plus chemotherapy in patients with epidermal growth factor receptor ( EGFR) mutation-positive advanced non-small-cell lung cancer with progression (Response Evaluation Criteria in Solid Tumors 1.1) after first-line gefitinib. Primary results indicated no difference between treatments in terms of progression-free survival (PFS). The current analysis presents final, mature, overall survival (OS) data, together with exploratory analyses that examined whether specific biomarkers, including T790M mutation status, were able to differentiate a relative treatment effect...
October 2, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28964888/egfr-her2-target-based-molecular-docking-analysis-in-vitro-screening-of-2-4-5-trisubstituted-imidazole-derivatives-as-potential-anti-oxidant-and-cytotoxic-agents
#15
Ramu Guda, Girijesh Kumar, Rajashekar Korra, Siripireddy Balaji, Govindu Dayakar, Rambabu Palabindela, Prabhakar Myadaraveni, Narsimha Reddy Yellu, Mamatha Kasula
In our endeavor towards the development of potent molecules for cancer diseases, we have designed and synthesized a series of 2,4,5-trisubstituted imidazole derivatives (B1-B24) and characterized by using various spectroscopic techniques. All these compounds are further evaluated for their in vitro anti-cancer, anti-oxidant activities and molecular docking studies against EGFR, HER2 protein receptors. The in vitro anti-cancer activity analysis reveals that compounds B11 and B16 were found to be effective scaffolds against the tested human cancer cell lines IMR-32, A549 and HeLa...
September 18, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28964539/gefitinib-for-patients-with-incurable-cutaneous-squamous-cell-carcinoma-a-single-arm-phase-ii-clinical-trial
#16
William N William, Lei Feng, Renata Ferrarotto, Lawrence Ginsberg, Merrill Kies, Scott Lippman, Bonnie Glisson, Edward S Kim
BACKGROUND: Preclinical data demonstrate a key role for the epidermal growth factor receptor (EGFR) in the carcinogenesis of cutaneous squamous cell carcinomas (CSCCs). There are, however, limited data on the efficacy of EGFR inhibitors in incurable, recurrent, and/or metastatic CSCC. OBJECTIVE: To determine the response rate to gefitinib in patients with CSCC not amenable to curative therapy including surgery or radiation. METHODS: This was a single-arm phase II study...
September 27, 2017: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/28961023/in-vitro-and-in-vivo-antitumor-effect-of-gefitinib-nanoparticles-on-human-lung-cancer
#17
Xiao Ling Ni, Long Xia Chen, Heng Zhang, Bo Yang, Shan Xu, Min Wu, Jing Liu, Ling Lin Yang, Yue Chen, Shao Zhi Fu, Jing Bo Wu
Gefitinib (GEF) is the first epidermal growth factor receptor (EGFR)-targeting agent launched as an anticancer drug. It is an accepted opinion that modifying GEF strong hydrophobicity and poor bioavailability would not only enhance its antitumor effects, but also reduce its side effects. In this study, GEF-loadedpoly(ε-caprolactone)-poly(ethyleneglycol)-poly(ε-caprolactone) (PCEC) -bearing nanoparticles (GEF-NPs) were prepared by a solid dispersion method and characterized. The particle sizes increased with the increase in GEF/PCEC mass ratio in feed...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28960861/lentivirus-mediated-a-disintegrin-and-metalloproteinase-17-rna-interference-reversed-the-acquired-resistance-to-gefitinib-in-lung-adenocarcinoma-cells-in-vitro
#18
Ya-Qing Li, Yuan-Shun Liu, Xi-Wang Ying, Hong-Bin Zhou, Zhehua Wang, Sheng-Chang Wu, Jian-Ping Yan, Yu-Ting Jing, Yang Yang
OBJECTIVE: The aim of the study is to evaluate the effects of silencing a disintegrin and metalloproteinase 17 (ADAM17) gene expression by lentivirus-mediated RNA interference (RNAi) in the gefitinib-resistant lung adenocarcinoma cells, and then to explore whether the recombinant lentivirus mediated ADAM17 RNAi reversed the acquired resistance of lung adenocarcinoma to gefitinib in vitro. METHODS: The gefitinib-resistant RPC-9 cells were established and the mutations of EGFR were detected by gene sequencing...
September 27, 2017: Biotechnology Progress
https://www.readbyqxmd.com/read/28958502/dacomitinib-versus-gefitinib-as-first-line-treatment-for-patients-with-egfr-mutation-positive-non-small-cell-lung-cancer-archer-1050-a-randomised-open-label-phase-3-trial
#19
Yi-Long Wu, Ying Cheng, Xiangdong Zhou, Ki Hyeong Lee, Kazuhiko Nakagawa, Seiji Niho, Fumito Tsuji, Rolf Linke, Rafael Rosell, Jesus Corral, Maria Rita Migliorino, Adam Pluzanski, Eric I Sbar, Tao Wang, Jane Liang White, Sashi Nadanaciva, Rickard Sandin, Tony S Mok
BACKGROUND: Dacomitinib is a second-generation, irreversible EGFR tyrosine kinase inhibitor. We compared its efficacy and safety with that of the reversible EGFR tyrosine kinase inhibitor gefitinib in the first-line treatment of patients with advanced EGFR-mutation-positive non-small-cell lung cancer (NSCLC). METHODS: In this international, multicentre, randomised, open-label, phase 3 study (ARCHER 1050), we enrolled adults (aged ≥18 years or ≥20 years in Japan and South Korea) with newly diagnosed advanced NSCLC and one EGFR mutation (exon 19 deletion or Leu858Arg) at 71 academic medical centres and university hospitals in seven countries or special administrative regions...
September 25, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/28956845/design-synthesis-and-antitumor-activity-of-novel-quinazoline-derivatives
#20
Liuchang Wang, Pengna Li, Baolin Li, Yawen Wang, Jiangtao Li, Limei Song
In an attempt to explore a new class of epidermal growth factor receptor (EGFR) inhibitors, novel 4-stilbenylamino quinazoline derivatives were synthesized through a Dimorth rearrangement reaction and characterized via IR, ¹H-NMR, (13)C-NMR, and HRMS. Methoxyl, methyl, halogen, and trifluoromethyl groups on stilbeneamino were detected. These synthesized compounds were evaluated for antitumor activity in vitro against eight human tumor cell lines with an MTS assay. Most synthesized compounds exhibited more potent activity (IC50 = ~2...
September 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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