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https://www.readbyqxmd.com/read/28639751/gefitinib-or-erlotinib-in-previously-treated-non-small-cell-lung-cancer-patients-a-cohort-study-in-taiwan
#1
Chia-Hao Chang, Chih-Hsin Lee, Jen-Chung Ko, Lih-Yu Chang, Ming-Chia Lee, Jann-Yuan Wang, Chong-Jen Yu
Among treatment modalities for lung cancer, the most promising therapy is the use of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs). Both erlotinib and gefitinib, the two first-generation EGFR-TKIs, exhibit significant clinical responses for patients with lung adenocarcinoma. However, few studies have compared the effects of these two drugs, and results have been inconclusive because of the small sample sizes in these studies. Therefore, this study was conducted to investigate this issue...
June 22, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28631808/fabrication-of-%C3%AE-cyclodextrin-mediated-single-bimolecular-inclusion-complex-characterization-molecular-docking-in-vitro-release-and-bioavailability-studies-for-gefitinib-and-simvastatin-conjugate
#2
Souvik Basak, Sandip Mondal, Suddhasattya Dey, Plaban Bhattacharya, Achintya Saha, Vinay Deep Punetha, Ali Abbas, Nanda Gopal Sahoo
OBJECTIVES: Introduction of multiple molecules in a single inclusion complex, albeit cheaper, lacks conclusive attempts in earlier drug delivery reports. This manuscript emphasizes simultaneous incorporation of two anticancer drugs, gefitinib (G) and simvastatin (S), in a single molecule of β-cyclodextrin for the first time to achieve effective drug delivery. METHODS: The inclusion complex (GSBCD) was prepared by cosolvent evaporation technique using β-cyclodextrin (BCD) as carrier...
June 20, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28625629/a-phase-ib-trial-of-continuous-once-daily-oral-afatinib-plus-sirolimus-in-patients-with-epidermal-growth-factor-receptor-mutation-positive-non-small-cell-lung-cancer-and-or-disease-progression-following-prior-erlotinib-or-gefitinib
#3
Teresa Moran, Ramón Palmero, Mariano Provencio, Amelia Insa, Margarita Majem, Noemí Reguart, Joaquim Bosch-Barrera, Dolores Isla, Enric Carcereny Costa, Chooi Lee, Marta Puig, Sandrine Kraemer, David Schnell, Rafael Rosell
OBJECTIVES: Dysregulation of the downstream PI3K/AKT/mTOR signaling pathway is a proposed mechanism of resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs). We investigated safety and antitumor activity of afatinib plus sirolimus as a potential combination to reverse acquired resistance to EGFR-TKIs in a phase IB trial in patients with EGFR mutation-positive non-small-cell lung cancer (EGFR mut NSCLC) and/or disease progression following prior erlotinib/gefitinib...
June 2017: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/28623122/a-randomized-phase-ii-study-comparing-nivolumab-with-carboplatin-pemetrexed-for-patients-with-egfr-mutation-positive-nonsquamous-non-small-cell-lung-cancer-who-acquire-resistance-to-tyrosine-kinase-inhibitors-not-due-to-a-secondary-t790m-mutation-rationale
#4
Hidetoshi Hayashi, Yasutaka Chiba, Kazuko Sakai, Tomonobu Fujita, Hiroshige Yoshioka, Daisuke Sakai, Chiyoe Kitagawa, Tateaki Naito, Koji Takeda, Isamu Okamoto, Tetsuya Mitsudomi, Yutaka Kawakami, Kazuto Nishio, Shinichiro Nakamura, Nobuyuki Yamamoto, Kazuhiko Nakagawa
Antibodies to programmed cell death-1 (PD-1), such as nivolumab, have shown promising clinical activity in patients with advanced non-small-cell lung cancer (NSCLC), but their efficacy appears to be less pronounced in patients with such tumors harboring epidermal growth factor receptor gene (EGFR) mutations. Recent findings suggest that patients with EGFR mutation-positive NSCLC who develop resistance to tyrosine kinase inhibitors (TKIs) due to mechanisms other than acquisition of the secondary T790M mutation of EGFR are more likely to benefit from nivolumab treatment, possibly as a result of a higher level of expression of the PD-1 ligand PD-L1, than are patients who are T790M-positive...
May 25, 2017: Clinical Lung Cancer
https://www.readbyqxmd.com/read/28619365/aucklandia-lappa-dc-extract-enhances-gefitinib-efficacy-in-gefitinib-resistance-secondary-epidermal-growth-factor-receptor-mutations
#5
Guan Huang, Yanli Tong, Qidi He, Jie Wang, Zuanguang Chen
ETHNOPHARMACOLOGICAL RELEVANCE: Aucklandia lappa DC. is a widely used medicinal plant in China, India and Pakistan for a long time. Previously, a number of different pharmacological experiments in vitro and in vivo have convincingly demonstrated the abilities of it to exhibit anticancer activities. Reynoutria japonica Houtt. has also been widely used as traditional Chinese medicinal plant. Previous studies have demonstrated that it is bioactive to exhibit anticancer activities. AIM OF THE STUDY: This study aims to investigate whether the extracts of Aucklandia lappa DC...
June 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28617069/simultaneous-determination-of-six-tyrosine-kinase-inhibitors-in-human-plasma-using-hplc-q-orbitrap-mass-spectrometry
#6
Mao-Wei Ni, Jie Zhou, Hui Li, Wei Chen, Han-Zhou Mou, Zhi-Guo Zheng
AIM: Gefitinib, erlotinib, icotinib, crizotinib, lapatinib and apatinib are targeted cancer therapy agents acting through inhibition of tyrosine kinase. Method for quantifying these six drugs in human plasma of patients was required. MATERIALS & METHODS: An HPLC-Q-Orbitrap method (based on HPLC-MS/MS) was developed and validated for the simultaneous detection and quantitation of six tyrosine kinase inhibitors in human plasma. Sample was extracted by liquid-liquid extraction (ethyl acetate: tert-Butyl methyl ether, 1:1 v/v)...
June 15, 2017: Bioanalysis
https://www.readbyqxmd.com/read/28616379/re-biopsy-after-relapse-of-targeted-therapy-t790m-after-epidermal-growth-factor-mutation-where-and-why-based-on-a-case-series
#7
Paul Zarogoulidis, Aggeliki Rapti, Chrysanthi Sardeli, Panagiotis Chinelis, Anastasia Athanasiadou, Katerina Paraskevaidou, Anastasios Kallianos, Lemonia Veletza, Georgia Trakada, Wolfgang Hohenforst-Schmidt, Haidong Huang
Guidelines for the treatment of non-small cell lung cancer adenocarcinoma positive in epidermal growth factor mutations indicate tyrosine kinase inhibitors. There are currently three tyrosine kinase inhibitors that can be used as first line treatment: gefitinib, erlotinib and afatinib. Regarding erlotinib and afatinib dosage can be modified in the case of severe adverse effects. In the case of disease relapse investigation for T790M mutation has to be made either with re-biopsy or liquid biopsy and osimertinib has to be administered when T790M is diagnosed...
2017: Respiratory Medicine Case Reports
https://www.readbyqxmd.com/read/28609695/what-do-we-need-to-make-circulating-tumour-dna-ctdna-a-routine-diagnostic-test-in-lung-cancer
#8
REVIEW
Reyes Bernabé, Nicholas Hickson, Andrew Wallace, Fiona Helen Blackhall
The gold standard test for detection of epidermal growth factor receptor (EGFR) mutation is to genotype somatic DNA extracted from a tissue biopsy or cytology specimen. Yet, in at least 20% of patients this is not possible for various reasons including insufficient availability of neoplastic tissue, lack of fitness of the available tissue for a biopsy or that a biopsy is not technically feasible. Consequently, there has been intense investigation of circulating tumour DNA (ctDNA), released into the plasma fraction of blood from cancer cells during apoptosis/necrosis, as a minimally invasive 'liquid biopsy' and surrogate for cancer tissue...
June 10, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28607578/osimertinib-in-patients-with-advanced-epidermal-growth-factor-receptor-t790m-mutation-positive-non-small-cell-lung-cancer-rationale-evidence-and-place-in-therapy
#9
REVIEW
Biagio Ricciuti, Sara Baglivo, Luca Paglialunga, Andrea De Giglio, Guido Bellezza, Rita Chiari, Lucio Crinò, Giulio Metro
The identification of epidermal growth factor receptor (EGFR) mutations represented a fundamental step forward in the treatment of advanced non-small cell lung cancer (NSCLC) as they define a subset of patients who benefit from the administration of specifically designed targeted therapies. The inhibition of mutant EGFR through EGFR-tyrosine kinase inhibitors (TKIs), either reversible, first-generation gefitinib and erlotinib, or irreversible, second-generation afatinib, has dramatically improved the prognosis of patients harboring this specific genetic alteration, leading to unexpected clinical benefit...
June 2017: Therapeutic Advances in Medical Oncology
https://www.readbyqxmd.com/read/28603991/trisubstituted-pyridinylimidazoles-as-potent-inhibitors-of-the-clinically-resistant-l858r-t790m-c797s-egfr-mutant-targeting-of-both-hydrophobic-regions-and-the-phosphate-binding-site
#10
Marcel Günther, Jonas Lategahn, Michael Juchum, Eva Döring, Marina Keul, Julian Engel, Hannah L Tumbrink, Daniel Rauh, Stefan Laufer
Inhibition of the epidermal growth factor receptor represents one of the most promising strategies in the treatment of lung cancer. Acquired resistance compromises the clinical efficacy of EGFR inhibitors during long-term treatment. The recently discovered EGFR-C797S mutation causes resistance against third-generation EGFR inhibitors. Here we present a rational approach based on extending the inhibition profile of a p38 MAP kinase inhibitor toward mutant EGFR inhibition. We used a privileged scaffold with proven cellular potency as well as in vivo efficacy and low toxicity...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28600491/development-and-evaluation-of-18-f-irs-for-molecular-imaging-mutant-egf-receptors-in-nsclc
#11
Yan Song, Zunyu Xiao, Kai Wang, Xiance Wang, Chongqing Zhang, Fang Fang, Xilin Sun, Baozhong Shen
To prepare and evaluate a new radiotracer (18)F-IRS for molecular imaging mutant EGF Receptors in vitro and vivo. Uptake and efflux of (18)F-IRS were performed with four NSCLC cell lines including HCC827, H1975, H358 and H520. In vivo tumor targeting and pharmacokinetics of the radiotracers were also evaluated in HCC827, H1975, H358 and H520 tumor-bearing nude mice by PET/CT imaging. Ex vivo biodistribution assays were performed to quantify the accumulation of (18)F-IRS in vivo. We also performed (18)F-IRS PET/CT imaging of three patients with NSCLC...
June 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28599456/dynamic-monitoring-of-egfr-mutations-in-circulating-cell-free-dna-for-egfr-mutant-metastatic-patients-with-lung-cancer-early-detection-of-drug-resistance-and-prognostic-significance
#12
Jianjiao Ni, Linqian Weng, Yi Liu, Zhao Sun, Chunmei Bai, Yingyi Wang
Detecting genetic mutations in circulating cell-free DNA (cfDNA) is a promising approach of liquid biopsy. Between June 2014 and May 2015, 168 plasma samples were collected monthly from 20 patients with metastatic lung adenocarcinoma with epidermal growth factor receptor (EGFR) mutation receiving gefitinib therapy. Clinically relevant EGFR mutations, including exon 19 deletion, L858R and T790M, were quantified using droplet digital polymerase chain reaction. In baseline samples, 19 (95.0%) patients had the same mutation with the matched tumors, and pretreatment T790M mutations were also detected in 3 (15...
June 2017: Oncology Letters
https://www.readbyqxmd.com/read/28599445/comparison-of-the-effectiveness-of-erlotinib-gefitinib-and-afatinib-for-treatment-of-non-small-cell-lung-cancer-in-patients-with-common-and-rare-egfr-gene-mutations
#13
Pawel Krawczyk, Dariusz M Kowalski, Rodryg Ramlau, Ewa Kalinka-Warzocha, Kinga Winiarczyk, Katarzyna Stencel, Tomasz Powrózek, Katarzyna Reszka, Kamila Wojas-Krawczyk, Maciej Bryl, Magdalena Wójcik-Superczyńska, Maciej Głogowski, Aleksander Barinow-Wojewódzki, Janusz Milanowski, Maciej Krzakowski
Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) are routinely used to treat non-small cell lung cancer (NSCLC) in patients with common activating mutations of the EGFR gene. The aim of the study was to compare the efficacies of EGFR-TKIs in patients with common (exon 19 deletions and exon 21 p.Leu858Arg) and rare EGFR mutations. A retrospective analysis of 180 NSCLC patients with common (n=167) and rare (n=13) EGFR mutations treated with erlotinib (n=98), gefitinib (n=66) and afatinib (n=16) was performed...
June 2017: Oncology Letters
https://www.readbyqxmd.com/read/28599309/marsdenia-tenacissima-extract-overcomes-axl-and-met-mediated-erlotinib-and-gefitinib-cross-resistance-in-non-small-cell-lung-cancer-cells
#14
Shu-Yan Han, Wei Zhao, Hai-Bo Han, Hong Sun, Dong Xue, Yan-Na Jiao, Xi-Ran He, Shan-Tong Jiang, Ping-Ping Li
Tyrosine kinase inhibitors (TKIs) are an effective treatment strategy for non-small cell lung cancer (NSCLC) patients harboring mutations that result in constitutive activation of the epidermal growth factor receptor (EGFR). However, most patients eventually develop resistance to TKIs. This occurs due to additional EGFR mutations or the activation of bypass signaling pathways. In our previous work, we demonstrated that Marsdenia tenacissima extract (MTE) restored gefitinib sensitivity in resistant NSCLC cells with EGFR T790M or K-ras mutations...
May 24, 2017: Oncotarget
https://www.readbyqxmd.com/read/28596498/somatic-mutations-in-salivary-duct-carcinoma-and-potential-therapeutic-targets
#15
Timothy K Khoo, Bing Yu, Joel A Smith, Angus J Clarke, Peter P Luk, Christina I Selinger, Kate L Mahon, Spiridoula Kraitsek, Carsten Palme, Michael J Boyer, Marcel E Dinger, Mark J Cowley, Sandra A O'Toole, Jonathan R Clark, Ruta Gupta
BACKGROUND: Salivary duct carcinomas (SDCa) are rare highly aggressive malignancies. Most patients die from distant metastatic disease within three years of diagnosis. There are limited therapeutic options for disseminated disease. RESULTS: 11 cases showed androgen receptor expression and 6 cases showed HER2 amplification. 6 Somatic mutations with additional available targeted therapies were identified: EGFR (p.G721A: Gefitinib), PDGFRA (p.H845Y: Imatinib and Crenolanib), PIK3CA (p...
May 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28596108/association-between-egfr-t790m-status-and-progression-patterns-during-initial-egfr-tki-treatment-in-patients-harboring-egfr-mutation
#16
Yuko Oya, Tatsuya Yoshida, Hiroaki Kuroda, Junichi Shimizu, Yoshitsugu Horio, Yukinori Sakao, Yoshitaka Inaba, Toyoaki Hida, Yasushi Yatabe
BACKGROUND: Emergence of the T790M point mutation in exon 20 of the epidermal growth factor receptor (EGFR) is the most common mechanism of resistance to EGFR tyrosine kinase inhibitors (EGFR-TKIs). The aim of this study was to investigate the association between T790M mutation status and the progression patterns during EGFR-TKI treatment. METHODS: We reviewed 181 patients with advanced non-small-cell lung cancer harboring EGFR mutation, who were evaluated for T790M mutation status after initial EGFR-TKI failure (gefitinib, erlotinib, or afatinib)...
May 10, 2017: Clinical Lung Cancer
https://www.readbyqxmd.com/read/28595906/construction-of-egfr-peptide-gefitinib-quantum-dots-long-circulating-polymeric-liposomes-for-treatment-and-detection-of-nasopharyngeal-carcinoma
#17
Yong Liu, Yi Zhao, Hao Luo, Fei Liu, YanMin Wu
Gefitinib/Quantum dots (QDs) loaded peptide long circulating liposomes (G/QDs-P-LCPL) were successfully prepared for treatment and detection by fluorescence labeling for nasopharyngeal carcinoma. Gefitinib was found to have marked inhibition which is dose- and time-dependent. Hoechst 33258 florescence staining and wound-healing assay indicated that as G/QDs-P-LCPL concentration increased, HONE1 staining cells decreased, while the amount of nucleus pyknosis and karyorrhexis grew. Florescence tracing result shows that the drug mainly distributed through tumors...
June 5, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28592790/mir-19a-contributes-to-gefitinib-resistance-and-epithelial-mesenchymal-transition-in-non-small-cell-lung-cancer-cells-by-targeting-c-met
#18
Xiaonian Cao, Senyan Lai, Fayong Hu, Guodong Li, Guihua Wang, Xuelai Luo, Xiangning Fu, Junbo Hu
Gefitinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, is used as a first-line treatment for advanced non-small cell lung cancer (NSCLC). However, most NSCLC patients inevitably develop gefitinib resistance, and the mechanisms underlying this resistance are not fully understood. In this study, we show that miR-19a is significantly down-regulated in gefitinib-resistant NSCLC cell lines compared with gefitinib-sensitive cell lines. In addition, the down-regulation of miR-19a suppressed the expression of epithelial markers but induced the expression levels of mesenchymal markers...
June 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28592399/dacomitinib-beats-gefitinib-for-egfr-nsclc
#19
(no author information available yet)
The irreversible EGFR inhibitor dacomitinib reduced the chance of lung cancer progression compared with an older, first-generation EGFR inhibitor, gefitinib, in a phase III trial. As reported at the 2017 American Society of Clinical Oncology Annual Meeting, the experimental drug also increased toxicity, which could limit its use, especially with a safer, more effective third-generation EGFR inhibitor not far behind in the development pipeline.
June 7, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28590931/multiple-receptor-tyrosine-kinase-activation-related-to-alk-inhibitor-resistance-in-lung-cancer-cells-with-alk-rearrangement
#20
Se Hoon Choi, Dong Ha Kim, Yun Jung Choi, Seon Ye Kim, Jung-Eun Lee, Ki Jung Sung, Woo Sung Kim, Chang-Min Choi, Jin Kyung Rho, Jae Cheol Lee
The activation of alternative receptor tyrosine kinases (RTKs) is known to mediate resistance to ALK inhibitors. However, the role of multiple RTK activation in resistance has yet to be determined. Two crizotinib-resistant (H3122/CR-1 and H3122/CR-2) and one TAE684-resistant (H2228/TR) cell lines were established. Multi-RTK arrays and Western blots were performed to detect the activation of bypass signals. There were no secondary mutations in the sequencing. EGFR and MET were activated in H3122/CR-1 cells whereas EGFR and IGF1R were activated in H3122/CR-2 cells...
May 8, 2017: Oncotarget
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