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https://www.readbyqxmd.com/read/29346507/activity-and-safety-of-afatinib-in-a-window-pre-operative-eortc-study-in-patients-with-squamous-cell-carcinoma-of-the-head-and-neck-scchn
#1
J P Machiels, P Bossi, J Menis, M Lia, C Fortpied, Y Liu, R Lhommel, M Lemort, S Schmitz, S Canevari, L De Cecco, M Guzzo, R Bianchi, P Quattrone, F Crippa, T Duprez, Y Lalami, M Quiriny, N de Saint Aubain, P M Clement, R Coropciuc, E Hauben, L F Licitra
Background: To investigate the activity and safety of afatinib in the pre-operative treatment of squamous cell carcinoma of the head and neck (SCCHN). Patients and methods: This study was an open-label, randomized, multicenter, phase II window of opportunity trial. Treatment-naïve SCCHN patients selected for primary curative surgery were randomized (5:1 ratio) to receive afatinib during 14 days (day -15 until day -1) before surgery (day 0) or no treatment. Tumor biopsies, 2-[fluorine-18]-fluoro-2-deoxy-D-glucose positron emission tomography (FDG-PET), and magnetic resonance imaging (MRI) were performed at diagnosis and just before surgery...
January 15, 2018: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29337963/phase-i-open-label-study-of-afatinib-plus-vinorelbine-in-patients-with-solid-tumours-overexpressing-egfr-and-or-her2
#2
Rastislav Bahleda, Andrea Varga, Yann Bergé, Jean-Charles Soria, David Schnell, Inga Tschoepe, Martina Uttenreuther-Fischer, Jean-Pierre Delord
BACKGROUND: This phase Ib study evaluated afatinib plus vinorelbine in patients with advanced solid tumours overexpressing epidermal growth factor receptor (EGFR) and/or human EGFR 2 (HER2). METHODS: Maximum tolerated doses (MTDs) were determined for afatinib (20, 40 or 50 mg, once daily) combined with standard intravenous vinorelbine (part A; 25 mg m-2 per week) or oral vinorelbine (part B; 60 mg m-2 per week, increased to 80 mg m-2 per week at week 3)...
January 16, 2018: British Journal of Cancer
https://www.readbyqxmd.com/read/29336166/optimizing-outcomes-in-egfr-mutation-positive-nsclc-which-tyrosine-kinase-inhibitor-and-when
#3
Nicolas Girard
Despite the efficacy of standard-of-care EGFR tyrosine kinase inhibitors (TKIs), erlotinib, gefitinib and afatinib, in EGFR mutation-positive non-small-cell lung cancer, resistance develops, most commonly due to the T790M mutation. Osimertinib showed clinical activity in the treatment of T790M-positive disease following progression on a first-line TKI, and is approved in this setting. Recently, osimertinib improved efficacy versus first-generation TKIs (erlotinib and gefitinib) in the first-line setting. Multiple factors can influence first-line treatment decisions, including subsequent therapy options, presence of brain metastases and tolerability, all of which should be considered in the long-term treatment plan...
January 16, 2018: Future Oncology
https://www.readbyqxmd.com/read/29331859/development-of-a-method-to-determine-axitinib-lapatinib-and-afatinib-in-plasma-by-micellar-liquid-chromatography-and-validation-by-the-european-medicines-agency-guidelines
#4
Jaume Albiol-Chiva, Josep Esteve-Romero, Juan Peris-Vicente
A method based on micellar liquid chromatography to quantify the tyrosine kinase inhibitors axitinib, lapatinib and afatinib in plasma is reported. The sample pretreatment was a simple 1/5-dilution in a pure micellar solution, filtration and direct injection, without requiring extraction or purification steps. The three drugs were resolved from the matrix in 17min, using an aqueous solution of 0.07M sodium dodecyl sulfate - 6.0% 1-pentanol, buffered at pH7 with 0.01M phosphate salt as mobile phase, running under isocratic mode at 1mL/min through a C18 column...
January 2, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29326440/braf-inhibition-upregulates-a-variety-of-receptor-tyrosine-kinases-and-their-downstream-effector-gab2-in-colorectal-cancer-cell-lines
#5
Ricarda Herr, Sebastian Halbach, Miriam Heizmann, Hauke Busch, Melanie Boerries, Tilman Brummer
BRAF mutations occur in ~10% of colorectal cancer (CRC) and are associated with poor prognosis. Inhibitors selective for the BRAFV600E oncoprotein, the most common BRAF mutant, elicit only poor response rates in BRAF-mutant CRC as single agents. This unresponsiveness was mechanistically attributed to the loss of negative feedbacks on the epidermal growth factor receptor (EGFR) and initiated clinical trials that combine BRAF (and MEK) inhibitors, either singly or in combination, with the anti-EGFR antibodies cetuximab or panitumumab...
January 12, 2018: Oncogene
https://www.readbyqxmd.com/read/29325228/effects-of-trastuzumab-and-afatinib-on-kinase-activity-in-gastric-cancer-cell-lines
#6
Simone Keller, Gwen Zwingenberger, Karolin Ebert, Jan Hasenauer, Jacqueline Wasmuth, Dieter Maier, Ivonne Haffner, Katrin Schierle, Gregor Weirich, Birgit Luber
The molecular mechanism of action of the HER2-targeted antibody trastuzumab is only partially understood, and the direct effects of trastuzumab on the gastric cancer signaling network are unknown. In this study, we compared the molecular effect of trastuzumab and the HER kinase inhibitor afatinib on the receptor tyrosine kinase (RTK) network and the downstream-acting intracellular kinases in gastric cancer cell lines. The molecular effects of trastuzumab and afatinib on the phosphorylation of 49 RTKs and 43 intracellular kinase phosphorylation sites were investigated in three gastric cancer cell lines (NCI-N87, MKN1 and MKN7) using proteome profiling...
January 11, 2018: Molecular Oncology
https://www.readbyqxmd.com/read/29321093/a-retrospective-comparison-of-the-clinical-efficacy-of-gefitinib-erlotinib-and-afatinib-in-japanese-patients-with-non-small-cell-lung-cancer
#7
Atsushi Fujiwara, Masamichi Yoshida, Hajime Fujimoto, Hiroki Nakahara, Kentaro Ito, Kota Nishihama, Taro Yasuma, Osamu Hataji, Osamu Taguchi, Corina N D'Alessandro-Gabazza, Esteban C Gabazza, Tetsu Kobayashi
Tyrosine kinase inhibitors (TKIs) are very effective against non-small-cell lung cancer caused by epidermal growth factor receptor (EGFR) mutation. Before the approval of osimertinib in March 2016, there were only three available EGFR TKIs (gefitinib, erlotinib and afatinib) for the therapy of non-small-cell lung cancer in Japan. Osimertinib can be indicated only against T790M (+) lung cancer as a second-line therapy. However, whether gefitinib, erlotinib or afatinib is most appropriate as a first-line therapy is still a controversial issue...
January 10, 2018: Oncology Research
https://www.readbyqxmd.com/read/29311018/melanoma-associated-antigen-a11-reduces-erlotinib-and-afatinib-efficacy-in-head-and-neck-cancer
#8
Stefan Hartmann, Leonie Zwick, Katja Maurus, Andreas R Fuchs, Roman C Brands, Axel Seher, Alexander C Kübler, Urs D A Müller-Richter
Melanoma-associated antigen A (MAGE-A) proteins are members of the cancer/testis antigens (CTA), and the expression of these proteins is almost exclusively limited to malignant cells, making them an attractive treatment target. MAGE-A expression is correlated with poor overall survival in several cancers, including head and neck squamous cell carcinoma (HNSCC). Among others, MAGE-A11 was found to be associated with resistance to different antineoplastic and targeted compounds, such as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs)...
December 24, 2017: Journal of Cranio-maxillo-facial Surgery
https://www.readbyqxmd.com/read/29290249/a-phase-i-trial-of-afatinib-and-bevacizumab-in-chemo-na%C3%A3-ve-patients-with-advanced-non-small-cell-lung-cancer-harboring-egfr-mutations-okayama-lung-cancer-study-group-trial-1404
#9
Takashi Ninomiya, Naoyuki Nogami, Toshiyuki Kozuki, Daijiro Harada, Toshio Kubo, Kadoaki Ohashi, Shoichi Kuyama, Kenichiro Kudo, Akihiro Bessho, Nobuaki Fukamatsu, Nobukazu Fujimoto, Keisuke Aoe, Takuo Shibayama, Keisuke Sugimoto, Nagio Takigawa, Katsuyuki Hotta, Katsuyuki Kiura
OBJECTIVE: In advanced epidermal growth factor receptor (EGFR)-mutant non-small-cell lung cancer (NSCLC), treatment with afatinib, a second-generation EGFR-tyrosine kinase inhibitor (TKI), confers a significant survival benefit over platinum-based chemotherapy. The first-generation EGFR-TKIs gefitinib and erlotinib in combination with bevacizumab have improved progression-free survival. We hypothesized that the combination of afatinib with bevacizumab would further improve efficacy, and conducted a phase I trial to test this hypothesis...
January 2018: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/29285266/characterization-of-the-efficacies-of-osimertinib-and-nazartinib-against-cells-expressing-clinically-relevant-epidermal-growth-factor-receptor-mutations
#10
Keita Masuzawa, Hiroyuki Yasuda, Junko Hamamoto, Shigenari Nukaga, Toshiyuki Hirano, Ichiro Kawada, Katsuhiko Naoki, Kenzo Soejima, Tomoko Betsuyaku
Third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (EGFR-TKIs) were developed to overcome EGFR T790M-mediated resistance to first- and second-generation EGFR-TKIs. Third-generation EGFR-TKIs, such as osimertinib and nazartinib, are effective for patients with the EGFR T790M mutation. However, there are no direct comparison data to guide the selection of a third-generation EGFR-TKI for patients with different EGFR mutations. We previously established an in vitro model to estimate the therapeutic windows of EGFR-TKIs by comparing their relative efficacies against cells expressing mutant or wild type EGFRs...
December 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/29251017/synthesis-and-biological-evaluation-of-2-styrylquinolines-as-antitumour-agents-and-egfr-kinase-inhibitors-molecular-docking-study
#11
Magda A-A El-Sayed, Walaa M El-Husseiny, Naglaa I Abdel-Aziz, Adel S El-Azab, Hatem A Abuelizz, Alaa A-M Abdel-Aziz
A new series of 4,6-disubstituted 2-(4-(dimethylamino)styryl)quinoline 4a,b-9a,b was synthesized by the reaction of 2-(4-(dimethylamino)styryl)-6-substituted quinoline-4-carboxylic acids 3a,b with thiosemicarbazide, p-hydroxybenzaldehyde, ethylcyanoacetate, and 2,4-pentandione. In addition, the antitumour activity of all synthesized compounds 3a,b-9a,b was studied via MTT assay against two cancer cell lines (HepG2 and HCT116). Furthermore, epidermal growth factor receptor (EGFR) inhibition, using the most potent antitumour compounds, 3a, 3b, 4a, 4b, and 8a, was evaluated...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29250200/update-on-squamous-cell-carcinoma-of-the-head-and-neck-asco-annual-meeting-2017
#12
REVIEW
Teresa Magnes, Alexander Egle, Richard Greil, Thomas Melchardt
At the annual ASCO meeting clinically relevant data concerning the management of advanced head and neck cancer that will influence clinical practice in the future were presented. Chemoradiation with high-dose cisplatin remains the mainstay of treatment for patients with locally advanced squamous cell head and neck cancer. Adjuvant therapy with afatinib following chemoradiation failed to show clinical benefit. The combination of bevacizumab with platinum-based chemotherapy improved progression-free survival but did not lead to a significant difference in overall survival compared to chemotherapy alone...
2017: Memo
https://www.readbyqxmd.com/read/29237806/afatinib-is-a-new-therapeutic-approach-in-chordoma-with-a-unique-ability-to-target-egfr-and-brachyury
#13
Paola Magnaghi, Barbara Salom, Liviana Cozzi, Nadia Amboldi, Dario Ballinari, Elena Tamborini, Fabio Gasparri, Alessia Montagnoli, Laura Raddrizzani, Alessio Somaschini, Roberta Bosotti, Christian Orrenius, Fabio Bozzi, Silvana Pilotti, Arturo Galvani, Josh Sommer, Silvia Stacchiotti, Antonella Isacchi
Chordomas are rare bone tumors with no approved therapy. These tumors express several activated tyrosine kinase receptors, which prompted attempts to treat patients with tyrosine kinase inhibitors. Although clinical benefit was observed in Phase II clinical trials with imatinib and sorafenib, and sporadically also with EGFR inhibitors, therapies evaluated to date have shown modest activity. With the goal of identifying new drugs with immediate therapeutic potential for chordoma patients, we collected clinically approved drugs and other advanced inhibitors of MET, PDGFRβ and EGFR tyrosine kinases, and assessed their anti-proliferative activity against a panel of chordoma cell lines...
December 13, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/29237484/the-clinical-efficacy-of-afatinib-30%C3%A2-mg-daily-as-starting-dose-may-not-be-inferior-to-afatinib-40%C3%A2-mg-daily-in-patients-with-stage-iv-lung-adenocarcinoma-harboring-exon-19-or-exon-21-mutations
#14
Chih-Jen Yang, Ming-Ju Tsai, Jen-Yu Hung, Mei-Hsuan Lee, Ying-Ming Tsai, Yu-Chen Tsai, Jui-Feng Hsu, Ta-Chih Liu, Ming-Shyan Huang, Inn-Wen Chong
BACKGROUND: Afatinib is a second-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). Compared to cytotoxic chemotherapy, afatinib has been shown to have better efficacy in the treatment of non-small cell lung cancer harboring EGFR mutations. However, 40 mg daily as the initial dose is often accompanied by serious adverse drug reactions (ADRs) and 28 to 53.3% of patients required a dose reduction. No previous study has compared the clinical efficacy and ADRs of different initial doses (40 mg vs...
December 13, 2017: BMC Pharmacology & Toxicology
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
#15
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/29225480/role-of-afatinib-in-the-treatment-of-advanced-lung-squamous-cell-carcinoma
#16
REVIEW
Tiziana Vavalà
Lung cancer treatment has considerably changed over the last few years: the identification of druggable oncogenic alterations and innovative immunotherapic approaches granted lung cancer patients the possibility of more efficient and less toxic therapeutic options than chemotherapy. Nowadays, lung squamous cell carcinomas (SqCCs) patients have the chance to benefit from novel treatment alternatives, including immune checkpoint blockade and anti-angiogenic agents and, given positive trial results, from afatinib, a second generation tyrosine kinase inhibitor (TKI) that irreversibly antagonizes ErbB family tyrosine kinase receptors...
2017: Clinical Pharmacology: Advances and Applications
https://www.readbyqxmd.com/read/29225262/the-effectiveness-of-afatinib-in-a-patient-with-advanced-lung-adenocarcinoma-harboring-rare-g719x-and-s768i-mutations
#17
Masahiro Watanabe, Satoshi Oizumi, Shizuka Kiuchi, Noriyuki Yamada, Hiroshi Yokouchi, Shinichi Fukumoto, Masao Harada
The uncommon mutations in the EGFR (the epithelial growth factor receptor) gene include a heterogeneous group of genomic alterations within exons 18-21. The clinical response of patients with such mutations to EGFR tyrosine kinase inhibitor (EGFR-TKI) treatment, however, remains unclear. We herein report a case of advanced lung adenocarcinoma harboring complex exon 18 G719X (Gly719Xaa) and exon 20 S768I (Ser768Ile) mutations. The patient started to receive afatinib and has exhibited good response without progression for 12 months...
December 8, 2017: Internal Medicine
https://www.readbyqxmd.com/read/29220734/high-throughput-routine-determination-of-17-tyrosine-kinase-inhibitors-by-lc-ms-ms
#18
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
#19
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/29180936/osimertinib-effective-treatment-of-nsclc-with-activating-egfr-mutations-after-progression-on-egfr-tyrosine-kinase-inhibitors
#20
Marcin Skrzypski, Amelia Szymanowska-Narloch, Rafał Dziadziuszko
Non-small cell lung cancer (NSCLC) driven by activating mutations in epidermal growth factor receptor (EGFR) constitutes up to 10% of NSCLC cases. According to the NCCN recommendations, all patients (with the exception of smoking patients with squamous cell lung cancer) should be screened for the presence of activating EGFR mutations, i.e. deletion in exon 19 or point mutation L858R in exon 21, in order to select the group that benefits from EGFR tyrosine kinase inhibitors (EGFR TKIs) treatment. Among approved agents there are the 1st generation reversible EGFR TKIs, erlotinib and gefitinib, and the 2nd generation irreversible EGFR TKI, afatinib...
2017: Contemporary Oncology Współczesna Onkologia
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