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https://www.readbyqxmd.com/read/27920501/three-generations-of-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitors-developed-to-revolutionize-the-therapy-of-lung-cancer
#1
REVIEW
Haijun Zhang
Lung cancer, ~80%-85% of which is non-small-cell lung cancer (NSCLC), is the leading cause of cancer-related mortality worldwide. Sensitizing mutations in epidermal growth factor receptor (EGFR) gene (EGFRm(+)), such as exon 19 deletions and exon 21 L858R point mutations, are the most important drivers in NSCLC patients. In this respect, small-molecule EGFR tyrosine kinase inhibitors (TKIs) have been designed and developed, which launched the era of targeted, personalized and precise medicine for lung cancer...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27913578/characterization-of-egfr-t790m-l792f-and-c797s-mutations-as-mechanisms-of-acquired-resistance-to-afatinib-in-lung-cancer
#2
Yoshihisa Kobayashi, Koichi Azuma, Hiroki Nagai, Young Hak Kim, Yosuke Togashi, Yuichi Sesumi, Masato Chiba, Masaki Shimoji, Katsuaki Sato, Kenji Tomizawa, Toshiki Takemoto, Kazuto Nishio, Tetsuya Mitsudomi
Lung cancers harboring common EGFR mutations respond to EGFR tyrosine kinase inhibitors (TKIs). We previously reported that tumors with exon 18 mutations are particularly sensitive to irreversible second-generation (2G) afatinib compared with 1G-TKIs. However, data on the mechanisms of acquired resistance to afatinib are limited. We established afatinib-resistant cells by transfecting Ba/F3 cells with common or exon 18 (G719A and Del18) mutations and subjecting them to chronic exposure to increasing concentrations of afatinib...
December 2, 2016: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/27912836/epidermal-growth-factor-receptor-mutated-advanced-non-small-cell-lung-cancer-a-changing-treatment-paradigm
#3
REVIEW
Suchita Pakkala, Suresh S Ramalingam
Activating mutations in the epidermal growth factor receptor (EGFR) are present in approximately 15% of US patients with lung adenocarcinoma. EGFR tyrosine kinase inhibitors are associated with high response rate and progression-free survival for patients with non-small cell lung cancer with this genotype. Gefitinib, erlotinib, and afatinib are the EGFR tyrosine kinase inhibitors that are presently in clinical use. Understanding resistance mechanisms has led to the identification of a secondary mutational target, T790M, in more than half of patients, for which osimertinib has been approved...
February 2017: Hematology/oncology Clinics of North America
https://www.readbyqxmd.com/read/27912760/update-on-recent-preclinical-and-clinical-studies-of-t790m-mutant-specific-irreversible-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitors
#4
REVIEW
Bin-Chi Liao, Chia-Chi Lin, Jih-Hsiang Lee, James Chih-Hsin Yang
The first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors (1/2G EGFR-TKIs) gefitinib, erlotinib, and afatinib have all been approved as standard first-line treatments for advanced EGFR mutation-positive non-small cell lung cancer. The third-generation (3G) EGFR-TKIs have been developed to overcome the EGFR T790M mutation, which is the most common mechanism of acquired resistance to 1/2G EGFR-TKI treatment. This resistance mutation develops in half of the patients who respond to 1/2G EGFR-TKI therapy...
December 3, 2016: Journal of Biomedical Science
https://www.readbyqxmd.com/read/27903463/her2-transmembrane-mutations-v659-g660-that-stabilize-homo-and-hetero-dimerization-are-rare-oncogenic-drivers-in-lung-adenocarcinoma-that-respond-to-afatinib
#5
Sai-Hong Ignatius Ou, Alexa B Schrock, Eduard V Bocharov, Samuel J Klempner, Carolina Kawamura Haddad, Gary Steinecker, Melissa Johnson, Barbara J Gitlitz, Jon Chung, Paulo V Campregher, Jeffrey S Ross, Philip J Stephens, Vincent A Miller, James H Suh, Siraj M Ali, Vamsidhar Velcheti
INTRODUCTION: HER2 transmembrane domain (TMD) mutations (HER2(V659E), HER2(G660D)) have previously been identified in lung adenocarcinomas, but their frequency and clinical significance is unknown. METHODS: We prospectively analyzed 8,551 consecutive lung adenocarcinomas using hybrid-capture based comprehensive genomic profiling (CGP) at the request of the individual treating physicians for the purpose of making therapy decisions. RESULTS: We identified 15 cases (0...
November 26, 2016: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/27902463/novel-multi-targeted-erbb-family-inhibitor-afatinib-blocks-egf-induced-signaling-and-induces-apoptosis-in-neuroblastoma
#6
Xinfang Mao, Zhenghu Chen, Yanling Zhao, Yang Yu, Shan Guan, Sarah E Woodfield, Sanjeev A Vasudevan, Ling Tao, Jonathan C Pang, Jiaxiong Lu, Huiyuan Zhang, Fuchun Zhang, Jianhua Yang
Neuroblastoma is the most common extracranial solid tumor in children. The ErbB family of proteins is a group of receptor tyrosine kinases that promote the progression of various malignant cancers including neuroblastoma. Thus, targeting them with small molecule inhibitors is a promising strategy for neuroblastoma therapy. In this study, we investigated the anti-tumor effect of afatinib, an irreversible inhibitor of members of the ErbB family, on neuroblastoma. We found that afatinib suppressed the proliferation and colony formation ability of neuroblastoma cell lines in a dose-dependent manner...
November 26, 2016: Oncotarget
https://www.readbyqxmd.com/read/27900441/successful-afatinib-treatment-of-advanced-non-small-cell-lung-cancer-patients-undergoing-hemodialysis
#7
Hisao Imai, Kyoichi Kaira, Ichiro Naruse, Hideki Hayashi, Hirotoshi Iihara, Yutaro Kita, Naoki Mizusaki, Takayuki Asao, Yoshinori Itoh, Tadashi Sugiyama, Koichi Minato, Masanobu Yamada
The treatment for patients with lung cancer undergoing hemodialysis, who are frequently elderly and have poor performance status, becomes a more important subject. However, the feasibility of afatinib in patients with chronic renal failure undergoing hemodialysis has not, so far, been reported. Here, afatinib was administered to three patients with NSCLC harboring EGFR mutation and chronic renal failure undergoing hemodialysis. Pharmacokinetic (PK) data of afatinib supported the safety of afatinib treatment...
November 29, 2016: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/27900074/afatinib-induced-acute-fatal-pneumonitis-in-metastatic-lung-adenocarcinoma
#8
Sang Hoon Yoo, Jin Ah Ryu, Seo Ree Kim, Su Yun Oh, Gu Sung Jung, Dong Jae Lee, Bong Gyu Kwak, Yu Hyun Nam, Kyung Hyun Kim, Young Jun Yang
Afatinib is an oral tyrosine kinase inhibitor (TKI) that inhibit Endothelial Growth Factor Receptor (EGFR), Human Epidermal Growth Factor Receptor 2 (HER2), and HER4. The common side effects of EGFR TKI are rash, acne, diarrhea, stomatitis, pruritus, nausea, and loss of appetite. Drug induced pneumonitis is the less common adverse effects of EGFR TKI. Afatinib, 2nd generation EGFR TKI is anticipated to overcome drug resistance from 1st generation EGFR TKI according to preclinical study, and several studies are being conducted to compare clinical efficacy between 1st and 2nd EGFR TKI...
November 2016: Korean Journal of Family Medicine
https://www.readbyqxmd.com/read/27898252/advanced-non-small-cell-lung-cancer-nsclc-with-activating-egfr-mutations-first-line-treatment-with-afatinib-and-other-egfr-tkis
#9
Wolfgang Brückl, Amanda Tufman, Rudolf Maria Huber
Based on the results of several randomised controlled trials, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have now replaced platinum-based chemotherapy as first-line therapy for advanced non-small cell lung cancer (NSCLC) harboring an activating EGFR mutation. Areas covered: This review describes the EGFR pathway and its abnormalities in NSCLC and discusses the differential molecular and clinical activity of first and next-generation EGFR TKIs in the first-line treatment of tumors with an activating EGFR mutation, with a special focus on the second-generation agent afatinib...
November 29, 2016: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/27886859/tolerability-and-efficacy-of-afatinib-at-a-low-starting-dosage-in-10-elderly-or-low-performance-status-patients-with-advanced-refractory-non-small-cell-lung-cancer
#10
Kosuke Kashiwabara, Hiroshi Semba, Shinji Fujii, Shinsuke Tsumura
BACKGROUND: Whether a full dosage of afatinib is tolerable and effective for elderly or low performance status (PS) patients with advanced refractory non-small-cell lung cancer (NSCLC) is unclear. METHODS: We retrospectively evaluated the tolerability and efficacy of afatinib in 10 patients (the majority elderly) with a low PS score (2 or 3), who had advanced refractory adenocarcinoma and were carrying active epidermal growth factor receptor mutations. Afatinib was administered at a starting dosage of 20 or 30mg/day, followed by 10mg increases in dose up to a maximum dosage of 40mg/day...
November 2016: Respiratory Investigation
https://www.readbyqxmd.com/read/27886858/clinical-analysis-of-patients-treated-with-afatinib-for-advanced-non-small-cell-lung-cancer-a-nagano-lung-cancer-research-group-observational-study
#11
Yosuke Wada, Shigeru Koyama, Hiroshi Kuraishi, Takashige Miyahara, Fumiaki Yoshiike, Toshihiko Agatsuma, Ryouhei Yamamoto, Yasushi Ono, Toshiro Suzuki, Tsutomu Hachiya, Daisuke Gomi, Kazunari Tateishi, Masayuki Hanaoka, Tomonobu Koizumi
BACKGROUND: Afatinib has been available in Japan for the treatment of epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC) since May 2014. We conducted an observational study in patients treated with afatinib in Nagano prefecture, focusing on response and associated toxicities. METHODS: We analyzed the clinical records of NSCLC patients treated with afatinib between May 2014 and February 2015. RESULTS: The records of a total of 73 patients (27 men, 46 women) with a median age of 69 years (range: 42-85 years) were analyzed...
November 2016: Respiratory Investigation
https://www.readbyqxmd.com/read/27873136/afatinib-a-review-in-advanced-non-small-cell-lung-cancer
#12
REVIEW
Gillian M Keating
Afatinib (Giotrif(®), Gilotrif(®)) is an orally administered, irreversible inhibitor of the ErbB family of tyrosine kinases. In the first-line treatment of patients with advanced lung adenocarcinoma with activating epidermal growth factor receptor (EGFR) mutations, afatinib significantly prolonged progression-free survival (PFS) and time to treatment failure (TTF), but not overall survival (OS), compared with gefitinib (LUX-Lung 7 trial). In the overall population of patients receiving first-line treatment for advanced lung adenocarcinoma with activating EGFR mutations, afatinib significantly prolonged PFS, but not OS, compared with pemetrexed plus cisplatin (LUX-Lung 3 trial) or gemcitabine plus cisplatin (LUX-Lung 6 trial)...
November 22, 2016: Targeted Oncology
https://www.readbyqxmd.com/read/27872953/a-phase-i-study-of-afatinib-combined-with-paclitaxel-and-bevacizumab-in-patients-with-advanced-solid-tumors
#13
James Spicer, Sheeba Irshad, Joo Ern Ang, Deborah Enting, Rebecca Kristeleit, Martina Uttenreuther-Fischer, Karine Pemberton, Katy Pelling, David Schnell, Johann de Bono
PURPOSE: The combination of afatinib, an irreversible ErbB family blocker, with paclitaxel and bevacizumab was assessed in patients with advanced solid tumors. METHODS: This phase I study used a 3 + 3 design to determine the maximum tolerated dose (MTD) of afatinib combined with paclitaxel and bevacizumab. Safety, pharmacokinetics, and anti-tumor activity were also assessed. The starting dose was oral afatinib 40 mg once daily plus intravenous paclitaxel (fixed dose 80 mg/m(2), Days 1, 8, and 15 of a 4-week cycle) and intravenous bevacizumab 5 mg/kg every 2 weeks...
November 21, 2016: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/27867999/afatinib-plus-chemotherapy-versus-chemotherapy-alone-after-progression-on-afatinib-new-insights-on-old-question
#14
COMMENT
Priyanka Bhateja, Neelesh Sharma
No abstract text is available yet for this article.
October 2016: Annals of Translational Medicine
https://www.readbyqxmd.com/read/27863924/successful-use-of-afatinib-after-erlotinib-induced-pneumonitis-in-a-patient-with-epidermal-growth-factor-receptor-mutant-lung-cancer
#15
Christopher D Jakubowski, Andrew J Plodkowski, Jason C Chang, Natasha Rekhtman, Afsheen Iqbal, Paul K Paik, Helena A Yu
No abstract text is available yet for this article.
October 26, 2016: Clinical Lung Cancer
https://www.readbyqxmd.com/read/27835594/characterization-of-osimertinib-azd9291-resistant-non-small-cell-lung-cancer-nci-h1975-osir-cell-line
#16
Zheng-Hai Tang, Xiao-Ming Jiang, Xia Guo, Chi Man Vivienne Fong, Xiuping Chen, Jin-Jian Lu
Osimertinib (OSI, also known as AZD9291) is the newest FDA-approved epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor for non-small cell lung cancer (NSCLC) patients with EGFR T790M mutation. However, resistance to OSI is likely to progress and the study of potential OSI-resistant mechanisms in advanced is necessary. Here, the OSI-resistant NCI-H1975/OSIR cells were established. After cells developed resistance to OSI, cell proliferation was decreased while cell migration and invasion were increased...
November 7, 2016: Oncotarget
https://www.readbyqxmd.com/read/27831000/targeted-therapies-for-the-treatment-of-non-small-cell-lung-cancer-monoclonal-antibodies-and-biological-inhibitors
#17
Ana P S Silva, Priscila V Coelho, Maristella Anazetti, Patricia U Simioni
The usual treatments for patients with non-small-cell lung cancer (NSCLC), such as advanced lung adenocarcinoma, are unspecific and aggressive, and include lung resection, radiotherapy and chemotherapy. Recently, treatment with monoclonal antibodies and biological inhibitors has emerged as an effective alternative, generating effective results with few side effects. In recent years, several clinical trials using monoclonal antibodies presented potential benefits to NSCLC, and four of them are already approved for the treatment of NSCLC, such as cetuximab, bevacizumab, nivolumab and pembrolizumab...
November 10, 2016: Human Vaccines & Immunotherapeutics
https://www.readbyqxmd.com/read/27830967/the-european-society-for-medical-oncology-magnitude-of-clinical-benefit-scale-esmo-mcbs-applied-to-pivotal-phase-iii-randomized-controlled-trials-of-tyrosine-kinase-inhibitors-in-first-line-for-advanced-non-small-cell-lung-cancer-with-activating-epidermal-growth
#18
Jacopo Giuliani, Andrea Remo, Andrea Bonetti
To examine the magnitude of the clinical benefit from first-line tyrosine kinase inhibitors (TKIs) advanced non-small cell lung cancer (NSCLC) with activating epidermal growth factor receptor (EGFR)-mutations. Areas covered: The present evaluation was restricted to pivotal phase III RCTs in first-line for advanced NSCLC with activating EGFR-mutations. We have subsequently applied the European Society for Medical Oncology-Magnitude of Clinical Benefit Scale (ESMO-MCBS) to the above pivotal phase III RCTs, to derive a relative ranking of the magnitude of clinically meaningful benefit...
November 21, 2016: Expert Review of Pharmacoeconomics & Outcomes Research
https://www.readbyqxmd.com/read/27825109/her2-mutations-in-chinese-patients-with-non-small-cell-lung-cancer
#19
Zhengbo Song, Xinmin Yu, Zhiyong Shi, Jun Zhao, Yiping Zhang
BACKGROUND: ERBB2 (HER2) is a driver gene identified in non-small cell lung cancer (NSCLC). The prevalence, clinicopathology, genetic variability and treatment of HER2-positive NSCLC in Chinese population are unclear. PATIENTS AND METHODS: Eight hundred and fifty-nine patients with pathologically confirmed NSCLC were screened for HER2 mutations using Sanger sequencing. Next-generation sequencing (NGS) was performed in positive cases. HER2 amplification was detected with FISH...
August 16, 2016: Oncotarget
https://www.readbyqxmd.com/read/27821794/understanding-mechanisms-of-resistance-in-the-epithelial-growth-factor-receptor-in-non-small-cell-lung-cancer-and-the-role-of-biopsy-at-progression
#20
REVIEW
Mark A Socinski, Liza C Villaruz, Jeffrey Ross
: : Molecular profiling and the discovery of drugs that target specific activating mutations have allowed the personalization of treatment for non-small cell lung cancer (NSCLC). The epithelial growth factor receptor (EGFR) is frequently overexpressed and/or aberrantly activated in different cancers, including NSCLC. The most common activating mutations of EGFR in NSCLC fall within the tyrosine kinase-binding domain. Three oral EGFR tyrosine kinase inhibitors (TKIs) have been approved by the U...
November 7, 2016: Oncologist
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