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Erlotinib

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https://www.readbyqxmd.com/read/29051215/kinome-and-transcriptome-profiling-reveal-broad-and-distinct-activities-of-erlotinib-sunitinib-and-sorafenib-in-the-mouse-heart-and-suggest-cardiotoxicity-from-combined-signal-transducer-and-activator-of-transcription-and-epidermal-growth-factor-receptor-inhibition
#1
Timothy J Stuhlmiller, Jon S Zawistowski, Xin Chen, Noah Sciaky, Steven P Angus, Sean T Hicks, Traci L Parry, Wei Huang, Ju Youn Beak, Monte S Willis, Gary L Johnson, Brian C Jensen
BACKGROUND: Most novel cancer therapeutics target kinases that are essential to tumor survival. Some of these kinase inhibitors are associated with cardiotoxicity, whereas others appear to be cardiosafe. The basis for this distinction is unclear, as are the molecular effects of kinase inhibitors in the heart. METHODS AND RESULTS: We administered clinically relevant doses of sorafenib, sunitinib (cardiotoxic multitargeted kinase inhibitors), or erlotinib (a cardiosafe epidermal growth factor receptor inhibitor) to mice daily for 2 weeks...
October 19, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29050315/the-activation-of-src-family-kinases-and-focal-adhesion-kinase-with-the-loss-of-the-amplified-mutated-egfr-gene-contributes-to-the-resistance-to-afatinib-erlotinib-and-osimertinib-in-human-lung-cancer-cells
#2
Yuichi Murakami, Kahori Sonoda, Hideyuki Abe, Kosuke Watari, Daiki Kusakabe, Koichi Azuma, Akihiko Kawahara, Jun Akiba, Chitose Oneyama, Jonathan A Pachter, Kazuko Sakai, Kazuto Nishio, Michihiko Kuwano, Mayumi Ono
Second- and third-generation inhibitors of epidermal growth factor receptor (EGFR) tyrosine kinase activity (EGFR-TKIs) are improving the treatment of patients with non-small cell lung cancer. Here we established two sublines (BR1-8 and BR2-3) resistant to a second-generation inhibitor, afatinib, from the human lung cancer cell line HCC827 that harbors a mutation that activates the tyrosine kinase activity of EGFR. These afatinib-resistant sublines were resistant to first-generation EGFR-TKIs, gefitinib and erlotinib, and a third-generation EGFR-TKI, osimertinib...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29050231/a-phase-i-study-of-foretinib-plus-erlotinib-in-patients-with-previously-treated-advanced-non-small-cell-lung-cancer-canadian-cancer-trials-group-ind-196
#3
Natasha B Leighl, Ming-Sound Tsao, Geoffrey Liu, Dongsheng Tu, Cheryl Ho, Frances A Shepherd, Nevin Murray, John R Goffin, Garth Nicholas, Shingo Sakashita, Zhuo Chen, Lucia Kim, Jean Powers, Lesley Seymour, Glenwood Goss, Penelope A Bradbury
PURPOSE: MET and AXL mediate resistance to EGFR TKI in NSCLC. Foretinib, a MET/RON/AXL/TIE-2/VEGFR kinase inhibitor may overcome EGFR kinase resistance. This dose escalation study combined foretinib and erlotinib in advanced pretreated NSCLC patients. EXPERIMENTAL DESIGN: The primary endpoint was to define the RP2D of foretinib plus erlotinib as continuous oral daily dosing. Secondary objectives included safety, pharmacokinetics, response and potential biomarkers of response including EGFR, KRAS genotype, MET, AXL expression, and circulating HGF levels...
September 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29043496/erlotinib-plus-bevacizumab-phase-ll-study-in-patients-with-advanced-non-small-cell-lung-cancer-jo25567-updated-safety-results
#4
Terufumi Kato, Takashi Seto, Makoto Nishio, Koichi Goto, Noboru Yamamoto, Isamu Okamoto, Liang Tao, Wei Yu, Tarik Khaznadar, Kosei Tajima, Masahiko Shibata, Akihiro Seki, Nobuyuki Yamamoto
INTRODUCTION: The phase II JO25567 study compared the efficacy and safety of erlotinib plus bevacizumab vs. erlotinib alone as first-line therapy for advanced epidermal growth factor receptor (EGFR) mutation-positive non-small-cell lung cancer (NSCLC). OBJECTIVE: Our objective is to provide updated analyses of safety and the assessment of manageability of specific adverse events. METHODS: Patients with stage IIIB/IV or recurrent, non-squamous, EGFR mutation-positive NSCLC were randomized to receive erlotinib plus bevacizumab or erlotinib...
October 17, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/29041833/healthcare-costs-in-patients-with-advanced-non-small-cell-lung-cancer-and-disease-progression-during-targeted-therapy-a-real-world-observational-study
#5
Karen E Skinner, Ancilla W Fernandes, Mark S Walker, Melissa Pavilack, Ari VanderWalde
AIMS: To assess healthcare costs during treatment with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) and following disease progression in patients with advanced non-small cell lung cancer (NSCLC). METHODS: A retrospective analysis of medical records of US community oncology practices was conducted. Eligible patients had advanced NSCLC (stage IIIB/IV) diagnosed between January 1, 2008 and January 1, 2015, initiated treatment with erlotinib or afatinib (first-line or second-line), and had disease progression...
October 18, 2017: Journal of Medical Economics
https://www.readbyqxmd.com/read/29039585/identification-of-genome-variations-in-patients-with-lung-adenocarcinoma-using-whole-genome-re%C3%A2-sequencing
#6
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/29035827/ginsenoside-rg3-enhances-the-anti-proliferative-activity-of-erlotinib-in-pancreatic-cancer-cell-lines-by-downregulation-of-egfr-pi3k-akt-signaling-pathway
#7
Jin Jiang, Zuguo Yuan, Yiqing Sun, Yuan Bu, Wenfeng Li, Zhenghua Fei
Erlotinib has shown activity in the management of pancreatic cancer. However, the benefit of EGFR blockade is limited due to EGFR independent PI3K/Akt signaling pathway. Studies have reported that Ginsenoside Rg3 strongly inhibited PI3K-Akt signaling pathway of many carcinomas. We aimed to investigate the activity of Ginsenoside Rg3 to sensitize erlotinib in treating pancreatic cancer in vitro and in vivo. Human pancreatic cancer cell lines BxPC-3 and AsPC-1 were used. Cell proliferation and colony formation assay, Annexin V/PI apoptosis analysis, Western blot analysis, immunohistochemistry and in vivo study were carried out...
October 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031620/targeting-non-small-cell-lung-cancer-with-small-molecule-egfr-tyrosine-kinase-inhibitors
#8
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/29028534/discovery-of-benzo-g-quinazolin-benzenesulfonamide-derivatives-as-dual-egfr-her2-inhibitors
#9
Mansour S Alsaid, Abdullah A Al-Mishari, Aiten M Soliman, Fatma A Ragab, Mostafa M Ghorab
An array of some new N-(substituted)-2-((4-oxo-3-(4-sulfamoylphenyl)-3,4-dihydrobenzo[g]quinazolin-2-yl)thio)acetamide 5-19 were synthesized from the starting compound 4-(2-mercapto-4-oxobenzo[g]quinazolin-3(4H)-yl)benzenesulfonamide 4, to be assessed for their cytotoxic activity against A549 lung cancer cell line and to determine their inhibitory effect on EGFR tyrosine kinase enzyme. Compounds 5-19 showed high activity towards A549 cell line with IC50 values of 0.12-8.70 μM. Compounds 6, 12 and 18 were the most potent in this series...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29018350/folliculin-interacts-with-rab35-to-regulate-egf-induced-egfr-degradation
#10
Jianchao Zheng, Biao Duan, Shixiu Sun, Jie Cui, Jun Du, Yujie Zhang
Aims and Hypothesis: This study aims to investigate the mechanism involved in intracellular regulation of EGFR degradation induced by EGF. Methods: Phosphorylation of proteins related to EGFR signaling was examined by western blot analysis. Activation, connection between Rab35 and folliculin (FLCN) were assessed by pulldown, coimmunoprecipitation assays separately. The relationship between FLCN and cell growth was detected using gene overexpression and knock-down techniques. Results: Here, we demonstrate that interfering with FLCN, a tumor suppressor, reduces the rate of EGF-induced EGFR degradation, resulting in prolonged activation of downstream signaling...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28992288/erlotinib-attenuates-the-progression-of-chronic-kidney-disease-in-rats-with-remnant-kidney
#11
Yasutaka Yamamoto, Masayuki Iyoda, Shohei Tachibana, Kei Matsumoto, Yukihiro Wada, Taihei Suzuki, Ken Iseri, Tomohiro Saito, Kei Fukuda-Hihara, Takanori Shibata
Background: Increasing evidence indicates that epidermal growth factor receptor (EGFR) has a pathogenic role in renal fibrosis. Currently no effective treatment can completely halt the progression of chronic kidney disease (CKD). This study was undertaken to investigate the renoprotective effects of erlotinib, a tyrosine kinase inhibitor that can block EGFR activity in the progression of CKD and the mechanisms involved. Methods: Sprague Dawley rats with 5/6 nephrectomy were administered either erlotinib or vehicle from 2 weeks after surgery and for a period of 8 weeks...
September 7, 2017: Nephrology, Dialysis, Transplantation
https://www.readbyqxmd.com/read/28990119/dual-src-and-egfr-inhibition-in-combination-with-gemcitabine-in-advanced-pancreatic-cancer-phase-i-results-a-phase-i-clinical-trial
#12
Dana B Cardin, Laura W Goff, Emily Chan, Jennifer G Whisenant, G Dan Ayers, Naoko Takebe, Lori R Arlinghaus, Thomas E Yankeelov, Jordan Berlin, Nipun Merchant
Pancreatic adenocarcinoma remains a major therapeutic challenge, as the poor (<8%) 5-year survival rate has not improved over the last three decades. Our previous preclinical data showed cooperative attenuation of pancreatic tumor growth when dasatinib (Src inhibitor) was added to erlotinib (EGFR inhibitor) and gemcitabine. Thus, this study was designed to determine the maximum-tolerated dose of the triplet combination. Standard 3 + 3 dose escalation was used, starting with daily oral doses of 70 mg dasatinib and 100 mg erlotinib with gemcitabine on days 1, 8, and 15 (800 mg/m(2)) of a 28-day cycle (L0)...
October 9, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28989102/comparative-evaluation-of-electrospraying-and-lyophilization-techniques-on-solid-state-properties-of-erlotinib-nanocrystals-assessment-of-in-vitro-cytotoxicity
#13
Shreya Thakkar, Dilip Sharma, Manju Misra
INTRODUCTION: Erlotinib is a well known FDA approved drug from category of tyrosine kinase inhibitors; used for the treatment of lung cancer. However its use is limited because of its poor water solubility. OBJECTIVE: The aim of present work was to improve solubility by developing a stable nanocrystal based drug delivery system of ERL with the aid of sodium lauryl sulfate as potential stabilizer and to carry out comparative evaluation of electrospraying and lyophilization as solidification techniques on its solid state properties...
October 6, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28987609/structure-based-design-and-synthesis-of-2-4-diaminopyrimidines-as-egfr-l858r-t790m-selective-inhibitors-for-nsclc
#14
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/28984139/neurological-improvement-of-perineural-and-leptomeningeal-spread-of-squamous-cell-carcinoma-treated-with-intrathecal-chemotherapy-and-systemic-egfr-inhibition
#15
Vincent Alexander van Vugt, Marlon Garzo Saria, Andres Javier, Navin Kesari, Tiffany Turpin, Santosh Kesari
Squamous cell carcinoma (SCC) is a common cancer of the skin. Risk factors include fair skin, excessive sun and ultraviolet light exposure, and history of xeroderma pigmentosa. Perineural invasion (PNI), an uncommon manifestation of SCC, involves microscopic tumor cells invading various layers of the nerve sheath. It is associated with a poorer prognosis. Standard treatment for PNI includes radiation therapy. Here, we describe a case an older gentleman with a history of SCC with PNI successfully treated with erlotinib and intrathecal chemotherapy...
October 6, 2017: CNS Oncology
https://www.readbyqxmd.com/read/28979818/erlotinib-in-combination-with-bevacizumab-and-folfox4-as-second-line-chemotherapy-for-patients-with-metastatic-colorectal-cancer
#16
Sha Shi, Kemei Lu, Hui Gao, Huidong Sun, Senlin Li
BACKGROUND: We conducted a phase II study by combining FOLFOX4 plus bevacizumab (BV) with erlotinib (ER) as second-line chemotherapy for patients with metastatic colorectal cancer (mCRC). METHODS: Patients were divided into two groups in randomized double-blind manner. One group was given FOLFOX4 plus 5 mg/kg BV on day 1 of 2-week cycle. The other group was given 2-week-cycle of BV + FOLFOX4, and 100 mg ER every day. The primary endpoint was progression-free survival (PFS)...
2017: American Journal of Cancer Research
https://www.readbyqxmd.com/read/28979142/the-non-small-cell-lung-cancer-egfr-extracellular-domain-mutation-m277e-is-oncogenic-and-drug-sensitive
#17
Su Yu, Yang Zhang, Yunjian Pan, Chao Cheng, Yihua Sun, Haiquan Chen
PURPOSE: To identify novel oncogenic mutations in non-small cell lung cancer patient specimens that lack mutations in known targetable genes ("pan-negative" patients). METHODS: Comprehensive mutational analyses were performed on 1,356 lung adenocarcinoma specimens. In this cohort of patients, common lung cancer oncogenic driver mutations were detected in the epidermal growth factor receptor (EGFR) kinase domain, the human epidermal growth factor receptor 2 kinase domain, as well as the KRAS, BRAF, ALK, ROS1 and RET genes...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28978110/increased-pd-l1-expression-in-erlotinib-resistant-nsclc-cells-with-met-gene-amplification-is-reversed-upon-met-tki-treatment
#18
Christina Demuth, Morten Nørgaard Andersen, Kristine Raaby Jakobsen, Anne Tranberg Madsen, Boe Sandahl Sørensen
INTRODUCTION: Cancer cells can achieve immune evasion by expressing the programmed death receptor 1 ligand (PD-L1) on the cell surface. Blockade of the receptor (PD-1) can avert this evasion. Here we aim at investigating PD-L1 expression in erlotinib-resistant lung cancer cells with MET proto-oncogene (MET) gene amplification. MATERIALS AND METHODS: We employed an erlotinib-resistant NSCLC cell line with MET gene amplification. PD-L1 mRNA (qPCR) and protein (flow cytometry) expression was investigated after treatment with MET and mitogen-activated protein kinase (MAPK) targeting drugs (crizotinib and SCH772984, respectively)...
September 15, 2017: Oncotarget
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
#19
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/28974758/evaluation-of-the-heterogeneous-tissue-distribution-of-erlotinib-in-lung-cancer-using-matrix-assisted-laser-desorption-ionization-mass-spectrometry-imaging
#20
Yukari Tsubata, Mitsuhiro Hayashi, Ryosuke Tanino, Hiroaki Aikawa, Mayu Ohuchi, Kenji Tamura, Yasuhiro Fujiwara, Takeshi Isobe, Akinobu Hamada
Although drug distribution in tumor tissues has a significant impact on efficacy, conventional pharmacokinetic analysis has some limitations with regard to its ability to provide a comprehensive assessment of drug tissue distribution. Erlotinib is a tyrosine kinase inhibitor that acts on the epidermal growth factor receptor; however, it is unclear how this drug is histologically distributed in lung cancer. We used matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI) and liquid chromatography-tandem mass spectrometry (LC-MS/MS) to analyze erlotinib distribution in the tumor and normal lung tissues of a mouse xenograft model and patient with non-small cell lung cancer...
October 3, 2017: Scientific Reports
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