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https://www.readbyqxmd.com/read/28544624/pyrimidine-containing-epidermal-growth-factor-receptor-kinase-inhibitors-synthesis-and-biological-evaluation
#1
Gaurav Joshi, Himanshu Nayyar, Sourav Kalra, Praveen Sharma, Anjana Munshi, Sandeep Singh, Raj Kumar
Structure based design and synthesis of pyrimidine containing reversible epidermal growth factor receptor (EGFR) inhibitors 1a-d are reported. The compounds (1a-d) inhibited the EGFR kinase activity in vitro with IC50 range 740 nM to 3 μM. mRNA expression of EGFR downstream target genes i.e. twist, c-fos and aurora were found to be altered upon treatment with compounds 1a-d. The compounds 1a-d exhibited excellent anticancer activity at low micromolar level (3.2-9 μM) in lung, colon and breast cancer cell lines...
May 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28541474/postmarketing-surveillance-study-of-erlotinib-plus-gemcitabine-for-pancreatic-cancer-in-japan-polaris-final-analysis
#2
Junji Furuse, Akihiko Gemma, Wataru Ichikawa, Takuji Okusaka, Akihiro Seki, Tadashi Ishii
Objective: Erlotinib plus gemcitabine is approved in Japan for the treatment of metastatic pancreatic cancer. The POLARIS surveillance study investigated safety (focusing on interstitial lung disease [ILD]) and efficacy of erlotinib plus gemcitabine in Japanese pancreatic cancer patients. Methods: Patients receiving erlotinib plus gemcitabine for pancreatic cancer in Japan between July 2011 and August 2012 were enrolled. ILD-like events were independently confirmed by a review committee...
May 24, 2017: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28538945/purpuric-drug-eruptions-caused-by-epidermal-growth-factor-receptor-inhibitors-for-non-small-cell-lung-cancer-a-clinicopathologic-study-of-32-cases
#3
Yung-Tsu Cho, Kai-Lung Chen, Yi-Shuan Sheen, Che-Wen Yang, Jau-Yu Liau, Yu-Pin Cheng, Chia-Yu Chu
Importance: Purpuric skin lesions have only rarely been reported in patients receiving epidermal growth factor receptor inhibitors. However, their clinical and histopathologic presentations have varied considerably. Objective: To characterize purpuric skin eruptions caused by epidermal growth factor receptor inhibitors. Design, Setting, and Participants: This prospective study enrolled 32 patients who presented to an integrated dermato-oncologic clinic in a tertiary referral medical center with purpuric skin lesions after using epidermal growth factor receptor inhibitors from January 1, 2013, through December 31, 2015...
May 24, 2017: JAMA Dermatology
https://www.readbyqxmd.com/read/28538407/unusual-jaw-metastasis-from-squamous-cell-lung-cancer-in-heavy-smoker-two-case-reports-and-review-of-the-literature
#4
Aldo Pezzuto, Michelangelo Morrone, Elidon Mici
RATIONALE: Jaw metastasis is a very rare condition associated with lung cancer evolution. In this paper we present two cases of patients who underwent different approach.Lung cancer is the leading cause of cancer related death worldwide. Survival depends on the staging and biology of tumor. Smoking may affect the prognosis. PATIENT CONCERNS: There are herein reported the cases of two patients affected by squamous cell lung cancer with spread to mandibular bone. DIAGNOSES: In the first case a computed tomography (CT scan) showed a large mass located in upper right lung , then bronchoscopy was performed with biopsies and the histology revealed a squamous cell carcinoma P63+ and TTF-...
May 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28538405/marked-response-to-nab-paclitaxel-in-egfr-mutated-lung-neuroendocrine-carcinoma-a-case-report
#5
Jin-Yan Liang, Fan Tong, Fei-Fei Gu, Yang-Yang Liu, Yu-Lan Zeng, Xiao-Hua Hong, Kai Zhang, Li Liu
RATIONALE: Lung cancer is the leading cause of cancer-related death in the world. Tyrosine kinase inhibitors (TKIs), which target mutated epidermal growth factor receptor (EGFR), have been the first-line treatment of late-stage lung adenocarcinoma harboring EGFR mutation. EGFR mutations are mostly identified in lung adenocarcinoma. However, it is rarely seen in lung neuroendocrine carcinoma, and treatment strategies remain under reported. PATIENT CONCERNS: Here, we describe a 54-year-old Chinese man diagnosed with lung adenocarcinoma (cT4N3M1b, stage IV) with neuroendocrine differentiation and L858R mutation on exon 21...
May 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28533646/image-findings-of-rare-case-of-peritoneal-carcinomatosis-from-non-small-cell-lung-cancer-and-response-to-erlotinib-in-f-18-fdg-positron-emission-tomography-computed-tomography
#6
Koramadai Karuppusamy Kamaleshwaran, Jephy Joseph, Radha Krishnan Kalarikal, Ajit Sugunan Shinto
Lung cancer is currently one of the most common malignancies in the world. Metastatic disease is observed in ~ 40% of patients with lung cancer, with the most common sites of metastasis being the bone, liver, brain and adrenal glands. Peritoneal carcinomatosis (PC) is defined as the progression of the primary cancer to the peritoneum. PC is a rare clinical event in lung cancer. Tyrosine kinase inhibitors targeting the epidermal growth factor receptor (EGFR), such as erlotinib are used for the treatment of patients with advanced non-small cell lung cancer (NSCLC)...
April 2017: Indian Journal of Nuclear Medicine: IJNM: the Official Journal of the Society of Nuclear Medicine, India
https://www.readbyqxmd.com/read/28530522/factors-associated-with-adherence-to-and-treatment-duration-of-erlotinib-among-patients-with-non-small-cell-lung-cancer
#7
Lisa M Hess, Anthony Louder, Katherine Winfree, Yajun E Zhu, Ana B Oton, Radhika Nair
BACKGROUND: In lung cancer, there is an increasing number of oral agents available for patients; however, little is known about the factors associated with adherence to and treatment duration on oral medications in non-small cell lung cancer (NSCLC). OBJECTIVE: To evaluate the clinical and demographic factors associated with adherence and treatment discontinuation, respectively, to oral oncolytics among patients with NSCLC. METHODS: A retrospective, claims-based analysis of the Humana Research Database supplemented with medical chart review was conducted among patients with NSCLC who started an oral oncolytic between January 1, 2008, and June 30, 2013...
June 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28529573/comparative-metabolomic-analysis-of-hpac-cells-following-the-acquisition-of-erlotinib-resistance
#8
Sooyeun Lee, Won-Jun Jang, Boyeon Choi, Sang Hoon Joo, Chul-Ho Jeong
Pancreatic cancer is one of the most lethal types of cancer, due to difficulty in early detection and the limited efficacy of available treatments. Erlotinib is used to inhibit the epidermal growth factor receptor for the treatment of pancreatic cancer; however, erlotinib resistance is a major issue and the mechanisms underlying the development of erlotinib resistance remain unclear. To better understand the alterations in tumor metabolism by acquired resistance to erlotinib, an erlotinib-resistant pancreatic cancer cell line (HPAC-ER) was established, followed by a comparison of the metabolic characteristics between these cells and their erlotinib-sensitive parental cells (HPAC)...
May 2017: Oncology Letters
https://www.readbyqxmd.com/read/28527899/egfr-mutation-analysis-for-prospective-patient-selection-in-two-phase-ii-registration-studies-of-osimertinib
#9
Suzanne Jenkins, James Chih-Hsin Yang, Pasi A Jänne, Kenneth S Thress, Karen Yu, Rachel Hodge, Susie Weston, Simon Dearden, Sabina Patel, Mireille Cantarini, Frances A Shepherd
INTRODUCTION: Osimertinib is an oral, CNS active, epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) for the treatment of EGFR T790M-positive advanced non-small cell lung cancer (NSCLC). Here we evaluate EGFR mutation frequencies in two Phase II studies of osimertinib (AURA extension and AURA2). METHODS: Patients with EGFR mutation-positive advanced NSCLC provided tumor samples following progression on their latest line of therapy for mandatory central T790M testing for study selection criteria...
May 17, 2017: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/28522592/sensitization-of-egfr-wild-type-non-small-cell-lung-cancer-cells-to-egfr-tyrosine-kinase-inhibitor-erlotinib
#10
Judith Raimbourg, Marie-Pierre Joalland, Mathilde Cabart, Ludmilla de Plater, Fanny Bouquet, Ariel Savina, Didier Decaudin, Jaafar Bennouna, François M Vallette, Lisenn Lalier
The benefit of EGFR-TKI in non-small cell lung cancer has been demonstrated in mutant EGFR tumors as first-line treatment but the benefit in wild-type EGFR tumors is marginal as well as restricted to maintenance therapy in pretreated patients. This work aimed at questioning the effects of cisplatin initial treatment on the EGFR pathway in non-small cell lung cancer and the functional consequences in vitro and in in vivo animal models of Patient-Derived Xenografts (PDX). We establish here that cisplatin pretreatment specifically sensitizes wild-type EGFR expressing cells to erlotinib, contrary to what happens in mutant-EGFR cells and with a blocking EGFR antibody, both in vitro and in vivo The sensitization entails the activation of the kinase Src upstream of EGFR, thereafter transactivating EGFR through a ligand-independent activation...
May 18, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28521433/effect-of-selective-small-molecule-inhibitors-on-mmp-9-and-vegfr-1-expression-in-p16-positive-and-negative-squamous-cell-carcinoma
#11
Benedikt Kramer, Johannes David Schultz, Clemens Hock, Alexander Sauter, Boris A Stuck, Karl Hörmann, Richard Birk, Christoph Aderhold
The identification of molecular targets in the therapy of human papilloma virus (HPV)-associated head and neck squamous cell carcinoma (HNSCC) is a primary aim of cancer research. Matrix metalloproteinase 9 (MMP-9) and vascular endothelial growth factor receptor (VEGFR) have important roles in the development of HNSCC. The tyrosine kinase inhibitors, nilotinib, dasatinib, erlotinib and gefitinib are well established in the targeted therapy of tumors other than HNSCC. The present study aimed to investigate the alteration of MMP-9 and VEGFR-1 expression patterns following treatment with these tyrosine kinase inhibitors in p16-positive and -negative squamous carcinoma cells...
May 2017: Oncology Letters
https://www.readbyqxmd.com/read/28521301/activation-of-signal-transducer-and-activator-of-transcription-3-stat3-signaling-in-egfr-mutant-non-small-cell-lung-cancer-nsclc
#12
Carles Codony-Servat, Jordi Codony-Servat, Niki Karachaliou, Miguel Angel Molina, Imane Chaib, Jose Luis Ramirez, Maria de Los Llanos Gil, Flavio Solca, Trever G Bivona, Rafael Rosell
Gefitinib, erlotinib or afatinib are the current treatment for non-small-cell lung cancer (NSCLC) harboring an activating mutation of the epidermal growth factor receptor (EGFR), but less than 5% of patients achieve a complete response and the median progression-free survival is no longer than 12 months. Early adaptive resistance can occur as soon as two hours after starting treatment by activating signal transducer and activation of transcription 3 (STAT3) signaling. We investigated the activation of STAT3 in a panel of gefitinib-sensitive EGFR mutant cell lines, and gefitinib-resistant PC9 cell lines developed in our laboratory...
May 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28515374/polyphyllin-i-overcomes-emt-associated%C3%A2-resistance%C3%A2-to-erlotinib-in-lung-cancer-cells-via-il-6-stat3-pathway-inhibition
#13
Wei Lou, Yan Chen, Ke-Ying Zhu, Huizi Deng, Tianhao Wu, Jun Wang
Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) is the most important limiting factor for treatment efficiency in EGFR-mutant non-small cell lung cancer (NSCLC). Much work has linked the epithelial-mesenchymal transition (EMT) to the emergence of drug resistance, consequently, ongoing research has been focused on exploring the therapeutic options to reverse EMT for delaying or preventing drug resistance. Polyphyllin I (PPI) is a natural compound isolated from Paris polyphylla rhizomes and displayed anti-cancer properties...
May 18, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28514740/differential-expression-of-circulating-biomarkers-of-tumor-phenotype-and-outcomes-in-previously-treated-non-small-cell-lung-cancer-patients-receiving-erlotinib-vs-cytotoxic-chemotherapy
#14
Mary Jo Fidler, Casey Frankenberger, Richard Seto, Gabriela C Lobato, Cristina L Fhied, Selina Sayidine, Sanjib Basu, Mark Pool, Reem Karmali, Marta Batus, Wen-Rong Lie, David Hayes, Jehangir Mistry, Philip Bonomi, Jeffrey A Borgia
BACKGROUND: The objective of this study was to identify serum biomarkers capable of predicting clinical outcomes in previously-treated NSCLC patients with wild-type for EGFR activating mutations or insufficient tissue for mutation status determination. METHODS: Sixty-six Luminex immunoassays representative of biological themes that emerged from a re-analysis of transcriptome data from the Cancer Genome Atlas (TCGA) were evaluate against pretreatment serum specimens from previously-treated advanced NSCLC patients received either cytotoxic chemotherapy (n=32) or erlotinib (n=79)...
April 28, 2017: Oncotarget
https://www.readbyqxmd.com/read/28513466/non-small-cell-lung-cancer-mutations-targeted-and-combination-therapy
#15
Justyna Kutkowska, Irena Porębska, Andrzej Rapak
Year after year, a growing number of cases of non-small cell lung cancer (NSCLC), mostly caused by smoking, have been noted. Most patients die because of the late detection of cancer and tumor resistance to treatment with cytostatics. Treatment of patients with advanced NSCLC is impeded by the low sensitivity of the tumor to cytostatic agents and the co-existence of many diseases, which substrate is, like lung cancer, cigarette smoking. Along with the development of molecular biology, targeted therapy has started to be used, affecting specific signaling pathways involved in the processes of oncogenesis...
May 17, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/28507201/sensitivity-of-non-small-cell-lung-cancer-to-erlotinib-is-regulated-by-the-notch-mir-223-fbxw7-pathway
#16
Haiwei Zhang, Fanglin Chen, Yongpeng He, Lin Yi, Chuang Ge, Xiaolong Shi, Chao Tang, Donglin Wang, Yongzhong Wu, Weiqi Nian
Recent evidence supports a role for microRNA-223 (miR-223) in modulating tumor cell sensitivity to chemotherapeutic drugs; however, its role in cellular resistance to the effects of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) used in treatment of non-small cell lung cancer (NSCLC) remains to be elucidated. The levels of miR-223 in parental cell line (HCC827) and erlotinib resistant HCC827 cell line (HCC827/ER)  were detected by qRT-PCR. HCC827/ER cells were treated with MK-2206 to block the Akt signaling pathway or RO4929097 to block the Notch signaling pathway, and then transfected with a miR-223 inhibitor or interference expression plasmid of F-Box/WD repeat-containing protein 7 (FBXW7) or insulin-like growth factor 1 receptor (IGF1R)...
May 15, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28506758/decreased-homodimerization-and-increased-timp-1-complexation-of-uteroplacental-and-uterine-arterial-matrix-metalloproteinase-9-during-hypertension-in-pregnancy
#17
Juanjuan Chen, Zongli Ren, Minglin Zhu, Raouf A Khalil
Preeclampsia is a complication of pregnancy manifested as hypertension-in-pregnancy (HTN-Preg) and often intrauterine growth restriction (IUGR). Placental ischemia could be an initiating event, but the molecular mechanisms are unclear. To test the hypothesis that dimerization of matrix metalloproteinases (MMPs) plays a role in HTN-Preg and IUGR, the levels/activity of MMP-9, tissue inhibitor of metalloproteinase (TIMP-1), and their dimerization forms were measured in the placenta, uterus, and uterine artery of normal pregnant (Preg) rats and a rat model of reduced uteroplacental perfusion pressure (RUPP)...
May 12, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28504890/a-brief-perspective-of-drug-resistance-toward-egfr-inhibitors-the-crystal-structures-of-egfrs-and-their-variants
#18
Haixing Guan, Yongli Du, Yang Ning, Xin Cao
The EGFR is one of the most popular targets for anticancer therapies and many drugs, such as erlotinib and gefitinib, have got enormous success in clinical treatments of cancer in past decade. However, the efficacy of these agents is often limited because of the quick emergence of drug resistance. Fundamental structure researches of EGFR in recent years have generally elucidated the mechanism of drug resistance. In this review, based on systematic resolution of full structures of EGFR and their variants via single crystal x-ray crystallography, the working and drug resistance mechanism of EGFR-targeted drugs are fully illustrated...
May 15, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28503420/oxidative-stress-affects-retinal-pigment-epithelial-cell-survival-through-epidermal-growth-factor-receptor-akt-signaling-pathway
#19
Xiao-Dong Chen, Ming-Yang Su, Tao-Tao Chen, Hai-Yan Hong, Ai-Dong Han, Wen-Sheng Li
AIM: To investigate the cross-talk between oxidative stress and the epidermal growth factor receptor (EGFR)/AKT signaling pathway in retinal pigment epithelial (RPE) cells. METHODS: Human RPE cell lines (ARPE-19 cell) were treated with different doses of epidermal growth factor (EGF) and hydrogen peroxide (H2O2). Cell viability was determined by a methyl thiazolyl tetrazolium assay. Cell proliferation was examined by a bromodeoxyuridine (BrdU) incorporation assay...
2017: International Journal of Ophthalmology
https://www.readbyqxmd.com/read/28503070/tyrosine-kinase-inhibitor-combination-therapy-in-first-line-treatment-of-non-small-cell-lung-cancer-systematic-review-and-network-meta-analysis
#20
Sarah Batson, Stephen A Mitchell, Ricarda Windisch, Elisabetta Damonte, Veronica C Munk, Noemi Reguart
INTRODUCTION: The introduction of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) has improved the outlook for patients with advanced non-small-cell lung cancer (NSCLC) with EGFR+ mutations. However, most patients develop resistance, with the result that median progression-free survival (PFS) iŝ12 months. Combining EGFR-TKIs with other agents, such as bevacizumab, is a promising approach to prolonging remission. This systematic review and network meta-analysis (NMA) were undertaken to assess available evidence regarding the benefits of first-line combination therapy involving EGFR-TKIs in patients with advanced NSCLC...
2017: OncoTargets and Therapy
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