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https://www.readbyqxmd.com/read/29234637/efficacy-and-safety-of-systemic-therapies-for-advanced-hepatocellular-carcinoma-a-network-meta-analysis-of-phase-iii-trials
#1
Alessandro Cucchetti, Fabio Piscaglia, Antonio Daniele Pinna, Benjamin Djulbegovic, Federico Mazzotti, Luigi Bolondi
Aim/Background: After the introduction of sorafenib in the treatment of advanced hepatocellular carcinoma (HCC), different studies tried to evaluate whether other systemic therapies can improve survival. To provide a comprehensive indirect treatment comparison of efficacy and safety of novel drugs, a network meta-analysis (NMA) of phase III randomized controlled trials was performed. Methods: After pertinent literature search up to November 1, 2016, 6 studies were eligible for the analysis including 4,812 individual patients with advanced HCC: 2,454 received sorafenib, 577 received brivanib, 530 received sunitinib, 514 received linifanib, 358 received sorafenib + erlotinib and 379 received placebo...
November 2017: Liver Cancer
https://www.readbyqxmd.com/read/29234062/development-of-erasin-a-chromone-based-stat3-inhibitor-which-induces-apoptosis-in-erlotinib-resistant-lung-cancer-cells
#2
Christian Lis, Stefan Rubner, Martin Roatsch, Angela Berg, Tyler Gilcrest, Darwin Fu, Elizabeth Nguyen, Anne-Marie Schmidt, Harald Krautscheid, Jens Meiler, Thorsten Berg
Inhibition of protein-protein interactions by small molecules offers tremendous opportunities for basic research and drug development. One of the fundamental challenges of this research field is the broad lack of available lead structures from nature. Here, we demonstrate that modifications of a chromone-based inhibitor of the Src homology 2 (SH2) domain of the transcription factor STAT5 confer inhibitory activity against STAT3. The binding mode of the most potent STAT3 inhibitor Erasin was analyzed by the investigation of structure-activity relationships, which was facilitated by chemical synthesis and biochemical activity analysis, in combination with molecular docking studies...
December 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29232766/combined-erlotinib-and-pf-03084014-treatment-contributes-to-synthetic-lethality-in-head-and-neck-squamous-cell-carcinoma
#3
Yang Zheng, Zhao Wang, Xu Ding, Yibo Dong, Wei Zhang, Wei Zhang, Yi Zhong, Wenyi Gu, Yunong Wu, Xiaomeng Song
OBJECTIVES: Head and neck squamous cell carcinoma (HNSCC) is characterized by high mortality and low survival rates. As an epidermal growth factor receptor (EGFR) inhibitor, Erlotinib has been approved for treatment of various tumours. PF-03084014 is a selective inhibitor of Notch1 signalling. This study aimed to explore new approaches for simultaneously targeting EGFR and Notch1 signalling to attenuate tumour growth and improve survival. MATERIALS AND METHODS: Cell proliferation was determined by CCK-8 assay and Flow cytometry...
December 12, 2017: Cell Proliferation
https://www.readbyqxmd.com/read/29228726/tyrosine-kinase-inhibitors-show-different-anti-brain-metastases-efficacy-in-nsclc-a-direct-comparative-analysis-of-icotinib-gefitinib-and-erlotinib-in-a-nude-mouse-model
#4
Jianlong Tan, Min Li, Wen Zhong, Chengping Hu, Qihua Gu, Yali Xie
Brain metastasis is an increasing problem in non-small cell lung cancer (NSCLC) patients. Tyrosine kinase inhibitors (TKIs), including gefitinib, erlotinib, and icotinib, are reported to be effective in patients with brain metastases. However, direct comparative studies of the pharmacokinetics and efficacy of these three drugs in treating brain metastases are lacking. In the present investigation, we found that gefitinib penetrated the blood-tumor barrier and was distributed to brain metastases more effectively than erlotinib or icotinib in a nude mouse model...
November 17, 2017: Oncotarget
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
#5
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/29222171/tankyrase-inhibition-enhances-the-anti-proliferative-effect-of-pi3k-and-egfr-inhibition-mutually-affecting-%C3%AE-catenin-and-akt-signaling-in-colorectal-cancer
#6
Nina T Solberg, Jo Waaler, Kaja Lund, Line Mygland, Petter A Olsen, Stefan Krauss
Over-activation of the WNT/β-catenin signaling axis is a common denominator in colorectal cancer (CRC). Currently there is no available WNT inhibitor in clinical practice. Although tankyrase inhibitors have been proposed as promising candidates there are many CRC models that do not respond positively to tankyrase inhibition in vitro and in vivo. Therefore, a combinatorial therapeutic approach combining a tankyrase inhibitor (G007-LK) with PI3K (BKM120) and EGFR (Erlotinib) inhibitors in CRC was investigated...
December 8, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/29222140/correction-to-td-19-an-erlotinib-derivative-induces-epidermal-growth-factor-receptor-wild-type-nonsmall-cell-lung-cancer-apoptosis-through-cip2a-mediated-pathway
#7
(no author information available yet)
No abstract text is available yet for this article.
January 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29221983/medication-related-osteonecrosis-of-the-jaws-associated-with-targeted-therapy-as-monotherapy-and-in-combination-with-antiresorptives-a-report-of-7-cases-from-the-copenhagen-cohort
#8
Hoda Abel Mahedi Mohamed, Charlotte Emilie Nor Nielsen, Morten Schiodt
OBJECTIVE: The aim of this study was to report cases of medication-related osteonecrosis of the jaws (MRONJ) associated with targeted therapy (TT) with or without concomitant antiresorptive treatment, among the Copenhagen ONJ cohort, which includes all consecutive cases of MRONJ seen in Copenhagen. STUDY DESIGN: We retrospectively studied the treatment of 204 consecutive patients with MRONJ, seen between January 2010 and May 2016, to identify those associated with TT...
November 6, 2017: Oral Surgery, Oral Medicine, Oral Pathology and Oral Radiology
https://www.readbyqxmd.com/read/29221754/up-regulation-of-ypel1-and-ypel5-and-down-regulation-of-itga2-in-erlotinib-treated-egfr-mutant-non-small-cell-lung-cancer-a-bioinformatic-analysis
#9
Xiaoli Wu
PURPOSE: This study aimed to identify genes with significant alteration following treatment of epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer (NSCLC) with tyrosine kinase inhibitors (TKIs). METHODS: We downloaded microarray data of GSE67051 from the Gene Expression Omnibus (GEO) database. Genes with differential expression were identified in two groups: erlotinib-treated versus DMSO-treated PC9 cells and erlotinib-treated versus DMSO-treated HCC827 cells...
December 5, 2017: Gene
https://www.readbyqxmd.com/read/29220734/high-throughput-routine-determination-of-17-tyrosine-kinase-inhibitors-by-lc-ms-ms
#10
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/29217088/induction-cisplatin-docetaxel-followed-by-surgery-and-erlotinib-in-non-small-cell-lung-cancer
#11
Tina Cascone, Kathryn A Gold, Stephen G Swisher, Diane D Liu, Frank V Fossella, Boris Sepesi, Apar Pataer, Annikka Weissferdt, Neda Kalhor, Ara A Vaporciyan, Wayne L Hofstetter, Ignacio I Wistuba, John V Heymach, Edward S Kim, William N William
BACKGROUND: Data from meta-analyses support the use of induction or adjuvant platinum-based chemotherapy for locally advanced non-small cell lung cancers (NSCLCs). This phase 2 study assessed the role of induction cisplatin and docetaxel followed by surgery in patients with resectable stage I to III NSCLCs, followed by 12 months of adjuvant erlotinib. METHODS: Patients with resectable stage I to III NSCLCs received cisplatin 80 mg/m2, docetaxel 75 mg/m2 every 21 days for 3 cycles, followed by surgery, followed by adjuvant erlotinib for 12 months...
December 4, 2017: Annals of Thoracic Surgery
https://www.readbyqxmd.com/read/29204173/synthesis-characterization-cytotoxic-screening-and-density-functional-theory-studies-of-new-derivatives-of-quinazolin-4-3h-one-schiff-bases
#12
Rezvan Rezaee Nasab, Farshid Hassanzadeh, Ghadam Ali Khodarahmi, Mahmoud Mirzaei, Mahboubeh Rostami, Ali Jahanian-Najaf Abadi
A series of novel derivatives of quinazolinone Schiff bases were synthesized from benzoic acid starting material and evaluated for potential cytotoxic activities against the human breast adenocarcinoma (MCF-7) and the human colon adenocarcinoma (HT-29) cell lines. Compared to the reference drug, these compounds showed good cytotoxic activities against studied cell lines especially compounds 4d and 4e. The ground-state geometries of these compounds (4a-g) were optimized at the B3LYP/6-31G* density functional theory (DFT) level...
December 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29199650/tuberculosis-in-epidermal-growth-factor-receptor-mutation-in-lung-adenocarcinoma-on-treatment-with-gefitinib-erlotinib
#13
EDITORIAL
D Gothi, S Spalgais
No abstract text is available yet for this article.
January 2017: Indian Journal of Cancer
https://www.readbyqxmd.com/read/29196706/maldi-mass-spectrometry-imaging-of-erlotinib-administered-in-combination-with-bevacizumab-in-xenograft-mice-bearing-b901l-egfr-mutated-nsclc-cells
#14
Masanobu Nishidate, Kaname Yamamoto, Chinami Masuda, Hiroaki Aikawa, Mitsuhiro Hayashi, Takehiko Kawanishi, Akinobu Hamada
Combination therapy of erlotinib plus bevacizumab improves progression-free survival of patients with epidermal growth factor receptor-mutated (EGFR-mutated) advanced non-small-cell lung cancer (NSCLC) compared with erlotinib alone. Although improved delivery and distribution of erlotinib to tumours as a result of the normalization of microvessels by bevacizumab is thought to be one of the underlying mechanisms, there is insufficient supporting evidence. B901L cells derived from EGFR-mutated NSCLC were subcutaneously implanted into mice, and mice were treated with bevacizumab or human IgG followed by treatment with erlotinib...
December 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29194843/discovery-of-potent-egfr-inhibitors-through-the-incorporation-of-a-3d-aromatic-boron-rich-cluster-into-the-4-anilinoquinazoline-scaffold-potential-drugs-for-glioma-treatment
#15
Hugo Eduardo Cerecetto
New 1,7-closo-carboranylanilinoquinazoline hybrids have been identified as EGFR inhibitors, one of them with higher affinity than the parent compound erlotinib. The comparative docking analysis with compounds bearing bioisoster-substructures, demonstrated the relevance of the 3D aromatic-boron-rich moiety for interacting into the EGFR ATP binding region. The capability to accumulate in glioma cells, the ability to cross the blood-brain barrier and the stability on simulated biological conditions, render these molecules as lead compounds for further structural modifications to obtain dual action drugs to treat glioblastoma...
November 30, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29193056/identification-of-a-novel-fusion-gene-hmga2-egfr-in-glioblastoma
#16
Akiyoshi Komuro, Erna Raja, Caname Iwata, Manabu Soda, Kazunobu Isogaya, Keiko Yuki, Yasushi Ino, Masato Morikawa, Tomoki Todo, Hiroyuki Aburatani, Hiromichi Suzuki, Melissa Ranjit, Atsushi Natsume, Akitake Mukasa, Nobuhito Saito, Hitoshi Okada, Hiroyuki Mano, Kohei Miyazono, Daizo Koinuma
Glioblastoma is one of the most malignant forms of cancer, for which no effective targeted therapy has been found. Although the Cancer Genome Atlas (TCGA) has provided a list of fusion genes in glioblastoma, their role in progression of glioblastoma remains largely unknown. To search for novel fusion genes, we obtained RNA-seq data from TGS-01 human glioma-initiating cells, and identified a novel fusion gene (HMGA2-EGFR), encoding a protein comprising the N-terminal region of the high mobility group AT hook protein 2 (HMGA2) fused to the C-terminal region of epidermal growth factor receptor (EGFR), which retained the transmembrane and kinase domains of the EGFR...
November 29, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/29190951/multi-omics-analysis-reveals-that-ornithine-decarboxylase-contributes-to-erlotinib-resistance-in-pancreatic-cancer-cells
#17
Won-Jun Jang, Boyeon Choi, Sang-Hoon Song, Naeun Lee, Dong-Joon Kim, Sooyeun Lee, Chul-Ho Jeong
Molecular and metabolic alterations in cancer cells are one of the leading causes of acquired resistance to chemotherapeutics. In this study, we explored an experimental strategy to identify which of these alterations can induce erlotinib resistance in human pancreatic cancer. Using genetically matched erlotinib-sensitive (BxPC-3) and erlotinib-resistant (BxPC-3ER) pancreatic cancer cells, we conducted a multi-omics analysis of metabolomes and transcriptomes in these cells. Untargeted and targeted metabolomic analyses revealed significant changes in metabolic pathways involved in the regulation of polyamines, amino acids, and fatty acids...
November 3, 2017: Oncotarget
https://www.readbyqxmd.com/read/29183267/in-silico-evaluation-of-the-resistance-of-the-t790m-variant-of-epidermal-growth-factor-receptor-kinase-to-cancer-drug-erlotinib
#18
Inderpal Singh, Shashank Singh, Vijeshwar Verma, Vladimir N Uversky, Ratna Chandra
Epidermal growth factor receptor (EGFR) kinase is implicated in cancer development due to either overexpression or activation variants in its functional intracellular kinase domain. Threonine to Methionine (Thr 790 Met) is one such variant observed commonly in patients showing resistance to kinase inhibitor drug Erlotinib. Two mechanisms for resistance have been proposed (1) steric hindrance and (2) enhanced binding to ATP. In this study, we employed molecular dynamics simulations and studied both the mechanisms...
November 28, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29180936/osimertinib-effective-treatment-of-nsclc-with-activating-egfr-mutations-after-progression-on-egfr-tyrosine-kinase-inhibitors
#19
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
https://www.readbyqxmd.com/read/29175983/molecular-imaging-of-abcb1-abcg2-inhibition-at-the-human-blood-brain-barrier-using-elacridar-and-11c-erlotinib-pet
#20
Remy B Verheijen, Maqsood M Yaqub, Emilia Sawicki, Olaf van Tellingen, Adriaan A Lammertsma, Bastiaan Nuijen, Jan H M Schellens, Jos H Beijnen, Alwin D R Huitema, N Harry Hendrikse, Neeltje Steeghs
Transporters such as ABCB1 and ABCG2 limit the exposure of several anti-cancer drugs to the brain, leading to suboptimal treatment in the central nervous system. The purpose of this study was to investigate the effects of the ABCB1/ABCG2 inhibitor elacridar on erlotinib brain uptake using 11C-erlotinib PET. Methods: Elacridar and cold erlotinib were administered orally to wild type (WT) and Abcb1a/b;Abcg2 knockout mice. In addition, brain uptake was measured using 11C-erlotinib imaging and ex vivo scintillation counting in knockout and WT mice...
November 24, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
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