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Erlotinib

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https://www.readbyqxmd.com/read/27909271/-epidermal-growth-factor-receptor-mutated-advanced-lung-adenocarcinoma-with-long-term-tumor-free-survival-by-chemotherapy-followed-by-tyrosine-kinase-inhibitor-treatment-after-reduction-surgery
#1
Atsushi Morio, Kazuki Nakahara, Toshirou Futagawa, Kenji Suzuki
A 67-year-old woman was detected stage III B adenocarcinoma of the left lung, with epidermal growth factor receptor(EGFR) -mutation. Since chest computed tomography showed enlarged lymph nodes in stations 7 and 1R-4R, radiochemotherapy was recommended. However, she declined radiochemotherapy and the chemotherapy after tumor reduction surgery was chosen. She underwent resection of the left lower lobe and lingular segment, and mediastinal lymph node dissection through a posterolateral thoracotomy by extended bronchoplasty(type C) due to the extranodal invasion of lymph nodes to the lingular segmental bronchus...
December 2016: Kyobu Geka. the Japanese Journal of Thoracic Surgery
https://www.readbyqxmd.com/read/27907909/egfr-kinase-inhibitors-and-gastric-acid-suppressants-in-egfr-mutant-nsclc-a-retrospective-database-analysis-of-potential-drug-interaction
#2
Nesaretnam Barr Kumarakulasinghe, Nicholas Syn, Yu Yang Soon, Atasha Asmat, Huili Zheng, En Yun Loy, Brendan Pang, Ross Andrew Soo
BACKGROUND: Erlotinib and gefitinib are weak base drugs whose absorption and clinical efficacy may be impaired by concomitant gastric acid suppressive (AS) therapy, yet proton pump inhibitors (PPIs) and histamine-2 receptor antagonists (H2As) are widely indicated in non-small cell lung cancer (NSCLC) patients for the prevention and treatment of erlotinib-induced gastrointestinal injury and corticosteroid-associated gastric irritation. We assessed the clinical relevance of this potential drug-drug interaction (DDI) in a retrospective cohort of EGFR-mutant NSCLC patients...
November 19, 2016: Oncotarget
https://www.readbyqxmd.com/read/27906420/the-effect-of-low-dosage-of-procaine-on-lung-cancer-cell-proliferation
#3
X-W Ma, Y Li, X-C Han, Q-Z Xin
OBJECTIVE: Non-small cell lung cancer (NSCLC) is the most common type of human lung cancer leading cause of cancer death worldwide. However, first-line drugs such as gefitinib and erlotinib showed great drug resistance in the clinical. MATERIALS AND METHODS: The cell proliferation was evaluated by MTT assay; gene expression was detected by qPCR assay. The protein expression was analyzed by Western blotting. RESULTS: Our results showed that in mouse models of lung cancer by A549 or NCI-H1975 xenograft, the local anesthetic drug Procaine (PCA) with 50 mg/kg specifically attenuated tumors compared with the vehicle-treated group...
November 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/27904686/fisetin-a-dietary-phytochemical-overcomes-erlotinib-resistance-of-lung-adenocarcinoma-cells-through-inhibition-of-mapk-and-akt-pathways
#4
Liang Zhang, Yi Huang, Wenlei Zhuo, Yi Zhu, Bo Zhu, Zhengtang Chen
Erlotinib (Tarceva) is a selective epidermal growth factor receptor tyrosine kinase inhibitor for treatment of non-small cell lung cancer (NSCLC). However, its efficacy is usually reduced by the occurrence of drug resistance. Our recent study showed that a flavonoid found in many plants, Fisetin, might have a potential to reverse the acquired Cisplatin-resistance of lung adenocarcinoma. In the present study, we aimed to test whether Fisetin could have the ability to reverse Erlotinib-resistance of lung cancer cells...
2016: American Journal of Translational Research
https://www.readbyqxmd.com/read/27900074/afatinib-induced-acute-fatal-pneumonitis-in-metastatic-lung-adenocarcinoma
#5
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/27899256/erlotinib-has-tumor-inhibitory-effect-in-human-retinoblastoma-cells
#6
Yi Shao, Yao Yu, Rongrong Zong, Luowa Quyang, Hui He, Qiong Zhou, Chonggang Pei
AIM: In this study, we explored the effect of erlotinib on the development of retinoblastoma (RB) cells both in vitro and in vivo. METHOD: RB cell lines, Y79 and WERI cells were treated with various concentrations of erlotinib in vitro to assess their cytotoxic profiles. In vitro proliferation, cell-cycle transition and migration were compared between RB cells treated with erlotinib and cells without erlotinib treatment. In in vivo tumorigenicity assay, mice were injected with Y79 cells and orally fed with erlotinib for 28days...
November 26, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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
#7
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/27895663/mir-30a-5p-overexpression-may-overcome-egfr-inhibitor-resistance-through-regulating-pi3k-akt-signaling-pathway-in-non-small-cell-lung-cancer-cell-lines
#8
Fei Meng, Fengfeng Wang, Lili Wang, S C Cesar Wong, William C S Cho, Lawrence W C Chan
Lung cancer is one of the most common deadly diseases worldwide, most of which is non-small cell lung cancer (NSCLC). The epidermal growth factor receptor (EGFR) mutant NSCLCs frequently respond to the EGFR tyrosine kinase inhibitors (EGFR-TKIs) treatment, such as Gefitinib and Erlotinib, but the development of acquired resistance limits the utility. Multiple resistance mechanisms have been explored, e.g., the activation of alternative tyrosine kinase receptors (TKRs) sharing similar downstream pathways to EGFR...
2016: Frontiers in Genetics
https://www.readbyqxmd.com/read/27894601/treatment-rationale-and-study-design-for-the-relay-study-a-multicenter-randomized-double-blind-study-of-erlotinib-with-ramucirumab-or-placebo-in-patients-with-epidermal-growth-factor-receptor-mutation-positive-metastatic-non-small-cell-lung-cancer
#9
Edward B Garon, Martin Reck, Luis Paz-Ares, Santiago Ponce, Jesus Corral Jaime, Oscar Juan, Ernest Nadal, Pablo Lee, Rita Dalal, Jingyi Liu, Shuang He, Joseph Treat, Kazuhiko Nakagawa
INTRODUCTION: We present the treatment rationale and study design for the RELAY study (NCT02411448 ). This phase Ib/III study will assess safety, tolerability, and efficacy of the combination of ramucirumab with erlotinib in previously untreated stage IV non-small-cell lung cancer patients with an activating epidermal growth factor receptor (EGFR) mutation. PATIENTS AND METHODS: The study is being conducted in approximately 120 sites in North America, Europe, and Asia and is currently open for enrollment...
June 8, 2016: Clinical Lung Cancer
https://www.readbyqxmd.com/read/27891677/staurosporine-scaffold-based-rational-discovery-of-the-wild-type-sparing-reversible-inhibitors-of-egfr-t790m-gatekeeper-mutant-in-lung-cancer-with-analog-sensitive-kinase-technology
#10
Xiaoyun Song, Xingcai Liu, Xi Ding
The human epidermal growth factor receptor (EGFR) has been established as an attractive target for lung cancer therapy. However, an acquired EGFR T790M gatekeeper mutation is frequently observed in patients treated with first-line anticancer agents such as gefitinib and erlotinib to cause drug resistance, largely limiting the application of small-molecule kinase inhibitors in EGFR-targeted chemotherapy. Previously, the reversible pan-kinase inhibitor staurosporine and its several analogs such as Gö6976 and K252a have been reported to selectively inhibit the EGFR T790M mutant (EGFR(T790M) ) over wild-type kinase (EGFR(WT) ), suggesting that the staurosporine scaffold is potentially to develop the wild-type sparing reversible inhibitors of EGFR(T790M) ...
November 28, 2016: Journal of Molecular Recognition: JMR
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
#11
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/27881453/cabozantinib-is-more-effective-than-erlotinib-in-egfr-wild-type-nsclc
#12
(no author information available yet)
Cabozantinib alone or in combination with erlotinib extended survival compared with erlotinib alone.
November 23, 2016: Cancer Discovery
https://www.readbyqxmd.com/read/27876230/intercalated-chemotherapy-and-epidermal-growth-factor-receptor-inhibitors-for-patients-with-advanced-non-small-cell-lung-cancer-a-systematic-review-and-meta-analysis
#13
REVIEW
Anna La Salvia, Antonio Rossi, Domenico Galetta, Elisa Gobbini, Emmanuele De Luca, Silvia Novello, Massimo Di Maio
Randomized clinical trials (RCTs) of concurrent epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) plus chemotherapy for unselected patients with advanced non-small-cell lung cancer (NSCLC) produced negative results. Intercalated administration could avoid the reduction of chemotherapy activity due to G1 cell-cycle arrest from EGFR-TKIs. A PubMed search was performed in December 2015 and updated in February 2016. The references from the selected studies were also checked to identify additional eligible trials...
October 28, 2016: Clinical Lung Cancer
https://www.readbyqxmd.com/read/27875304/rapid-renal-regulation-of-peroxisome-proliferator-activated-receptor-gamma-coactivator-1%C3%AE-by-extracellular-regulated-kinase-1-2-in-physiological-and-pathological-conditions
#14
Justin B Collier, Ryan M Whitaker, Scott T Eblen, Rick G Schnellmann
Previous studies have shown that extracellular regulated kinase 1/2 (ERK1/2) directly inhibits mitochondrial function during cellular injury. We evaluated the role of ERK1/2 on the expression of peroxisome proliferator-activated receptor gamma coactivator-1α (PGC-1α) gene, a master regulator of mitochondrial function. The potent and specific MEK1/2 inhibitor trametinib rapidly blocked ERK1/2 phosphorylation, decreased cytosolic and nuclear FOXO3a/1 phosphorylation, and increased PGC-1α gene expression and its downstream mitochondrial biogenesis (MB) targets under physiological conditions in the kidney cortex and in primary renal cell cultures...
November 14, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27873136/afatinib-a-review-in-advanced-non-small-cell-lung-cancer
#15
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/27871355/desquamative-dermatitis-caused-by-erlotinib-an-underreported-cutaneous-adverse-event
#16
Miriam L Vega, Natalie C Yin, Matthew Keller
No abstract text is available yet for this article.
2016: Skinmed
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
#17
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/27861317/development-and-validation-of-a-simultaneous-quantification-method-of-fourteen-tyrosine-kinase-inhibitors-in-human-plasma-using-lc-ms-ms
#18
Huu-Hien Huynh, Claire Pressiat, Hélène Sauvageon, Isabelle Madelaine, Patricia Maslanka, Céleste Lebbé, Catherine Thieblemont, Lauriane Goldwirt, Samia Mourah
BACKGROUND: A sensitive LC-MS/MS method for the analysis in a small volume of plasma of 14 tyrosine kinase inhibitors (TKIs) currently used (imatinib, dasatinib, ibrutinib, ponatinib, trametinib, sunitinib, cobimetinib, dabrafenib, erlotinib, lapatinib, nilotinib, bosutinib, sorafenib, and vemurafenib) has been developed and validated. This multi-analyte LC-MS/MS assay is of interest for anticancer drug combination therapy. METHODS: After a simple protein precipitation of plasma samples, the chromatographic separation was performed using a UPLC system coupled with MS/MS in a positive ionization mode...
November 16, 2016: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/27853997/a-phase-i-trial-investigating-pulsatile-erlotinib-in-combination-with-gemcitabine-and-oxaliplatin-in-advanced-biliary-tract-cancers
#19
Laura W Goff, Dana B Cardin, Jennifer G Whisenant, Liping Du, Tatsuki Koyama, Kimberly B Dahlman, Safia N Salaria, Ruth T Young, Kristen K Ciombor, Jill Gilbert, Stephen James Smith, Emily Chan, Jordan Berlin
Advanced biliary tract cancers (ABTC) are among the deadliest malignancies with limited treatment options after progression on standard-of-care chemotherapy, which includes gemcitabine (GEM) and oxaliplatin (OX). The epidermal growth factor receptor inhibitor erlotinib has been explored in ABTC with modest efficacy. Erlotinib given continuously may antagonize the action of chemotherapy against cycling tumor cells, but pulsatile dosing of erlotinib with chemotherapy may improve efficacy. The purpose of this study was to assess the safety of pulsatile erlotinib with GEMOX...
November 16, 2016: Investigational New Drugs
https://www.readbyqxmd.com/read/27851685/a-simple-high-performance-liquid-chromatography-for-determining-lapatinib-and-erlotinib-in-human-plasma
#20
Masahiro Ohgami, Masato Homma, Yoshiharu Suzuki, Kanako Naito, Motoko Yamada, Shoichi Mitsuhashi, Fumie Fujisawa, Hiroshi Kojima, Takayuki Kaburagi, Keiko Uchiumi, Yutaka Yamada, Hiroko Bando, Hisato Hara, Keiji Takei
BACKGROUND: Lapatinib and erlotinib are used for cancer treatment, showing large interindividual variability. Therapeutic drug monitoring may be useful for assessing the clinical outcomes and adverse events. A simple high-performance liquid chromatography UV method was developed for the determination of lapatinib and erlotinib in human plasma. METHODS: An aliquot of plasma sample spiked with internal standard was treated with acetonitrile to precipitate the proteins...
December 2016: Therapeutic Drug Monitoring
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