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https://www.readbyqxmd.com/read/29146616/therapeutic-potential-of-afatinib-for-cancers-with-erbb2-her2-transmembrane-domain-mutations-g660d-and-v659e
#1
Hiromasa Yamamoto, Shinichi Toyooka, Takashi Ninomiya, Shigemi Matsumoto, Masashi Kanai, Shuta Tomida, Katsuyuki Kiura, Manabu Muto, Ken Suzawa, Patrice Desmeules, Mark G Kris, Bob T Li, Marc Ladanyi
We previously reported on a family with hereditary lung cancer, in which a germline mutation in the transmembrane domain (G660D) of avian erythroblastic leukemia viral oncogene homolog 2 (erb-b2 receptor tyrosine kinase 2) (ERBB2; human epidermal growth factor receptor 2 [HER2]) seemed to be responsible for the cancer predisposition. Although few data are available on treatment, anti-ERBB2 therapeutic agents may be effective for ERBB2-mutant cancers. The familial lung cancer patient in one of the authors' institutes developed bone metastasis with enlarging lung tumors and was treated with the ERBB2 inhibitor afatinib...
November 16, 2017: Oncologist
https://www.readbyqxmd.com/read/29123418/evaluating-the-cost-effectiveness-of-afatinib-after-platinum-based-therapy-for-the-treatment-of-squamous-non-small-cell-lung-cancer-in-france
#2
Maud Pignata, Christos Chouaid, Katell Le Lay, Laura Luciani, Ceilidh McConnachie, James Gordon, Stéphane Roze
Background and aims: Lung cancer has the highest mortality rate of all cancers worldwide. Non-small-cell lung cancer (NSCLC) accounts for 85% of all lung cancers and has an extremely poor prognosis. Afatinib is an irreversible ErbB family blocker designed to suppress cellular signaling and inhibit cellular growth and is approved in Europe after platinum-based therapy for squamous NSCLC. The objective of the present analysis was to evaluate the cost-effectiveness of afatinib after platinum-based therapy for squamous NSCLC in France...
2017: ClinicoEconomics and Outcomes Research: CEOR
https://www.readbyqxmd.com/read/29123409/preventive-effect-of-kampo-medicine-hangeshashin-to-tj-14-plus-minocycline-against-afatinib-induced-diarrhea-and-skin-rash-in-patients-with-non-small-cell-lung-cancer
#3
Masao Ichiki, Hiroshi Wataya, Kazuhiko Yamada, Nobuko Tsuruta, Hiroaki Takeoka, Yusuke Okayama, Jun Sasaki, Tomoaki Hoshino
Purpose: Diarrhea and oral mucositis induced by afatinib can cause devastating quality of life issues for patients undergoing afatinib treatment. Several studies have shown that hangeshashin-to (TJ-14) might be useful for chemotherapy-induced diarrhea and oral mucositis. In this study, we investigated the prophylactic effects of TJ-14 for afatinib-induced diarrhea and oral mucositis and minocycline for afatinib-induced skin rash. Patients and methods: First- and second-generation epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors have become the standard first-line treatment in patients with EGFR-mutated non-small cell lung cancer...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29113230/squamous-cell-transformation-and-egfr-t790m-mutation-as-acquired-resistance-mechanisms-in-a-patient-with-lung-adenocarcinoma-treated-with-a-tyrosine-kinase-inhibitor-a-case-report
#4
Rossella Bruno, Agnese Proietti, Greta Alì, Gianfranco Puppo, Alessandro Ribechini, Antonio Chella, Gabriella Fontanini
The present case report describes the infrequent coexistence of squamous cell transformation and the epidermal growth factor receptor (EGFR) T790M mutation as resistance mechanisms to first line treatment with tyrosine kinase inhibitors. The patient was a 44-year-old female, diagnosed with a primitive advanced lung adenocarcinoma with bone metastases. The tumor was positive for the EGFR exon 19 deletion, therefore the patient was treated with afatinib (40 mg/day, orally) and radiotherapy for bone lesions. After 16 months, the patient developed resistance...
November 2017: Oncology Letters
https://www.readbyqxmd.com/read/29110849/continued-use-of-afatinib-with-the-addition-of-cetuximab-after-progression-on-afatinib-in-patients-with-egfr-mutation-positive-non-small-cell-lung-cancer-and-acquired-resistance-to-gefitinib-or-erlotinib
#5
Leora Horn, Scott Gettinger, D Ross Camidge, Egbert F Smit, Yelena Y Janjigian, Vincent A Miller, William Pao, Matthias Freiwald, Jean Fan, Bushi Wang, Vikram K Chand, Harry J M Groen
OBJECTIVES: In a phase Ib trial, afatinib plus cetuximab demonstrated promising clinical activity (objective response rate [ORR]: 29%; median progression-free survival [PFS]: 4.7 months) in patients with epidermal growth factor receptor (EGFR) mutation-positive non-small-cell lung cancer (NSCLC) with acquired resistance to erlotinib or gefitinib. Here, a separate cohort exploring afatinib plus cetuximab after progression on afatinib is reported. MATERIALS AND METHODS: Patients with EGFR mutation-positive NSCLC who progressed on erlotinib or gefitinib received afatinib 40mg daily until progression, followed by afatinib daily plus cetuximab 500mg/m(2) every 2 weeks until progression or intolerable adverse events (AEs)...
November 2017: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/29110836/next-generation-sequencing-reveals-novel-resistance-mechanisms-and-molecular-heterogeneity-in-egfr-mutant-non-small-cell-lung-cancer-with-acquired-resistance-to-egfr-tkis
#6
Choong-Kun Lee, Sora Kim, Jae Seok Lee, Jeong Eun Lee, Sung-Moo Kim, In Seok Yang, Hye Ryun Kim, Jeong Ho Lee, Sangwoo Kim, Byoung Chul Cho
OBJECTIVES: Despite initial responses to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in EGFR mutant non-small cell lung cancer, patients invariably develop acquired resistance. In this study, we performed next-generation sequencing in pre- and post-EGFR-TKI tumor samples to identify novel resistance mechanisms to EGFR-TKIs. MATERIAL AND METHODS: We collected tumor tissues before EGFR-TKI treatment and after progression from 19 NSCLC patients to analyze genomic alterations in 409 cancer related genes...
November 2017: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
https://www.readbyqxmd.com/read/29103264/suppressors-for-human-epidermal-growth-factor-receptor-2-4-her2-4-a-new-family-of-anti-toxoplasmic-agents-in-arpe-19-cells
#7
Yeong Hoon Kim, Lokraj Bhatt, Hye-Jin Ahn, Zhaoshou Yang, Won-Kyu Lee, Ho-Woo Nam
The effects of tyrosine kinase inhibitors (TKIs) were evaluated on growth inhibition of intracellular Toxoplasma gondii in host ARPE-19 cells. The number of tachyzoites per parasitophorous vacuolar membrane (PVM) was counted after treatment with TKIs. T. gondii protein expression was assessed by western blot. Immunofluorescence assay was performed using Programmed Cell Death 4 (PDCD4) and T. gondii GRA3 antibodies. The TKIs were divided into 3 groups; non-epidermal growth factor receptor (non-EGFR), anti-human EGFR 2 (anti-HER2), and anti-HER2/4 TKIs, respectively...
October 2017: Korean Journal of Parasitology
https://www.readbyqxmd.com/read/29095090/pharmacokinetic-drug-evaluation-of-osimertinib-for-the-treatment-of-non-small-cell-lung-cancer
#8
Antonio Rossi, Lucia Anna Muscarella, Concetta Di Micco, Cristiano Carbonelli, Vito D'alessandro, Stefano Notarangelo, Giuseppe Palomba, Gerardo Sanpaolo, Marco Taurchini, Paolo Graziano, Evaristo Maiello
First- and second-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib, erlotinib, icotinib, and afatinib are the standard-of-care for first-line therapy of non-small-cell lung cancer (NSCLC) harboring activating EGFR mutations. Unfortunately, after initial activity of an average 9-13 months, disease progression has been reported in the majority of patients. In about 50% of cases the progression is due to the onset of the T790M mutation in exon 20 of the EGFR gene...
November 12, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29073606/inhibitory-effect-of-afatinib-on-platelet-activation-and-apoptosis
#9
Hang Cao, Abdulla Al Mamun Bhuyan, Anja T Umbach, Rosi Bissinger, Meinrad Gawaz, Florian Lang
BACKGROUND/AIMS: The epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor afatinib is used for the treatment of several malignancies. Afatinib is at least partially effective by triggering apoptosis of tumor cells. Platelets may similarly undergo apoptosis, which is characterized by caspase 3 activation, cell shrinkage and phosphatidylserine translocation. However, an effect of afatinib on platelets has never been reported. The present study explored whether treatment of platelets with afatinib modifies platelet activation and apoptosis in the absence and presence of platelet activators thrombin or collagen related peptide (CRP)...
October 27, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29063709/pitfalls-in-diagnosis-with-the-use-of-circulating-tumor-derived-epidermal-growth-factor-receptor-mutations-in-lung-cancer-harboring-pretreatment-t790m
#10
Daiki Ogawara, Hiroshi Soda, Takayuki Suyama, Masataka Yoshida, Tatsuhiko Harada, Yuichi Fukuda, Hiroshi Mukae
The circulating tumor DNA (ctDNA) assay has recently been approved for the selection of EGFR-tyrosine kinase inhibitors as first-line treatment in lung cancer. However, it remains to be determined whether this assay can detect all complex EGFR mutations within a single tumor. We report a case of an elderly woman with stage IV lung adenocarcinoma, in which EGFR mutation assays detected L858R and pretreatment T790M from a tissue biopsy. In contrast, the circulating tumor DNA assay detected L858R, but not pretreatment T790M in the plasma, regardless of the fact that similar amounts of each mutation were present in the biopsy specimen...
October 24, 2017: Thoracic Cancer
https://www.readbyqxmd.com/read/29061656/synergistic-antiproliferative-activity-of-the-rad51-inhibitor-ibr2-with-inhibitors-of-receptor-tyrosine-kinases-and-microtubule-protein
#11
Peter J Ferguson, Mark D Vincent, James Koropatnick
Although cancer cell genetic instability contributes to characteristics that mediate tumorigenicity, it also contributes to the tumor-selective toxicity of some chemotherapy drugs. This "synthetic lethality" can be enhanced by inhibitors of DNA repair. To exploit this potential "Achilles heel", we tested the ability of a RAD51 inhibitor to potentiate the cytotoxicity of chemotherapy drugs. 2-(benzylsulfonyl)-1-(1H-indol-3-yl)-1,2-dihydroisoquinoline (IBR2) inhibits RAD51-mediated DNA double-strand break repair but also enhances cytotoxicity of the Bcr-Abl inhibitor imatinib...
October 23, 2017: Journal of Pharmacology and Experimental Therapeutics
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
#12
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/29041833/healthcare-costs-in-patients-with-advanced-non-small-cell-lung-cancer-and-disease-progression-during-targeted-therapy-a-real-world-observational-study
#13
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
#14
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...
December 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29034773/substrate-dependent-effects-of-molecular-targeted-anticancer-agents-on-activity-of-organic-anion-transporting-polypeptide-1b1
#15
Hiroyoshi Koide, Masayuki Tsujimoto, Ai Takeuchi, Miyu Tanaka, Yoko Ikegami, Mayu Tagami, Syoko Abe, Miki Hashimoto, Tetsuya Minegaki, Kohshi Nishiguchi
1. Organic anion-transporting polypeptide 1B1 (OATP1B1) plays an important role in the hepatic uptake of a broad range of substrate drugs. In vitro experiments show that molecular-targeted agents do not always have similar effects on OATP1B1 activity. 2. The purpose of this study was to clarify whether the effects of molecular-targeted agents on OATP1B1 are substrate-dependent. We used OATP1B1-transfected cells to compare the effects of molecular-targeted agents on OATP1B1-mediated uptake of fluorescein (FL), 2',7'-dichlorofluorescein (DCF), atorvastatin, SN-38, and valsartan...
October 16, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29031620/targeting-non-small-cell-lung-cancer-with-small-molecule-egfr-tyrosine-kinase-inhibitors
#16
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/29027754/afatinib-treatment-of-a-squamous-lung-cancer-after-tumor-progression-of-nivolumab
#17
Yinghua Jin, Qiuying Jiang, Tao Xin
Nivolumab prolonged disease control in a patient with advanced squamous lung cancer that was refractory to multiple treatments. The rapid eradication of cancer after the administration of nivolumab caused hemoptysis and repeated infection. Six months after immunotherapy, mediastinal lymph node metastasis developed and afatinib effectively relieved dysphonia associated with nerve paralysis.
October 13, 2017: Thoracic Cancer
https://www.readbyqxmd.com/read/28980030/-hyponatremia-in-a-58-year-old-female-patient-with-egfr-positive-lung-adenocarcinoma
#18
M Koch, K Utpatel, C Schulz
The case of a 58-year old female patient with epidermal growth factor-positive pulmonary adenocarcinoma treated with the tyrosine kinase inhibitor afatinib is reported. After several months of first-line therapy the patient developed severe hyponatremia and tumor reassessment revealed a progressive course of the lung cancer. Rebiopsy showed transformation of the tumor into small-cell lung cancer. Therapy with afatinib was stopped immediately and platin-based chemotherapy was started. This case shows that tumor transformation under tyrosine kinase inhibitor therapy from non-small-cell into small-cell lung cancer can occur in rare cases...
October 4, 2017: Der Internist
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/28969097/clinical-strategies-for-acquired-epidermal-growth-factor-receptor-tyrosine-kinase-inhibitor-resistance-in-non-small-cell-lung-cancer-patients
#20
REVIEW
Lijun Dong, Dan Lei, Haijun Zhang
Epidermal growth factor receptor (EGFR) mutations (EGFRm(+)) occur in 10-35% of non-small-cell lung cancer (NSCLC) cases and confer sensitivity to EGFR tyrosine kinase inhibitors (TKIs). EGFR TKIs are standard treatments for NSCLC patients harboring EGFR exon 19 deletions or exon 21 L858R point mutations. Despite initial benefit, most patients develop drug resistance, posing a challenge to oncologists. The secondary T790M point mutation in EGFR exon 20 contributes to approximately 60% of resistance cases. Optimum strategies for overcoming acquired EGFR TKI resistance are not clearly defined, although current common practice is to switch to platinum-based chemotherapy following resistance onset...
September 8, 2017: Oncotarget
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