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Kwon-Yeon Weon, Min Gi Kim, Soyoung Shin, Tae Hwan Kim, Sang Hoon Joo, Eunsook Ma, Seok Won Jeong, Sun Dong Yoo, Yu Seok Youn, Beom Soo Shin
OBJECTIVE: To evaluate the potential pharmacokinetic interactions of the anticancer agent gefifitinib (Iressa®) and the oriental medications Guipi Decoction (, GPD, Guibi-tang in Korean) and Bawu Decoction (, BWD, Palmul-tang in Korean). METHODS: Methylcellulose (MC, control), GPD (1,200 mg/kg), or BWD (6,000 mg/kg) was orally administered to rats either as a single dose or multiple doses prior to gefitinib administration. To examine the effects of a single dose of the herbal medicines, gefifitinib (10 mg/kg) was orally administered after 5 min or 1 h of MC or the herbal medicine pretreatments...
January 15, 2018: Chinese Journal of Integrative Medicine
Jing Wang, Pengchao Hu, Ying Wang, Youhong Dong
PURPOSE: This study was designed to investigate the therapeutic effect of gefitinib in advanced non-small cell lung cancer (NSCLC) and its effect on the level of epidermal growth factor receptor (EGFR) in peripheral blood. METHODS: A total of 58 patients with NSCLC were treated with gefinitib (iressa) (250 mg per day). EGFR levels in the peripheral blood were measured with ELISA assay before and after treatment. Statistical analyses of patient quality of life, survival and other clinical data were conducted including logistic regression analysis, x2 test and t-test...
November 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
Tracey Gaspari, Iressa Spizzo, HongBin Liu, Yunshan Hu, Richard W Simpson, Robert E Widdop, Anthony E Dear
BACKGROUND: Sodium glucose transporter type 2 inhibitors may reduce cardiovascular events in type 2 diabetes. Our study aimed to determine the effect of the sodium glucose transporter type 2 inhibitor dapagliflozin on endothelial cell activation, vasoreactivity and atherogenesis using in vitro and in vivo models and identify associated molecular mechanisms. METHODS: In vitro studies utilised human vascular endothelial cells stimulated with tumour necrosis factor α or hyperglycaemic conditions...
October 1, 2017: Diabetes & Vascular Disease Research
Tony S K Mok, Sang-We Kim, Yi-Long Wu, Kazuhiko Nakagawa, Jin-Ji Yang, Myung-Ju Ahn, Jie Wang, James Chih-Hsin Yang, You Lu, Shinji Atagi, Santiago Ponce, Xiaojin Shi, Yuri Rukazenkov, Vincent Haddad, Kenneth S Thress, Jean-Charles Soria
Purpose The Iressa Mutation-Positive Multicentre Treatment Beyond ProgRESsion Study (IMPRESS) compared the continuation of gefitinib plus chemotherapy with placebo plus chemotherapy in patients with epidermal growth factor receptor ( EGFR) mutation-positive advanced non-small-cell lung cancer with progression (Response Evaluation Criteria in Solid Tumors 1.1) after first-line gefitinib. Primary results indicated no difference between treatments in terms of progression-free survival (PFS). The current analysis presents final, mature, overall survival (OS) data, together with exploratory analyses that examined whether specific biomarkers, including T790M mutation status, were able to differentiate a relative treatment effect...
October 2, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
Guan-Can Liang, Hao-Feng Zheng, Yan-Xiong Chen, Teng-Cheng Li, Wei Liu, You-Qiang Fang
OBJECTIVE: The mechanism underlying the therapeutic effects of combi-molecule JDF12 on prostate cancer (PCa) DU145 cells remains still unclear. This study aimed to investigate the proteomic profile after JDF12 treatment in DU145 cells by comparing with that in Iressa treated cells and untreated cells. METHODS: MTT was used to evaluate drug cytotoxicity, DAPI staining was done to assess apoptosis of cells, and flow cytometry was used to analyze cell cycle. iTRAQ and qPCR were employed to obtain the proteomic profiles of JDF12 treated, Iressa treated, and untreated DU145 cells, and validate the expression of selected differentially expressed proteins, respectively...
2017: American Journal of Translational Research
Kyoung Eun Lee, Eunsil Hahm, Seyeon Bae, Jae Seung Kang, Wang Jae Lee
Despite documentation of successful therapy with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in patients with lung cancer, the response rate of patients treated with this therapy remains low. The present study investigated whether L-ascorbic acid serves an adjuvant role in vitro when combined with the EGFR tyrosine kinase inhibitor gefitinib (Iressa(®)) in lung cancer cell lines. A total of three human lung cancer cell lines were used. The antiproliferative effects and changes in the cell cycle and expression of intracellular signaling molecules, including extracellular signal-regulated kinases (Erk), signal transducer and activator of transcription 3 (Stat3) and protein kinase B (Akt), were measured in cells treated with gefitinib and/or L-ascorbic acid at various concentrations...
July 2017: Oncology Letters
Hyun Chang, Ji Hea Sung, Sung Ung Moon, Han Soo Kim, Jin Won Kim, Jong Seok Lee
PURPOSE: Rearrangement of the proto-oncogene rearranged during transfection (RET) has been newly identified potential driver mutation in lung adenocarcinoma. Clinically available tyrosine kinase inhibitors (TKIs) target RET kinase activity, which suggests that patients with RET fusion genes may be treatable with a kinase inhibitor. Nevertheless, the mechanisms of resistance to these agents remain largely unknown. Thus, the present study aimed to determine whether epidermal growth factor (EGF) and hepatocyte growth factor (HGF) trigger RET inhibitor resistance in LC-2/ad cells with CCDC6-RET fusion genes...
January 2017: Yonsei Medical Journal
Lin Mu, Tianjiao Wang, Yanwei Chen, Xinqiang Tang, Yuhui Yuan, Yongshun Zhao
Glioblastoma multiforme (GBM) is the most common and severe form of primary tumor in the central nervous system of adults which has poor prognosis and limited therapeutic options. Epidermal growth factor receptor (EGFR) inhibitor, such as gefitinib (brand name Iressa, ZD1839), has been approved as a targeted medicine for several types of tumor including glioblastoma multiforme. However, gefitinib exerted very limited effects on some glioblastoma multiforme patients after a period of treatment due to intrinsic and acquired drug resistance...
October 2016: International Journal of Oncology
Xiaobo He, Yang Zhang, Yuxiang Ma, Ting Zhou, Jianwei Zhang, Shaodong Hong, Jin Sheng, Zhonghan Zhang, Yunpeng Yang, Yan Huang, Li Zhang, Hongyun Zhao
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are used as standard therapies for advanced nonsmall cell lung cancer (NSCLC) patients with EGFR mutation positive. Because these targeted therapies could cause tumor necrosis and shrinkage, the purpose of the study is to search for a value of optimal tumor shrinkage as an appropriate indicator of outcome for advanced NSCLC.A total of 88 NSCLC enrollees of 3 clinical trials (IRESSA registration clinical trial, TRUST study and ZD6474 study), who received Gefitinib (250 mg, QD), Erlotinib (150 mg, QD), and ZD6474 (100 mg, QD), respectively, during December 2003 and October 2007, were retrospectively analyzed...
August 2016: Medicine (Baltimore)
Can Zhao, Shu-Yan Han, Ping-Ping Li
Gefitinib (Iressa, AstraZeneca) has been widely used for the treatment of locally advanced or metastatic non-small cell lung cancer. A number of studies have been reported on its pharmacokinetics profiles, especially on the metabolism. In this review, we have comprehensively summarized the pharmacokinetic characteristics of gefitinib: absorption, distribution, metabolism and excretion (ADME). Overall, gefitinib reached the maximum plasma level relatively fast and distributed extensively. It underwent extensive biotransformation and predominantly excreted in feces, with less than 7% in the urine...
2017: Current Drug Delivery
Chien-Chang Huang, Cheng-Che Lee, Hsiao-Han Lin, Jang-Yang Chang
EGF-mediated EGFR endocytosis plays a crucial role in the attenuation of EGFR activation by sorting from early endosomes to late endosomes and transporting them into lysosomes for the final proteolytic degradation. We previously observed that cathepsin S (CTSS) inhibition induces tumour cell autophagy through the EGFR-mediated signalling pathway. In this study, we further clarified the relationship between CTSS activities and EGFR signalling regulation. Our results revealed that CTSS can regulate EGFR signalling by facilitating EGF-mediated EGFR degradation...
2016: Scientific Reports
Manisha Yadav, Abhishek Kumar Singh, Harish Kumar, Geeta Rao, Bandana Chakravarti, Anagha Gurjar, Shalini Dogra, Sapana Kushwaha, Achchhe Lal Vishwakarma, Prem Narayan Yadav, Dipak Datta, Anil Kumar Tripathi, Naibedya Chattopadhyay, Arun Kumar Trivedi, Sabyasachi Sanyal
BACKGROUND: Epidermal growth factor receptor (EGFR) inhibitor gefitinib (Iressa) is used for treating non-small cell lung cancer. Gefitinib also induces differentiation in acute myeloid leukemia (AML) cell lines and patient samples lacking EGFR by an unknown mechanism. Here we dissected the mechanism of gefitinib action responsible for its EGFR-independent effects. METHODS: Signaling events were analyzed by homogenous time-resolved fluorescence and immunoblotting...
October 2016: Biochimica et Biophysica Acta
Mikkel Staberg, Signe Regner Michaelsen, Louise Stobbe Olsen, Mette Kjølhede Nedergaard, Mette Villingshøj, Marie-Thérése Stockhausen, Petra Hamerlik, Hans Skovgaard Poulsen
BACKGROUND: For Glioblastoma (GBM) patients, a number of anti-neoplastic strategies using specifically targeting drugs have been tested; however, the effects on survival have been limited. One explanation could be treatment resistance due to redundant signaling pathways, which substantiates the need for combination therapies. In GBM, both the epidermal growth factor receptor (EGFR) and the notch signaling pathways are often deregulated and linked to cellular growth, invasion and angiogenesis...
2016: Cancer Cell International
Dickran Kazandjian, Gideon M Blumenthal, Weishi Yuan, Kun He, Patricia Keegan, Richard Pazdur
On July 13, 2015, the FDA approved gefitinib (Iressa; AstraZeneca UK Limited) for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test. Concurrently, a labeling expansion of the therascreen EGFR RGQ PCR Kit (Qiagen) as a companion diagnostic test was approved. The approval was based on the results of a multicenter, single-arm, open-label clinical study of 106 treatment-naïve patients with metastatic EGFR mutation-positive NSCLC who received gefitinib, 250 mg daily, until disease progression or intolerable toxicity...
March 15, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Aby Joiakim, Patricia A Mathieu, Catherine Shelp, Julie Boerner, John J Reiners
CYP1A1 and CYP1A2 are transcriptionally activated in the human normal breast epithelial cell line MCF10A following exposure to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). Shifting MCF10A cultures to medium deficient in serum and epidermal growth factor (EGF) caused rapid reductions in the activated (i.e., phosphorylated) forms of extracellular regulated kinases (ERKs) and the epidermal growth factor receptor (EGFR). Shifting to serum/EGF-deficient medium also enhanced TCDD-mediated induction of cytochrome P450 (CYP)1A1 Treatment of cells cultured in complete medium with the EGFR inhibitors gefitinib (Iressa), AG1478, and CI-1033 resulted in concentration-dependent reductions of active EGFR and ERKs, and increased CYP1A1 mRNA content ∼3- to 18-fold above basal level...
May 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Brian S Bogdanowicz, Matthew A Hoch, Megan E Hartranft
Purpose The approval history, pharmacology, pharmacokinetics, clinical trials, efficacy, dosing recommendations, drug interactions, safety, place in therapy, and economic considerations of gefitinib are reviewed. Summary Lung cancer is one of the most commonly diagnosed cancers and is the leading cause of cancer death. Platinum-based chemotherapy and tyrosine kinase inhibitors, such as erlotinib and afatinib, are recommended therapies for nonsmall cell lung cancer. The European Medicines Association based their approval of gefitinib on the randomized, multicenter Iressa Pan-Asia Study (IPASS, NCT00322452) and a single-arm study showing effectiveness in Caucasians (IFUM, NCT01203917)...
April 2017: Journal of Oncology Pharmacy Practice
B O Zhou, Jun Nie, Weidong Yang, Chenhong Huang, Y E Huang, Hongfei Zhao
Lung cancer is a malignancy with the highest incidence of morbidity and mortality worldwide. The lack of effective detection methods leads to the ineffectiveness of convetional therapy. The aim of the current study was to analyze the hydrothorax epidermal growth factor receptor (EGFR) mutation in patients with advanced non-small lung cancer (NSCLC) and malignant pleural effusion. A new method for clinical treatment was developed through a comparison of the difference of EGFR tyrosine kinase inhibitor (EGFR-TKI)-targeted therapy...
February 2016: Oncology Letters
Nan Zheng, Can Zhao, Xi-Ran He, Shan-Tong Jiang, Shu-Yan Han, Guo-Bing Xu, Ping-Ping Li
Gefitinib (Iressa) is the first oral EGFR tyrosine kinase inhibitor and it brings benefits to non-small cell lung cancer patients with EGFR mutation. In this study, a simple, rapid and credible high performance liquid chromatography-tandem mass spectrometry method was established and validated for the simultaneous quantification of gefitinib and its main metabolites M523595, M537194, M387783 and M608236 in NSCLC tumor-bearing mouse plasma. Sample extraction was done by protein precipitation using acetonitrile containing dasatinib as the internal standard...
February 1, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Oliver Gautschi, Carola Stadelmann, Franziska Aebersold-Keller, Katharina König, Reinhard Büttner, Lukas C Heukamp, Daniel Betticher, Christa Baumann, Katharina Buser, Antonello Calderoni, Adrian Casty, Giannicola DʼAddario, Claudius Irlé, Christoph Mamot, Rudolf Morant, Andreas Trojan, Erica Pellicioli, Sonja Jehle-Schwertfeger, Stefan Aebi, Joachim Diebold
BACKGROUND: The role of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKI) in the treatment of patients with advanced non-small cell lung cancer (NSCLC) and unknown EGFR mutation status has recently been questioned. PATIENTS AND METHODS: We conducted a retrospective study of patients with unknown EGFR mutation status and long-term response (LTR) to gefitinib in the Swiss Iressa expanded access program (EAP). We assessed patient characteristics, and performed Sanger sequencing and next generation sequencing on archived tumor tissue...
2015: Oncology Research and Treatment
Youwei Bi, Jiexin Deng, Daryl J Murry, Guohua An
Gefitinib (Iressa) is a selective and potent EGFR tyrosine kinase inhibitor. It received an accelerated FDA approval in 2003 for the treatment of patients with nonsmall cell lung cancer (NSCLC) and represents the first-line therapy for NSCLC with EGFR mutations. In the work presented herein, the disposition of gefitinib was investigated extensively in mouse in both plasma and 11 organs (liver, heart, lung, spleen, gut, brain, skin, fat, eye, kidney, and muscle) after a single IV dose of 20 mg/kg. Gefitinib demonstrated extensive distribution in most tissues, except for the brain, and tissue to plasma partition coefficients (K pt) ranged from 0...
January 2016: AAPS Journal
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