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https://www.readbyqxmd.com/read/28301155/exploration-of-2-pyridin-4-ylmethyl-amino-nicotinamide-derivatives-as-potent-reversal-agents-against-p-glycoprotein-mediated-multidrug-resistance
#1
Qianqian Qiu, Wei Shi, Zheng Li, Bo Zhang, Miaobo Pan, Jian Cui, Yuxuan Dai, Wenlong Huang, Hai Qian
Overexpression of the ATP-binding cassette (ABC) transport proteins, like ABCB1, commonly referred to as P-glycoprotein (P-gp), initiates active efflux of a broad spectrum of unrelated chemotherapeutic drugs in structure and function, leading to chemotherapy failure. A series of 2-((pyridin-4-ylmethyl)amino)nicotinamide derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance (MDR) were designed and synthesized. The majority of target compounds displayed great reversal potency, especially 9n...
March 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28248891/concurrent-apatinib-and-local-radiation-therapy-for-advanced-gastric-cancer-a-case-report-and-review-of-the-literature
#2
Ming Zhang, Weiye Deng, Xiaoci Cao, Xiaoming Shi, Huanfen Zhao, Zheping Duan, Bonan Lv, Bin Liu
RATIONALE: Apatinib is a novel anti-angiogenic agent targeting vascular endothelial growth factor receptor-2, which is effective in patients with chemotherapy-refractory gastric cancer. There are no reports of concurrent apatinib with local radiation therapy in elderly patients with advanced gastric cancer. PATIENT CONCERNS AND DIAGNOSES:: we present the first published report of a 70-year-old male patient with advanced gastric cancer who received concurrent apatinib and local radiation therapy after failure of oxaliplatin and S-1 chemotherapy...
March 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28243119/successful-treatment-with-apatinib-for-refractory-recurrent-malignant-gliomas-a-case-series
#3
Honghong Zhang, Fangfang Chen, Zhiqiang Wang, Shaoxiong Wu
Malignant glioma (MG) is a common and refractory primary tumor with a high recurrence rate. There is still a lack of effective therapy for recurrent MG (rMG). We present here two cases of refractory rMG treated using apatinib, which is a new highly selective inhibitor to VEGFR. Case 1, a 37-year-old female, was diagnosed with recurrent intracerebral high-grade glioma and failed to almost all treatments (including temozolomide, bevacizumab, nimotuzumab, reradiation, etc) during her second relapse. Case 2, a 40-year-old male, was diagnosed with recurrent glioblastoma multiforme for the third time following multiple treatments including resurgery, temozolomide and radiation...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28178685/overwhelming-rapid-metabolic-and-structural-response-to-apatinib-in-radioiodine-refractory-differentiated-thyroid-cancer
#4
Yansong Lin, Chen Wang, Wen Gao, Ruixue Cui, Jun Liang
Currently, patients with radioiodine refractory differentiated thyroid cancer (RAIR-DTC) have limited treatment options. In this study, we aimed to assess the short-term efficacy and safety of apatinib in RAIR-DTC. Ten adult patients were prospectively enrolled to receive oral apatinib (750 mg q.d). The primary endpoints were change in serum thyroglobulin (Tg) concentration, disease control rate (DCR) and objective response rate (ORR) based on RECIST 1.1 criteria. The secondary endpoints included change in glucose metabolism, evaluated by maximum standard uptake value (SUVmax), and safety...
February 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28176910/apatinib-as-post-second-line-therapy-in-egfr-wild-type-and-alk-negative-advanced-lung-adenocarcinoma
#5
Shen-Cun Fang, Hai-Tao Zhang, Ying-Ming Zhang, Wei-Ping Xie
In the absence of a driver mutation, chemotherapy is the standard treatment option as first- and second-line therapy for advanced non-small-cell lung cancer (NSCLC). Though a large number of patients are suitable for post second-line therapies, the quality and quantity of the available drugs in this setting is poor. Apatinib, a small molecule vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor, is a first-generation oral antiangiogenesis drug approved in the People's Republic of China for use as a subsequent line of treatment for advanced gastric cancer...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28103584/significant-efficacy-and-well-safety-of-apatinib-in-an-advanced-liver-cancer-patient-a-case-report-and-literature-review
#6
Peisi Kou, Yan Zhang, Wenbo Shao, Hui Zhu, Jingze Zhang, Haiyong Wang, Li Kong, Jinming Yu
Apatinib is a novel and highly selective tyrosine kinase inhibitor of vascular endothelial growth factor receptor-2. Previous studies have suggested that apatinib is safe and effective in some solid tumors. We report one case with advanced hepatocellular carcinoma (HCC), who received apatinib combined with transhepatic arterial chemotherapy and embolization (TACE), and chemotherapy respectively. TACE was administered three times once a month, using lipiodol 10ml, oxaliplatin 150mg, and tegafur 1g. The dose of apatinib was 500 mg/d from day 4 to 24...
January 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28094573/advanced-gastric-adenocarcinoma-optimizing-therapy-options
#7
REVIEW
Dilsa Mizrak Kaya, Kazuto Harada, Yusuke Shimodaira, Fatemeh G Amlashi, Quan Lin, Jaffer A Ajani
Gastric adenocarcinoma (GAC) is the fifth most common cancer and third leading cause of cancer related mortality worldwide. When localized, cure is achievable with surgery and adjunctive therapies in some patients, however, once advanced, GAC is not a curable condition. Only two targeted agents (trastuzumab and ramucirumab) have been approved and apatinib was approved only in China. Because of the heterogeneous nature of GAC, it is not possible to assess a standard therapeutic approach. Areas covered: In this review, we aimed to describe the optimal systemic therapy regimens for advanced GAC...
March 2017: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/28061477/autocrine-vegf-signaling-promotes-cell-proliferation-through-a-plc-dependent-pathway-and-modulates-apatinib-treatment-efficacy-in-gastric-cancer
#8
Yi Lin, Ertao Zhai, Bing Liao, Lixia Xu, Xinhua Zhang, Sui Peng, Yulong He, Shirong Cai, Zhirong Zeng, Minhu Chen
BACKGROUND: Tumor cells produce vascular endothelial growth factor (VEGF) which interact with the membrane or cytoplasmic VEGF receptors (VEGFRs) to promote cell growth in an angiogenesis-independent fashion. Apatinib, a highly selective VEGFR2 inhibitor, is the only effective drug for patients with terminal gastric cancer (GC) who have no other chemotherapeutic options. However, its treatment efficacy is still controversy and the mechanism behind remains undetermined. In this study, we aimed to investigate the role of autocrine VEGF signaling in the growth of gastric cancer cells and the efficacy of Apatinib treatment...
January 3, 2017: Oncotarget
https://www.readbyqxmd.com/read/28052652/anti-angiogenic-therapy-in-patients-with-advanced-gastric-and-gastroesophageal-junction-cancer-a-systematic-review
#9
Li-Tzong Chen, Do-Youn Oh, Min-Hee Ryu, Kun-Huei Yeh, Winnie Yeo, Roberto Carlesi, Rebecca Cheng, Jongseok Kim, Mauro Orlando, Yoon-Koo Kang
Despite advancements in therapy for advanced gastric and gastroesophageal junction cancers, their prognosis remains dismal. Tumor angiogenesis plays a key role in cancer growth and metastasis, and recent studies indicate that pharmacologic blockade of angiogenesis is a promising approach to therapy. In this systematic review, we summarize current literature on the clinical benefit of anti-angiogenic agents in advanced gastric cancer. We conducted a systematic search of PubMed and conference proceedings including the American Society of Clinical Oncology, the European Society for Medical Oncology, and the European Cancer Congress...
January 3, 2017: Cancer Research and Treatment: Official Journal of Korean Cancer Association
https://www.readbyqxmd.com/read/28028915/apatinib-in-gastric-carcinoma-a-case-report-of-partial-response-for-first-line-treatment-in-advanced-disease
#10
Yaping Wang, Minghong Bi, Haoran Zhang, Zhenyuan Gao, Hairong Zhou, Shu Chang
Gastric cancer (GC) is the most common gastrointestinal malignant tumor, with a gradual increasing incidence throughout the world. Mostly GC is diagnosed in its late stage. To date, there is no usable standardized treatment regimen for patients with advanced GC. Apatinib mesylate, small-molecule vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor (TKI), has been approved as third-line treatment for patients with advanced gastric adenocarcinoma in China, October, 2014. Till now, there is no case report about apatinib as first-line treatment for patients with advanced GC in literature...
December 28, 2016: Asia-Pacific Journal of Clinical Oncology
https://www.readbyqxmd.com/read/27928929/angiogenesis-and-apatinib-a-new-hope-for-patients-with-advanced-gastric-cancer
#11
EDITORIAL
Ramon Andrade de Mello, Jailson de Oliveira, Georgios Antoniou
No abstract text is available yet for this article.
February 2017: Future Oncology
https://www.readbyqxmd.com/read/27798730/cost-effectiveness-analysis-of-apatinib-treatment-for-chemotherapy-refractory-advanced-gastric-cancer
#12
Hong-Dou Chen, Jing Zhou, Feng Wen, Peng-Fei Zhang, Ke-Xun Zhou, Han-Rui Zheng, Yu Yang, Qiu Li
BACKGROUND: Apatinib, a third-line or later treatment for advanced gastric cancer (aGC), was shown to improve overall survival and progression-free survival (PFS) compared with placebo in the phase III trial. Given the modest benefit with high costs, we further evaluated the cost-effectiveness of apatinib for patients with chemotherapy-refractory aGC. METHODS: A Markov model was developed to simulate the disease process of aGC (PFS, progressive disease, and death) and estimate the incremental cost-effectiveness ratio (ICER) of apatinib to placebo...
February 2017: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/27793017/therapeutic-effect-of-apatinib-on-overall-survival-is-mediated-by-prolonged-progression-free-survival-in-advanced-gastric-cancer-patients
#13
Lihong Huang, Yongyue Wei, Sipeng Shen, Qianwen Shi, Jianling Bai, Jin Li, Shukui Qin, Hao Yu, Feng Chen
Apatinib is reported to significantly improve the overall survival (OS) of patients with advanced gastric cancer who have previously failed second-line chemotherapy. However, it is not well understood whether apatinib acts by improving progression or by prolonging post-progression survival. Here, based on phase III clinical trial data, the mediating effect of apatinib on patient overall survival was systematically quantified, through progression-free survival (PFS), post-progression survival (PPS), and the disease control rate (DCR)...
October 25, 2016: Oncotarget
https://www.readbyqxmd.com/read/27781258/-research-status-quo-and-progression-in-targeted-therapy-for-advanced-gastric-cancer
#14
Rui Feng, Xiaotian Zhang, Sheng Yang
With the deeper research of the proliferation, invasion and metastasis mechanisms of the gastric cancer, targeted therapy has become a hot spot in this field. The exploration of targeted agents for gastric cancer is mainly concentrated upon the drugs that target human epidermal growth factor receptor (HER) family, the vascular endothelial growth factor (VEGF), the phosphatidylinositol 3-kinase-protein kinase/mammalian target of rapamycin (PI3K/mTOR) and the NF-κB signaling pathways. The targeted drugs relevant to HER family include the Cetuximab, Nimotuzumab, Matuzumab, Panitumumab and Erlotinib which are aimed at HER-1, the Trastuzumab, Pertuzumab and T-DM1 (trastuzumab emtansine) which are aimed at HER-2, and the Lapatinib and Afatinib which are the multi-target agents of HER...
October 25, 2016: Zhonghua Wei Chang Wai Ke za Zhi, Chinese Journal of Gastrointestinal Surgery
https://www.readbyqxmd.com/read/27738308/response-to-apatinib-in-chemotherapy-failed-advanced-spindle-cell-breast-carcinoma
#15
Na Zhou, Congmin Liu, Helei Hou, Chuantao Zhang, Dong Liu, Guanqun Wang, Kewei Liu, Jingjuan Zhu, Hongying Lv, Tianjun Li, Xiaochun Zhang
Spindle cell carcinoma of the breast is a rare subtype of metaplastic carcinoma, and no effective chemotherapy special for metaplastic carcinoma exists until now. As spindle cell carcinomas of the breast are typically "Triple Negative", endocrine therapy and molecular therapy targeted to Her2 might not be favorable, resulting in poor prognosis. Apatinib is currently being tested in patients with breast or lung cancers. Here we report a successful case using Apatinib to treat spindle cell carcinoma of breast...
November 1, 2016: Oncotarget
https://www.readbyqxmd.com/read/27631210/a-case-report-of-targeted-therapy-with-apatinib-in-a-patient-with-advanced-gastric-cancer-and-high-serum-level-of-alpha-fetoprotein
#16
Xue-Ru Zhu, Mei-Ling Zhu, Qing Wang, Wen-Ji Xue, Yi-Wei Wang, Rui-Fen Wang, Si-Yu Chen, Lei-Zhen Zheng
BACKGROUND: Alpha-fetoprotein (AFP) is an important marker for hepatocellular carcinoma, and the detection of serum AFP is currently the principle method for the diagnosis of hepatocellular carcinoma. The prevalence of gastric cancer (GC) with high level of serum AFP is extremely rare, but has unique clinical features. CASE SUMMARY: We herein present a rare case with GC and high level of serum AFP. A 64-year-old Chinese female underwent gastrectomy was diagnosed as gastric adenocarcinoma and the pathological stage was T1bN0M0, IA...
September 2016: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27568322/targeted-therapies-for-advanced-and-metastatic-adenocarcinoma-of-the-gastroesophageal-junction-is-there-something-new
#17
REVIEW
Felice Pasini, Anna Paola Fraccon, Yasmina Modena, Maria Bencivenga, Simone Giacopuzzi, Francesca La Russa, Milena Gusella, Giovanni de Manzoni
Despite improvements in systemic chemotherapy (CT), the prognosis of metastatic adenocarcinoma of the gastroesophageal junction remains poor. Over the years, new targeting agents have become available and were tested, with or without CT, in first or subsequent lines of therapy. The epidermal growth factor receptor family was targeted with monoclonal antibodies (MoAbs) (trastuzumab, cetuximab, panitumumab) and tyrosin kinase inhibitors (TKIs) (lapatinib, erlotinib, gefitinib). Only trastuzumab, in combination with cisplatin and fluoropyrimidines, significantly improved overall survival (OS) in first-line therapy (13...
January 2017: Gastric Cancer
https://www.readbyqxmd.com/read/27563253/successful-treatment-of-angiosarcoma-of-the-scalp-with-apatinib-a-case-report
#18
Guanghui Ji, Liu Hong, Ping Yang
Angiosarcoma is a rare and aggressive vascular malignancy with a poor prognosis. There is no standard chemotherapy regime for advanced angiosarcoma. Here, we report a case of advanced angiosarcoma that was successfully treated with apatinib, an oral tyrosine kinase inhibitor targeting the intracellular domain of vascular endothelial growth factor receptor-2 (VEGFR-2). To our knowledge, this is the first case to report the successful use of apatinib for angiosarcoma. Furthermore, the administration of apatinib results in fewer toxic effects than traditional cytotoxic chemotherapy...
2016: OncoTargets and Therapy
https://www.readbyqxmd.com/read/27549930/3d-microtumors-in-vitro-supported-by-perfused-vascular-networks
#19
Agua Sobrino, Duc T T Phan, Rupsa Datta, Xiaolin Wang, Stephanie J Hachey, Mónica Romero-López, Enrico Gratton, Abraham P Lee, Steven C George, Christopher C W Hughes
There is a growing interest in developing microphysiological systems that can be used to model both normal and pathological human organs in vitro. This "organs-on-chips" approach aims to capture key structural and physiological characteristics of the target tissue. Here we describe in vitro vascularized microtumors (VMTs). This "tumor-on-a-chip" platform incorporates human tumor and stromal cells that grow in a 3D extracellular matrix and that depend for survival on nutrient delivery through living, perfused microvessels...
August 23, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27531538/gastric-cancer-clinical-and-epidemiological-aspects
#20
REVIEW
Marino Venerito, Alexander Link, Theodoros Rokkas, Peter Malfertheiner
Gastric cancer (GC) ranks fifth for cancer incidence and second for cancer deaths. Epidemiological data showed that survivors of Hodgkin's lymphoma and patients with pernicious anemia etiologically linked to autoimmune gastritis are at increased risk of GC. Screening of patients with autoimmune thyroid disease by means of pepsinogen (PG) I and PG I/II detected autoimmune gastritis with oxyntic gastric atrophy in one of four patients and may be recommended for GC prevention purposes. The International Agency for Research on Cancer reported a positive association between consumption of processed meet and increased GC risk...
September 2016: Helicobacter
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