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https://www.readbyqxmd.com/read/28822888/apatinib-enhances-antitumour-activity-of-egfr-tkis-in-non-small-cell-lung-cancer-with-egfr-tki-resistance
#1
Fang Li, Tengjiao Zhu, Baoshan Cao, Jiadong Wang, Li Liang
BACKGROUND: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs)-rechallenged therapy for EGFR-mutant non-small cell lung cancer (NSCLC) patients who acquired resistance showed moderate efficacy. Considering the high interrelation between EGFR and vascular endothelial growth factor/vascular endothelial growth factor receptor (VEGF/VEGFR) pathways, we firstly evaluated EGFR-TKI combined with apatinib (a highly selective VEGFR2 inhibitor) in EGFR-TKI-resistant model and patients...
August 17, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28816958/effective-apatinib-treatment-of-pleomorphic-liposarcoma-a-case-report
#2
Peng Yan, Mei-Li Sun, Yu-Ping Sun, Chuan-Yong Liu
RATIONALE: Pleomorphic liposarcoma (PLS) is a rare and aggressive malignant tumor, and both radiation and conventional cytotoxic chemotherapy remain controversial for metastatic or unresectable disease. PATIENT CONCERNS: We presented an 81-year-old Chinese woman with advanced PLS who received apatinib after failure chemotherapy. DIAGNOSES: The patient was diagnosed as having PLS by biopsy. INTERVENTIONS: After a failed chemotherapy, apatinib started to be taken orally 425 mg per day...
August 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28740436/the-effect-of-apatinib-in-the-treatment-of-metastatic-renal-cell-carcinoma-a-case-report-and-review-of-the-literature
#3
Jinling Bi, Haiyuan Liu, Yong Huang
The aim of this study was to explore the effect of apatinib in the treatment of metastatic renal cell carcinoma (mRCC) and related adverse events. A case of mRCC was reported which recurred after surgery and roferon treatment. The patient was treated with apatinib at a dose of 500 mg orally, twice daily, 28 days/cycle. The metastatic lesions improved based on computed tomography after apatinib administration in the fourth and eighth month. The progression-free survival of the patient had increased almost to 8 months...
2017: International Medical Case Reports Journal
https://www.readbyqxmd.com/read/28740387/apatinib-loaded-nanoparticles-suppress-vascular-endothelial-growth-factor-induced-angiogenesis-and-experimental-corneal-neovascularization
#4
Jung Eun Lee, Koung Li Kim, Danbi Kim, Yeongju Yeo, Hyounkoo Han, Myung Goo Kim, Sun Hwa Kim, Hyuncheol Kim, Ji Hoon Jeong, Wonhee Suh
Pathological angiogenesis is one of the major symptoms of severe ocular diseases, including corneal neovascularization. The blockade of vascular endothelial growth factor (VEGF) action has been recognized as an efficient strategy for treating corneal neovascularization. In this study, we aimed to investigate whether nanoparticle-based delivery of apatinib, a novel and selective inhibitor of VEGF receptor 2, inhibits VEGF-mediated angiogenesis and suppresses experimental corneal neovascularization. Water-insoluble apatinib was encapsulated in nanoparticles composed of human serum albumin (HSA)-conjugated polyethylene glycol (PEG)...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28736629/biologic-therapy-in-esophageal-and-gastric-malignancies-current-therapies-and-future-directions
#5
REVIEW
Pamela Samson, A Craig Lockhart
Biologic agents, including targeted antibodies as well as immunomodulators, are demonstrating unparalleled development and study across the entire spectrum of human malignancy. This review summarizes the current state of biologic therapies for esophageal, esophagogastric, and gastric malignancies, including those that target human epidermal growth factor receptor 2 (HER2), epidermal growth factor receptor (EGFR), vascular endothelial growth factor (VEGF), c-Met, mechanistic target of rapamycin (mTOR) and immunomodulators...
June 2017: Journal of Gastrointestinal Oncology
https://www.readbyqxmd.com/read/28715845/apatinib-an-inhibitor-of-vascular-endothelial-growth-factor-receptor-2-suppresses-pathologic-ocular-neovascularization-in-mice
#6
Koung Li Kim, Wonhee Suh
Purpose: Vascular endothelial growth factor (VEGF) signaling via VEGF receptor 2 (VEGFR2) plays a crucial role in pathologic ocular neovascularization. In this study, we investigated the antiangiogenic effect of apatinib, a pharmacologic inhibitor of VEGFR2 tyrosine kinase, against oxygen-induced retinopathy (OIR) and laser-induced choroidal neovascularization (CNV) in mice. Methods: Western blotting and in vitro angiogenesis assays were performed using human retinal microvascular endothelial cells (HRMECs)...
July 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28679123/advanced-alveolar-soft-part-sarcoma-responds-to-apatinib
#7
Yong Zhou, Fan Tang, Yiying Wang, Li Min, Yi Luo, Wenli Zhang, Rui Shi, Hong Duan, Chongqi Tu
Alveolar soft part sarcoma (ASPS) is a rare, hypervascular soft tissue sarcoma with a low chemotherapy response rate. Here, we report an ASPS case with multiple lung metastases on initial presentation. The primary tumor, a hypervascular soft tissue mass 4.1×3.2×2.0 cm, located in the right thigh, was resected prior to chemotherapy. The patient suffered disease progression after two cycles of gemcitabine-docetaxel treatment. Immunohistochemical examination of the tumor tissue revealed strong positive staining for vascular endothelial growth factor (VEGF) and VEGF receptor-2 (VEGFR-2)...
July 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28678611/successful-treatment-of-advanced-pancreatic-liposarcoma-with-apatinib-a-case-report-and-literature-review
#8
Tao Han, Yuting Luan, Ying Xu, Xiaodan Yang, Jing Li, Ran Liu, Qing Li, Zhendong Zheng
Pancreatic liposarcoma is a malignant tumor originated from the pancreas mesenchymal tissue and mostly presented in skin, subcutaneous, periosteum, and long bone on both sides. Both conventional chemotherapy and radiotherapy have limited efficacy and poor prognosis for advanced pancreatic liposarcoma. Here, we reported a case of advanced pancreatic liposarcoma and reviewed the literature specific for liposarcoma of the pancreas and discuss the emerging options of treatment. The patient was treated with apatinib and a cross-line rescue therapy combined with paclitaxel after progressive disease...
July 5, 2017: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/28639910/apatinib-for-metastatic-breast-cancer-in-non-clinical-trial-setting-satisfying-efficacy-regardless-of-previous-anti-angiogenic-treatment
#9
Ying Lin, Zheng Wu, Jian Zhang, Xichun Hu, Zhonghua Wang, Biyun Wang, Jun Cao, Leiping Wang
Apatinib is a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 2. This study aimed to evaluate the efficacy and safety of apatinib in metastatic breast cancer (MBC) under non-clinical trial setting, and to study the impact of previous antiangiogenic treatment to the efficacy of apatinib. 52 MBC patients treated with apatinib under non-clinical trial setting in Fudan University Shanghai Cancer Center between January 1st 2015 and October 1st 2016 were included. All patients were included in time-to-treatment failure (TTF) analysis, while 45 patients were enrolled for progression-free survival (PFS) and overall survival (OS) analysis because 7 of the patients with treatment discontinuation due to intolerable toxicities had too short time for efficacy assessment...
June 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28617069/simultaneous-determination-of-six-tyrosine-kinase-inhibitors-in-human-plasma-using-hplc-q-orbitrap-mass-spectrometry
#10
Mao-Wei Ni, Jie Zhou, Hui Li, Wei Chen, Han-Zhou Mou, Zhi-Guo Zheng
AIM: Gefitinib, erlotinib, icotinib, crizotinib, lapatinib and apatinib are targeted cancer therapy agents acting through inhibition of tyrosine kinase. Method for quantifying these six drugs in human plasma of patients was required. MATERIALS & METHODS: An HPLC-Q-Orbitrap method (based on HPLC-MS/MS) was developed and validated for the simultaneous detection and quantitation of six tyrosine kinase inhibitors in human plasma. Sample was extracted by liquid-liquid extraction (ethyl acetate: tert-Butyl methyl ether, 1:1 v/v)...
June 2017: Bioanalysis
https://www.readbyqxmd.com/read/28548587/comparison-of-efficacy-between-tace-combined-with-apatinib-and-tace-alone-in-the-treatment-of-intermediate-and-advanced-hepatocellular-carcinoma-a-single-center-randomized-controlled-trial
#11
Wei Lu, Xin-Li Jin, Chao Yang, Peng Du, Fu-Qiang Jiang, Jun-Peng Ma, Jian Yang, Peng Xie, Zhe Zhang
OBJECTIVE: This study was designed to compare the clinical efficacy and safety of transcatheter arterial chemoembolization (TACE) combined with apatinib and TACE alone in the treatment of intermediate and advanced hepatocellular carcinoma (HCC). METHODS: From March 2015 to August 2015, a total of 44 patients with moderate and advanced HCC, who were admitted in the Navy General Hospital of China, were included into this study. These patients were randomly divided into 2 groups: group A and group B...
June 3, 2017: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/28490886/apatinib-to-combat-egfr-tki-resistance-in-an-advanced-non-small-cell-lung-cancer-patient-with-unknown-egfr-status-a-case-report
#12
Yanmei Peng, Huijuan Cui, Zhe Liu, Daiwei Liu, Fan Liu, Yazhong Song, Hua Duan, Yuqin Qiu, Qiang Li
Lung adenocarcinoma is the most common pathological pattern of lung cancer. During the past decades, a number of targeted agents have been explored to treat advanced lung adenocarcinoma. In the present clinical practice, antagonists of the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor (VEGF)-directed therapies are widely used. In the former category, the agent erlotinib (tyrosine kinase inhibitor) has shown obvious advantages over cytotoxic therapy. Anti-VEGF therapy bevacizumab used for lung adenocarcinoma was recommended in NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines) as first-line therapy...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28477033/apatinib-inhibits-vegfr-2-and-angiogenesis-in-an-in-vivo-murine-model-of-nasopharyngeal-carcinoma
#13
Qiu-Xia Peng, Yun-Wei Han, Yan-Ling Zhang, Jie Hu, Juan Fan, Shao-Zhi Fu, Shan Xu, Qiang Wan
Angiogenesis is initiated by the activation of the vascular epidermal growth factor receptor-2 (VEGFR-2) by the vascular epidermal growth factor (VEGF) ligand. Overexpression of VEGFR-2 increases the growth of nasopharyngeal carcinomas (NPC). Apatinib (YN968D1) is a highly-selective inhibitor of VEGFR-2, but its effects on NPC have not been hitherto investigated. In the present study, CNE-2 NPC cells were xenografted into 132 nude mice, which were treated with one of 6 drug regimens of apatinib administered alone or in combination with cisplatin (DDP)...
April 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/28415807/efficacy-and-safety-of-apatinib-in-stage-iv-sarcomas-experience-of-a-major-sarcoma-center-in-china
#14
Feng Li, Zhichao Liao, Jun Zhao, Gang Zhao, Xubin Li, Xiaoling Du, Yun Yang, Jilong Yang
PURPOSE: This study was conducted to review the efficacy and safety of Apatinib in stage IV sarcoma patients who failed previous chemotherapy. MATERIALS AND METHODS: The clinical information on 16 patients with stage IV sarcomas who failed in prior chemotherapy and subsequently received Apatinib treatment was collected. Apatinib was given 500mg/daily and 4 weeks as a cycle. All patients had at least one measurable extracranial tumor according to Response Evaluation Criteria In Solid Tumors 1...
March 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28403086/a-case-report-of-apatinib-in-treating-osteosarcoma-with-pulmonary-metastases
#15
Yong Zhou, Wengeng Zhang, Fan Tang, Yi Luo, Li Min, Wenli Zhang, Rui Shi, Hong Duan, Chongqi Tu
RATIONALE: Osteosarcoma is the most common malignant bone tumor in children and adolescents. Pulmonary metastases lead to a significantly increased risk of death. Apatinib, a new potent oral small-molecule tyrosine kinase inhibitor targeting the intracellular domain of vascular endothelial growth factor receptor 2 (VEGFR-2), shows survival benefits in treating advanced or metastatic gastric adenocarcinoma, non-squamous non-small cell lung cancer and metastatic breast cancer. However, its efficacy in metastatic osteosarcoma has not been reported yet...
April 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28383032/anti-tumour-activity-of-tivozanib-a-pan-inhibitor-of-vegf-receptors-in-therapy-resistant-ovarian-carcinoma-cells
#16
Majid Momeny, Zahra Sabourinejad, Ghazaleh Zarrinrad, Farima Moghaddaskho, Haniyeh Eyvani, Hassan Yousefi, Shahab Mirshahvaladi, Ensieh M Poursani, Farinaz Barghi, Arash Poursheikhani, Leila Dardaei, Davood Bashash, Mahmoud Ghazi-Khansari, Seyyed M Tavangar, Ahmad R Dehpour, Marjan Yaghmaie, Kamran Alimoghaddam, Ardeshir Ghavamzadeh, Seyed H Ghaffari
Epithelial ovarian cancer (EOC) is the most fatal gynaecological malignancy. Despite initial therapeutic response, the majority of advanced-stage patients relapse and succumb to chemoresistant disease. Overcoming drug resistance is the key to successful treatment of EOC. Members of vascular endothelial growth factor (VEGF) family are overexpressed in EOC and play key roles in its malignant progression though their contribution in development of the chemoresistant disease remains elusive. Here we show that expression of the VEGF family is higher in therapy-resistant EOC cells compared to sensitive ones...
April 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28377354/-inhibitory-effect-of-apatinib-on-hct-116-cells-and-its-mechanism
#17
Liang Yin, Jin Wang, Feng-Chang Huang, Yun-Fei Zhang, Ning Xu, Zheng-Qi Wen, Wen-Liang Li, Jian Dong
OBJECTIVE: To investigate the inhibitory effects of apatinib on colorectal carcinoma HCT-116 cells in vitro and the signaling pathways involved. METHODS: The cytotoxicity of different concentrations (0, 0.5, 1, 1.5, and 2 µmol/L) of apatinib in HCT-116 cells was assessed by MTT assay, using capecitabine as the positive control. The apoptosis rate of apatinib-treated HCT-116 cells was detected using flow cytometry, and the expressions of Bcl-2, Bax, and caspase-3 were determined with quantitative real-time PCR and Western blotting...
March 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/28367065/salvage-treatment-with-apatinib-for-advanced-non-small-cell-lung-cancer
#18
Zhengbo Song, Xinmin Yu, Guangyuan Lou, Xun Shi, Yiping Zhang
OBJECTIVE: No definitive chemotherapeutic regimen has been established in patients with non-small-cell lung cancer (NSCLC) who failed second- or third-line treatment. The aim of this study was to evaluate apatinib, a VEGFR-2 inhibitor, in advanced NSCLC as salvage treatment. METHODS: We evaluated the efficacy and toxicity of apatinib in patients with previously treated advanced NSCLC from 2014 to 2015 in Zhejiang Cancer Hospital. Survival analysis was performed by the Kaplan-Meier method...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28352185/apatinib-treatment-combined-with-chemotherapy-for-advanced-epithelial-ovarian-cancer-a-case-report
#19
Linghui Deng, Yue Wang, Wenbin Lu, Qian Liu, Jie Wu, Jianhua Jin
Apatinib is a novel oral tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor-2, which has been proved by clinical trials to be effective and safe for patients with chemotherapy-refractory gastric cancer. To date, there is no study or case report on apatinib treatment for patients with ovarian cancer. Here, we present the case of a 50-year-old Chinese woman with advanced ovarian cancer, who received apatinib at a daily dose of 500 mg for 28 days per cycle after failure of fourth-line chemotherapy...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28331317/cyclic-rgd-peptide-modified-liposomal-drug-delivery-system-for-targeted-oral-apatinib-administration-enhanced-cellular-uptake-and-improved-therapeutic-effects
#20
Zhiwang Song, Yun Lin, Xia Zhang, Chan Feng, Yonglin Lu, Yong Gao, Chunyan Dong
Apatinib is an oral tyrosine kinase inhibitor, which selectively targets vascular endothelial growth factor receptor 2 and has the potential to treat many tumors therapeutically. Cyclic arginylglycylaspartic acid (cRGD)- and polyethylene glycol (PEG)-modified liposomes (cRGD-Lipo-PEG) were constructed to act as a targeted delivery system for the delivery of apatinib to the human colonic cancer cell line, HCT116. These cRGD-modified liposomes specifically recognized integrin αvβ3 and exhibited greater uptake efficiency with respect to delivering liposomes into HCT116 cells when compared to nontargeted liposomes (Lipo-PEG), as well as greater death of tumor cells and apoptosis...
2017: International Journal of Nanomedicine
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