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https://www.readbyqxmd.com/read/28715845/apatinib-an-inhibitor-of-vascular-endothelial-growth-factor-receptor-2-suppresses-pathologic-ocular-neovascularization-in-mice
#1
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
#2
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)...
June 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28678611/successful-treatment-of-advanced-pancreatic-liposarcoma-with-apatinib-a-case-report-and-literature-review
#3
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
#4
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
#5
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
#6
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...
May 26, 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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
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
#16
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...
April 13, 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
#17
REVIEW
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
#18
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
#19
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...
June 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28176910/apatinib-as-post-second-line-therapy-in-egfr-wild-type-and-alk-negative-advanced-lung-adenocarcinoma
#20
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
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