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https://www.readbyqxmd.com/read/29675102/synergistic-antitumor-effects-of-cmet-inhibitor-in-combination-with-anti-vegf-in-colorectal-cancer-patient-derived-xenograft-models
#1
Xiangheng Chen, Zhonghai Guan, Jun Lu, Haohao Wang, Zhongkun Zuo, Fei Ye, Jiangsheng Huang, Lisong Teng
cMet signaling pathway is involved in the resistance to anti-VEGF therapy and cMet overexpression is associated with tumor progression and poor prognosis. In this study, the expression of cMet in 146 Chinese colorectal cancer (CRC) patients was examined by immunohistochemistry staining. Our data demonstrated that cMet overexpression rate was 42.5% (62/146) and cMet overexpression was closely correlated with distant metastasis of CRC. Using CRC patient-derived xenograft (PDX) mouse models we investigated antitumor activity of a novel selective cMet inhibitor volitinib alone or in combination with anti-VEGF inhibitor apatinib in vivo ...
2018: Journal of Cancer
https://www.readbyqxmd.com/read/29670374/multiline-treatment-combining-apatinib-with-toptecan-for-platinum-resistant-recurrent-ovarian-cancer-patients-a-report-of-three-cases
#2
Yuan Cheng, Juan Zhang, Haiyun Geng, Shukui Qin, Haiqing Hua
The aim of this study was to observe the efficacy and safety of apatinib combined with toptecan therapy in the multiline treatment of platinum-resistant recurrent ovarian cancer patients. The clinical records of three patients with platinum-resistant recurrent ovarian cancer treated with apatinib combined with toptecan therapy were analyzed and followed up for 3 months, and the related literatures were reviewed. The three patients achieved partial response and the tumor marker CA125 levels decreased significantly as an outcome of the treatment...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29663291/apatinib-a-review-in-advanced-gastric-cancer-and-other-advanced-cancers
#3
Lesley J Scott
Apatinib [AiTan™ (China); Rivoceranib® (global)] is a novel, small molecule, selective vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor and is the second anti-angiogenic drug to be approved in China for the treatment of advanced or metastatic gastric cancer. This article summarizes the pharmacological properties of apatinib and reviews its clinical use in chemotherapy-experienced patients with advanced gastric adenocarcinoma, including gastroesophageal adenocarcinoma (GEA), or with other advanced cancers such as non-small cell lung cancer (NSCLC), breast cancer, gynaecological cancers, hepatocellular carcinoma (HCC), thyroid cancer and sarcomas...
April 16, 2018: Drugs
https://www.readbyqxmd.com/read/29662638/an-open-label-single-armed-exploratory-study-of-apatinib-a-novel-vegfr-2-tyrosine-kinase-inhibitor-in-patients-with-relapsed-or-refractory-non-hodgkin-lymphoma
#4
Ling Li, Sa Xiao, Lei Zhang, Xin Li, Xiaorui Fu, Xinhua Wang, Jingjing Wu, Zhenchang Sun, Xudong Zhang, Yu Chang, Feifei Nan, Jiaqin Yan, Zhaoming Li, Mengyuan Shi, Ken H Young, Mingzhi Zhang
Background: Apatinib, a novel small molecule vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor, have shown remarkable efficacy in many solid cancers. But evidence of antitumor activity in patients with lymphoma is still limited. We conducted an open-label, single-armed, exploratory study in relapse or refractory non-Hodgkin lymphoma patients for the efficacy and safety of apatinib. Experimental design: Patients with relapse or refractory non-Hodgkin patients meet the criteria were eligible for enrollment...
March 23, 2018: Oncotarget
https://www.readbyqxmd.com/read/29625604/apatinib-for-advanced-sarcoma-results-from-multiple-institutions-off-label-use-in-china
#5
Lu Xie, Wei Guo, Ye Wang, Taiqiang Yan, Tao Ji, Jie Xu
BACKGROUND: Anti-angiogenesis Tyrosine kinase inhibitors (TKIs) have been proved to show promising effects on prolonging progression-free survival (PFS) for advanced sarcoma after failure of standard multimodal Therapy. Methylsulfonic apatinib is one of those TKIs which specifically inhibits VEGFR-2. This paper summarizes the experience of three Peking University affiliated hospitals in off-label use of apatinib in the treatment of extensively pre-treated sarcoma. METHODS: We retrospectively analysed files of patients with advanced sarcoma not amenable to curative treatment, who were receiving an apatinib-containing regimen between June 1, 2015 and December 1, 2016...
April 6, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29618578/pet-response-assessment-in-apatinib-treated-radioactive-iodine-refractory-thyroid-cancer
#6
Chen Wang, Xin Zhang, Xue Yang, Hui Li, Ruixue Cui, Wenmin Guan, Xin Li, Zhaohui Zhu, Yansong Lin
This work evaluated the use of the positron emission tomography/computed tomography (PET/CT) technique to assess the early therapeutic response and predict the prognosis of patients with radioactive iodine-refractory differentiated thyroid cancer (RAIR-DTC) who underwent apatinib therapy. Standardised uptake value (SUV), metabolic tumour volume (MTV) and total lesion glycolysis (TLG), derived from 18FDG PET/CT and SUV from 68Ga-NOTA-PRGD2 PET/CT, were evaluated. Tumour response was evaluated using the Response Evaluation Criteria in Solid Tumors (RECIST) 1...
April 4, 2018: Endocrine-related Cancer
https://www.readbyqxmd.com/read/29587657/effective-treatment-of-apatinib-in-desmoplastic-small-round-cell-tumor-a-case-report-and-literature-review
#7
Chunyu Shi, Ye Feng, Lei Chao Zhang, Da Yong Ding, Ming Yu Yan, Lu Pan
BACKGROUND: Desmoplastic small round cell tumor (DSRCT) is a rare malignant sarcoma with poor prognosis due to lack of effective treatments. Apatinib is a new potent oral small-molecule tyrosine kinase inhibitor, and targets the intracellular domain of vascular endothelial growth factor receptor 2 (VEGFR-2). In this study, we presented a case of intra-abdominal DSRCT which was effectively treated by apatinib. CASE PRESENTATION: A 32-year-old man was admitted due to increasing urination frequency and palpable mass in right lower abdomen for 2 months...
March 27, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29576426/a-pilot-study-of-apatinib-as-third-line-treatment-in-patients-with-heavily-treated-metastatic-colorectal-cancer
#8
Lijun Liang, Lei Wang, Panrong Zhu, Youyou Xia, Yun Qiao, Jiang Wu, Wei Zhuang, Jiayan Fei, Yixuan Wen, Xiaodong Jiang
BACKGROUND: Antiangiogenic therapy has shown improved clinical outcome in metastatic colorectal cancer (mCRC). After the failure of standard treatments, regorafenib and TAS-102 would be recommended for patients with mCRC, however, they have not been approved in China during this study period. PATIENTS AND METHODS: This pilot study aimed to assess the efficacy and safety of apatinib, a novel oral inhibitor targeting vascular endothelial growth factor receptor 2, as third-line treatment for patients with mCRC refractory to standard therapies...
March 2, 2018: Clinical Colorectal Cancer
https://www.readbyqxmd.com/read/29575765/combination-therapy-of-apatinib-with-icotinib-for-primary-acquired-icotinib-resistance-in-patients-with-advanced-pulmonary-adenocarcinoma-with-egfr-mutation
#9
Pinghui Xia, Jinlin Cao, Xiayi Lv, Luming Wang, Wang Lv, Jian Hu
Multi-targeted agents represent the next generation of targeted therapies for solid tumors, and patients with acquired resistance to EGFR-tyrosine kinase inhibitors (TKIs) may also benefit from their combination with TKI therapy. Third-generation targeted drugs, such as osimertinib, are very expensive, thus a more economical solution is required. The aim of this study was to explore the use of apatinib combined with icotinib therapy for primary acquired resistance to icotinib in three patients with advanced pulmonary adenocarcinoma with EGFR mutations...
March 24, 2018: Thoracic Cancer
https://www.readbyqxmd.com/read/29573236/efficacy-safety-and-predictive-indicators-of-apatinib-after-multilines-treatment-in-advanced-nonsquamous-nonsmall-cell-lung-cancer-apatinib-treatment-in-nonsquamous-nsclc
#10
Di Wu, Li Liang, Ligong Nie, Jun Nie, Ling Dai, Weiheng Hu, Jie Zhang, Xiaoling Chen, Jindi Han, Xiangjuan Ma, Guangming Tian, Sen Han, Jieran Long, Yang Wang, Ziran Zhang, Tao Xin, Jian Fang
AIM: Patients with advanced nonsquamous nonsmall cell lung cancer (NSCLC) who experienced progression with two or more lines chemotherapy have no treatment options that clearly confer a survival benefit. As a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, apatinib has a certain antitumor effect for various solid tumors. The present study evaluated the efficacy and safety of apatinib in advanced nonsquamous NSCLC as salvage treatment in Chinese real-world practice...
March 24, 2018: Asia-Pacific Journal of Clinical Oncology
https://www.readbyqxmd.com/read/29552208/apatinib-promotes-apoptosis-of-the-smmc-7721-hepatocellular-carcinoma-cell-line-via-the-pi3k-akt-pathway
#11
Hua Zhang, Yumei Cao, Yuru Chen, Guangxi Li, Hanshu Yu
The present study investigated the inhibitory effects of apatinib on the proliferation of the SMMC-7721 hepatocellular carcinoma cell line to explore the possible mechanism. The MTT assay was used to detect the inhibitory effects of the different concentrations of apatinib on the proliferation of SMMC-7721 cells. Annexin V/PI double staining was performed to investigate the effects of apatinib on the apoptosis of SMMC-7721 cells. Expression of the apoptosis-related genes Bcl-2, Bax and caspase-9 after apatinib treatment was detected by reverse transcription-quantitative PCR (RT-qPCR) and western blot analysis...
April 2018: Oncology Letters
https://www.readbyqxmd.com/read/29549743/application-of-liquid-chromatography-tandem-mass-spectrometry-to-study-the-effect-of-docetaxel-on-pharmacokinetics-and-tissue-distribution-of-apatinib-in-mice
#12
Siqi Feng, Jingwei Zhang, Ying Wang, Runbin Sun, Dong Feng, Ying Peng, Na Yang, Yue Zhang, Haoxue Gao, Huilin Gu, Guangji Wang, Jiye Aa, Fang Zhou
Apatinib, a highly selective small-molecule inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2), has attracted many attentions due to its anticancer activity in various malignancies containing non-small-cell lung cancer (NSCLC). Our previous preclinical study confirmed the enhanced anti-tumor efficacy of combined treatment between apatinib and docetaxel for NSCLC. However, the effects of docetaxel on pharmacokinetics and tissue distribution of apatinib are not clear. In present study, a reliable HPLC-MS/MS method was established for determination of apatinib...
March 10, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29545575/efficacy-and-safety-of-apatinib-in-patients-with-previously-treated-metastatic-colorectal-cancer-a-real-world-retrospective-study
#13
Miaomiao Gou, Haiyan Si, Yong Zhang, Niansong Qian, Zhikuan Wang, Weiwei Shi, Guanghai Dai
No definitive treatment strategy has been established for patients with metastatic colorectal cancer (mCRC) who experienced progression after three or more lines of chemotherapy. A total of 36 mCRC patients were enrolled in this retrospective study who received apatinib therapy under non-clinical trial setting after progression in People's liberation army general Hospital from March 2015 and August 2017. Progression free survival (PFS), overall survival (OS), disease control rate (DCR), objective response rate (ORR) and treatment-related adverse events (AEs) were reviewed and evaluated...
March 15, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29516980/apatinib-for-advanced-nonsmall-cell-lung-cancer-a-retrospective-case-series-analysis
#14
Chengxi Yang, Wen Feng, Di Wu
Objectives: Apatinib, a tyrosine kinase inhibitor which selectively inhibits vascular endothelial growth factor receptor-2, has been shown to be beneficial to patients with a variety of cancers, including advanced nonsmall-cell lung cancer (NSCLC). Thus, this study was aimed to retrospectively assess the efficacy and safety of apatinib in patients with advanced/metastatic NSCLC who failed more than two lines of treatment. Methods: Twenty-three NSCLC patients were involved in this study, who received oral apatinib at a daily dose of 250/500/750 mg, with the progression after the failure of second-line therapy...
January 2018: Journal of Cancer Research and Therapeutics
https://www.readbyqxmd.com/read/29505543/apatinib-in-refractory-radiation-induced-brain-edema-a-case-report-erratum
#15
(no author information available yet)
No abstract text is available yet for this article.
January 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29505026/efficacy-and-safety-of-apatinib-in-patients-with-intermediate-advanced-hepatocellular-carcinoma-a-prospective-observation-study
#16
Wen-Chang Yu, Kong-Zhi Zhang, Shi-Guang Chen, Wei-Fu Liu
This prospective study aimed to evaluate the efficacy and safety of apatinib in patients with intermediate/advanced hepatocellular carcinoma (HCC).The patients with intermediate/advanced HCC, who met predetermined inclusion and exclusion criteria, underwent oral treatment of apatinib 500 mg daily. The drug-related adverse effects were monitored by regular follow-up and workup including laboratory tests and imaging examinations. Tumor response was assessed by response evaluation criteria in solid tumor criteria...
January 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29502367/-triptolide-reverses-apatinib-resistance-in-gastric-cancer-cell-line-mkn45-via-inhibition-of-heat-shock-protein-70
#17
F Teng, Z Y Xu, H Lyu, Y P Wang, L J Wang, T Huang, J C Sun, H T Zhu, Y X Ni, X D Cheng
Objective: To investigate the effect of triptolide, a specific inhibitor of heat shock protein 70 (HSP70), on apatinib resistance in gastric cancer cells line MKN45. Methods: The apatinib-resistant cells (MKN45/AR) and MKN45 parental cells were treated with apatinib, triptolide and apatinib combined with triptolide, respectively. CCK-8 assay was performed to determine the half maximal inhibitory concentration (IC(50)) of MKN45/AR and MKN45 cells in the presence of different treatment. The mRNA expression of heat shock protein gene (HSPA1A and HSPA1B) was detected by RT-PCR, while the protein expression of heat shock protein 70 was analyzed using Western blot in MKN45/AR and MKN45 cells...
February 23, 2018: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
https://www.readbyqxmd.com/read/29497319/successful-treatment-of-metastatic-colorectal-cancer-with-apatinib-report-of-two-cases-and-literature-review
#18
Minghong Bi, Jingru Yang, Yaping Wang, Haoran Zhang, Zhenyuan Gao, Hairong Zhou, Mohan Shi
Apatinib, a novel small molecule tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor-2, was approved for metastatic gastric adenocarcinoma in China in Oct 2014. This is the first report on its use for advanced colorectal cancer as a kind of third-line therapy to date. Here we report two Chinese patients who presented with metastatic colorectal cancer who received apatinib 850 mg daily as a third-line therapy. Both the patients achieved favorable benefits in outcomes after the administration of apatinib...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29490645/apatinib-exhibits-anti-leukemia-activity-in-preclinical-models-of-acute-lymphoblastic-leukemia
#19
Manman Deng, Jie Zha, Zhiwu Jiang, Xian Jia, Yuanfei Shi, Peng Li, Xiao Lei Chen, Zhihong Fang, Zhiqiang Du, Bing Xu
BACKGROUND: Acute lymphoblastic leukemia (ALL) is a clonal malignant disorder characterized by an uncontrolled proliferation of immature B or T lymphocytes. Extensive studies have suggested an involvement of angiogenesis signaling in ALL progression and resistance to treatment. Thus, targeting angiogenesis with anti-angiogenic drugs may be a promising approach for ALL treatment. In this study, we investigated the effectiveness of Apatinib, a novel receptor tyrosine kinase inhibitor selectively targeting VEGFR-2 in ALL cells...
February 28, 2018: Journal of Translational Medicine
https://www.readbyqxmd.com/read/29486282/novel-role-of-apatinib-as-a-multi-target-rtk-inhibitor-in-the-direct-suppression-of-hepatocellular-carcinoma-cells
#20
Xiaojin Li, Anjian Xu, Huihui Li, Bei Zhang, Bangwei Cao, Jian Huang
Although apatinib has been demonstrated with potential antitumor activity in multiple solid tumors, the underlying mechanism of apatinib for the treatment of hepatocellular carcinoma (HCC) remains unclear. In the present study, we explored if there are any direct suppression effects of apatinib on HCC cells and its relevant targets. We investigated the effect of apatinib on viability of five HCC cell lines and an intrahepatic cholangiocarcinoma cell line, and colony formation, apoptosis and migration of representative HCC cells in vitro; and HCC progression in a xenograft mouse model...
February 24, 2018: Biochimica et Biophysica Acta
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