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https://www.readbyqxmd.com/read/29029508/efficiency-of-low-dosage-apatinib-in-post-first-line-treatment-of-advanced-lung-adenocarcinoma
#1
Da-Xiong Zeng, Chang-Guo Wang, Wei Lei, Jian-An Huang, Jun-Hong Jiang
Chemotherapy is the standard treatment of in advanced lung adenocarcinoma patients without driver mutation. However, few drugs could be selected when diseases progressed after second-line treatment. As a small molecule inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2), apatinib was suggested mainly using in advanced gastric cancer. In this study, we showed the results of apatinib as second-line to fourth-line treatment in EGFR wild-type advanced lung adenocarcinoma patients. 16 EGFR wild-type advanced lung adenocarcinoma patients were administrated apatinib (250-500 mg/d) orally...
September 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/28969086/efficacy-and-safety-of-apatinib-in-stage-iv-sarcomas-experience-of-a-major-sarcoma-center-in-china
#2
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...
September 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28967981/pharmacokinetic-drug-interactions-of-apatinib-with-rifampin-and-itraconazole
#3
Xiaoyun Liu, Yifan Zhang, Qian Chen, Yan Zhan, Quanren Wang, Chaoying Hu, Chen Yu, Zitao Guo, Xiaoyan Chen, Dafang Zhong
Apatinib is a small-molecule tyrosine kinase inhibitor that has been approved for the treatment of patients with advanced-stage gastric cancer or gastroesophageal junction cancer who have progressed or recurred after at least 2 kinds of systemic chemotherapy. In vitro data indicate that cytochrome P450 (CYP) 3A4 is the primary CYP isoenzyme involved in the metabolism of apatinib. Pharmacokinetic drug-drug interactions of apatinib and (1) a CYP3A4 inducer (rifampin) or (2) a CYP3A inhibitor (itraconazole) were clinically evaluated in healthy volunteers...
October 2, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28935022/-report-of-successful-treatment-of-a-rectal-cancer-patient-with-endobronchial-%C3%A2-metastasis-by-bronchial-stent-implantation-combined-with-chemotherapy-and-apatinib
#4
Qiuqi Lin, Ling Ding, Cheng Chen, Yehan Zhu
The lungs are the most common sites of metastases from non-pulmonary malignancies. On the other hand, endobronchial metastases are rare. Various tumors have been associated with endobronchial metastasis, most commonly renal, breast and colorectal cancer. Advanced rectal cancerwith lung metastasis is common. However, endobronchial metastasis without lung metastasis of rectal cancer is rare, and easily misdiagnosed. We report one case of postoperative rectal cancer with endobronchial, pleuralcavity, pericardial cavitymetastasis, giving the comprehensive treatment of bronchial stentimplantation, chemotherapy, targeted drugs and remission...
September 20, 2017: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
https://www.readbyqxmd.com/read/28927587/ph-responsive-carboxymethyl-chitosan-derived-micelles-as-apatinib-carriers-for-effective-anti-angiogenesis-activity-preparation-and-in-vitro-evaluation
#5
Yixing Dai, Shuo Wang, Weibin Shi, Meidong Lang
In this study, carboxymethyl chitosan-graft-poly-(ε-caprolactone) copolymers (CMCS-g-PCL) were synthesized and used to encapsulate apatinib to prepare apatinib-loaded CMCS-g-PCL (CPA) micelles. CPA micelles' sizes were 100-150nm at pH 7.4 while aggregated to 300-350nm at pH 6.4, and the release rate at pH 6.4 was faster than pH 7.4, indicating CPA micelles have a pH-responsive activity. Furthermore, the release rate decreased with an increased grafting ratio of CMCS-g-PCL, which was shown by the results of release experiments from CPA-2 to CPA-10 micelles...
November 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28894382/apatinib-in-the-treatment-of-advanced-lung-adenocarcinoma-with-kras-mutation
#6
Da-Xiong Zeng, Chang-Guo Wang, Jian-An Huang, Jun-Hong Jiang
Activating KRAS mutations in lung adenocarcinoma are characterized with treatment resistance and poor prognosis. As a small molecule inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase, apatinib has been proven successful in advanced gastric cancer and breast cancer. In this study, we show the result of apatinib as salvage treatment in lung adenocarcinoma patients with KRAS mutation. Four advanced lung adenocarcinoma patients with KRAS mutation were orally administered apatinib (250 mg/d) after second-line treatment...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28892250/case-report-of-apatinib-mesylate-treatment-in-rare-advanced-tracheal-adenoid-cystic-carcinoma
#7
Hongmei Wang
A 57-year-old man was admitted to our department 10 years ago, diagnosed with tracheal adenoid cystic carcinoma. After discontinuing chemotherapy and radiotherapy, the disease recurred in December 2016. Apatinib mesylate (500 mg/day) was administered and computed tomography revealed that his symptoms were significantly relieved. Treatment with apatinib mesylate represents a novel method of treatment for tracheal adenoid cystic carcinoma.
September 11, 2017: Thoracic Cancer
https://www.readbyqxmd.com/read/28881773/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)...
August 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28870253/early-presence-of-anti-angiogenesis-related-adverse-events-as-a-potential-biomarker-of-antitumor-efficacy-in-metastatic-gastric-cancer-patients-treated-with-apatinib-a-cohort-study
#9
Xinyang Liu, Shukui Qin, Zhichao Wang, Jianming Xu, Jianping Xiong, Yuxian Bai, Zhehai Wang, Yan Yang, Guoping Sun, Liwei Wang, Leizhen Zheng, Nong Xu, Ying Cheng, Weijian Guo, Hao Yu, Tianshu Liu, Pagona Lagiou, Jin Li
BACKGROUND: Reliable biomarkers of apatinib response in gastric cancer (GC) are lacking. We investigated the association between early presence of common adverse events (AEs) and clinical outcomes in metastatic GC patients. PATIENTS AND METHODS: We conducted a retrospective cohort study using data on 269 apatinib-treated GC patients in two clinical trials. AEs were assessed at baseline until 28 days after the last dose of apatinib. Clinical outcomes were compared between patients with and without hypertension (HTN), proteinuria, or hand and foot syndrome (HFS) in the first 4 weeks...
September 5, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28860804/efficacy-and-safety-of-apatinib-treatment-for-advanced-esophageal-squamous-cell-carcinoma
#10
Jianqiang Li, Lifen Wang
OBJECTIVE: No standard chemotherapy is available for patients with advanced esophageal squamous cell carcinoma (ESCC) who have failed prior first-line chemotherapy. The aim of this study was to evaluate the efficacy and safety of apatinib, an oral VEGFR-2 inhibitor, as salvage treatment for advanced ESCC. PATIENTS AND METHODS: After apatinib dosing, the efficacy and toxicity were evaluated in 62 patients with pretreated advanced ESCC from 2014 to 2016 at Zhejiang Cancer Hospital...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28837148/apatinib-promotes-autophagy-and-apoptosis-through-vegfr2-stat3-bcl-2-signaling-in-osteosarcoma
#11
Kuisheng Liu, Tingting Ren, Yi Huang, Kunkun Sun, Xing Bao, Shidong Wang, Bingxin Zheng, Wei Guo
The cure rate of osteosarcoma has not improved in the past 30 years. The search for new treatments and drugs is urgently needed. Apatinib is a high selectivity inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2) tyrosine kinase, exerting promising antitumoral effect in various tumors. The antitumor effect of Apatinib in human osteosarcoma has never been reported. We investigated the effects of Apatinib in osteosarcoma in vitro and in vivo. Osteosarcoma patients with high levels of VEGFR2 have poor prognosis...
August 24, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28822888/apatinib-enhances-antitumour-activity-of-egfr-tkis-in-non-small-cell-lung-cancer-with-egfr-tki-resistance
#12
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...
October 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28816958/effective-apatinib-treatment-of-pleomorphic-liposarcoma-a-case-report
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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