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Jing Tang, Xu Yong Li, Jing Bo Liang, De Wu, Li Peng, Xiaobing Li
Apatinib is an oral TKI with anti-angiogenesis properties, and it is currently approved for the treatment of advanced gastric cancer in China. This agent has also been tested in other human solid tumors, including non-small cell lung cancer (NSCLC). Since the combination of chemotherapy and an anti-angiogenesis agent has been shown to be feasible strategy in NSCLC, it is conceivable that a similar approach combining apatinib with chemotherapy may yield clinical activity. With this in mind, we investigated the efficiency of apatinib in combination with pemetrexed or docetaxel in advanced NSCLC...
June 21, 2018: Oncology Research
Huihui Li, Yichang Fan, Fan Yang, Lei Zhao, Bangwei Cao
As a novel vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor, Apatinib has exhibited antitumor effects in a variety of solid tumors. Extracts of Chinese herbal medicines have emerged as a promising alternative option to increase the sensitivity of patients to chemotherapeutics while alleviating side effects. The present study aimed to investigate the effects of Apatinib and the traditional Chinese herb Tripterine on the proliferation, invasion and apoptosis of human hepatoma Hep3B cells...
July 2018: Oncology Letters
Yizhuo Wang, Qing Gou, Rongde Xu, Xiaoming Chen, Zejian Zhou
Objective: To compare the efficacy and safety profiles of sorafenib and apatinib in patients with intermediate- and advanced-stage hepatocellular carcinoma (HCC). Methods: This was a single-center, retrospective study where we collected the clinical data of 72 patients, diagnosed with intermediate or advanced HCC from January 2014 to December 2016. Depending on the treatment received, 38 patients were categorized into group S (sorafenib group) and 34 into group A (apatinib group)...
2018: OncoTargets and Therapy
Hong Zhu, Xiaojun Ma, Yaqin Zhao, Ji Duo
RATIONALE: Hepatocellular carcinoma (HCC) is a highly invasive cancer associated with high mortality rates. Although sorafenib is currently recommended as standard treatment for advanced HCC, its treatment efficacy is limited. Effective treatments for patients with advanced HCC that progresses on or after sorafenib treatment or patients who are intolerant of sorafenib remain an unmet medical need. PATIENT CONCERNS: We report an advanced HCC patient with many lung metastases who failed sorafenib treatment...
June 2018: Medicine (Baltimore)
Y He, S Liu, M E, C Wang, M Shi, G Liu, N Abiyasi
Apatinib is a novel oral, anti-tumor, angiogenic-targeting drug that can selectively target vascular endothelial growth factor receptor-2 (VEGFR-2). In clinical trials, this new tyrosine kinase inhibitor (TKI) has been shown to be an effective and safe treatment for a variety of malignancies. Currently, there is a lack of studies of patients with thymic carcinoma; therefore, we present a case of advanced thymic carcinoma treated with apatinib after chemotherapy failure with multiple lung metastases. This patient has been taking a dose of 500 mg of apatinib per day, and his efficacy has achieved partial response (PR), according to the RECIST 1...
May 2018: Journal of Biological Regulators and Homeostatic Agents
Hui Xie, Shengtao Tian, Haipeng Yu, Xueling Yang, Jia Liu, Huaming Wang, Fan Feng, Zhi Guo
Introduction: Radiofrequency ablation (RFA) is the foremost treatment option for advanced hepatocellular carcinoma (HCC), however, rapid and aggressive recurrence of HCC often occurs after RFA due to epithelial-mesenchymal transition process. Although combination of RFA with sorafenib, a molecular targeted agent, could attenuate the recurrence of HCC, application of this molecular targeted agent poses a heavy medical burden and oral administration of sorafenib also brings severe side effects...
2018: OncoTargets and Therapy
Haifeng Qiu, Jing Li, Qiuli Liu, Mei Tang, Yuan Wang
Apatinib is a novel tyrosine kinase inhibitor that targets VEGFR2 signal and exhibits potent anti-tumor effects in human cancers. In this study, we aim to investigate the efficacy of Apatinib in cervical cancer. The protein expression of VEGFR2 and its relationships with clinical parameters were investigated in a panel of cervical cancer patients. In vitro, a series of experiments were performed to detect the effects of Apatinib on the proliferation, apoptosis and cell cycle in cervical cancer cells. Both the immortalized cell lines and primary cultured tissues were used to investigate the synergy between Apatinib and chemotherapeutic drugs...
June 9, 2018: Cell Cycle
Jiuhuan Feng, Shukui Qin
Introduction: Methylsulfonic apatinib (hereinafter referred to as Apatinib) is a small-molecule angiogenesis inhibitor highly and selectively targeted to vascular endothelial growth factor receptor-2. At present, a series of basic and clinical studies have confirmed that Apatinib mono-therapy can inhibit the growth of different carcinomas. Our experiment aimed to determine whether there is a synergistic effect between the combination of the traditional cytotoxic chemotherapy drugs paclitaxel (TAX), oxaliplatin (L-OHP), 5-fluorouracil (5-FU), and Apatinib...
2018: OncoTargets and Therapy
Xi Cheng, Haoran Feng, Haoxuan Wu, Zhijian Jin, Xiaonan Shen, Jie Kuang, Zhen Huo, Xianze Chen, Haoji Gao, Feng Ye, Xiaopin Ji, Xiaoqian Jing, Yaqi Zhang, Tao Zhang, Weihua Qiu, Ren Zhao
Apatinib, a novel tyrosine kinase inhibitor (TKI), has been confirmed for its efficacy and safety in the treatment of advanced gastric carcinoma and some other solid tumors. However, the direct functional mechanisms of tumor lethality mediated by apatinib have not yet been fully characterized, and the precise mechanisms of drug resistance are largely unknown. Here, in this study, we demonstrated that apatinib could induce both apoptosis and autophagy in human colorectal cancer (CRC) via a mechanism that involved endoplasmic reticulum (ER) stress...
May 30, 2018: Cancer Letters
Xiuping Ding, Jujie Sun, Tingyong Fan, Baosheng Li
RATIONALE: Despite the approval of antiangiogenic therapy for high grade glioma (HGG) patients, survival benefits are still limited. New treatment plans have always been developed to improve the survival. PATIENT CONCERNS: A 26-year-old woman was admitted to our hospital for distending pain of head and eye. DIAGNOSES: Resonance imaging (MRI) revealed a large spherical heterogeneously enhancing, mixed cystic and solid mass in the right frontal region, and the midline shifted...
June 2018: Medicine (Baltimore)
Feng Li, Zhichao Liao, Chao Zhang, Jun Zhao, Ruwei Xing, Sheng Teng, Jin Zhang, Yun Yang, Jilong Yang
Sarcomas are a group of malignant tumors originating from mesenchymal tissue with a variety of cell subtypes. Despite several major treatment breakthroughs, standard treatment using surgery, radiation, and chemotherapy has failed to improve overall survival. Therefore, there is an urgent need to explore new strategies and innovative therapies to further improve the survival rates of patients with sarcomas. Pathological angiogenesis has an important role in the growth and metastasis of tumors. Vascular endothelial growth factor (VEGF) and vascular endothelial growth factor receptors (VEGFRs) play a central role in tumor angiogenesis and represent potential targets for anticancer therapy...
May 11, 2018: Oncotarget
Xiaowu Li, Lechao Le, Liang Han, Youwei Zhang, Sanyuan Sun
OBJECTIVE: To evaluate the short-term efficacy and safety of apatinib alone or combined with chemotherapy in the treatment of advanced squamous cell lung cancer. METHODS: Forty patients with advanced squamous cell lung carcinoma were enrolled in this study, who were treated in Xuzhou Central Hospital from 2014 to 2015. All patients underwent first-line or more chemotherapy. Patients were administrated with apatinib 425 mg/day, alone or combined with chemotherapy...
July 2017: Indian Journal of Cancer
Jun Wu, Jing Wang, Qiang Su, Wei Ding, Teng Li, Junxian Yu, Bangwei Cao
Background: Traditional chemotherapy and molecular targeted therapy have shown modest effects on the survival of patients with pancreatic cancer. The current study aimed to investigate the antitumor effects of apatinib, Astragalus polysaccharide (APS), and the combination of both the drugs in pancreatic cancer cells and further explore the molecular mechanisms in vitro. Materials and methods: Expression of vascular endothelial growth factor receptor-2 (VEGFR-2) in human pancreatic cancer cell lines ASPC-1, PANC-1, and SW1990 was detected by Western blotting...
2018: OncoTargets and Therapy
Yang Zhao, Ye Chen, Ke Cheng, Zhi-Ping Li, Hao Zeng, Ji-Yan Liu
Renal Ewing sarcoma (RES) is an extremely rare disease. The standard treatment for this disease is lacking, and clinical experience needs to be accumulated. Here, we report a case of RES that rapidly developed to metastatic disease and was refractory to radiotherapy and chemotherapy; however, the case obtained a partial response based on Choi criteria by orally taking antiangiogenic drug apatinib. Our case suggests that apatinib may be a therapeutic option for RES.
May 18, 2018: Anti-cancer Drugs
Y Yang, X Pei, M Yang
WHAT IS KNOWN AND OBJECTIVES: Gastric cancer is the most common gastrointestinal malignant tumour in China, which rarely metastasizes into the central nervous system. However, brain metastasis leads to increased risk of death. CASE SUMMARY: Here, we report a case of brain metastasis from gastric cancer, which was treated with apatinib and continual nutritional support, with a survival time of 2 years. WHAT IS NEW AND CONCLUSION: The combination of apatinib and continual nutritional support may be an option for the treatment of brain metastasis from gastric cancer...
May 18, 2018: Journal of Clinical Pharmacy and Therapeutics
Chenxi Hu, Panrong Zhu, Youyou Xia, Kaiyuan Hui, Mei Wang, Xiaodong Jiang
PURPOSE: To determine if inhibiting neuropilin-1 (NRP-1) affects the radiosensitivity of NSCLC cells through a vascular endothelial growth factor receptor 2 (VEGFR2)-independent pathway, and to assess the underlying mechanisms. METHODS: The expression of VEGFR2, NRP-1, related signaling molecules, abelson murine leukemia viral oncogene homolog 1 (ABL-1), and RAD51 were determined by RT-PCR and Western blotting, respectively. Radiosensitivity was assessed using the colony-forming assay, and the cell apoptosis were analyzed by flow cytometry...
May 17, 2018: Journal of Cancer Research and Clinical Oncology
Si-Qi Feng, Guang-Ji Wang, Jing-Wei Zhang, Yuan Xie, Run-Bin Sun, Fei Fei, Jing-Qiu Huang, Ying Wang, Ji-Ye Aa, Fang Zhou
Apatinib, a small-molecule inhibitor of VEGFR-2, has attracted much attention due to its encouraging anticancer activity in third-line clinical treatment for many malignancies, including non-small cell lung cancer (NSCLC). Its usage in second-line therapy with chemotherapeutic drugs is still under exploration. In this study we investigated the antitumor effect of apatinib combined with docetaxel against NSCLC and its cellular pharmacokinetic basis. A549 xenograft nude mice were treated with apatinib (100 mg/kg every day for 20 days) combined with docetaxel (8 mg/kg, ip, every four days for 5 times)...
May 17, 2018: Acta Pharmacologica Sinica
Wei Wang, Lin Zhang, Yan Xie, Tianchang Zhen, Gongzhang Su, Qi Zang
Targeted therapy is commonly used for treating advanced malignant tumors. Compared with cytotoxic drugs, targeted drugs have the characteristics of good curative results, less adverse effects, and convenient oral administration. Hence, they are especially suitable for patients with cancer who are not able to tolerate chemotherapy. Anti-angiogenic therapy can achieve the objective by inhibiting the formation of new blood vessels in tumors. Apatinib is a novel tyrosine kinase inhibitor targeting the intracellular domain of vascular endothelial growth factor receptor-2...
2018: OncoTargets and Therapy
H M Lü, M W Zhang, L M Niu, H A Zeng, M Yan
Objective: To assess the clinical efficacy and adverse outcomes of apatinib mesylate for the treatment of multi-drug resistant advanced breast cancer. Methods: A total of 24 patients with multi-drug-resistant advanced breast cancer who underwent apatinib mesylate treatment were retrospectively analyzed at the Diagnosis and Treatment Center for Breast Cancer of Henan Cancer Hospital. Patients were reviewed every 4 weeks after initial treatment and then every 8 weeks after stable disease. Objective response rate (ORR), progression free survival (PFS), overall survival (OS) , toxicity and adverse outcomes of apatinib mesylate treatment were evaluated by imaging examinations...
April 24, 2018: Zhonghua Yi Xue za Zhi [Chinese medical journal]
Su Yudong, Meng Zhaoting, Wang Xinyue, Lin Li, Xu Xiaoyan, Zuo Ran, Chen Jinliang, Chen Peng
Thymic carcinoma (TC) is a rare malignant tumor of the mediastinum with occult onset, rapid development, and poor prognosis. Surgery is the main treatment for early TC, but the majority of patients are diagnosed at Masaoka-Koga stage III or IV with local invasion or distant metastasis. Platinum and anthracyclines are currently considered key components of first-line chemotherapy for advanced TC; however, there are no standard treatment plans for patients who are refractory to first-line and further chemotherapy...
May 8, 2018: Thoracic Cancer
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