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Lijun Liang, Kaiyuan Hui, Chenxi Hu, Yixuan Wen, Shikun Yang, Panrong Zhu, Lei Wang, Youyou Xia, Yun Qiao, Wen Sun, Jiayan Fei, Ting Chen, Fenghua Zhao, Baocheng Yang, Xiaodong Jiang
BACKGROUND: The efficacy and safety of multikinase inhibitor anlotinib have been confirmed in the treatment of advanced non-small cell lung cancer (NSCLC). However, the direct functional mechanisms of tumor lethality mediated by anlotinib were not fully elucidated, and the underlying mechanisms related to resistance remain largely elusive. METHODS: Cell viability, colony formation, apoptosis and tumor growth assays were performed to examine the effect of anlotinib on lung cancer cells in vitro and in vivo...
February 12, 2019: Journal of Experimental & Clinical Cancer Research: CR
Gangyang Wang, Mengxiong Sun, Yafei Jiang, Tao Zhang, Wei Sun, Hongsheng Wang, Fei Yin, Zhuoying Wang, Weilin Sang, Jing Xu, Min Mao, Dongqing Zuo, Zifei Zhou, Chongren Wang, Zeze Fu, Zongyi Wang, Zhenfeng Duan, Yingqi Hua, Zhengdong Cai
Osteosarcoma is the most common primary malignant bone tumor in children and adolescents, with highly aggressive behavior and early systemic metastasis. The survival rates for osteosarcoma remain unchanged over the past two decades. Studies aiming to find new or alternative therapies for patients with refractory osteosarcoma are urgently needed. Anlotinib, a novel multi-targeted tyrosine kinase inhibitor (TKI), has exhibited encouraging clinical activity in NSLCC and soft tissue sarcoma, whereas its effect on osteosarcoma has not been studied...
February 4, 2019: International Journal of Cancer. Journal International du Cancer
Changkun Huang, Xuan Zhu, Wei Xiong, Xiaokun Zhao, Ran Xu
RATIONALE: Primary osteosarcoma of the kidney is a very rare subtype of renal neoplasms. There are only 27 cases reported in the literature since 1936. In addition, it has a high risk of metastasis and very low survival rate. PATIENT'S CONCERNS: In this report, we present a case of unique large osteosarcoma originated from the left kidney (21 cm × 18 cm × 11 cm) with lung metastasis. A 48-year-old female patient presented with intermittent abdominal distension and gross hematuria...
January 2019: Medicine (Baltimore)
Xiaoyan Si, Li Zhang, Hanping Wang, Xiaotong Zhang, Mengzhao Wang, Baohui Han, Kai Li, Qiming Wang, Jianhua Shi, Zhehai Wang, Ying Cheng, Yuankai Shi, Weiqiang Chen, Xiuwen Wang, Yi Luo, Kejun Nan, Faguang Jin
BACKGROUND: Anlotinib is an oral tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor, fibroblast growth factor receptor, platelet-derived growth factor receptor, and stem cell factor receptor (c-Kit). In the phase III ALTER-0303 trial (Clinical Trial Registry ID: NCT 02388919), anlotinib significantly improved overall survival versus placebo in advanced non-small cell lung cancer patients who had received at least two previous chemotherapy and epidermal growth factor receptor/anaplastic lymphoma kinase targeted therapy regimens...
January 21, 2019: Thoracic Cancer
Hui-Min Chen, Ge Feng
Background: Intra-abdominal desmoplastic small round cell tumor (IADSRCT) is a highly invasive malignant tumor that is rare in clinical practice. Anlotinib is a multitarget receptor tyrosine kinase inhibitor which inhibits vascular endothelial growth factor receptor (VEGFR) 1-3, fibroblast growth factor receptor (FGFR) 1-4, platelet-derived growth factor receptors (PDGFR) α/β, c-Kit, and Met. In our study, we present a record of IADSRCT which was validly treated by anlotinib. Case presentation: A 38-year-old man was admitted due to anterior abdominal wall nodule for 1 month...
2019: OncoTargets and Therapy
Jun Lu, Hua Zhong, Tianqing Chu, Xueyan Zhang, Rong Li, Jiayuan Sun, Runbo Zhong, Yuqin Yang, Mohammad Shah Alam, Yuqing Lou, Jianlin Xu, Yanwei Zhang, Jun Wu, Xiaowei Li, Xiaodong Zhao, Kai Li, Liming Lu, Baohui Han
BACKGROUND: Anlotinib has been demonstrated in clinical trials to be effective in prolonging the progression-free survival (PFS) and overall survival (OS) of refractory advanced non-small cell lung cancer (NSCLC) patients. However, the underlying molecular mechanisms and predictive biomarkers of anlotinib are still unclear. METHODS: A retrospective analysis of anlotinib administered to 294 NSCLC patients was performed to screen for underlying biomarkers of anlotinib-responsive patients...
December 21, 2018: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
Xin-Zu Chen
No abstract text is available yet for this article.
November 29, 2018: JAMA Oncology
Guoshuang Shen, Fangchao Zheng, Dengfeng Ren, Feng Du, Qiuxia Dong, Ziyi Wang, Fuxing Zhao, Raees Ahmad, Jiuda Zhao
Anlotinib is a new, orally administered tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptors (PDGFR), and c-kit. Compared to the effect of placebo, it improved both progression-free survival (PFS) and overall survival (OS) in a phase III trial in patients with advanced non-small-cell lung cancer (NSCLC), despite progression of the cancer after two lines of prior treatments. Recently, the China Food and Drug Administration (CFDA) approved single agent anlotinib as a third-line treatment for patients with advanced NSCLC...
September 19, 2018: Journal of Hematology & Oncology
Wenshuai Liu, Quan Jiang, Yuhong Zhou
Soft-tissue sarcoma (STS) is a group of rare but highly heterogeneous neoplasms. Systemic treatment with cytotoxic chemotherapy and targeted agents is one of the main therapeutic modalities in patients with unresectable or metastatic disease, while adjuvant and neoadjuvant chemotherapy for adult-type sarcomas remain controversial. Although an anthracycline (doxorubicin) and ifosfamide remain the cornerstone for chemotherapy, advances have been made recently to exceed its limited efficacy, other agents such as trabectedin, eribulin have been approved...
August 2018: Chinese Clinical Oncology
Chao He, Tingting Wu, Yongqiang Hao
Although anlotinib, a multi-targeted receptor tyrosine kinase inhibitor has been reported have antitumor effects in many preclinical and clinical trials, little is known about its effect on hepatocellular carcinoma (HCC). Here, we have shown the antitumor effects of anlotinib on HCC. Data indicated that anlotinib application significantly inhibited HCC cell viability, proliferation, colony formation, and prompted apoptosis in vitro. Furthermore, animal experiments also illustrated that anlotinib alleviated HCC progression...
September 18, 2018: Biochemical and Biophysical Research Communications
Yongkun Sun, Feng Du, Ming Gao, Qinghai Ji, Zhendong Li, Yuan Zhang, Zhuming Guo, Jun Wang, Xiangjin Chen, Jinwan Wang, Yihebali Chi, Pingzhang Tang
BACKGROUND: The prognosis of advanced or metastatic medullary thyroid carcinoma (MTC) is poor, and there are few therapeutic options. Anlotinib has previously shown promising antitumor activity on MTC in preclinical models and a Phase I study. This Phase II clinical trial was devised to confirm the antitumor activity of anlotinib in patients with advanced or metastatic MTC. METHODS: Patients with unresectable locally advanced or metastatic MTC received once daily oral anlotinib 12 mg, two weeks on/one week off, until disease progression, death, unacceptable toxicity, or withdrawal of consent for any reason...
November 2018: Thyroid: Official Journal of the American Thyroid Association
Xianhui Ruan, Xianle Shi, Qiman Dong, Yang Yu, Xiukun Hou, Xinhao Song, Xi Wei, Lingyi Chen, Ming Gao
There is no effective treatment for patients with poorly differentiated papillary thyroid cancer or anaplastic thyroid cancer (ATC). Anlotinib, a multi-kinase inhibitor, has already shown antitumor effects in various types of carcinoma in a phase I clinical trial. In this study, we aimed to better understand the effect and efficacy of anlotinib against thyroid carcinoma cells in vitro and in vivo. We found that anlotinib inhibits the cell viability of papillary thyroid cancer and ATC cell lines, likely due to abnormal spindle assembly, G2/M arrest, and activation of TP53 upon anlotinib treatment...
January 1, 2019: Endocrine-related Cancer
Baohui Han, Kai Li, Qiming Wang, Li Zhang, Jianhua Shi, Zhehai Wang, Ying Cheng, Jianxing He, Yuankai Shi, Yizhuo Zhao, Hao Yu, Yang Zhao, Weiqiang Chen, Yi Luo, Lin Wu, Xiuwen Wang, Robert Pirker, Kejun Nan, Faguang Jin, Jian Dong, Baolan Li, Yan Sun
Importance: Anlotinib is a novel multitarget tyrosine kinase inhibitor for tumor angiogenesis and proliferative signaling. A phase 2 trial showed anlotinib to improve progression-free survival with a potential benefit of overall survival, leading to the phase 3 trial to confirm the drug's efficacy in advanced non-small cell lung cancer (NSCLC). Objective: To investigate the efficacy of anlotinib on overall survival of patients with advanced NSCLC progressing after second-line or further treatment...
November 1, 2018: JAMA Oncology
Yahiya Y Syed
Following a once-daily on days 1-14 of each 21-day cycle regimen, plasma concentrations of anlotinib reached maximum on day 14 and decreased subsequently with the 7-day rest period until the start of the next treatment cycle [2].
August 2018: Drugs
Xiaoyan Si, Li Zhang, Hanping Wang, Xiaotong Zhang, Mengzhao Wang, Baohui Han, Kai Li, Qiming Wang, Jianhua Shi, Zhehai Wang, Yin Cheng, Jianxing He, Yuankai Shi, Weiqiang Chen, Xiuwen Wang, Yi Luo, Kejun Nan, Faguang Jin, Baolan Li, Yinlan Chen, Jianying Zhou, Donglin Wang
OBJECTIVES: Anlotinib is a novel multi-target tyrosine Kinase inhibitor that inhibits VEGFR2/3, FGFR1-4, PDGFD α/β, c-Kit and Ret. In the phase III ALTER-0303 trial (Clinical Trial Registry ID: NCT 02388919), anlotinib significantly improved overall survival versus placebo in advanced non-small-cell lung cancer (NSCLC) patients who had received at least two previous chemotherapy and epidermal growth factor receptor/anaplastic lymphoma kinase targeted therapy regimens. This study assessed quality of life (QoL) in these patients...
August 2018: Lung Cancer: Journal of the International Association for the Study of Lung Cancer
Yahiya Y Syed
Jiangsu Chia-Tai Tianqing Pharmaceutical and Advenchen Laboratories are co-developing anlotinib (Focus V® ) for the treatment of advanced cancer. Anlotinib is an oral small molecule inhibitor of multiple receptor tyrosine kinases, with a broad spectrum of inhibitory effects on tumour angiogenesis and growth. Anlotinib is approved in China for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have undergone progression or recurrence after ≥ 2 lines of systemic chemotherapy...
July 2018: Drugs
Yihebali Chi, Zhiwei Fang, Xiaonan Hong, Yang Yao, Ping Sun, Guowen Wang, Feng Du, Yongkun Sun, Qiong Wu, Guofan Qu, Shusen Wang, Jianmin Song, Jianchun Yu, Yongkui Lu, Xia Zhu, Xiaohui Niu, Zhiyong He, Jinwan Wang, Hao Yu, Jianqiang Cai
Purpose: The prognosis for patients with refractory soft-tissue sarcoma (STS) is dismal. Anlotinib has previously shown antitumor activity on STS in preclinical and phase I studies. Patients and Methods: Patients 18 years and older, progressing after anthracycline-based chemotherapy, naïve from angiogenesis inhibitors, with at least one measurable lesion according to RECIST 1.1, were enrolled. The main subtypes eligible were undifferentiated pleomorphic sarcoma (UPS), liposarcoma (LPS), leiomyosarcoma (LMS), synovial sarcoma (SS), fibrosarcoma (FS), alveolar soft-part sarcoma (ASPS), and clear cell sarcoma (CCS)...
November 1, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Yudong Su, Zhaoting Meng, Xiaoyan Xu, XinYue Wang, Ran Zuo, Yunxia Hou, Kai Li, Peng Chen
In recent years, the number of advanced non-small cell lung cancer (NSCLC) patients has gradually increased, and the treatment methods have also been significantly increased. However, there are no standard treatment plans at home and abroad for third-line and above patients who are refractory to targeted therapy epidermal growth factor receptor (EGFR)/anaplastic lymphoma kinase (ALK) or chemotherapy. The clinical treatment effect is also not satisfactory. Anlotinib is a novel TKI targeting the vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptor (PDGFR) and c-Kit...
May 20, 2018: Zhongguo Fei Ai za Zhi, Chinese Journal of Lung Cancer
Chen-Chun Zhong, Feng Chen, Jun-Ling Yang, Wei-Wei Jia, Li Li, Chen Cheng, Fei-Fei Du, Su-Ping Zhang, Cheng-Ying Xie, Na-Ting Zhang, Olajide E Olaleye, Feng-Qing Wang, Fang Xu, Li-Guang Lou, Dong-Ying Chen, Wei Niu, Chuan Li
Anlotinib is a new oral tyrosine kinase inhibitor; this study was designed to characterize its pharmacokinetics and disposition. Anlotinib was evaluated in rats, tumor-bearing mice, and dogs and also assessed in vitro to characterize its pharmacokinetics and disposition and drug interaction potential. Samples were analyzed by liquid chromatography/mass spectrometry. Anlotinib, having good membrane permeability, was rapidly absorbed with oral bioavailability of 28%-58% in rats and 41%-77% in dogs. Terminal half-life of anlotinib in dogs (22...
June 2018: Acta Pharmacologica Sinica
Binyan Lin, Xiuming Song, Dawei Yang, Dongsheng Bai, Yuyuan Yao, Na Lu
Tumor cells recruit vascular endothelial cells and circulating endothelial progenitor cells to form new vessels to support their own growth and metastasis. VEGF, PDGF-BB and FGF-2 are three major pro-angiogenic factors and applied to promote angiogenesis. In this research, we demonstrated that anlotinib, a potent multi-tyrosine kinases inhibitor (TKI), showed a significant inhibitory effect on VEGF/PDGF-BB/FGF-2-induced angiogenesis in vitro and in vivo. Wound healing assay, chamber directional migration assay and tube formation assay indicated that anlotinib inhibited VEGF/PDGF-BB/FGF-2-induced cell migration and formation of capillary-like tubes in endothelial cells...
May 15, 2018: Gene
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