DEXUE FAN^1,#, WEI SU^2,#, ZHAOWEN BI³, XINXING WANG¹, XIANWEN XU¹, MINGZE MA⁴, LICHAO ZHU⁵, ZHENHAI ZHANG^1,3,*, JUNLIN GAO^2,*

Oncology Research, Vol.33, No.6, pp. 1459-1472, 2025, DOI:10.32604/or.2025.060407 - 29 May 2025

Abstract Objectives: Apatinib has been reported to be a promising treatment for sorafenib-resistant hepatocellular carcinoma (HCC) patients. However, the underlying mechanism remains ambiguous. The study aimed to explore the efficacy of apatinib in sorafenib-resistant HCC and the underlying mechanism both in vitro and in vivo. Methods: After observing epithelial-mesenchymal transformation (EMT) changes in HepG2 and HepG2/Sorafenib cells, we treated them with varying concentrations of apatinib to assess its impact on sorafenib-resistant HCC. Subsequently, specific inhibitors of c-Jun N-terminal kinase (JNK, SP600125) and extracellular signal-regulated kinase (ERK, PD98059) were introduced to investigate whether apatinib influenced sorafenib-resistant HCC via modulation… More >

XIAOXIAO HE¹, XUEQING ZHOU², JINPENG ZHANG², MINGFEI ZHANG², DANHONG ZENG², HENG ZHANG¹, SHUCAI YANG^2,*

BIOCELL, Vol.48, No.9, pp. 1331-1341, 2024, DOI:10.32604/biocell.2024.052625 - 04 September 2024

Abstract Objectives: This investigation aimed to elucidate the inhibitory impact of apatinib on the multidrug resistance of liver cancer both in vivo and in vitro. Methods: To establish a Hep3B/5-Fu resistant cell line, 5-Fu concentrations were gradually increased in the culture media. Hep3B/5-Fu cells drug resistance and its alleviation by apatinib were confirmed via flow cytometry and Cell Counting Kit 8 (CCK8) test. Further, Nuclear factor kappa B (NF-κB) siRNA was transfected into Hep3B/5-Fu cells to assess alterations in the expression of multidrug resistance (MDR)-related genes and proteins. Nude mice were injected with Hep3B/5-Fu cells to establish subcutaneous… More >

WEIXUE WANG^#, TONGTONG WANG^#, YAN ZHANG, TING DENG, HAIYANG ZHANG^*, YI BA^*

Oncology Research, Vol.32, No.3, pp. 489-502, 2024, DOI:10.32604/or.2023.046676 - 06 February 2024

Abstract Different from necrosis, apoptosis, autophagy and other forms of cell death, ferroptosis is a mechanism that catalyzes lipid peroxidation of polyunsaturated fatty acids under the action of iron divalent or lipoxygenase, leading to cell death. Apatinib is currently used in the third-line standard treatment of advanced gastric cancer, targeting the anti-angiogenesis pathway. However, Apatinib-mediated ferroptosis in vascular endothelial cells has not been reported yet. Tumor-secreted exosomes can be taken up into target cells to regulate tumor development, but the mechanism related to vascular endothelial cell ferroptosis has not yet been discovered. Here, we show that More >

Jianping Xu, Xiaoyan Liu, Sheng Yang, Yuankai Shi

Oncology Research, Vol.28, No.2, pp. 127-133, 2020, DOI:10.3727/096504019X15707896762251

Abstract Apatinib, an oral small molecular receptor tyrosine kinase inhibitor (TKI) developed first in China, exerts antiangiogenic and antineoplastic function through selectively binding and inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2). In this study, we aimed to explore the efficacy and safety profile of apatinib monotherapy, or combined with chemotherapy or endothelial growth factor receptor (EGFR)-TKI in heavily pretreated non-small cell lung cancer (NSCLC) patients with brain metastases. We performed a retrospective analysis for relapsed NSCLC patients with brain metastases from our institute, who received apatinib (250 mg or 500 mg p.o. qd) monotherapy, or… More >

Jing Tang^*1, Xu Yong Li^†1, Jing Bo Liang^‡, De Wu^§, Li Peng^¶, Xiaobing Li^¶

Oncology Research, Vol.27, No.6, pp. 635-641, 2019, DOI:10.3727/096504018X15288447760357

Abstract Apatinib is an oral TKI with antiangiogenic 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 antiangiogenic agent has been shown to be a 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. We treated a… More >