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2016
DOI: 10.1080/17474124.2016.1209407
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Apatinib for the treatment of gastric cancer

Abstract: Apatinib's efficacy, tolerability and safety have been evaluated in one Phase II and one Phase III study in metastatic/advanced gastric cancer. In this review, we focus on the mechanism of action of apatinib, its pharmacokinetic profile and its clinical activity in the treatment of advanced/metastatic gastric cancer. Expert commentary: Unfortunately, as yet, there is no definitive biomarker data for apatinib in gastric cancer.

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Cited by 42 publications
(38 citation statements)
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“…For instance, BLU-667 is a potent RET inhibitor designed to target RET directly, which has successfully induced tumor regression without notable toxicity in patients harboring RET alterations, exhibiting enormous therapeutic potential (26). Finally, we chose apatinib for its broad antineoplastic efficacy (27)(28)(29)(30) and fewer side effects compared with sorafenib (30). Apatinib, a multikinase inhibitor, specifically targets VEGFR-2 to partially block the pathways of mitogenic and angiogenic, by which it plays an essential role in tumor oncogenesis and metastasis (31).…”
Section: Discussionmentioning
confidence: 99%
“…For instance, BLU-667 is a potent RET inhibitor designed to target RET directly, which has successfully induced tumor regression without notable toxicity in patients harboring RET alterations, exhibiting enormous therapeutic potential (26). Finally, we chose apatinib for its broad antineoplastic efficacy (27)(28)(29)(30) and fewer side effects compared with sorafenib (30). Apatinib, a multikinase inhibitor, specifically targets VEGFR-2 to partially block the pathways of mitogenic and angiogenic, by which it plays an essential role in tumor oncogenesis and metastasis (31).…”
Section: Discussionmentioning
confidence: 99%
“…When targeting to VEGFR-2, the tyrosine kinase activity of the cells was inhibited, resulting in the inhibition of VEGF/VEGFR-2 signaling pathway and subsequent inhibition of tumor angiogenesis and tumor progression. The process of inhibiting tumor angiogenesis can effectively reduce tumor progression and metastasis [30].…”
Section: Discussionmentioning
confidence: 99%
“…Thus, the therapy of targeting VEGF or VEGFR is mainly to focus on anti-angiogenesis. Apatinib, also known as Aitan (brand name in China) and developed independently by Shanghai Hengrui Pharmaceutical Co., Ltd (Shanghai, China) [22], is a typical representative of anti-angiogenesis agents for antineoplastic functions, which could induce apoptosis and suppress tumor proliferation either alone or in combination with chemotherapy across a variety of advanced solid malignancies [23][24][25][26][27][28]. What needs to be emphasized is that, the e cacy of apatinib is comparable to that of sorafenib or lenvatinib, but with more manageable safety pro le and faster therapeutic response [26, [29][30][31].…”
Section: Discussionmentioning
confidence: 99%