Section of Pharmacology and University Center DIFF - Drug Innovation Forward Future, Department of Molecular and Translational Medicine, University of Brescia, Viale Europa 11, 25124 Brescia, Italy; Unit of Molecular Therapy and Pharmacogenomic, AO Azienda Istituti Ospitalieri di Cremona, Viale Concordia 1, 26100 Cremona, Italy.
Unit of Molecular Therapy and Pharmacogenomic, AO Azienda Istituti Ospitalieri di Cremona, Viale Concordia 1, 26100 Cremona, Italy; Section of Experimental Oncology, Department of Clinical and Experimental Medicine, University of Parma, Via Università, 12, 43121 Parma, Italy.
Cancer Lett. 2016 Mar 28;372(2):187-91. doi: 10.1016/j.canlet.2016.01.014. Epub 2016 Jan 18.
Metastatic gastric cancer is a lethal disease characterized by a very short overall survival, underlining a critical need of new therapeutic options. Unfortunately, although several molecular targets have been investigated, only very few recently approved agents, such as trastuzumab in the HER2-positive setting and ramucirumab, led to a clinical improvement in the outcome of metastatic gastric cancer patients. VEGF (vascular endothelial growth factor) is one of the most potent angiogenic factors and is a signalling molecule secreted by many solid tumours. Since high VEGF expression is one of the characteristic features of gastric carcinomas, targeting VEGF is therefore considered as a promising therapeutic strategy for gastric cancer. In the scenario of possible new target therapies with particular regard to angiogenesis, apatinib is a novel receptor tyrosine kinase inhibitor selectively targeting VEGFR-2. It is an orally-bioavailable agent currently being studied in several solid tumour types showing a promising activity in gastric cancer. Due to the recent positive results as a third line of treatment for metastatic gastric cancer patients, apatinib may be an interesting and novel type of targeted treatment for metastatic gastric cancer in several lines of therapy. In this review, we summarize the available data of apatinib, mainly focused on the clinical aspect, in advanced/metastatic gastric cancer.
转移性胃癌是一种致命疾病,总生存期极短,这突显了对新治疗选择的迫切需求。不幸的是,尽管已经研究了多个分子靶点,但只有少数最近批准的药物,如曲妥珠单抗在 HER2 阳性环境中和雷莫芦单抗,导致转移性胃癌患者的结局得到了临床改善。VEGF(血管内皮生长因子)是最有效的血管生成因子之一,也是许多实体瘤分泌的信号分子。由于高 VEGF 表达是胃癌的特征之一,因此靶向 VEGF 被认为是胃癌的一种有前途的治疗策略。在可能的新靶向治疗方案中,特别是针对血管生成的治疗方案,阿帕替尼是一种新型的受体酪氨酸激酶抑制剂,选择性靶向 VEGFR-2。它是一种口服生物利用的药物,目前正在研究多种实体瘤类型,在胃癌中显示出有希望的活性。由于最近作为转移性胃癌三线治疗的阳性结果,阿帕替尼可能是转移性胃癌的一种有趣且新颖的靶向治疗方法,适用于多种治疗线。在这篇综述中,我们总结了阿帕替尼的现有数据,主要集中在晚期/转移性胃癌的临床方面。