The safety of apatinib for the treatment of gastric cancer
The safety of apatinib for the treatment of gastric cancer
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DOI：
10.1080/14740338.2018.1535592
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发表时间：
2018-11-02
影响因子：
3.1
通讯作者：
Zhao, Lin
中科院分区：
文献类型：
--
作者：
Geng, Ruixuan;Song, Li;Zhao, Lin
简介：阿帕替尼是一种口服小分子血管内皮生长因子受体2抑制剂。在中国，它已被批准并适用于二线或二线以上全身治疗失败后的晚期胃癌。涵盖的领域：本综述总结了阿帕替尼的机制，临床应用和安全性评价。阿帕替尼耐受性良好，其最常见的不良反应包括手足综合征、高血压、蛋白尿和中性粒细胞减少。主要3/4级不良反应为手足综合征。专家意见：阿帕替尼是治疗晚期胃癌患者的有效、安全的药物，毒性反应可耐受、可控。但是，有出血倾向或有穿孔风险的患者应避免使用。需要在全球范围内对其有效性和安全性进行评估。此外，抗血管生成相关不良事件的早期出现可能预测阿帕替尼的药物疗效。缩略语列表：气相色谱法：胃癌; mOS：中位总生存期; TKI：酪氨酸激酶抑制剂; EGFR：表皮生长因子受体; HER2：人表皮生长因子受体2; VEGFR：血管内皮生长因子受体; mTOR：雷帕霉素的哺乳动物靶标; HGFR：肝细胞生长因子受体; HR：风险比; CI：置信区间; mPFS：中位无进展生存期; Tmax：中位达峰药物浓度时间; C-max：最大血药浓度; AUC（0- 24 h）：0 -24 h浓度-时间曲线下面积; CFDA：国家食品药品监督管理总局; FAS：全分析集; ORR：客观缓解率; DCR：疾病控制率; PR：部分缓解; SD：疾病稳定; MTD：最大耐受剂量; AE：不良事件; IC 50：50%中位抑制浓度
Introduction: Apatinib is an orally administered small-molecule vascular endothelial growth factor receptor 2 inhibitor. It has been approved and indicated for advanced gastric cancer after the failure of two or more lines of systemic therapy in China. Areas covered: This review summarizes the mechanisms, clinical applications and safety evaluations of apatinib. Apatinib is well tolerated, and its most common adverse effects include hand-foot syndrome, hypertension, proteinuria and neutropenia. Its major grade 3/4 adverse effect is hand-foot syndrome. Expert opinion: Apatinib is an effective and safe drug for advanced gastric cancer patients that shows tolerable and manageable toxicity. However, it should be avoided in patients with a bleeding tendency or at risk of perforation. Worldwide assessments of its efficacy and safety are needed. Additionally, the early presence of antiangiogenesis-related adverse events may predict the drug efficacy of apatinib. List of Abbreviations: GC: gastric cancer; mOS: median overall survival; TKI: tyrosine kinase inhibitor; EGFR: epidermal growth factor receptor; HER2: human epidermal growth factor receptor 2; VEGFR: vascular endothelial growth factor receptor; mTOR: mammalian target of rapamycin; HGFR: hepatocyte growth factor receptor; HR: hazard ratio; CI: confidence interval; mPFS: median progression-free survival; T-max: median time to peak drug concentration; C-max: maximum plasma drug concentration; AUC(0-24h): areas under the concentration-time curve 0-24 h; CFDA: China Food and Drug Administration; FAS: full analysis set; ORR: objective response rate; DCR: disease control rate; PR: partial response; SD: stable disease; MTD: maximum tolerated dose; AEs: adverse events; IC50: 50% median inhibitory concentration