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阿帕替尼:一种在多种实体瘤治疗中颇具前景的口服抗血管生成药物。

Apatinib: a promising oral antiangiogenic agent in the treatment of multiple solid tumors.

作者信息

Scott A J, Messersmith W A, Jimeno A

机构信息

Division of Hematology and Oncology, University of Colorado Cancer Center, Aurora, Colorado, USA.

出版信息

Drugs Today (Barc). 2015 Apr;51(4):223-9. doi: 10.1358/dot.2015.51.4.2320599.

DOI:10.1358/dot.2015.51.4.2320599
PMID:26020064
Abstract

Aberrant proangiogenic pathways have long been implicated in tumorigenesis and metastasis. Antiangiogenic therapies have shown efficacy in the treatment of a variety of solid tumors including lung, breast, colon, glioblastomas, and other solid tumor types. Apatinib, a small-molecule inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2), is an orally bioavailable agent currently being studied in multiple tumor types. Apatinib has shown a survival benefit in gastric cancer in a phase III trial and non-small cell lung cancer in a phase II trial. With a favorable side effect profile and improved outcomes, apatinib has demonstrated a substantial potential to augment therapeutic options in a variety of tumor types.

摘要

异常的促血管生成途径长期以来一直与肿瘤发生和转移有关。抗血管生成疗法已在包括肺癌、乳腺癌、结肠癌、胶质母细胞瘤和其他实体瘤类型在内的多种实体瘤治疗中显示出疗效。阿帕替尼是一种血管内皮生长因子受体2(VEGFR-2)的小分子抑制剂,是一种目前正在多种肿瘤类型中进行研究的口服生物可利用药物。阿帕替尼在一项III期试验中显示出对胃癌有生存获益,在一项II期试验中对非小细胞肺癌有生存获益。由于具有良好的副作用特征和改善的疗效,阿帕替尼已显示出在多种肿瘤类型中增加治疗选择的巨大潜力。

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