Sonpavde Guru, Hutson Thomas E, Rini Brian I
Genitourinary Oncology Program, Texas Oncology PA, Houston, TX 77598, USA.
Expert Opin Investig Drugs. 2008 May;17(5):741-8. doi: 10.1517/13543784.17.5.741.
BACKGROUND: The approval of sunitinib, sorafenib and temsirolimus has dramatically altered the management of renal cell carcinoma (RCC). Bevacizumab plus IFN may also be added to the therapeutic armamentarium. Axitinib (AG-013736) is an oral and selective tyrosine kinase inhibitor. OBJECTIVE: Data supporting the development of axitinib for RCC are reviewed. METHODS: Preclinical and clinical data available for axitinib for RCC are presented. RESULTS: Axitinib inhibits VEGFR-1, VEGFR-2 and VEGFR-3 with picomolar potencies, and PDGFR-alpha, PDGFR-beta and c-kit with nanomolar potencies. Phase II clinical trials of axitinib in pretreated RCC following sorafenib or cytokine treatment have demonstrated promising activity accompanied by a favorable toxicity profile. Further development of axitinib for RCC is warranted.
背景：舒尼替尼、索拉非尼和替西罗莫司的获批显著改变了肾细胞癌（RCC）的治疗方式。贝伐单抗加干扰素也可能被纳入治疗手段。阿昔替尼（AG - 013736）是一种口服选择性酪氨酸激酶抑制剂。 目的：综述支持阿昔替尼用于肾细胞癌治疗研发的数据。 方法：列出阿昔替尼用于肾细胞癌的临床前和临床数据。 结果：阿昔替尼对血管内皮生长因子受体-1（VEGFR-1）、血管内皮生长因子受体-2（VEGFR-2）和血管内皮生长因子受体-3（VEGFR-3）具有皮摩尔级别的抑制效力，对血小板衍生生长因子受体-α（PDGFR-α）、血小板衍生生长因子受体-β（PDGFR-β）和c-kit具有纳摩尔级别的抑制效力。阿昔替尼在索拉非尼或细胞因子治疗后预处理的肾细胞癌患者中进行的II期临床试验已显示出有前景的活性以及良好的毒性特征。阿昔替尼用于肾细胞癌的进一步研发是有必要的。
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