多靶点酪氨酸激酶抑制剂舒尼替尼的研究进展

Advance in research of sunitinib,a multitargeted receptor tyrosine kinase inhibitor

近年来各种酪氨酸激酶抑制剂不断涌现,以酪氨酸激酶抑制剂为代表的分子靶向治疗已成为抗肿瘤研究的热点。舒尼替尼(sunitinib,商品名Sutent)是一种小分子多靶点酪氨酸激酶抑制剂,对血小板衍生生长因子受体(PDGFR)、血管内皮生长因子受体(VEGFR)、干细胞因子受体(C-Kit)等多种受体酪氨酸激酶具有抑制作用,已于2006年1月被美国FDA批准用于临床上晚期肾细胞癌(RCC)和对伊马替尼(ima-tinib)耐药和(或)治疗失败的胃肠道间质瘤(GIST)的治疗,并在其他多种肿瘤的临床试验中也显示显著抗肿瘤活性,文中综述了该药的临床前研究及临床研究进展。

Many tyrosine kinase inhibitors continue to emerge in recent years. As a representative of the molecular targets for anti-cancer therapy, tyrosine kinase inhibitors have become the spot in this field. Sunitinb （brand name： Sutent） is a small-molecule inhibitor of multiple receptor tyrosine kinases involved in platelet-derived growth factor receptor （PDGFR）, vascular endothelial growth factor receptor （VEGFR）, Kit receptor and other receptors. It was approved by the US Food and Administration （FDA） in January 2006 for the treatment of advanced renal cell carcinoma （RCC） and gastrointestinal stromal tumors （GIST） in patients who are resistant to imatinib or failed to therapy. Moreover, sunitinib had shown significant anti-tumor activities in other clinical trials. In this article, we reviewed the development of sunitinib in preclinical and clinical research.