University of Chicago, Chicago, Illinois 60637, USA.
Clin Cancer Res. 2010 Dec 15;16(24):5923-7. doi: 10.1158/1078-0432.CCR-10-0728. Epub 2010 Nov 8.
Pazopanib is an oral, multitargeted tyrosine kinase inhibitor that has been approved by the U.S. Food and Drug Administration for treatment of patients with advanced renal cell cancer on the basis of a randomized, double-blind, placebo-controlled, phase III trial, which showed that once a day dosing of 800 mg of pazopanib resulted in progression free survival of 9.2 months versus 4.2 months (P < 0.0001). Pazopanib thus joins sorafenib and sunitinib as one of the clinically available VEGF receptor (VEGFR)-targeted drugs for the treatment of patients with advanced clear cell renal cell cancer. The mechanism of action, preclinical and clinical data, and a comparison with the other drugs in its class are outlined below.
帕唑帕尼是一种口服、多靶点的酪氨酸激酶抑制剂,已被美国食品和药物管理局批准用于治疗晚期肾细胞癌患者,其依据是一项随机、双盲、安慰剂对照的 III 期临床试验,结果显示每天一次 800mg 帕唑帕尼的给药方案可使无进展生存期达到 9.2 个月,而安慰剂组为 4.2 个月(P<0.0001)。因此,帕唑帕尼与索拉非尼和舒尼替尼一起成为临床上可用于治疗晚期透明细胞肾细胞癌的血管内皮生长因子受体(VEGFR)靶向药物之一。以下概述了其作用机制、临床前和临床数据,并与该类中的其他药物进行了比较。