Sonpavde Guru, Hutson Thomas E, Sternberg Cora N
Texas Oncology, USA.
Drugs Today (Barc). 2009 Sep;45(9):651-61.
Pazopanib (GW-786034) is a second-generation multitargeted tyrosine kinase inhibitor against VEGFR1, -2 and -3, PDGFRalpha, PDGFRbeta and c-Kit. Preclinical evaluation has revealed excellent anti-angiogenic and antitumor activity in several tumors. A phase II clinical trial of pazopanib in untreated or cytokine/bevacizumab-pretreated renal cell carcinoma (RCC) has demonstrated promising activity accompanied by a favorable toxicity profile. A placebo-controlled phase III trial in untreated or cytokine-treated patients with RCC demonstrated a significant improvement in progression-free survival. Ongoing trials are further evaluating pazopanib in a variety of other malignancies.
帕唑帕尼(GW - 786034)是一种第二代多靶点酪氨酸激酶抑制剂,可作用于血管内皮生长因子受体1、-2和-3(VEGFR1、-2和-3)、血小板衍生生长因子受体α(PDGFRα)、血小板衍生生长因子受体β(PDGFRβ)和干细胞生长因子受体(c-Kit)。临床前评估显示,其在多种肿瘤中具有出色的抗血管生成和抗肿瘤活性。一项关于帕唑帕尼治疗未经治疗或经细胞因子/贝伐单抗预处理的肾细胞癌(RCC)的II期临床试验已证明其具有良好的活性,且毒性特征良好。一项在未经治疗或经细胞因子治疗的RCC患者中进行的安慰剂对照III期试验表明,无进展生存期有显著改善。正在进行的试验正在进一步评估帕唑帕尼在多种其他恶性肿瘤中的疗效。