Adis, 41 Centorian Drive, Mairangi Bay, Auckland, New Zealand.
BioDrugs. 2010 Oct 1;24(5):279-86. doi: 10.2165/11205480-000000000-00000.
Pazopanib is an orally administered, multi-tyrosine kinase inhibitor that interrupts tumor growth in renal cell carcinoma. In a randomized, double-blind, placebo-controlled, multinational trial in patients with locally advanced or metastatic renal cell carcinoma, the median progression-free survival (PFS) of patients who were treated with pazopanib 800 mg once daily was significantly longer than that of placebo recipients (9.2 vs 4.2 months; hazard ratio 0.46 [95% CI 0.34, 0.62]). In prespecified analyses in treatment-naive and cytokine-pretreated patients, grouped according to prior treatment history, age, sex, Memorial Sloan-Kettering Cancer Center risk category, and Eastern Cooperative Oncology Group performance status, median PFS was significantly longer in pazopanib than placebo recipients in all subgroups. Pazopanib recipients also had a significantly higher overall response rate than placebo recipients; in pazopanib recipients, the median time to response was 11.9 weeks and the median duration of response was 58.7 weeks. Oral pazopanib had an acceptable tolerability profile in patients with advanced renal cell carcinoma. Adverse events were common in pazopanib and placebo recipients and were mostly of mild to moderate severity.
帕唑帕尼是一种口服的多酪氨酸激酶抑制剂，可中断肾细胞癌的肿瘤生长。在一项针对局部晚期或转移性肾细胞癌患者的随机、双盲、安慰剂对照、多中心试验中，接受帕唑帕尼 800mg 每日一次治疗的患者的中位无进展生存期（PFS）明显长于安慰剂组（9.2 对 4.2 个月；风险比 0.46 [95%CI 0.34, 0.62]）。根据既往治疗史、年龄、性别、纪念斯隆-凯特琳癌症中心风险类别和东部合作肿瘤学组表现状态，在未经治疗和细胞因子预处理的患者中预先设定的分析中，按治疗史、年龄、性别、纪念斯隆-凯特琳癌症中心风险类别和东部合作肿瘤学组表现状态分组，与安慰剂组相比，帕唑帕尼组的中位 PFS 在所有亚组中均显著延长。帕唑帕尼组的总缓解率也显著高于安慰剂组；在帕唑帕尼组中，中位缓解时间为 11.9 周，中位缓解持续时间为 58.7 周。口服帕唑帕尼在晚期肾细胞癌患者中的耐受性良好。帕唑帕尼和安慰剂组均常见不良反应，且大多为轻至中度。
