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Drugs. 2014 Jul;74(10):1111-25. doi: 10.1007/s40265-014-0243-3.
Pazopanib (Votrient(®)) is an orally administered multi-tyrosine kinase inhibitor that is approved in the EU, the US and other countries for the treatment of advanced renal cell carcinoma. Pazopanib predominantly inhibits vascular endothelial growth factor receptor-1, -2 and -3, platelet-derived growth factor receptor-α and -β, and the stem cell factor receptor c-Kit, resulting in inhibition of tumour angiogenesis, cell growth and survival. In randomized controlled trials in patients with advanced, predominantly clear-cell, renal cell carcinoma, progression-free survival (PFS) and the objective response rate were significantly greater in pazopanib recipients than in placebo recipients (VEG105192 trial), and pazopanib was noninferior to sunitinib with respect to PFS (COMPARZ study). In a patient-preference, crossover study involving 10 weeks of treatment with each drug (PISCES study), significantly more patients expressed a preference for pazopanib than for sunitinib, with their preference being based primarily on tolerability and quality-of-life issues. Health-related quality-of-life (HR-QOL) assessments generally favoured pazopanib over sunitinib in COMPARZ, and pazopanib did not cause deterioration in HR-QOL compared with placebo in VEG105192. Pazopanib caused less myelosuppression, hand-foot syndrome, mucositis/stomatitis, dysgeusia and fatigue than sunitinib, but more abnormal liver function tests. Therefore, pazopanib was noninferior to sunitinib with respect to efficacy in the treatment of advanced renal cell carcinoma, but had a differentiated tolerability profile, which affected HR-QOL and patient preference.
帕唑帕尼（Votrient(®)）是一种口服多靶点酪氨酸激酶抑制剂，在欧盟、美国和其他国家被批准用于治疗晚期肾细胞癌。帕唑帕尼主要抑制血管内皮生长因子受体-1、-2 和 -3、血小板衍生生长因子受体-α 和 -β 以及干细胞因子受体 c-Kit，从而抑制肿瘤血管生成、细胞生长和存活。在晚期、主要为透明细胞肾细胞癌患者的随机对照试验中，与安慰剂组相比，接受帕唑帕尼治疗的患者无进展生存期（PFS）和客观缓解率显著更高（VEG105192 试验），且在 PFS 方面，帕唑帕尼与舒尼替尼相比非劣效（COMPARZ 研究）。在一项涉及每种药物 10 周治疗的患者偏好、交叉研究（PISCES 研究）中，与舒尼替尼相比，明显更多的患者表示更喜欢帕唑帕尼，他们的偏好主要基于耐受性和生活质量问题。在 COMPARZ 中，一般来说，健康相关生活质量（HR-QOL）评估倾向于帕唑帕尼优于舒尼替尼，且在 VEG105192 中，与安慰剂相比，帕唑帕尼未导致 HR-QOL 恶化。与舒尼替尼相比，帕唑帕尼引起的骨髓抑制、手足综合征、黏膜炎/口腔炎、味觉障碍和疲劳较少，但导致更多的肝功能异常。因此，在治疗晚期肾细胞癌方面，帕唑帕尼与舒尼替尼疗效相当，但具有不同的耐受性特征，这影响了 HR-QOL 和患者偏好。
