Erasmus MC Cancer Institute, Department of Medical Oncology, ' s-Gravendijkwal 230, Room He-116, 3015 CE Rotterdam, The Netherlands.
Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14.
Pazopanib (GW786034, Votrient®) is a vascular endothelial growth factor receptor-focused multi-tyrosine kinase inhibitor involved in inhibiting the angiogenesis pathway. The agent was recently registered for use in soft tissue sarcomas, a group of diseases with a major unmet medical need.
The relevance of angiogenesis in soft tissue sarcomas is discussed. These data were the basis to decide on the development of pazopanib in these diseases. The clinical pharmacology of pazopanib, as far as practically relevant, is summarized. After the first observations of possible activity in soft tissue sarcomas in the Phase I study, a Phase II and subsequent randomized placebo-controlled Phase III study were performed and are being put into perspective in this review.
Pazopanib is an active drug for the treatment of chemotherapy-failing nonadipocytic soft tissue sarcomas. It almost triples progression-free survival significantly from 1.6 to 4.6 months in this heavily pretreated population. The safety profile is manageable, exemplified by the high dose intensity that can be achieved over time. Pazopanib can be considered as part of the standard of care for patients with soft tissue sarcomas.
帕唑帕尼(GW786034,Votrient®)是一种血管内皮生长因子受体靶向的多酪氨酸激酶抑制剂,可抑制血管生成途径。该药物最近被注册用于软组织肉瘤,这是一组具有重大未满足医疗需求的疾病。
讨论了血管生成在软组织肉瘤中的相关性。这些数据是决定在这些疾病中开发帕唑帕尼的基础。概述了帕唑帕尼的临床药理学,只要实际相关。在 I 期研究中首次观察到软组织肉瘤可能具有活性后,进行了 II 期和随后的随机安慰剂对照 III 期研究,并在本综述中进行了分析。
帕唑帕尼是一种治疗化疗失败的非脂肪性软组织肉瘤的有效药物。在这个预处理人群中,它将无进展生存期从 1.6 个月显著延长至 4.6 个月,几乎增加了两倍。其安全性可管理,表现在随着时间的推移可以实现高剂量强度。帕唑帕尼可以被认为是软组织肉瘤患者标准治疗的一部分。