帕唑帕尼，一种用于治疗肾细胞癌的强效口服小分子多靶点酪氨酸激酶抑制剂。
Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma.
作者信息
Sonpavde Guru, Hutson Thomas E, Sternberg Cora N
机构信息
Genitourinary Oncology Program, Texas Oncology, PA, US Oncology Research, 501 Medical Center Blvd, Webster, TX 77598, USA.
出版信息
Expert Opin Investig Drugs. 2008 Feb;17(2):253-61. doi: 10.1517/13543784.17.2.253.
BACKGROUND
The recent approvals of sunitinib, sorafenib and temsirolimus have revolutionized the management of renal cell carcinoma (RCC). Pazopanib (GW-786034) is a second-generation multitargeted tyrosine kinase inhibitor against VEGFR-1, 2 and 3, platelet-derived growth factor receptor (PDGFR)-alpha, PDGFR-beta and c-kit.
OBJECTIVE
Data supporting the development of pazopanib for RCC are reviewed.
METHODS
Preclinical and clinical data available for pazopanib are presented.
RESULTS
Preclinical evaluation has revealed excellent anti-angiogenic and anti-tumor activity in several mouse models. A Phase II clinical trial of pazopanib in untreated or cytokine/bevacizumab pretreated RCC has demonstrated promising activity accompanied by a favorable toxicity profile. A placebo-controlled Phase III trial is ongoing in untreated or cytokine-treated patients with RCC. Ongoing trials are further evaluating pazopanib in a variety of other malignancies.
背景
舒尼替尼、索拉非尼和替西罗莫司近期获批，彻底改变了肾细胞癌（RCC）的治疗方式。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（VEGFR）-1、2和3、血小板衍生生长因子受体（PDGFR）-α、PDGFR-β以及c - kit。
目的
综述支持帕唑帕尼用于治疗肾细胞癌的相关数据。
方法
列出帕唑帕尼可用的临床前和临床数据。
结果
临床前评估显示，帕唑帕尼在多种小鼠模型中具有出色的抗血管生成和抗肿瘤活性。帕唑帕尼在未经治疗或经细胞因子/贝伐单抗预处理的肾细胞癌患者中进行的II期临床试验已显示出有前景的活性，且毒性特征良好。一项在未经治疗或经细胞因子治疗的肾细胞癌患者中进行的安慰剂对照III期试验正在进行。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作用。
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