Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma

被引：83

作者：

Sonpavde, Guru ^{[1
]}

Hutson, Thomas E.

Sternberg, Cora N. ^{[1
]}

机构：

[1] San Camillo & Forlanini Hosp, Rome, Italy

来源：

EXPERT OPINION ON INVESTIGATIONAL DRUGS | 2008年 / 17卷 / 02期

基金：

英国医学研究理事会;

关键词：

multitargeted tyrosine kinase inhibitor; pazopanib; renal cell carcinoma;

D O I：

10.1517/13543784.17.2.253

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 11 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.

引用

页码：253 / 261

页数：9

共 52 条

[1] A strategy for the design of multiplex inhibitors for kinase-mediated signalling in angiogenesis [J].