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Expert Opin Investig Drugs. 2008 Feb;17(2):253-61. doi: 10.1517/13543784.17.2.253.

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

Author information

1
Genitourinary Oncology Program, Texas Oncology, PA, US Oncology Research, 501 Medical Center Blvd, Webster, TX 77598, USA. guru.sonpavde@usoncology.com

Abstract

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.

PMID:
18230058
DOI:
10.1517/13543784.17.2.253
[Indexed for MEDLINE]

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