Axitinib for renal cell carcinoma

Guru Sonpavde, Thomas E Hutson, Brian I Rini
Expert Opinion on Investigational Drugs 2008, 17 (5): 741-8

BACKGROUND: The approval of sunitinib, sorafenib and temsirolimus has dramatically altered the management of renal cell carcinoma (RCC). Bevacizumab plus IFN may also be added to the therapeutic armamentarium. Axitinib (AG-013736) is an oral and selective tyrosine kinase inhibitor.

OBJECTIVE: Data supporting the development of axitinib for RCC are reviewed.

METHODS: Preclinical and clinical data available for axitinib for RCC are presented.

RESULTS: Axitinib inhibits VEGFR-1, VEGFR-2 and VEGFR-3 with picomolar potencies, and PDGFR-alpha, PDGFR-beta and c-kit with nanomolar potencies. Phase II clinical trials of axitinib in pretreated RCC following sorafenib or cytokine treatment have demonstrated promising activity accompanied by a favorable toxicity profile. Further development of axitinib for RCC is warranted.

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