Axitinib for renal cell carcinoma.
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.
Sonpavde
Guru
G
Genitourinary Oncology Program, Texas Oncology PA, Houston, TX 77598, USA.
Hutson
Thomas E
TE
Rini
Brian I
BI
D020533:Angiogenesis Inhibitors / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000077784:Axitinib; D002292:Carcinoma, Renal Cell / Q000188:drug therapy* / Q000401:mortality; D002986:Clinical Trials as Topic; D018572:Disease-Free Survival; D004341:Drug Evaluation; D006801:Humans; D007093:Imidazoles / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D007191:Indazoles / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D007680:Kidney Neoplasms / Q000188:drug therapy* / Q000401:mortality
D020533:Angiogenesis Inhibitors; D007093:Imidazoles; D007191:Indazoles; D000077784:Axitinib