Related Experiment Video
Updated: Jul 5, 2026

Modeling Spontaneous Metastatic Renal Cell Carcinoma (mRCC) in Mice Following Nephrectomy
Published on: April 29, 2014
Axitinib for renal cell carcinoma
Guru Sonpavde1, Thomas E Hutson, Brian I Rini
1Genitourinary Oncology Program, Texas Oncology PA, Houston, TX 77598, USA.
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.
Insights
Axitinib is a new oral tyrosine kinase inhibitor showing promise for renal cell carcinoma (RCC) treatment. Clinical trials indicate favorable activity and toxicity profiles in patients previously treated for RCC.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Renal cell carcinoma (RCC) management has been transformed by targeted therapies like sunitinib, sorafenib, and temsirolimus.
- Bevacizumab plus interferon (IFN) is another therapeutic option for RCC.
- Axitinib (AG-013736) represents a novel oral, selective tyrosine kinase inhibitor.
Purpose of the Study:
- To review preclinical and clinical data supporting axitinib's development for renal cell carcinoma.
- To evaluate the efficacy and safety of axitinib in RCC treatment.
Main Methods:
- Preclinical studies assessing axitinib's inhibitory profile.
- Phase II clinical trials in patients with pretreated RCC.
Main Results:
- Axitinib potently inhibits vascular endothelial growth factor receptors (VEGFR-1, -2, -3) and platelet-derived growth factor receptors (PDGFR-alpha, -beta), as well as c-kit.
- Phase II trials demonstrated promising anti-cancer activity in RCC patients previously treated with sorafenib or cytokines.
- Axitinib exhibited a favorable toxicity profile in clinical studies.
Conclusions:
- Axitinib demonstrates significant preclinical potency and promising clinical activity in advanced renal cell carcinoma.
- The favorable safety profile supports further investigation and development of axitinib for RCC treatment.
Related Concept Videos
Acute Kidney Injury IV: Diagnostic Studies and Prevention
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
Inhibition of Cdk Activity
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Antihypertensive Drugs: Direct Renin Inhibitors