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Updated: Jun 19, 2026

A Simple Bioassay for the Evaluation of Vascular Endothelial Growth Factors
Published on: March 15, 2016
Axitinib--a selective inhibitor of the vascular endothelial growth factor (VEGF) receptor
1National Cancer Institute, Medical Oncology Branch, Center for Cancer Research, Bethesda, MD 20892, USA.
Abstract:
An improved understanding of the molecular biology involved in many solid tumors has led to the development of novel targeted agents. Axitinib is a potent and selective inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases 1, 2, and 3. This review presents preclinical and clinical data available for axitinib, including findings from key phase II clinical trials in a wide variety of tumors including melanomas and renal, pancreatic, thyroid, breast, lung, and colorectal carcinomas. The differences between axitinib and other VEGFR inhibitors are explored and details of the possible use of blood pressure elevation and erythropoietin blood levels as predictive markers of VEGF/VEGFR pathway inhibition are outlined. Ongoing Phase III studies in pancreatic and metastatic renal cell carcinoma should help to determine the optimum utilization of these agents at the appropriate stage of disease.
Insights
Axitinib, a targeted therapy, shows promise in treating various solid tumors by inhibiting vascular endothelial growth factor (VEGF) receptors. Further research is ongoing to optimize its use in specific cancers.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Advances in understanding tumor molecular biology have enabled targeted therapies.
- Axitinib targets vascular endothelial growth factor (VEGF) receptor tyrosine kinases 1, 2, and 3.
Purpose of the Study:
- To review preclinical and clinical data for axitinib.
- To explore axitinib's efficacy across various solid tumors.
- To compare axitinib with other VEGF receptor inhibitors.
Main Methods:
- Review of preclinical studies.
- Analysis of Phase II clinical trial data in diverse tumor types (melanoma, renal, pancreatic, thyroid, breast, lung, colorectal).
- Exploration of potential predictive biomarkers (blood pressure, erythropoietin levels).
Main Results:
- Axitinib demonstrates activity in a range of solid tumors.
- Potential predictive markers for VEGF/VEGFR pathway inhibition were identified.
Conclusions:
- Axitinib is a potent VEGF receptor inhibitor with broad potential in solid tumors.
- Ongoing Phase III trials will define optimal use in pancreatic and metastatic renal cell carcinoma.
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