Related Experiment Video
Updated: Jun 17, 2026
Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Axitinib (AG-013736)
Ronan Joseph Kelly1, Olivier Rixe
1Thoracic Oncology Department Medical Oncology Branch, National Cancer Institute, Bethesda, MD 20892, USA. kellyro@mail.nih.gov
Abstract:
The vascular endothelial growth factor (VEGF)/VEGF receptor tyrosine kinase (RTK) signaling pathway plays a pivotal role in tumor angiogenesis. Neovascularization promotes increased tumor cell proliferation, survival and metasasis. Many antiangiogenic agents including multi-RTK inhibitors are either approved or are undergoing testing in clinical trials. Axitinib is a potent and selective inhibitor of VEGF RTK 1, 2, and 3. This chapter discusses the stucture of axitinib as well as its toxicities and drug interactions. Important preclinical and clinical data for axitinib are presented including findings from phase II studies in many tumor types including malignant melanoma and renal, pancreatic, thyroid, breast, lung and colorectal carcinomas. Ongoing phase III studies in pancreatic and metastatic renal cell carcinoma will ultimately define the therapeutic role of this targeted agent.
Insights
Axitinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, shows promise in treating various cancers by blocking tumor angiogenesis. Further phase III studies will define its therapeutic role.
Area of Science:
- Oncology
- Pharmacology
Background:
- Tumor angiogenesis, driven by vascular endothelial growth factor (VEGF)/VEGF receptor tyrosine kinase (RTK) signaling, is crucial for tumor growth and metastasis.
- Antiangiogenic agents, including multi-RTK inhibitors, are vital in cancer therapy.
- Axitinib selectively inhibits VEGF RTK 1, 2, and 3.
Purpose of the Study:
- To discuss the structure, toxicities, and drug interactions of axitinib.
- To present preclinical and clinical data for axitinib in various tumor types.
Main Methods:
- Review of preclinical data.
- Analysis of phase II clinical trial findings in multiple cancer types.
- Discussion of ongoing phase III studies.
Main Results:
- Axitinib demonstrates activity in preclinical models and phase II trials across several malignancies.
- Ongoing phase III trials are evaluating axitinib in pancreatic and metastatic renal cell carcinoma.
Conclusions:
- Axitinib is a potent VEGF RTK inhibitor with potential therapeutic applications in oncology.
- Further research, particularly phase III trials, is necessary to establish the definitive role of axitinib in cancer treatment.
