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axitinib + afatinib + linifanib
- Development stage
- Discontinued
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This is a hypothetical oral combination therapy composed of **axitinib**, **afatinib**, and **linifanib**, three small molecule tyrosine kinase inhibitors. Each agent targets multiple kinases involved in tumor angiogenesis and cellular proliferation. Axitinib is a selective inhibitor of vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), afatinib is an irreversible inhibitor of the ErbB family of receptors (including EGFR/ErbB1, HER2/ErbB2, and HER4/ErbB4), and linifanib is a dual inhibitor of VEGF and platelet-derived growth factor receptors (PDGFR). This potent multi-kinase blockade is theoretically designed for enhanced antitumor activity in cancers driven by VEGF and ErbB/EGFR pathways. As of now, there is no evidence that this specific combination has been clinically developed or evaluated in trials or is marketed as a fixed combination. The individual drugs have been studied and marketed as monotherapy or in other combinations in oncology, mainly for renal cell carcinoma and non-small cell lung cancer.
- Other names
- axitinib + afatinib + linifanib
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)EGFR (Epidermal growth factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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