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lenvatinib + gefitinib
- Development stage
- Unknown
- Lead developer
- Eisai
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Lenvatinib + gefitinib is an oral combination therapy of two small molecule tyrosine kinase inhibitors. Lenvatinib inhibits multiple receptor tyrosine kinases, including vascular endothelial growth factor receptors (VEGFR1-3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptor alpha (PDGFRα), KIT, and RET. Gefitinib is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. This combination has been investigated as a targeted therapy for advanced hepatocellular carcinoma (HCC), particularly in patients with high EGFR expression or those who have developed resistance to lenvatinib monotherapy. Mechanistically, inhibition of FGFR by lenvatinib can lead to feedback activation of the EGFR-PAK2-ERK5 signaling axis; this feedback is blocked by concurrent EGFR inhibition with gefitinib, resulting in synergistic anti-tumor effects and potential remodeling of the tumor immune microenvironment[1][2][3].
- Other names
- 仑伐替尼+吉非替尼
02
Targets
EGFR (Epidermal growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)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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