Drug intelligence / Profile preview

lenvatinib + erlotinib

Development stage
Phase 1
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral
01

Overview

Lenvatinib + erlotinib is an investigational combination therapy consisting of two small molecule tyrosine kinase inhibitors. Lenvatinib inhibits multiple receptor tyrosine kinases involved in tumor angiogenesis and proliferation, including vascular endothelial growth factor receptors 1–3 (VEGFR1–3), fibroblast growth factor receptors 1–4 (FGFR1–4), platelet-derived growth factor receptor alpha (PDGFRα), KIT, and RET. Erlotinib selectively inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase. The rationale for combining these agents is based on evidence that EGFR activation can mediate resistance to lenvatinib in certain cancers such as hepatocellular carcinoma; thus, dual inhibition may overcome resistance mechanisms and enhance antitumor efficacy[1][5]. This combination is under clinical investigation for advanced solid tumors, including hepatocellular carcinoma[3][4][6].

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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