Drug intelligence / Profile preview

golvatinib + lenvatinib

Development stage
Preclinical
Lead developer
Eisai
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Golvatinib + lenvatinib is an investigational combination therapy consisting of two small molecule tyrosine kinase inhibitors. Golvatinib (E7050) is a multi-targeted tyrosine kinase inhibitor that primarily targets the MET receptor and other kinases involved in tumor growth and angiogenesis. Lenvatinib (E7080), marketed as Lenvima or Kisplyx, is a potent multikinase inhibitor targeting vascular endothelial growth factor receptors (VEGFR1-3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptor alpha (PDGFRα), RET, and KIT. Both agents are designed to inhibit pathways critical for tumor proliferation and angiogenesis. While lenvatinib has multiple approved indications as monotherapy or in combination with other agents such as pembrolizumab or everolimus for various cancers—including thyroid cancer, renal cell carcinoma, hepatocellular carcinoma, and endometrial cancer—golvatinib remains investigational. The combination of these two drugs aims to provide enhanced antitumor activity by simultaneously blocking complementary signaling pathways involved in cancer progression.

Other names
golvatinib + lenvatinib
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)MET (Mesenchymal-epithelial transition factor receptor)TEK (Tie2)VEGFR-1 (Vascular endothelial growth factor receptor 1)FGFR3 (Fibroblast growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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