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lenvatinib + temozolomide
- Development stage
- Unknown
- Lead developer
- Eisai
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
The combination of **lenvatinib** (a small-molecule multi-kinase inhibitor) and **temozolomide** (an oral alkylating agent) has been investigated primarily for advanced melanoma and brain tumors such as glioblastoma. Lenvatinib inhibits vascular endothelial growth factor receptors (VEGFR1-3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptor alpha (PDGFRα), KIT, and RET, thereby blocking angiogenesis and tumor growth. Temozolomide is a DNA-alkylating agent that induces cytotoxicity by damaging DNA. Combination therapy has demonstrated an acceptable safety profile and modest clinical activity in phase 1b trials and has been considered as a strategy to improve the effectiveness and pharmacological properties of each agent in melanoma, glioma, and related cancers[1][2][3][5].
- Other names
- lenvatinib plus temozolomidelenvatinib and temozolomide
02
Targets
AGT (O6-methylguanine-DNA methyltransferase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)FGFR (FGFR family)RET (Rearranged during transfection receptor tyrosine kinase)
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