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fostroxacitabine bralpamide + lenvatinib
- Development stage
- Unknown
- Lead developer
- Medivir
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Fostroxacitabine bralpamide (fostrox, also known as MIV-818) is an orally administered anti-tumor drug designed to selectively target cancer cells in the liver while minimizing effects on other tissues. It is a nucleoside analog prodrug that becomes activated in the liver, leading to DNA damage and cell death specifically in hepatocellular carcinoma (HCC) cells. Lenvatinib is a small molecule receptor tyrosine kinase inhibitor that blocks multiple targets involved in tumor angiogenesis and growth, including VEGFR1–3, FGFR1–4, PDGFRα, KIT, and RET. The combination of fostroxacitabine bralpamide with lenvatinib has shown acceptable safety and promising efficacy for patients with advanced or unresectable HCC who have progressed on prior systemic therapies. This combination is being developed by Medivir AB and evaluated in clinical trials for second-line or later treatment of HCC[2][3][4][5][8].
- Brand names
- Lenvima
- Other names
- fostrox
02
Targets
FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)DNAFGFR1 (Fibroblast growth factor receptor 1)PDGFRB (Platelet-derived growth factor receptor beta)CES1 (Liver carboxylesterase 1)RAF1 (c-Raf-1 (Y340D/Y341D))FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)SFK (SRC family kinases)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)POLA1 (DNA polymerase alpha)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)
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