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sorafenib + eribulin
- Development stage
- Phase 1
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**Sorafenib + eribulin** is an investigational combination regimen of two small molecule anticancer drugs: - **Sorafenib** is a multikinase inhibitor targeting intracellular serine/threonine kinases (including Raf-1, wild-type and mutant B-Raf) and surface tyrosine kinase receptors such as KIT, FLT-3, RET, VEGFR-1/2/3, and PDGFR-β. It inhibits tumor cell signaling, proliferation, angiogenesis, and promotes apoptosis[1]. - **Eribulin** is a synthetic analog of halichondrin B, functioning as a microtubule-depolymerizing agent. It binds to microtubule ends, sequesters tubulin, disrupts mitotic spindles, causing irreversible mitotic blockage and apoptosis. Unique effects include remodeling tumor vasculature (improving perfusion and reducing hypoxia), reversing EMT, and inhibiting angiogenesis via suppression of VEGF, TGF-β, and bFGF pathways[2][4]. - The combination, studied primarily in metastatic cancer, is hypothesized to provide synergistic antitumor activity with limited overlapping toxicities[3][5].
- Brand names
- NexavarSorafenib Accord
- Other names
- sorafeniberibulineribulin mesylate
02
Targets
BRAF (B-Raf proto-oncogene, serine/threonine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)FGFR1 (Fibroblast growth factor receptor 1)TGFBR (TGF-beta receptor)TUBB (Tubulin (alpha and beta subunits))VEGFR-1 (Vascular endothelial growth factor receptor 1)
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