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refametinib + sorafenib
- Development stage
- Discontinued
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Refametinib (BAY86-9766) is an oral, allosteric inhibitor of MEK1/2 (mitogen-activated protein kinase kinases 1 and 2), developed for the treatment of cancers driven by aberrant MAPK pathway signaling. Sorafenib is a multikinase inhibitor that targets several tyrosine protein kinases including RAF kinases and vascular endothelial growth factor receptors (VEGFR). The combination of refametinib and sorafenib has been investigated primarily in hepatocellular carcinoma (HCC), particularly in patients with RAS mutations. Preclinical studies demonstrated synergistic antitumor activity through dual inhibition of the MAPK pathway and angiogenesis. Clinical trials showed that this combination had antitumor activity but required frequent dose modifications due to adverse events[2][4][5]. Refametinib was developed by Bayer.
- Brand names
- Nexavar
- Other names
- refametinib + sorafenib
02
Targets
VEGFR2 (Vascular endothelial growth factor receptor 2)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)RET (Rearranged during transfection receptor tyrosine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)BRAF (B-Raf proto-oncogene, serine/threonine kinase)VEGFR3 (Vascular endothelial growth factor receptor 3)FLT3 (Fms related receptor tyrosine kinase 3)RAF1 (c-Raf-1 (Y340D/Y341D))
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