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Drug intelligence / Profile preview
N-desmethyl regorafenib N-oxide
- Development stage
- Unknown
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
M-5 (also known as BAY 81-8752 or N-desmethyl regorafenib N-oxide) is one of the two major active metabolites of regorafenib (Stivarga), an oral multikinase inhibitor developed by Bayer. Formed in vivo primarily via cytochrome P450 3A4 (CYP3A4) metabolism, M-5 exhibits a similar multikinase inhibition profile to its parent compound, regorafenib. It potently inhibits multiple receptor tyrosine kinases involved in tumor angiogenesis (VEGFR1-3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF), and the tumor microenvironment (PDGFR-beta, FGFR1). At steady state in cancer patients, M-5 achieves systemic exposure levels comparable to regorafenib, thereby significantly contributing to the overall clinical antitumor efficacy of regorafenib in indications such as metastatic colorectal cancer (mCRC), gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC).
- Other names
- M-5M5M 5N-desmethyl regorafenib pyridine-N-oxideN-desmethylregorafenib N-oxidedemethylated regorafenib N-oxideregorafenib M5 metaboliteregorafenib metabolite M5
02
Targets
ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)BRAF (B-Raf proto-oncogene, serine/threonine kinase)CSF1R (Macrophage colony-stimulating factor receptor)DDR2 (Discoidin domain receptor tyrosine kinase 2)EPHA2 (Ephrin type-A receptor 2)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FRK (Fyn-related Src family tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MAPK14 (p38 mitogen-activated protein kinase alpha)NTRK1 (Tropomyosin-related receptor kinase A)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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