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Regorafenib is a multi-kinase inhibitor developed by Bayer HealthCare Pharmaceuticals that is structurally identical to sorafenib apart from a single fluorine atom added to the central aromatic ring. It has multiple tyrosine kinase and serine/threonine kinase targets which include vascular endothelial growth factor receptors 1–3 (VEGFR1–3), platelet-derived growth factor receptor-β (PDGFRβ), fibroblast growth factor receptor 1 (FGFR1), Raf-1, tyrosine kinase with immunoglobulin and epidermal growth factor homology domain 2 (TIE2), and the oncogenic kinases c-KIT, RET, C-RAF, B-RAF, and B-RAF V600E mutant. Regorafenib has been demonstrated to improve the overall survival of patients with heavily pretreated, metastatic colorectal cancer (mCRC) and to significantly improve progression-free survival in treatment-refractory gastrointestinal stromal tumors (GIST).
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Chemical Name
4-[4-({[4-Chloro-3-(trifluoromethyl)phen...
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References
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Waddell, T., Cunningham, D. (2014). Regorafenib. In: Schwab, M. (eds) Encyclopedia of Cancer. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-27841-9_7189-4
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DOI: https://doi.org/10.1007/978-3-642-27841-9_7189-4
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Publisher Name: Springer, Berlin, Heidelberg
Online ISBN: 978-3-642-27841-9
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