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Similarly to sorafenib, regorafenib is a bi-aryl urea class of drug. The sole difference between sorafenib and regorafenib is the presence of a fluorine atom (red arrow) in the latter. Due to a mechanism that has not yet been fully defined, this one unique difference produces a wider kinase inhibitory profile. In complement to the targets that are inhibited by sorafenib, regorafenib also blocks the signaling pathway of Tie2, the receptor for angiopoietin-2, a pro-angiogenic cytokine.
