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Regorafenib, a potent medication belonging to the Multi-Tyrosine Kinase Inhibitors class, targets various tyrosine kinases crucial for tumor angiogenesis (such as VEGFR1, -2, -3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF, BRAFV600E), and the tumor microenvironment (PDGFR, FGFR). By inhibiting these proteins, Regorafenib effectively impedes tumor growth, proliferation, and angiogenesis within tumors, particularly inhibiting mutated KIT, a significant driver of oncogenesis in GIST.