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Regorafenib is an orally administered small molecule multikinase inhibitor used primarily for the treatment of metastatic colorectal cancer, unresectable or metastatic gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma. It works by inhibiting multiple membrane-bound and intracellular kinases involved in oncogenesis (tumor growth), angiogenesis (formation of new blood vessels that supply tumors), and maintenance of the tumor microenvironment. Key targets include VEGFR1/2/3, RET, KIT, PDGFR-alpha/beta, FGFR1/2, TIE2, DDR2, TrkA, Eph2A, RAF-1/BRAF/BRAFV600E among others[5][6][8]. Regorafenib is developed by Bayer and marketed under the brand name Stivarga[5]. Rifampin is a well-known antibiotic primarily used to treat tuberculosis and other bacterial infections. It acts as a potent inducer of cytochrome P450 enzymes (notably CYP3A4) in the liver. The combination "regorafenib + rifampin" is not an approved therapy but may be referenced in drug interaction studies because co-administration can significantly reduce plasma concentrations of regorafenib due to induction of its metabolism by rifampin.
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