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Regorafenib + immune checkpoint inhibitor is a combination therapy consisting of regorafenib, an oral multi-kinase inhibitor, and an immune checkpoint inhibitor (ICI), typically targeting PD-1 or PD-L1. Regorafenib inhibits multiple protein kinases involved in tumor angiogenesis (such as VEGFR), oncogenesis (such as KIT, RET), and the tumor microenvironment. Immune checkpoint inhibitors block inhibitory pathways in T cells—most commonly the PD-1/PD-L1 axis—thereby enhancing anti-tumor immunity. This combination aims to overcome resistance to immunotherapy seen in certain cancers by modulating both the tumor vasculature/microenvironment and reactivating anti-tumor immune responses. The regimen has been studied primarily in metastatic colorectal cancer, hepatocellular carcinoma, and biliary tract cancer[1][2][3][4].
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