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Regorafenib + anti-PD-1 antibodies is a combination therapy consisting of regorafenib, an oral small molecule multi-kinase inhibitor, and monoclonal antibodies targeting programmed cell death protein 1 (PD-1). Regorafenib inhibits multiple kinases involved in tumor angiogenesis (such as VEGFR), oncogenesis (including KIT, RET), and the tumor microenvironment (CSF1R, FGFR). Anti-PD-1 antibodies block the PD-1 immune checkpoint on T cells, enhancing antitumor immune responses. The combination has shown synergistic effects in preclinical models by normalizing tumor vasculature, increasing CD8+ T-cell infiltration via CXCL10/CXCR3 signaling, reducing immunosuppressive macrophages and regulatory T cells, and improving overall antitumor efficacy. Clinically investigated primarily for advanced or refractory solid tumors such as microsatellite stable metastatic colorectal cancer (MSS mCRC) and hepatocellular carcinoma (HCC), this regimen demonstrates promising efficacy with manageable safety profiles[4][5][6][8][9].
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