capecitabine + regorafenib

**Capecitabine + regorafenib** is an oral combination of two small molecule drugs used in oncology, most notably explored for metastatic colorectal cancer and locally advanced rectal cancer. **Capecitabine** is a fluoropyrimidine prodrug that is enzymatically converted to 5-fluorouracil (5-FU) in the body, acting primarily as a cytotoxic antimetabolite via inhibition of thymidylate synthase, disrupting DNA synthesis and repair in tumor cells. **Regorafenib** is a multi-kinase inhibitor that blocks several protein kinases involved in angiogenesis (vascular endothelial growth factor receptors VEGFR1-3, TIE2), tumor proliferation (KIT, RET, PDGFR-β, FGFR, c-RAF, B-RAF), and the tumor microenvironment, thereby impeding tumor growth, metastasis, and promoting cell death. The combination provides both cytotoxic and targeted anti-cancer effects, and has shown feasible safety and preliminary efficacy in patients with refractory metastatic colorectal cancers, including those who failed on monotherapy with either agent[1][3][5][7]. The combination is investigational and not approved as a fixed pharmaceutical product.