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Apatinib + S-1 is a combination therapy regimen being evaluated for the treatment of advanced or metastatic colorectal cancer. Apatinib is an oral, small-molecule tyrosine kinase inhibitor that highly selectively binds to and inhibits vascular endothelial growth factor receptor 2 (VEGFR-2), thereby inhibiting tumor angiogenesis. S-1 is an oral fluoropyrimidine chemotherapy agent consisting of tegafur (a 5-fluorouracil prodrug), gimeracil (a dihydropyrimidine dehydrogenase inhibitor), and oteracil (an orotate phosphoribosyltransferase inhibitor). This combination was studied in a Phase II trial led by Henan Cancer Hospital as a third-line treatment option for patients who had failed second-line chemotherapy. The regimen aims to combine the anti-angiogenic effects of apatinib with the cytotoxic effects of S-1 to improve outcomes in refractory colorectal cancer populations.
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