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The combination of 5-fluorouracil (5-FU) and leucovorin is a chemotherapy regimen primarily used in the treatment of colorectal cancer. 5-fluorouracil is a pyrimidine analog that inhibits DNA synthesis by blocking thymidylate synthase, leading to cell death. Leucovorin, a reduced folate (folinic acid), enhances the cytotoxic effect of 5-fluorouracil by stabilizing the binding of its active metabolite (FdUMP) to thymidylate synthase, resulting in more pronounced and prolonged inhibition of DNA synthesis[3][6][8]. This combination increases the efficacy of fluorouracil against tumor cells. The regimen is widely used as first-line therapy for advanced or metastatic colorectal cancer and may also be employed in other gastrointestinal malignancies[8].
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