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This entry refers to two related chemotherapy regimens used primarily in the treatment of advanced or metastatic colorectal cancer and other gastrointestinal cancers. The first is a combination of leucovorin (also known as folinic acid), a reduced form of vitamin B9 that enhances the efficacy of certain chemotherapies; and fluorouracil (5-FU), an antimetabolite chemotherapy that inhibits DNA synthesis in rapidly dividing cells. The second regimen adds irinotecan, a topoisomerase I inhibitor that prevents DNA replication in cancer cells. Leucovorin is not itself cytotoxic but increases the binding affinity of 5-FU to its target enzyme thymidylate synthase, thereby enhancing its anticancer effect[1][2][3][6]. The addition of irinotecan further improves response rates and progression-free survival compared to just leucovorin plus 5-FU[6]. These regimens are administered intravenously in cycles every two weeks.
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