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Fluorouracil + levoleucovorin is a combination chemotherapy regimen used primarily in the treatment of metastatic colorectal cancer and other gastrointestinal malignancies. Fluorouracil (5-FU) is an antimetabolite that inhibits thymidylate synthase, thereby interfering with DNA synthesis and function, leading to cell death in rapidly dividing cancer cells. Levoleucovorin is the pharmacologically active enantiomer of folinic acid (leucovorin) and acts as a folate analog. When administered with fluorouracil, levoleucovorin enhances the binding of 5-FU to thymidylate synthase, increasing its cytotoxic effect on tumor cells. This combination improves response rates compared to fluorouracil alone[1][2][3][5][6].
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