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Leucovorin

Leucovorin

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Most insurance accepted

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Available nationwide

What is Leucovorin?

Leucovorin is a form of folinic acid—an active form of the B vitamin folate—used in medicine primarily to protect normal cells from the toxic effects of methotrexate chemotherapy (a process called leucovorin rescue), and to enhance the anti-cancer effectiveness of 5-fluorouracil in colorectal cancer treatment. It's also co-administered with pyrimethamine (Daraprim) to prevent the folate deficiency and bone marrow suppression that drug can cause. Unlike folic acid supplements, Leucovorin bypasses the enzyme that methotrexate blocks, allowing normal cells to maintain folate metabolism even during high-dose methotrexate therapy.

Methotrexate rescue

Leucovorin bypasses the dihydrofolate reductase enzyme that methotrexate inhibits, restoring folate-dependent metabolic pathways in normal tissues—protecting bone marrow, GI mucosa, and other rapidly dividing healthy cells from methotrexate toxicity after high-dose chemotherapy.

5-FU chemotherapy enhancement

Stabilizes the bond between 5-fluorouracil and thymidylate synthase, the enzyme 5-FU targets in cancer cells—increasing the duration and potency of 5-FU's DNA-blocking activity and improving its effectiveness in colorectal cancer treatment.

Folate pathway bypass

As a pre-reduced form of folate, Leucovorin can be directly used by cells without enzymatic activation—allowing normal folate metabolism to continue in situations where key folate enzymes are blocked by antifolate drugs or genetic defects.

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