Leucovorin (Wellcovorin, Fusilev, generic leucovorin calcium)
Other Medications · Approved since 1952
Description
Leucovorin is a folate analog that serves as a biochemical modulator in colorectal cancer treatment, specifically used to enhance the efficacy of 5-fluorouracil (5-FU) based chemotherapy regimens. It is a standard component of combination protocols such as FOLFOX and FOLFIRI for both adjuvant treatment of stage III disease and first-line therapy for metastatic colorectal cancer. Leucovorin functions by stabilizing the binding of 5-FU metabolites to thymidylate synthase, thereby potentiating the cytotoxic effects of fluoropyrimidine chemotherapy across all molecular subtypes of colorectal cancer including microsatellite stable (MSS) and microsatellite instability-high (MSI-H) tumors.
Mechanism of Action
Leucovorin is converted intracellularly to 5,10-methylenetetrahydrofolate, which forms a stable ternary complex with thymidylate synthase and 5-FU metabolites, prolonging enzyme inhibition. This enhanced binding prevents DNA synthesis by blocking the conversion of deoxyuridine monophosphate to deoxythymidine monophosphate, leading to thymine nucleotide depletion and incorporation of fraudulent nucleotides into DNA. The result is enhanced cytotoxicity of 5-FU against rapidly dividing cancer cells.
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Wellcovorin, Fusilev, generic leucovorin calcium |
| Category | Other Medications |
 Status | FDA Approved |
 EMA Status | EMA Approved |
 Spain Access | Funded by SNS other indication |
| Administration | IV |
| Year Approved | 1952 |
| Clinical Trials | 641 |
Regimens with this Drug
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.