Levoleucovorin (Fusilev, Khapzory)
Other Medications · Approved since 2008
Description
Levoleucovorin is a folate analog and the active L-isomer of leucovorin that serves as an essential component of fluorouracil-based chemotherapy regimens for colorectal cancer. It functions as a biochemical modulator that enhances the cytotoxic activity of 5-fluorouracil by stabilizing the binding of 5-FU metabolites to thymidylate synthase. In colorectal cancer treatment, levoleucovorin is combined with 5-fluorouracil and oxaliplatin in the mFOLFOX6 regimen, which represents a standard backbone for both adjuvant and metastatic disease treatment.
Mechanism of Action
Levoleucovorin is converted intracellularly to 5,10-methylenetetrahydrofolate, which forms a stable ternary complex with thymidylate synthase and fluorodeoxyuridine monophosphate (the active metabolite of 5-fluorouracil). This ternary complex formation significantly prolongs the inhibition of thymidylate synthase, the enzyme responsible for converting deoxyuridine monophosphate to deoxythymidine monophosphate, which is essential for DNA synthesis and repair.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Fusilev, Khapzory |
| Category | Other Medications |
 Status | FDA Approved |
| Administration | IV |
| Year Approved | 2008 |
| Clinical Trials | 2 |
Related Medications
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.