Active Ingredient History

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  • Now
Levoleucovorin is the pharmacologically active isomer of leucovorin or 5-formyl tetrahydrofolic acid, a folate analog . Levoleucovorin does not require reduction by the enzyme dihydrofolate reductase in order to participate in reactions utilizing folates as a source of “onecarbon” moieties. Administration of levoleucovorin can counteract the therapeutic and toxic effects of folic acid antagonists such as methotrexate, which act by inhibiting dihydrofolate reductase. Levoleucovorin can enhance the therapeutic and toxic effects of fluoropyrimidines used in cancer therapy such as 5-fluorouracil. 5-fluorouracil is metabolized to 5-fluoro-2'-deoxyuridine-5'-monophosphate (FdUMP), which binds to and inhibits thymidylate synthase (an enzyme important in DNA repair and replication). Levoleucovorin is readily converted to another reduced folate, 5,10-methylenetetrahydrofolate, which acts to stabilize the binding of FdUMP to thymidylate synthase and thereby enhances the inhibition of this enzyme. Fusilev® (levoleucovorin) is approved by FDA for i) rescue after high-dose methotrexate therapy in osteosarcoma, ii) diminishing the toxicity and counteracting the effects of impaired methotrexate elimination and of inadvertent overdosage of folic acid antagonists and iii) in combination chemotherapy with 5-fluorouracil in the palliative treatment of patients with advanced metastatic colorectal cancer.   NCATS

More Chemistry
  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Parenteral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$32.3653 - $48.0500
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

(6s)-5-formyl-5,6,7,8-tetrahydrofolic acid | (6s)-5-formyltetrahydrofolic acid | (6s)-folinic acid | (6s)-leucovorin | calcium levofolinate | cl-307782 | levofolene | levofolinate | levofolinate calcium | levo-folinic acid | levofolinic acid | levoleucovorin | levo-leucovorin | levoleucovorin calcium | levoleucovorin calcium pentahydrate | l-folinic acid | l-leucovorin | n-[4-({[(6s)-2-amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl]methyl}amino)benzoyl]-l-glutamic acid | (s)-leucovorin

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