Drug intelligence / Profile preview

leucovorin sodium

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Leucovorin sodium is the sodium salt form of leucovorin, an active metabolite of folic acid and a chemically reduced derivative known as folinic acid. It acts as an essential coenzyme for nucleic acid synthesis and is classified as a folic acid analog. Leucovorin is primarily used to counteract the toxic effects of antifolate drugs such as methotrexate by bypassing dihydrofolate reductase inhibition, thereby rescuing healthy cells from toxicity while allowing methotrexate to exert its anticancer effects. Additionally, it enhances the efficacy of fluorouracil (5-FU) in colorectal cancer by stabilizing the binding of 5-FU’s active metabolite to thymidylate synthase, prolonging drug activity. Indications include rescue therapy after high-dose methotrexate in osteosarcoma, treatment of megaloblastic anemia due to folic acid deficiency when oral therapy is not feasible, and use with 5-fluorouracil for advanced colorectal cancer[1][3][4][6].

Brand names
Lederle LeucovorinOncofolic
Other names
leucovorinfolinic acidcalcium folinatecitrovorum factor5-formyl tetrahydrofolate
02

Targets

TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)

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