Leucovorin (Folinic acid) Calcium Pentahydrate

Leucovorin administration increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase in two murine colon tumors. ^[1] Leucovorin, Gemcitabine, Oxaliplatin, and 5-fluorouracil is a powerful antitumor and immunomodulating regimen that can make the tumor cells a suitable means to induce an Ag-specific CTL response. ^[2] Leucovorin (20 mM) increases the cytotoxicity in all three replicate experiments in 10 of the 11 human colorectal carcinoma cell lines. ^[3] Leucovorin enhances cytotoxicity of trimetrexate/fluorouracil, but not methotrexate/fluorouracil, in CCRF-CEM cells. ^[4] Leucovorin (LV) is a reduced folate cofactor that competes with RTX for transport and polyglutamation in both tumor and normal tissues and thus has potential as a rescue agent. Leucovorin reverses the growth-inhibitory, and potentially cytotoxic, effects of RTX on populations of viable cells. ^[5]

Leucovorin (200 mg/kg), which is given after the onset of severe weight loss and diarrhea (twice daily, days 5-7) in mice, prevents further weight loss and induces earlier recovery. Leucovorin (100 or 200 mg/kg; twice daily on days 4-6) reduces the RTX concentration in the liver 2-4-fold on days 7, 9, and 11 compared with controls. ^[5] Leucovorin/5-FU and Gastrimmune (200 mg/mL) combinations (12.5 and 20 mg/kg) increase the therapeutic effects on the in vivo growth of DHDK12 tumors when compared to the agents given singly. ^[6]