fluorouracil + leucovorin + trimetrexate

This is a combination chemotherapy regimen consisting of three agents: - **Fluorouracil (5-FU):** A pyrimidine analog antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis and function. - **Leucovorin (folinic acid):** A reduced folate that enhances the binding of 5-FU to thymidylate synthase, thereby potentiating its cytotoxic effects. Leucovorin also serves as a "rescue" agent to reduce toxicity from antifolate drugs. - **Trimetrexate:** A non-classical antifolate that inhibits dihydrofolate reductase (DHFR), leading to depletion of reduced folates and further disruption of DNA synthesis. Unlike methotrexate, trimetrexate does not compete with leucovorin for cellular uptake or polyglutamylation. The combination is primarily used in the treatment of advanced or metastatic colorectal cancer. Trimetrexate acts as a biochemical modulator, enhancing the efficacy of 5-FU/leucovorin regimens by increasing intracellular phosphoribosylpyrophosphate levels and facilitating greater cytotoxicity when combined with these agents[1][2][3][4]. Clinical studies have shown this regimen can improve progression-free survival compared to standard 5-FU/leucovorin therapy in advanced colorectal cancer[2].

Other names

5-fluorouracil + leucovorin + trimetrexate5FU/LV/TMTX