methotrexate + leucovorin calcium

Methotrexate is a folate analogue metabolic inhibitor that functions as an antineoplastic agent. It works by competitively inhibiting the enzyme dihydrofolate reductase (DHFR), which prevents the formation of tetrahydrofolate, a necessary cofactor for the synthesis of thymidylate and purine nucleotides required for DNA replication. In the specific clinical trial context led by the Eastern Cooperative Oncology Group (ECOG), high-dose methotrexate was investigated for the treatment of newly diagnosed glioblastoma multiforme (GBM). This regimen (NCT00082797) utilized systemic high-dose intravenous methotrexate followed by leucovorin calcium rescue to minimize systemic toxicity while attempting to achieve therapeutic concentrations within the central nervous system to treat primary brain tumors.

Brand names

TrexallRheumatrex

Other names

methotrexateleucovorin calciumMTXAmethopterinfolinic acid