Lometrexol

General information

Lometrexol is a folic acid analogue, 5,10-dideaza-5,6,7,8-tetrahydrofolic acid, which acts as an antifolate drug and targets de novo purine synthesis in tumor cells by inhibiting glycinamide ribonucleotide formyltransferase (GARFT), a folate-dependent enzyme [ , ]. Folic acid supplementation improves efficacy and without it severe cumulative toxicity on the bone marrow and the mucosa is likely [ , ].

Drug studies