Lometrexol (DDATHF) disodium is a potent inhibitor of human serine hydroxymethyltransferase 1/2 (hSHMT1/2) and antifolate, which reduces the activity of glycinamide ribonucleotide formyltransferase (GARFT) without causing detectable levels of DNA strand breaks. Lometrexol disodium exhibits anticancer effects by inhibiting the de novo synthesis of purines, causing abnormal cell proliferation, apoptosis and cell cycle arrest.