3,4-Dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one, Methazolastone, M&B 39831, Temodal, Temodar; CCRG 81045, TMZ; NSC 362856

Imidazotetrazine alkylating agent. An antineoplastic. A cell-permeable, orally bioavailable, blood-brain barrier-permeant MTIC [5-(3-methyltriazen-1-yl-)-imidazole-4-carboxamide] prodrug whose in vivo DNA alkylating activity is employed in anticancer therapy. MGMT (O6-methylguanine DNA methyl transferase) repairs TMZ-damaged DNA lesion by covalently transferring O6-methylation on guanine residues to a cysteine residue on the MGMT, forming the basis of TMZ-resistance in cancer treatment.