COMMON BRAND NAME(S): Temodar
GENERIC NAME(S): TEMOZOLOMIDE
Description: Temozolomide, a triazene, is an inactive prodrug. It is chemically hydrolysed to 3-methyl-(triazen-1-yl) imidazole-4-carboxamide (MTIC), the active metabolite of dacarbazine. The cytotoxicity of MTIC is believed to be due alkylation of DNA, mainly at the O6 and N7 positions of guanine.
Absorption: Rapidly and completely absorbed from GI tract. Peak plasma concentration: 0.5-1.5 hr. Rate and extent of absorption decreased by food.
Distribution: Protein binding: 15%. Cross blood-brain barrier.
Metabolism: Undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound MTIC and to temozolomide acid metabolite. MTIC is further hydrolysed to 5-amino-imidazole-4-carboxamide (AIC) and methylhydrazine.
Excretion: Excreted mainly in urine as unchanged drug, AIC, temozolomide acid metabolite and unidentified polar metabolites. Plasma half life: 1.8 hr.