Temozolomide-d3 (Synonyms: Methazolastone-d3, TMZ-d3)

Temozolomide-d₃ (TMZ-d₃) contains three deuterium atoms located on the methyl group. It is intended for use as an internal standard for the quantification of temozolomide by GC- or LC-MS. TMZ is an imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells.¹ TMZ is rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.¹ Formulations containing TMZ are effective in a variety of types of cancer, including aggressive brain cancers.^1,2,3

1.Marchesi, F., Turriziani, M., Tortorelli, G., et al.Triazene compounds: Mechanism of action and related DNA repair systemsPharmacol. Res.56(4)275-287(2007) 2.Khan, O.A., Ranson, M., Michael, M., et al.A phase II trial of lomeguatrib and temozolomide in metastatic colorectal cancerBr. J. Cancer98(10)1614-1618(2008) 3.Daniel, R.A., Rozanska, A.L., Mulligan, E.A., et al.Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699Br. J. Cancer103(10)1588-1596(2010)