Temozolomide is an highly orally-available, imidazotetrazine-based, monofunctional DNA alkylating agent. In vivo it spontaneously degrades and reacts with water to release a methyldiazonium cation which preferentially methylates DNA at N7 positions of guanine in guanine rich regions. The active agent also methylates N3 adenine and O6 guanine. [1]

Temozolomide, which enters the cerebrospinal fluid and does not require hepatic metabolism, demonstrates schedule-dependent antitumor activity against highly-resistant gliomas. [2] In Phase 1 clinical studies, temozolomide showed 100% p.o. bioavailability.

In L-1210 leukemia cells, temozolomide caused a dose-dependent accumulation of cells in the SL-G2-M phase. [3]

Temozolomide is an highly orally-available, imidazotetrazine-based, monofunctional DNA alkylating agent. In vivo it spontaneously degrades and reacts with water to release a methyldiazonium cation which preferentially methylates DNA at N7 positions of guanine in guanine rich regions. The active agent also methylates N3 adenine and O6 guanine. [1]

Temozolomide, which enters the cerebrospinal fluid and does not require hepatic metabolism, demonstrates schedule-dependent antitumor activity against highly-resistant gliomas. [2] In Phase 1 clinical studies, temozolomide showed 100% p.o. bioavailability.

In L-1210 leukemia cells, temozolomide caused a dose-dependent accumulation of cells in the SL-G2-M phase. [3]