Chemotherapy is assuming an increasingly important role in the treatment of malignant gliomas, of which temozolomide (TMZ) is a key part. TMZ belongs to a class of second-generation imidazotetrazinone prodrugs that exhibit linear pharmacokinetics and do not require hepatic metabolism for activation to the active metabolite. New intravenous (iv) TMZ formulations have recently been approved based on studies of bioequivalence between iv and oral TMZ. The efficacy of TMZ was initially evaluated in patients with recurrent disease but phase II and III trials in newly diagnosed gliomas are available. The results of a large phase III trial that compared RT alone vs RT concomitant with oral TMZ created a new standard of adjuvant treatment. Efficacy data for iv TMZ on which its approval was based are those extrapolated from clinical trials with oral TMZ. No comparative data are available on the differences in tolerability and patient satisfaction between oral and iv formulations of TMZ, or for quality of life. New oral formulations could encourage the adherence of patients to treatment. Although patients presumably would prefer oral treatment, iv formulations may be an alternative in noncompliant patients or patients for whom good adherence could not be expected.
Keywords: brain tumors; chemotherapy; glioblastoma; new formulations; patient considerations; temozolomide.