Pharmacokinetics of diaziquone after three different dosage regimens.

Diaziquone (AZQ) is a benzoquinone derivative exhibiting significant effects against CNS tumors. This study investigates the pharmacokinetics of AZQ for three different durations of continuous iv infusions, over 20 mins, 4 hrs, and 6 hrs, in nine patients with CNS malignancies. Total AZQ doses varied from 10 to 20 mg. The average elimination half-life was 37.2 +/- 13.9 mins, the total clearance was 515 +/- 280 ml/min or 11.3 +/- 5.9 ml/min/kg, and the apparent volume of distribution by area was 26.5 +/- 14.7 L or 0.62 +/- 0.50 L/kg. Peak concentrations after the 20-min infusions (three patients) varied from 0.58 to 1.20 micrograms/ml, whereas concentrations during the 4-hr infusions (three patients) varied from 0.02 to 0.37 micrograms/ml, and during the 6-hr infusions (three patients) varied from 0.02 to 0.61 micrograms/ml. These results indicate that concentrations found to exhibit minimum inhibitory effects in in vitro cell studies are achievable during prolonged iv infusions of AZQ.

Duke Scholars

Author Henry Seth Friedman Neurosurgery, Neuro-Oncology

Author John Matthew Falletta Pediatrics, Hematology-Oncology