Table 4.

Pharmacokinetic parameters of temozolomide and MTIC

Dosage level
267 mg/m2 (n = 5)355 mg/m2 (n = 4)472 mg/m2 (n = 11)628 mg/m2 (n = 5)835 mg/m2 (n = 3)
TMZ Cmax (μg/mL)6.6 (2.7-19.5)17.8 (13.2-19.6)11.6 (6.3-26.5)13.4 (9.5-18.8)14.1 (5.2-22.3)
TMZ Tmax (h)1.2 (0.2-1.5)1.1 (0.5-1.2)1.7 (0.2-2.4)1.5 (1.2-9)1.2 (1-2.7)
CLTMZ (L/h/m2)11.0 (4.3-28.3)5.2 (4.5-8)9.6 (5.1-15.9)9.2 (2.5-11.2)11.4 (11.1-12)
TMZ AUC0→∞ (μg·mL·h)29.4 (17-62.3)68.0 (58.7-78.9)49.4 (29.6-91.9)68 (56-174.8)72.7 (69.5-72.7)
MTIC AUC0→∞ (μg·mL·h)0.9 (0.5-4.1)2.25 (2.1-3.6)2.7 (2-5.4)4.4 (3.4-6.7)6 (0.9-7)
  • NOTE: n, number of patients. Results are shown as median values and range in parenthesis.

    Abbreviations: TMZ, temozolomide; Cmax, maximal concentration; Tmax, time for maximal concentration; CL, apparent oral clearance; AUC0→∞, area under concentration-time curve from zero to infinity.