Table 5

Perifosine plasma pharmacokinetics

Dose level (LD, mg × no.; mg daily)NConcentration of perifosine* (mean ± SE)Css per μg/mL (mean ± SE)Cl/F (L/h)
Level 1100 × 4; 5034.29 ± 0.903.34 ± 0.670.68 ± 0.15
Level 2150 × 4; 5066.05 ± 0.763.44 ± 0.600.75 ± 0.12
Mean at 50 daily (range)9NA3.40 ± 0.43 (1.8–5.8)0.72 ± 0.88 (0.46–1.19)
Level 3150 × 4; 100125.96 ± 0.785.90 ± 0.820.88 ± 0.15
Level 4150 × 6; 100126.99 ± 0.64 *6.63 ± 0.510.67 ± 0.05
Mean at 100 daily (range)24NA6.32 ± 0.52 (1.8–12.6)0.79 ± 0.09 (0.33–2.26)
Level 5150 × 6; 15066.54 ± 0.615.99 ± 0.88 1.18 ± 0.22
Mean end 150 × 4 (range)185.99 ± 0.57 (2.41–10.2)NANA
Mean end 150 × 6 (range)176.83 ± 0.45 (4.4–11.9)NANA
N = 11 *N = 4 N = 4
  • * Concentration of perifosine was determined on day 2, 2 hours after the last dose of the loading dose.

  • Determined by averaging day 8 and thereafter concentrations.