Table 6.
Summary of pharmacokinetic parameters of perifosine in patients with refractory neoplasms
| Dose level | LD (mg) | MD (mg) | N | Ka (l/h) | CL/F (L/h) | Vd/F(L) | Tl/2 (h) | Day 21a (µg/mL) | |
|---|---|---|---|---|---|---|---|---|---|
| I | 300 | 50 | 3 | Median | 0.28 | 0.56 | 136.3 | 168.4 | 3.12 |
| Mean | 0.31 | 0.68 | 152.3 | 150.8 | 3.17 | ||||
| SD | 0.13 | 0.20 | 74.9 | 38.7 | 0.76 | ||||
| II | 600 | 100 | 3 | Median | 0.10 | 0.77 | 84.2 | 76.5 | 5.03 |
| Mean | 0.07 | 0.81 | 79.9 | 75.1 | 5.28 | ||||
| SD | 0.05 | 0.08 | 16.5 | 19.2 | 0.81 | ||||
| III | 900 | 150 | 8 | Median | 0.07 | 0.76 | 115.5 | 98.5 | 8.32 |
| Mean | 0.19 | 0.78 | 120.6 | 111.5 | 8.02 | ||||
| SD | 0.26 | 0.19 | 31.9 | 34.9 | 2.06 | ||||
| Total (I-III) | Median | 0.10 | 0.77 | 108.1 | 98.8 | ||||
| Mean | 0.19 | 0.76 | 118.6 | 112.1 | |||||
| SD | 0.21 | 0.17 | 45.4 | 40. l | |||||
| IV | 1,200 | 200 | 7 | Median | 0.20 | 1.24 | 185.0 | 108.5 | 5.73 |
| Mean | 0.41 | l.37 | 225.8 | 112.3 | 5.53 | ||||
| SD | 0.53 | 0.45 | 121.2 | 29. l | 2.07 | ||||
| V | 1,500 | 250 | 3 | Median | 0.08 | 0.98 | 193.6 | 117.l | 10.30 |
| Mean | 0.22 | l.14 | 192.l | 143.4 | 10.30 | ||||
| SD | 0.24 | 0.66 | 25. l | 79.8 | 8.77 |
One compartmental model analysis was used to calculate the pharmacokinetic parameters. Data from cycle I were used LD loading dose, MD maintenance dose
a
Perifosine concentration at day 21 of cycle 1