Table 3. Pharmacokinetic profile of enzastaurin, LSN326020, and total analytes (enzastaurin + LSN326020 + LSN485912 + LSN2406799).
| Parameter (unit) | Geometric Mean (% CV) | ||
|---|---|---|---|
| Enzastaurin | LSN326020 | Total Analytes | |
| N | 23 | 23 | 23 |
| Cmax, ss (nmol/L) | 2370 (112) | 1070 (38.4) | 4140 (81.5) |
| tmax, ss (h)a | 4.00 (2.0–8.17) | 5.97 (0.00–24.00) | 4.00 (2.0–8.17) |
| AUCτ, ss (nmol·h/L) | 29100 (128) | 21800 (45.5) | 89000 (91.9) |
| Cav, ss (nmol/L) | 1210 (128) | 907 (45.5) | 2650 (86.1) |
| CL/F (L/h) | 33.3 (128) | NC | NC |
| t1/2 (h)b | 14.0 (5.82–38.5)c | 42.0 (21.8–157)c | NC |
| RA(ratio) | 1.50 (28.4)c | 3.09 (35.3)c | NC |
| MR(ratio) | NC | 0.749 (80.5) | NC |
a
Median and range.
b
Geometric mean and range.
c
N = 21.
AUCτ, ss, area under the plasma concentration-time curve during 1 dosing interval at the steady state; Cav, ss, the average drug concentration under steady-state conditions; CL/F, apparent clearance of drug calculated after extravascular administration; Cmax, ss, maximum observed plasma concentration at the steady state; CV, coefficient of variation; MR, metabolite-to-parent ratio; N, number of patients used in the pharmacokinetic analysis; NC, not calculated; RA, accumulation index; t½, half-life; tmax, ss, time of maximum observed plasma concentration at the steady state.