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. 2010 Jul 13;101(10):2193–2199. doi: 10.1111/j.1349-7006.2010.01677.x

Table 3.

 Pharmacokinetic parameters of enzastaurin and its active metabolites in cycle 0

Analyte Parameters Geometric mean (coefficient of variation %)
Dose of enzastaurin (mg)
250 375 500 750
Enzastaurin N 7 6 6 4
Cmax (nmol/L) 1090 (57.5) 968 (61.3) 2070 (40.2) 1910 (73.3)
tmax (h)* 4.07 (2.87–8.92) 3.96 (3.00–6.10) 5.96 (3.00–9.03) 3.92 (3.15–4.00)
AUC0–∞ (h μmol/L) 12.7 (78.7) 12.9 (77.6) 29.5 (70.2) 23.5 (96.6)
CL/F (L/h) 38.0 (78.7) 56.4 (77.6) 32.9 (70.2) 61.9 (96.6)
Vz/F (L) 651 (70.7) 820 (69.1) 632 (39.1) 957 (68.5)
t1/2 (h)† 11.9 (7.6–17.0) 10.1 (7.5–16.4) 13.3 (8.4–20.3) 10.7 (8.2–14.1)
LY326020 N 7 6 6 4
Cmax (nmol/L) 285 (36.7) 308 (24.3) 494 (39.9) 548 (53.1)
tmax (h)* 5.77 (2.87–8.97) 5.01 (4.00–9.02) 9.02 (4.00–24.02) 5.00 (3.92–6.00)
AUC0–∞ (h μmol/L) 12.2 (50.2) 14.6 (46.8) 27.8 (61.1) 26.3 (65.5)
t 1/2 (h)† 38.2 (27.2–55.6) 34.8 (28.9–40.5) 37.8 (26.6–55.6) 38.4 (33.2–41.1)
MR 0.961 (60.7) 1.13 (37.3) 0.942 (46.9) 1.12 (23.7)
LY485912 N 7 6 6 4
Cmax (nmol/L) 122 (57.3) 107 (48.8) 258 (50.2) 218 (77.7)
tmax (h)* 5.77 (3.93–8.97) 6.10 (4.02–9.02) 9.02 (6.20–24.02) 5.00 (3.92–9.07)
AUC0–∞ (h μmol/L) 2.25 (88.4) 2.17 (91.3) 5.88 (103) 4.54 (132)
t 1/2 (h)† 12.0 (7.7–19.7) 10.5 (9.4–14.0) 12.6 (8.7–19.6) 11.5 (6.8–17.7)
MR 0.176 (15.3) 0.168 (15.8) 0.199 (33.3) 0.193 (19.8)
LSN2406799 N 7 6 6 4
Cmax (nmol/L) 145 (34.0) 143 (41.3) 276 (31.8) 242 (92.8)
tmax (h)* 4.02 (2.87–6.07) 3.96 (3.00–6.10) 4.96 (3.00–9.03) 3.92 (3.15–4.00)
AUC0–∞ (h μmol/L) 1.40 (68.4) 1.49 (60.8) 3.25 (49.6) 2.71 (92.6)
t 1/2 (h)† 10.5 (7.1–13.7) 8.70 (7.1–11.9) 11.6 (6.1–17.1) 10.3 (5.7–19.7)
MR 0.110 (9.2) 0.115 (15.3) 0.110 (18.7) 0.115 (12.5)

*Median (range). †Geometric mean (range). AUC0–∞, area under the concentration vs time curve from 0 to infinity; CL/F, apparent total body clearance calculated after oral dosing; Cmax, maximum plasma concentration; MR, metabolic ratio; tmax, median time to reach maximum concentration; t1/2, half‐life associated with the terminal rate constant; Vz/F, apparent volume of distribution after oral administration.