Table 2.
Summary of enasidenib plasma pharmacokinetic parameters by race and dose level
| Dose (mg) | Race | AUC0‐t (ng h/mL) | AUC0‐inf (ng h/mL) | C max (ng/mL) | t max a(h) | t 1/2 (h) | CL/F (mL/h) | Vz/F (mL) |
|---|---|---|---|---|---|---|---|---|
| 50 | Japanese (n = 10) | 21800 (46.9) | 21900 (46.7) | 533 (41.0) | 3.98 (0.98, 8.95) | 21.1 (31.6) | 2290 (46.7) | 69700 (40.9) |
| Caucasian (n = 9) | 17800 (55.0) | 18000 (55.0) | 406 (34.9) | 4.00 (2.02, 24.0) | 23.0 (47.4) | 2780 (55.0) | 92300 (44.5) | |
| 100 | Japanese (n = 11) | 40500 (47.2) | 40700 (47.3) | 786 (27.1) | 4.00 (1.97, 24.0) | 19.5 (45.6) | 2460 (47.3) | 69000 (25.1) |
| Caucasian (n = 10) | 49200 (27.5) | 49500 (27.8) | 822 (38.5) | 2.99 (1.03, 9.08) | 25.5 (51.4) | 2020 (27.8) | 74400 (41.2) | |
| 300 | Japanese (n = 10) | 168000 (44.7) | 170000 (44.6) | 2030 (34.3) | 13.4 (1.00, 48.0) | 27.7 (35.6) | 1760 (44.6) | 70300 (15.3) |
| Caucasian (n = 10) | 163000 (44.8) | 163000 (44.9) | 1780 (27.8) | 10.5 (1.97, 24.0) | 28.3 (32.0) | 1840 (44.9) | 74900 (26.9) |
AUC0‐t, AUC from time zero to time t, where t is the last measurable time point; AUC0‐inf,AUC from time zero extrapolated to infinity; CL/F, apparent total plasma clearance; C max, maximum observed plasma concentration; CV%, percent coefficient of variation; t 1/2, estimate of the terminal elimination half‐life; t max, time to C max; V z/F = apparent total volume of distribution.
Geometric mean (Geometric CV%) data are presented.
a
Median (min, max) data are presented.