TABLE 5.
Summary of 4-OH-DiPT Plasma PK Parameters by Dose (PK Evaluable Population).
| Plasma PK Parameters | RE104 Dose | |||||
|---|---|---|---|---|---|---|
| 5 mg (n=6) | 10 mg (n=6) | 20 mg (n=6) | 30 mg (n=9) | 35 mg (n=6) | 40 mg (n=3) | |
| Summary Statistics | ||||||
| Cmax (ng/mL) | 17.175 (30.5) | 57.004 (39.4) | 73.045 (35.7) | 127.814 (40.5) | 120.192 (28.7) | 274.200 (9.2) |
| Tmax (h) | 1.125 (0.75-1.50) | 1.125 (0.75-2.00) | 1.125 (0.75-3.00) | 1.250 (0.12-1.50) | 1.000 (0.50-2.00) | 1.250 (1.00-1.50) |
| Tlast (h) | 12.000 (8.00-24.08) | 24.000 (8.00-24.02) | 14.075 (6.00-24.00) | 15.967 (8.00-24.03) | 23.842 (12.00-24.07) | 24.000 (15.98-24.00) |
| Tlag (h) | 0 | 0 | 0 | 0 | 0 | 0 |
| kel (1/h) | 0.2656 (0.13427) | 0.2622 (0.25123) | 0.3590 (0.24571) | 0.2973 (0.11225) | 0.3076 (0.14506)* | 0.2419 (0.14377) |
| t½ (h) | 3.416 (2.1483) | 4.116 (2.2212) | 3.269 (2.7176) | 2.782 (1.4450) | 2.718 (1.2911)* | 3.677 (2.1759) |
| AUC0-t (h*ng/mL) | 75.29 (60.1) | 260.2 (64.7) | 300.9 (102.6) | 430.7 (49.7) | 494.1 (61.9) | 1376 (54.5) |
| AUC0-inf (h*ng/mL) | 79.89 (59.4) | 268.0 (66.8) | 311.9 (108.4) | 439.3 (50.9) | 422.4 (47.6)* | 1405 (57.1) |
| %AUCext (%) | 5.702 (3.5031) | 2.882 (3.5558) | 3.465 (3.2720) | 1.923 (2.3039) | 0.7741 (0.39408)* | 2.017 (2.6801) |
| Cmax/dose (ng/mL/mg) | 3.435 (30.5) | 5.700 (39.4) | 3.652 (35.7) | 4.260 (40.5) | 3.479 (28.7) | 6.855 (9.2) |
| AUC0-t/dose (h*ng/mL/mg) | 15.06 (60.1) | 26.02 (64.7) | 15.05 (102.6) | 14.36 (49.7) | 14.30 (61.9) | 34.40 (54.5) |
| AUC0-inf/dose (h*ng/mL/mg) | 15.98 (59.4) | 26.80 (66.8) | 15.59 (108.4) | 14.64 (50.9) | 12.23 (47.6) | 35.12 (57.1) |
AUCs, Cmax, and their dose-normalized transformations are presented as geometric mean (geometric CV%);
Tmax, Tlast, and Tlag are presented as median (min-max); n=number of observations.
*
N=5.