Table 1.
Summary of Serum Pharmacokinetic Parameters for TV‐1106 in Japanese and Caucasian Subjects
| TV‐1106 Dose | |||||
|---|---|---|---|---|---|
| Population | Parameter (Unit)a | 7.5 mg | 15 mg | 50 mg | 100 mg |
| Japanese | n | 8 | 8 | 7 | 8 |
| Cmax (ng/mL) | 50.06 (67.05) | 68.16 (64.52) | 1031.76 (578.84) | 4516.45 (3438.02) | |
| tmax (h) | 14.00 (4.00, 18.00) | 10.00 (8.00, 48.00) | 18.00 (10.00, 36.00) | 30.00 (16.00, 72.77) | |
| AUC0–t (ng·h/mL) | 938.01 (1445.83) | 1376.15 (1062.82) | 33 950.37 (28 787.01) | 207 742.14 (130 678.73) | |
| AUC0–168 (ng·h/mL)b | —c | 2108.71 (1074.17) | 34 001.52 (28 766.35) | 207 746.35 (130 690.17) | |
| AUC0–inf (ng·h/mL)b | —c | 2222 (114.88) | 34 299.88 (28 873.49) | 210 077.27 (129 234.41) | |
| t1/2 (h)b | —c | 36.02 (8.73) | 30.01 (9.17) | 27.85 (13.13) | |
| CL/F (L/h)b | —c | 7.94 (3.31) | 2.21 (1.21) | 0.66 (0.37) | |
| Vz/F (L)b | —c | 409 (183) | 104 (71.5) | 31.0 (28.4) | |
| Caucasian | n | 8 | 8 | 8 | 8 |
| Cmax (ng/mL) | 25.70 (31.94) | 70.78 (42.87) | 844.73 (748.33) | 3931.05 (3416.77) | |
| tmax (h) | 12.00 (6.00, 36.00) | 10.00 (8.00, 36.00) | 22.00 (10.00, 36.00) | 30.00 (14.00, 72.33) | |
| AUC0–t (ng·h/mL) | 563.47 (566.06) | 1924.16 (899.10) | 20 850.25 (15 691.54) | 168 944.61 (128 206.73) | |
| AUC0–168 (ng·h/mL)d | — | 2281 (805.29) | 20 962 (15 630.57) | 168 363.58 (128 246.44) | |
| AUC0–inf (ng·h/mL)e | — | 2643.29 (660.61) | 21 170.02 (15 666.63) | 169898.21 (125799.41) | |
| t1/2 (h)e | — | 35.39 (8.20) | 25.97 (3.93) | 31.38 (12.65) | |
| CL/F (L/h)e | — | 6.04 (1.81) | 4.25 (3.17) | 1.27 (1.47) | |
| Vz/F (L)e | — | 301 (81) | 158 (120) | 65.8 (82.8) | |
Cmax, maximum observed concentration; tmax, time of observed maximum concentration; AUC0–t, area under the concentration–time curve from 0 to the time of the last quantifiable concentration; AUC0–168, area under the concentration–time curve from 0 to 168 hours postdose; AUC0–inf, area under the concentration–time curve from 0 extrapolated to infinity; t1/2, terminal half‐life; CL/F, apparent total body clearance; Vz/F, apparent volume of distribution.
Parameters are presented as arithmetic mean (standard deviation) except for tmax, which is median (minimum, maximum).
n = 3 for 7.5 mg and n = 4 for 15 mg.
Less than 50% of the population had evaluable parameters at this dose, and hence summary statistics have not been reported.
n = 7 for 15 mg.
n = 6 for 15 mg.