Table 3.
Summary of TAC-101 pharmacokinetics
| Parameter | N | Mean | Range | % CV |
|---|---|---|---|---|
| 20 mg dose level | ||||
| AUC0–24 (ng h/mL) | 4 | 3067.6 | 1575.2–4325.1 | 38 |
| AUC0–∞ (ng/h/mL) | 3 | 4241.2 | 2998.4–4995.1 | 26 |
| C max (ng/mL) | 5 | 242.0 | 131–351 | 33 |
| T 1/2 (mins) | 3 | 483.1 | 272.1–788 | 56 |
| 40 mg dose level | ||||
| AUC0–24 (ng h/mL) | 5 | 6871.8 | 4248.4–9278.5 | 35 |
| AUC0–∞ (ng/h/mL) | 2 | 6841.8 | 4570.1–9113.5 | 47 |
| C max (ng/mL) | 5 | 542.0 | 376–718 | 23 |
| T 1/2 (mins) | 2 | 340.5 | 323.2–357.7 | 7.17 |
AUC0–24 area under the TAC-101 time, concentration curve from time 0 to 24 h (i.e., dosing interval), AUC0-∞ area under the TAC-101 time, concentration curve from time 0 extrapolated to infinity; t1/2 half-life; Cmax: maximal concentration of TAC-101
Note: Only patients in Phase I underwent PK analysis (N = 11). One 20 mg patient did not have sufficient samples for any PK analysis; one 20-mg patient had no 24-h sample collected; two 40-mg patients had no 8-h sample collected; one 40-mg and one 20-mg patient had relatively delayed absorption which disallowed accurate estimation of the terminal elimination rate