Table 2. PK Parameters of LEN Following Subcutaneous Administration of LEN in Aqueous Suspension to Male WH Ratsabcde.
| group ID | dose (mg/kg)b | dose volume (mL/kg) | AUC0–72 h (μM·h) | AUC0–672 h (μM·h) | AUClast (μM·h) | AUCinf (μM·h) | Cmax (μM) | Tmax (h) | t1/2 (h) | % of AUCinf on day 3 | % of AUCinf on day 28 | F%e |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 | 10 | 0.10 | 32.5 + 20.8 | 194 + 14 | 236 + 36 | 236 + 36 | 0.671 + 0.198 | 25 + 23 | 219 + 81 | 14 | 82 | 118 ± 18 |
| 2 | 30 | 0.30 | 20.6 ± 3.9 | 343 ± 63 | 663 ± 83 | 664 ± 83 | 0.724 ± 0.222 | 224 ± 97 | 263 ± 31 | 3 | 52 | 110 ± 14 |
| 3 | 100 | 1.0 | 68.0 ± 27.2 | 900 ± 89 | 1545c | 1554c | 1.91 ± 0.33 | 224 ± 97 | 397c | 4 | 58c | 78c |
| 4 | 200 | 1.0 × 2d | 180 ± 93 | 1498 ± 223 | 2499 ± 188 | 2517 ± 194 | 3.81 ± 1.08 | 120 ± 83 | 403 ± 50 | 7 | 60 | 63 ± 5 |
Values are the mean ± SD from 3 animals. AUC0–72 h = 3-day AUC; AUC0–672 h = 28-day AUC; SD = standard deviation.
Formulation concentration at 100 mg/mL LEN.
Only mean value was reported because one animal died at 2112 h postdose. This animal had appeared normal at the daily regular check time of 2088 h.
Two injections, each at a distinct site.
F% = total fraction dose released = 100 × dose-normalized SC AUCinf-to-IV AUCinf ratio.