Table 4. PK Parameters of LEN Following Subcutaneous Administration of LEN in a PEG/Water Solution Formulation to Male WH Ratsabc.
| group ID | dose (mg/kg) | 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 | mean F%c |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 21 | 50 | 0.12 | 7.86 ± 1.47 | 152 ± 49 | 774 ± 74 | 789 ± 61 | 0.469 ± 0.120 | 718 ± 257 | 1056 ± 504 | 0.68 | 13 | 79 ± 6 |
| 22 | 100 | 0.33 | 16.2 ± 6.2 | 216 ± 113 | 1330 ± 238 | 1340 ± 228 | 0.500 ± 0.138 | 1064 ± 257 | 1240 ± 281 | 0.71 | 9.4 | 67 ± 11 |
| 23 | 150 | 0.5 | 21.7 ± 3.6 | 282 ± 14 | 2160 ± 211 | 2190 ± 205 | 0.765 ± 0.092 | 1120 ± 194 | 1420 ± 403 | 0.63 | 8.2 | 73 ± 7 |
| 24 | 450 | 1.5 | 75.7 ± 12.1 | 926 ± 164 | 5360 ± 787 | 5400 ± 837 | 1.95 ± 0.306 | 840 ± 444 | 1330 ± 263 | 0.73 | 9.0 | 60 ± 9 |
| 25 | 200 | 0.33 × 2b | 32.3 ± 4.7 | 507 gf± 147 | 2410 ± 60 | 2410 ± 60 | 1.09 ± 0.17 | 728 ± 256 | 647 ± 28 | 0.71 | 11 | 60 ± 1 |
| 26 | 300 | 0.5 × 2b | 41.1 ± 1.3 | 550 ± 54 | 3630 ± 189 | 3660 ± 184 | 1.35 ± 0.09 | 896 ± 775 | 1110 ± 299 | 0.60 | 8.0 | 61 ± 3 |
| 27 | 900 | 1.5 × 2b | 99.4 ± 22.2 | 1140 ± 239 | 8400 ± 1160 | 8620 ± 1250 | 2.22 ± 0.35 | 1288 ± 423 | 1360 ± 156 | 0.48 | 5.5 | 48 ± 7 |
Values are the mean ± SD from 3 animals. AUC0–72 h = 3-day AUC; AUC0–672 h = 28-day AUC; SD = standard deviation.
Two injections, each at a distinct site
F% = Total fraction dose released = 100 × dose-normalized SC AUCinf-to-IV AUCinf ratio.